WO2014048060A1 - Anti-inflammatory drug against cancer and aids with radiotherapy and preparation method thereof - Google Patents

Anti-inflammatory drug against cancer and aids with radiotherapy and preparation method thereof Download PDF

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Publication number
WO2014048060A1
WO2014048060A1 PCT/CN2013/001069 CN2013001069W WO2014048060A1 WO 2014048060 A1 WO2014048060 A1 WO 2014048060A1 CN 2013001069 W CN2013001069 W CN 2013001069W WO 2014048060 A1 WO2014048060 A1 WO 2014048060A1
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Prior art keywords
radioactive
mesoporous
nano
cancer
aids
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PCT/CN2013/001069
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French (fr)
Chinese (zh)
Inventor
唐伟钊
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Tang Weizhao
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Priority claimed from CN201210388401.XA external-priority patent/CN103656692A/en
Priority claimed from CN201210437128.5A external-priority patent/CN103768621A/en
Application filed by Tang Weizhao filed Critical Tang Weizhao
Publication of WO2014048060A1 publication Critical patent/WO2014048060A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/12Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules
    • A61K51/1241Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules particles, powders, lyophilizates, adsorbates, e.g. polymers or resins for adsorption or ion-exchange resins
    • A61K51/1244Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes, characterized by a special physical form, e.g. emulsions, dispersions, microcapsules particles, powders, lyophilizates, adsorbates, e.g. polymers or resins for adsorption or ion-exchange resins microparticles or nanoparticles, e.g. polymeric nanoparticles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Definitions

  • the invention relates to a nanometer manufacturing, a molecular biological anticancer drug and a radiotherapy anticancer technology, in particular to an anticancer anti-AIDS anti-inflammatory drug with radiotherapy and a preparation method thereof.
  • Anticancer drugs At present, cancer treatment at home and abroad is often treated by radiotherapy and chemotherapy, surgery or Chinese medicine. The radioactive substances used in hospital radiotherapy are only used by cancer patients. In order to deal with tumors, although there will be Dangerously, but the two evils are light and have to be used. The second treatment of cancer's traditional treatment method is greater than the cancer itself. This has been a global problem that has plagued modern medical treatment of cancer. One of the biggest obstacles to the application of traditional anti-cancer treatment is to kill tumor cells and often affect normal tissues. Cells that cause a variety of complications. Cancer Pathogenesis Cancer, also known as malignant tumor, is a disease caused by the abnormality of the cell growth and proliferation mechanism.
  • cancer cells can locally invade surrounding normal tissues and even transfer to other parts of the body via the circulatory system or lymphatic system. Because cancer cells can spread, metastasize or recur, many cancer patients often spend a lot of money after treatment. In general, the survival period is 3-5 years, and the extended life expectancy is very limited.
  • Traditional anti-cancer technology has obvious defects of secondary injury to cancer patients, shortcomings of short survival and high cost. Radiotherapy and chemotherapy can lead to greatly reduced immunity of cancer patients who have been destroyed by visceral function, and pose a greater hidden danger for cancer spread, metastasis and recurrence. This technology uses targeted or conventional anticancer drugs with radiotherapy, using targets.
  • Synergistic treatment and sustained-release treatment of other drugs increasing the intensity of treatment, on the one hand, greatly reducing the damage of skin and subcutaneous tissues and organs caused by traditional radiotherapy, greatly controlling the growth rate of cancer cells, on the other hand, relative Improve the patient's immunity and win valuable for treatment Time, the chance of eradicating the spread or transfer of mild cancer cells is greatly improved.
  • Anti-AIDS and anti-inflammatory drugs such as nucleoside reverse transcriptase inhibitors such as zidovudine, stavudine, didanosine, etc.
  • nucleoside reverse transcriptase inhibitors such as zidovudine, stavudine, didanosine, etc.
  • Non-nucleoside reverse transcriptase inhibitors such as nevirapine, protease inhibitors such as indinavir. They are used to treat AIDS by forming four internationally recognized "cocktail therapies": zidovudine + didanosine + nevirapine, didanosine + stavudine + nevirapine, zidovudine + dehydroxyl Inosine + indinavir, stavudine + didanosine + indinavir.
  • HIV genes can mutate and hide where drugs can't be killed, even when antiretroviral drugs (ARVs) are used to clear HIV in the body.
  • ARVs antiretroviral drugs
  • the level of blood is difficult to detect, some viruses remain active in tissues.
  • all anti-AIDS drugs at home and abroad can not cure AIDS patients fundamentally, but can effectively prolong the life of patients, which has been A global problem that plagues modern medicine for the treatment of AIDS.
  • This technology uses targeted or conventional anti-AIDS or anti-inflammatory infections with radiotherapy, and uses synergistic and sustained-release treatments for targeted drugs to increase the intensity of treatment.
  • the target with radiotherapy function Transmitting HIV or other anti-inflammatory or anti-inflammatory drugs to HIV-infected tissues and organs to kill HIV.
  • killing HIV through the humoral circulation and relatively improving the patient's immunity To gain valuable time for treatment, the chances of eliminating variability, spread, and metastasis of HIV have been greatly improved.
  • mesoporous radioactive nanospheres From the inside to the outside, mesoporous radioactive nanospheres, anti-radiation inert metal layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-AIDS anti-inflammatory drug layer can also be eliminated; mesopores Put The surface of the radioactive nanospheres has a plurality of mesoporous radioactive nanospheres radiating mesopores and nano anti-radiation valves, and the nano anti-radiation valve is connected with the mesoporous radioactive nanospheres radiation mesopores; mesoporous radioactive nanospheres It can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
  • mesoporous radioactive nanospheres From the inside to the outside, mesoporous radioactive nanospheres, absorbing membrane layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-AIDS anti-inflammatory drug layer can also be eliminated; mesoporous radioactivity
  • the surface of the nanosphere has a plurality of mesoporous radioactive nanospheres radiating mesopores and a nanometer radiation protection valve, and the nanometer radiation shielding gate is connected with the mesoporous radioactive nanospheres radiation mesopores; the mesoporous radioactive nanospheres can be They were made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
  • mesoporous radioactive nanospheres From the inside to the outside, there are mesoporous radioactive nanospheres, anti-radiation active metal film layer, metal and organic pollution protection film layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and can also eliminate the anti-antibody Cancer anti-AIDS anti-inflammatory drug layer; mesoporous radioactive nanospheres have numerous mesoporous radioactive nanospheres radiation mesopores and nano anti-radiation valves, nano anti-radiation valves and mesoporous radioactive nanospheres radiation mesoporous phase Connected and connected; mesoporous radioactive nanospheres can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
  • mesoporous radioactive nanospheres From the inside to the outside, there are mesoporous radioactive nanospheres, absorbing membrane layer, metal and organic pollution protection membrane layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-cancer AIDS anti-inflammatory drug layer; when the absorbing membrane layer adopts non-toxic and non-bioreactive materials, the protective film layer against metal and organic pollution is removed; the mesoporous radioactive nanospheres have numerous mesoporous radioactive nanospheres radiating mesopores The mouth and nano radiation protection valve, the nano radiation protection wide door is connected with the mesoporous radioactive nano microsphere radiation mesoporous mouth; the mesoporous radioactive nano microsphere can be added with anti-cancer anti-AIDS anti-inflammatory by using radioactive material and internal mesoporous channel respectively The way the drug is made and the way the pure radioactive material is made.
  • mesoporous radioactive nanospheres From the inside to the outside, mesoporous radioactive nanospheres, radioactive metal film layer, anti-radiation layer, anti-cancer
  • the anti-AIDS anti-inflammatory drug layer and the nano-targeting carrier layer can also eliminate the anti-cancer anti-AIDS anti-inflammatory drug layer;
  • the mesoporous radioactive nanospheres have numerous mesoporous radioactive nano-microsphere radiation mesopores and nano anti-radiation valves.
  • the nano-radiation-proof valve is connected with the mesoporous radioactive nano-microsphere radiation mesopores; the mesoporous radioactive nano-spheres can be supplemented with radioactive materials and internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials. Way of making.
  • this technology uses targeted or conventional anti-cancer anti-inflammatory drugs with radiotherapy function, using targeted drugs Synergistic treatment and sustained-release treatment, increase the intensity of treatment, to achieve "significant reduction of skin and subcutaneous tissues and organs caused by traditional radiotherapy, greatly control the growth rate of cancer cells, HIV and inflammation, and relatively improve patients
  • the immunity for the treatment to win valuable time, the existing refractory cancer cells, HIV and inflammation or the spread or metastasis of mild cancer cells HIV and inflammation also eliminate the chance of a clean increase "good effect.
  • Radioactive nanospheres can be made of natural or artificial radioactive materials that can release particles or rays (such as alpha rays, 3 rays, xenon rays, etc.) from inside the nucleus.
  • the radiant energy is uranium (U). ⁇ (Th) and radium (Ra), or potassium - 40 (40K), ⁇ (Rb) and ⁇ (Cs), etc., or a mixture of radioactive materials and ceramic powder, and determine the required radioactive material according to actual conditions. kind of.
  • the specific gravity concentration of the drug after preparation is preferably consistent with the blood, for example, the specific gravity does not exceed the specific gravity of the blood 1. 05, so as to avoid precipitation.
  • the thickness is preferably thicker than 23 ⁇ m.
  • the radiation-proof inert metal or absorbing layer may be made of various radiation-proof inert metals such as gold or silver or silica gel.
  • the solution of the drug can be filtered by a set aperture.
  • individual drugs may not be completely excreted by metabolism within the specified time, and may be filtered by hemodialysis. If necessary, magnetic substances may be added to both the filter membrane and the mesoporous radioactive nanospheres. Magnetic absorption and other methods are better filtered.
  • the anti-cancer anti-AIDS anti-inflammatory drug layer may be a targeted or conventional drug layer.
  • mesoporous radioactive nanospheres From the inside to the outside, mesoporous radioactive nanospheres, anti-radiation inert metal layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-AIDS anti-inflammatory drug layer can also be eliminated; mesopores
  • the surface of the radioactive nanospheres has a plurality of mesoporous radioactive nanospheres radiating mesopores and nano anti-radiation valves, and the nano anti-radiation valve is connected with the mesoporous radioactive nanospheres radiation mesopores; the mesoporous radioactive nanospheres can be They were made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
  • mesoporous radioactive nanospheres From the inside to the outside, mesoporous radioactive nanospheres, absorbing membrane layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-AIDS anti-inflammatory drug layer can also be eliminated; mesoporous radioactivity
  • the surface of the nanosphere has a plurality of mesoporous radioactive nanospheres radiating mesopores and a nanometer radiation protection valve, and the nanometer radiation protection valve is connected with the mesoporous radioactive nanospheres radiation mesopores; the mesoporous radioactive nanospheres can be separately It is made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials. 3.
  • mesoporous radioactive nanospheres From the inside to the outside, there are mesoporous radioactive nanospheres, anti-radiation active metal film layer, metal and organic pollution protection film layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and can also eliminate the anti-antibody Cancer anti-AIDS anti-inflammatory drug layer; mesoporous radioactive nanospheres have numerous mesoporous radioactive nanospheres radiation mesopores and nano anti-radiation valves, nano anti-radiation valves and mesoporous radioactive nanospheres radiation mesoporous phase Connected and connected; mesoporous radioactive nanospheres can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
  • mesoporous radioactive nanospheres From the inside to the outside, there are mesoporous radioactive nanospheres, absorbing membrane layer, metal and organic pollution protection membrane layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-cancer AIDS anti-inflammatory drug layer; when the absorbing membrane layer adopts non-toxic and non-bioreactive materials, the protective film layer against metal and organic pollution is removed; the mesoporous radioactive nanospheres have numerous mesoporous radioactive nanospheres radiating mesopores The mouth and nano anti-radiation valve, the nano anti-radiation valve is connected with the mesoporous radioactive nano-microsphere radiation mesopores; the mesoporous radioactive nano-spheres can be added with anti-cancer anti-inflammatory drugs by radioactive materials and internal mesoporous channels, respectively. The way and the way of purely radioactive materials are produced.
  • mesoporous radioactive nanospheres From the inside to the outside, mesoporous radioactive nanospheres, radioactive metal film layer, radiation protection layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-AIDS anti-inflammatory drug layer can also be eliminated.
  • the mesoporous radioactive nanospheres have a plurality of mesoporous radioactive nanospheres radiating mesopores and nanometer radiation protection valves, and the nanometer radiation protection valve is connected with the mesoporous radioactive nanospheres radiation mesopores; mesoporous radioactive nanometers; Microspheres can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
  • the mesoporous size of mesoporous radioactive nanospheres is preferably controlled in the range of 2 to 50 nm.
  • mesoporous radioactive nanospheres and nano-radiation-proof wide doors can be assembled by assembly or other chemical methods, but self-assembly is preferred to achieve mass production.
  • Mesoporous radioactive nanospheres can be prepared by adding radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs or pure radioactive materials.
  • this technology uses targeted or conventional anti-cancer anti-inflammatory drugs with radiotherapy, targeting drugs Synergistic treatment and sustained-release treatment, increase the intensity of treatment, to achieve "significant reduction of skin and subcutaneous tissues and organs caused by traditional radiotherapy, greatly control the growth rate of cancer cells, HIV and inflammation, and relatively improve patients
  • the immunity for the treatment to win valuable time, the existing refractory cancer cells, HIV and inflammation or the spread or metastasis of mild cancer cells HIV and inflammation also eliminate the chance of a clean increase "good effect.
  • Figure 1 is a cross-sectional view and a schematic view of the present invention.
  • mesoporous radioactive nanospheres 21A, radiation-proof inert metal layer, 3A, anti-cancer anti-AIDS anti-inflammatory drug layer, 4, mesoporous radioactive nanospheres radiation mesopores, 5, nano-anti Radiation valve, 5A, quasi-rotaxane or rim "spool", 6, nano-targeting carrier layer.
  • Figure 2 is a cross-sectional view of the present invention.
  • Figure 3 is a cross-sectional view of the present invention.
  • Figure 4 is a cross-sectional view of the present invention.
  • Figure 5 is a cross-sectional view of the present invention.
  • Fig. 6 is a super-molecular structure diagram of a pseudo-rotaxane in which a radiation-proof metal cluster of one of the structures of the nano-radiation-proof valve (5) is a core.
  • FIG. 1 and FIG. 2 are respectively a structural enlarged cross-sectional view of an anti-cancer anti-inflammatory anti-inflammatory drug with radiotherapy and a preparation method thereof.
  • Step 1 Preparation of a nano-radiation-proof valve with a radiation-proof metal ion on the surface (5) Functional mesoporous radioactivity Nanospheres (1):
  • Radioactive materials such as natural or artificial uranium (U), thorium (Th) and radium (Ra), or potassium-40 (40K) that emit particles or rays (such as d-rays, beta rays, xenon rays, etc.) from inside the nucleus.
  • Radioactive materials such as lanthanum (Rb) and lanthanum (Cs) and silica hybrid materials or individual radioactive materials are used as substrates, by chemical or biosynthetic or mechanical methods such as coprecipitation, sol-gel, dispersion polymerization or Controlled free radical polymerization to synthesize uniform size, large pore volume (for example, 0. 6-5cm3/g), high specific surface area (for example, 700--1500 m2/g), high-density modified radioactive mesoporous radioactive nanometer Microspheres (1), for example: can be prepared by the following methods, etc.
  • Method 1 After mixing the calcium carbonate and radium radioactive materials, the mechanically ground powder is added to the nanometer size, and the gel is desolvated and washed with dilute acid.
  • the preparation method comprises: preparing radioactive particles by coprecipitation; then dispersing the washed radioactive particles directly into an aqueous solution of a SiO2-containing water-soluble inorganic salt for coating or mixing with an inorganic silicon source; Trimethylammonium bromide is used as a templating agent, and tetraethyl orthosilicate is a silicon source for mesoporous silica coating or mixing.
  • Method 3 using a sodium hypophosphite liquid phase reduction method to prepare a nano-ray sol, and then using tetraethyl orthosilicate as a silicon source, cetyltrimethylammonium bromide as a template, using a sol-gel method,
  • the silica spherical shell was grown in situ on the surface of the radium particles in the prepared nano-laser sol, and then the organic template was removed by solvent extraction, and the mesoporous silica-coated radium nanoparticles were prepared by supercritical drying.
  • Method 4 if the patent number is 03153265, the name is "a preparation method of a micrometer spherical mesoporous silica", and the patentee is authorized by the "Institute of Physical and Chemical Technology of the Chinese Academy of Sciences", and can be prepared by the following method steps,
  • the method comprises the following steps: (1) preparing an acid solution, the concentration of the acid is Q. 0 1 ⁇ 10 mol/L; 2) adding a surfactant to the solution of the step (1), so that the cetyltrimethyl group in the mixed solution
  • the concentration of ammonium halide is 0. 0 0 1 ⁇ 5 mol / liter, the concentration of polyvinyl alcohol is 0.
  • the mesoporous surface inside the mesoporous radioactive nanospheres (1) is successfully grafted or physically adsorbed against the anti-cancer anti-inflammatory drugs, and the anti-cancer, anti-AIDS and anti-inflammatory drugs are prepared.
  • the drug's pore radioactive nanospheres (1); mesoporous radioactive nanospheres (1) can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs or pure radioactive materials.
  • a method such as a volatilization method for example, a metal rim having a function of a nano-radiation-proof valve (5) having a radiation-proof metal ion on the surface or a metal rim having a function of a nano-radioactive material (5) having a radiotherapy function, for example, (1):
  • a volatilization method for example, a metal rim having a function of a nano-radiation-proof valve (5) having a radiation-proof metal ion on the surface or a metal rim having a function of a nano-radioactive material (5) having a radiotherapy function, for example, (1):
  • the artificial radioisotope cobalt 60 which can replace X-rays for the treatment of cancer and AIDS, as an example, the rotaxane produced by cucurbituril and spermine hydrochloride is self-assembled with hydrated alkyl cobalt ruthenium.
  • New methods of self-assembly (if they or the unit has applied for a patent, they need to obtain the license of the patentee), specifically: use Radiation metal cluster core conduct self-assembly as a ligand, namely: synthetic anionic organic ligand radiation regulatory guidance metal clusters, then macrocycle Coordination with a radiation-proof metal cluster to produce a radiation-proof metal cluster assembly having a specific coordination direction, and then using other ligands as a linker, thereby obtaining a quasi-rim, a hydrocarbon-locking, etc.
  • Radiation metal cluster core conduct self-assembly as a ligand, namely: synthetic anionic organic ligand radiation regulatory guidance metal clusters, then macrocycle Coordination with a radiation-proof metal cluster to produce a radiation-proof metal cluster assembly having a specific coordination direction, and then using other ligands as a linker, thereby obtaining a quasi-rim, a hydrocarbon-locking, etc.
  • a radiation-proof metal cluster as a core Molecular structure; for example, (3):
  • metal ions as a template or the introduction of metal ions and their complexes in supermolecular systems such as rotaxanes and hydrocarbons has synthesized a variety of novel supermolecules such as metal rotaxanes and hydrocarbons.
  • the supermolecular quasi-rim or rim of silver metal is constructed on the surface of mesoporous radioactive nanospheres (1) by means of self-assembly, etc., and functionalized nano-silica or nano-silver is used as a bobbin molecule, and super-molecules such as silver metal can be online.
  • a supramolecular nano-radiation-proof valve (5) that slides on the shaft, controls the release and the new function of the switch, thereby obtaining a mesoporous radioactive nanosphere (1) with a functional anti-radiation metal ion on the surface of the nano-radiation-proof valve (5) Controlled release of supramolecular nanovalves such as silver metal by pH and competition combined with dual channels, etc., to meet various release and switching requirements of the set conditions.
  • the mesoporous radioactive nanospheres (1) are nano-containers, and the nano-targeting carrier layer (6) is controlled release of a supramolecular nano-valve such as silver metal induced by an amino acid decarboxylase, which has biological targeting and switching functions.
  • the switch of the nano-radiation-proof valve (5) is automatically opened, and the anti-cancer anti-inflammatory and anti-inflammatory drugs inside the mesoporous radioactive nanospheres (1) pass through the mesoporous radioactivity.
  • the nano-microspheres radiate mesopores (4) to release outward, and "chemotherapy” kills cancer cells, HIV and inflammation; the switch of nano-radiation-proof valve (5) is automatically opened while mesoporous radioactivity
  • the radiation inside the nanosphere (1) is radiated externally through the mesoporous radioactive nanosphere irradiation mesopores (4), and the cancer cells, HIV and inflammation of the target cancer tissue are "radiated”;
  • the anti-cancer anti-inflammatory anti-inflammatory drug layer (3A) routinely kills cancer cells, HIV and inflammatory chemotherapy or Chinese medicine treatment of target cancer cells; the above process is performed separately or simultaneously with radiotherapy and chemotherapy.
  • Step 2 Coating or plating the radiation-proof inert metal layer (21A) or the absorber film layer (21B) onto the mesoporous radioactive nanospheres (1):
  • Step 3 Coating, covering or adsorbing the anti-cancer anti-inflammatory drug layer (3A) in the radiation-proof inert metal layer (21A) or sucking by physical adsorption, chemical infiltration, copolymerization, magnetization, surface modification, etc. On the wave film layer (21B).
  • Step 4 Prepare a nano-targeted carrier layer by compounding a targeting agent such as lipase by chemical modification and polymerization (6).
  • Step 5 The nano-targeting carrier layer (6) is coated and covered on the anti-cancer anti-inflammatory anti-inflammatory drug layer (3A) by modification, magnetization, copolymerization and the like.
  • Radioactive nanospheres (1), anti-radiation inert metal layer (21A) or absorbing membrane layer (21B), anti-cancer anti-AIDS anti-inflammatory drug layer (3A), mesoporous radioactive nanospheres radiation mesoporous ( 4), a nano-radiation-proof broad-door (5), a nano-targeted carrier layer (6), a radiotherapy-resistant anti-cancer anti-inflammatory drug and a preparation method thereof, as an injection for blood injection or intramuscular injection or incision injection or After oral administration as an oral drug, the drug is absorbed into the blood circulation system and the lymphatic system of the body with blood or gastrointestinal absorption.
  • the anti-cancer anti-AIDS anti-inflammatory drug is caused by the organism.
  • the guiding effect is concentrated on the target site cancer tissues and cancer cells, HIV and inflammatory cells; anti-cancer anti-AIDS anti-inflammatory drugs are killed with the blood circulation to the whole body of cancer tissue cells, in the external electricity, light, magnetic,
  • the valve is "open" when the molecular ring of the quasi-rotaxane or rim “spool” (5A) in the nano-radiation-proof valve (5) is driven upward by electrical or magnetic force.
  • the radiation in the mesoporous radioactive nanospheres (1) is killed by mesoporous radioactive nanospheres through the mesopores (4) to kill cancer cells, HIV and inflammation of the target cancer tissue;
  • Nano micro The anti-cancer anti-inflammatory and anti-inflammatory drugs adsorbed by the mesoporous channel of the ball (1) are released through the mesoporous radioactive nanospheres through the mesopores (4), and the cancer cells, HIV and inflammation of the target cancer tissues are carried out.
  • Radioactive nanospheres (1), anti-radiation inert metal layer (21A) or absorbing membrane layer (21B), anti-cancer anti-AIDS anti-inflammatory drug layer (3A), mesoporous radioactive nanospheres radiation mesoporous ( 4), a nano-anti-radiation valve (5), a nano-targeting carrier layer (6), a radiotherapy-resistant anti-cancer anti-inflammatory drug and a preparation method thereof, as an injection for blood injection or intramuscular injection or incision injection or as an injection After oral administration, the drug is absorbed into the blood circulation system and lymphatic system of the body with blood or gastrointestinal absorption.
  • the anti-cancer and anti-AIDS resistance due to biological guidance Inflammatory drugs are concentrated in cancerous tissues and cancer cells, HIV and inflammatory cells at target sites, killing cancer cells, HIV and inflammation; and anti-cancer anti-inflammatory drugs are circulating to the whole body of cancer tissue cells with blood circulation. Killing, this is the process of releasing anti-cancer anti-inflammatory drugs.
  • Fig. 3 or Fig. 4 are respectively a macroscopic enlarged view of a structural section of an anticancer, anti-AIDS and anti-inflammatory drug with radiotherapy and a preparation method thereof:
  • Step 1 Preparation of a nano-radiation-proof valve with a radiation-proof metal ion on the surface (5) Mesoporous radioactivity of a functional group Nanospheres (1):
  • a radioactive material and a silica hybrid material or a separate radioactive material as a substrate, using chemical or biosynthetic or mechanical methods such as coprecipitation, sol-gel method, dispersion polymerization or controllable freedom
  • Base polymerization method for synthesizing uniform size, large pore volume (for example, 0.6--5 cm3/g), high specific surface area (for example, 700-1500 m2/g), high density modified radioactive mesoporous radioactive nanospheres ( 1) for example: It can be prepared by the following methods, etc. The following methods are the same as those in Fig. 1, and are omitted.
  • the mesoporous surface inside the mesoporous radioactive nanospheres (1) is successfully grafted or physically adsorbed against the anti-cancer anti-inflammatory drugs, and the anti-cancer, anti-AIDS and anti-inflammatory drugs are prepared.
  • the drug's pore radioactive nanospheres (1); mesoporous radioactive nanospheres (1) can be prepared by adding radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs or by using pure radioactive materials alone.
  • the following method is used to obtain a metal rim of a nano-radiation-proof wide gate (5) functional group having a radiation-proof metal ion on the surface, specifically a rim-like rim produced by cucurbituril and spermine hydrochloride, and a hydrated ruthenium-based cobalt
  • a new type of metal rotaxane is formed in the aqueous solution, which is one of the methods to be realized.
  • the supermolecular quasi-rim or rim of silver metal is constructed on the surface of mesoporous radioactive nanospheres (1) by means of self-assembly, etc., and functionalized nano-silica or nano-silver is used as a bobbin molecule, and super-molecules such as silver metal can be online.
  • a supramolecular nano-radiation-proof valve (5) that slides on the shaft, controls the release and the new function of the switch, thereby obtaining a mesoporous radioactive nanosphere (1) with a functional base of a nano-radiation-proof valve (5) with a radiation-proof metal ion on the surface (1)
  • the mesoporous radioactive nanospheres (1) are nano-containers
  • the nano-targeting carrier layer (6) such as an amino acid decarboxylase, is a supramolecular nanovalve such as silver metal.
  • the transport system has biological targeting and switching capabilities and is capable of controlled release in multiple steps as needed.
  • the switch of the nano-radiation-proof valve (5) is automatically opened, and the anti-cancer anti-inflammatory and anti-inflammatory drugs inside the mesoporous radioactive nanospheres (1) pass through the mesoporous radioactivity.
  • the nano-microspheres radiate mesopores (4) to release outward, and "chemotherapy” kills cancer cells, HIV and inflammation; the switch of nano-radiation-proof valve (5) is automatically opened while mesoporous radioactivity
  • the radiation inside the nanosphere (1) is radiated externally through the mesoporous radioactive nanosphere irradiation mesopores (4), and the cancer cells, HIV and inflammation of the target cancer tissue are "radiated”;
  • the anti-cancer anti-inflammatory anti-inflammatory drug layer (3A) routinely kills cancer cells, HIV and inflammatory chemotherapy or Chinese medicine treatment of target cancer cells; the above process is performed separately or simultaneously with radiotherapy and chemotherapy.
  • Step 2 Coating or plating the radiation-proof active metal film layer (22A) or the absorber film layer (21B) onto the mesoporous radioactive nanospheres (1): radiation-proof active metal film layer (22A) or absorbing wave
  • the film layer (21B) is subjected to physical adsorption method, arc discharge method, plasma polymerization method, laser chemical vapor deposition method, chemical replacement method, emulsion polymerization method, surface deposition method (electroless plating method, heterogeneous precipitation method), and the like.
  • the metal or organic contamination protective film layer (31) is coated or plated onto the mesoporous radioactive nanospheres (1).
  • Step 3 The metal or organic contamination protective film layer (31) is coated or plated onto the radiation-proof active metal film layer (22A) or the moisture absorbing film layer (21B).
  • Step 4 Coating, covering or adsorbing the anti-cancer anti-inflammatory anti-inflammatory drug layer (3A) in a metal or organic-protective protective film layer by physical adsorption, chemical infiltration, copolymerization, magnetization, surface modification, etc. (31 ).
  • Step 5 Prepare a nano-targeted carrier layer by compounding a targeting agent such as lipase by chemical modification and polymerization (6).
  • Step 6 The nano-targeting carrier layer (6) is coated and covered on the anti-cancer anti-AIDS anti-inflammatory drug layer (3A) by means of modification, magnetization, copolymerization and the like.
  • 3A anti-cancer anti-AIDS anti-inflammatory drug layer
  • Radioactive nanospheres (1), radiation-proof active metal film layer (22A) or absorbing film layer (21B), metal or organic-protective protective film layer (31), anti-cancer anti-AIDS anti-inflammatory drug layer (3A a mesoporous radioactive nano-microsphere radiation mesoporous (4), nano-radiation-proof valve (5), quasi-rim or rotaxane "broad core” (5A), nano-targeting carrier layer (6)
  • anti-cancer anti-AIDS and anti-inflammatory drugs are concentrated to target sites of cancer tissues and cancer cells, HIV and inflammatory cells due to biological targeting; anti-cancer and anti-AIDS resistance Inflammatory drugs are killed by the blood cells circulating to the whole body of cancer tissue cells.
  • the molecular ring of the "spool” (5A) When the molecular ring of the "spool” (5A) is driven upward by electric or magnetic force, the valve is in the "on” state, and the radiation in the mesoporous radioactive nanosphere (1) passes through the mesoporous radioactive nanometer
  • the spherical radiation mesopores (4) kill cancer cells, HIV and inflammation of the target cancer tissue; and the anticancer anti-AIDS anti-inflammatory drugs adsorbed by mesoporous radioactive nanospheres (1) mesoporous channels Through the mesoporous radioactive nanospheres, the radiation mesopores (4) are released to the outside, and the cancer cells, HIV and inflammation of the target cancer tissue are killed; when the nano-radiation valve (5) is quasi-rotaxane or The rim "spool" (5A) The downward movement of the molecular ring blocks the mesopor
  • the mesoporous radioactive nanospheres are irradiated.
  • the mesopores (4) are closed, and the radiation in the mesoporous radioactive nanospheres (1) and the anticancer anti-inflammatory anti-inflammatory drugs in the mesopores stop the radiation or anti-cancer anti-inflammatory drugs. This is radiotherapy. And sustained release anti-cancer anti-AIDS Process control anti-inflammatory drugs.
  • the anti-cancer, anti-inflammatory and anti-inflammatory effects due to biological guidance Drugs are concentrated in target sites, cancerous tissues and cancer cells, HIV and inflammatory cells, killing cancer cells, HIV and inflammation; while anti-cancer, anti-AIDS and anti-inflammatory drugs are carried out with blood circulation to cancer cells of the body. Killing, this is the process of releasing anti-cancer, anti-AIDS and anti-inflammatory drugs.
  • Figure 5 is a macroscopic enlarged view of a structural cross-sectional view of an anti-cancer anti-inflammatory drug with radiotherapy and a preparation method thereof:
  • Step 1 Prepare a nano-radiation-proof valve with a radiation-proof metal ion on the surface (5) Mesoporous radioactivity of the functional group Nanospheres (1):
  • a large pore volume for example, 0.6- 5 cm3/g
  • a high specific surface area for example, 700-1500 m2/g
  • a high-density modified radioactive mesoporous radioactive nanosphere (1) for example -
  • the following methods are used to prepare, etc., and the following methods are the same as those in Fig. 1, and are omitted.
  • the mesoporous radioactive nanospheres (1) After the mesoporous radioactive nanospheres (1) are prepared, the mesoporous surface inside the mesoporous radioactive nanospheres (1) is successfully grafted or physically adsorbed against the anti-cancer anti-inflammatory drugs, and the anti-cancer, anti-AIDS and anti-inflammatory drugs are prepared.
  • the drug's pore radioactive nanospheres (1); mesoporous radioactive nanospheres (1) can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs or pure radioactive materials. Due to the strong or very strong coordination bond between metal ions and metal and ligand, it becomes the driving force for self-assembly of supramolecules.
  • the structural and functional components or building blocks of molecules such as molecules are assembled into new supramolecular compounds in a designed manner, and the surface-radioactive nano-radiation-proof valves are obtained by interaction or bonding between metal and metal molecules (5)
  • the functional group of mesoporous radioactive nanospheres (1) can be directly bound or obtained by chemical modification.
  • the following method is used to obtain a metal rotaxane having a functional surface of a radioactive nano-radiation-proof valve (5), specifically a rim-like rim produced by cucurbituril and spermine hydrochloride, and self-assembled with hydrated ruthenium-based cobalt ruthenium. After the reaction, a new type of metal rim is formed in the aqueous solution, which is one of the methods implemented.
  • a supermolecular quasi-rim or rim of silver metal is constructed on the surface of mesoporous radioactive nanospheres (1) by self-assembly, etc., and functionalized nano-silica or nano-silver is used as a bobbin molecule, and supramolecules such as silver metal can be online.
  • a supramolecular nano-radiation-proof valve (5) that slides on the shaft, controls the release and the new function of the switch, thereby obtaining a mesoporous radioactive nanosphere (1) with a functional surface-based radioactive nano-radiation-proof valve (5), through pH Combined with competition, the dual-channel and other super-molecular nano-controlled release such as silver metal can meet the various release and switching requirements of the set conditions.
  • the mesoporous radioactive nanospheres (1) are nano-containers, and the nano-targeting carrier layer (6) is controlled release of a supramolecular nano-valve such as silver metal induced by an amino acid decarboxylase, which has biological targeting and switching functions. And can control the release in multiple steps as needed. Under the action and control of the external electricity, light, magnetism, sound, etc., the switch of the nano-radiation-proof valve (5) is automatically opened, and the anti-cancer, anti-inflammatory and anti-inflammatory drugs inside the mesoporous radioactive nanospheres (1) are introduced.
  • a supramolecular nano-valve such as silver metal induced by an amino acid decarboxylase
  • the radioactive nano-microspheres radiate mesopores (4) to release outward, and "chemotherapy” kills cancer cells, HIV and inflammation; the switch of the nano-radiation valve (5) is automatically opened,
  • the radiation inside the porous radioactive nanosphere (1) radiates externally through the mesoporous radioactive nano-microsphere radiation mesopores (4) and the radiation of the nano-radiation-proof valve (5) itself, and the cancer of the target cancer tissue Cells, HIV and inflammation undergo “radiotherapy”killing; on the other hand, anti-cancer anti-inflammatory anti-inflammatory drug layer (3A) targets cancer cells, HIV and inflammatory chemotherapy or Traditional Chinese medicine treatment is routinely and rapidly killed; the above process is performed by radiotherapy and chemotherapy alone or simultaneously.
  • Step 2 Coating or plating the radioactive metal film layer (21C) onto the mesoporous radioactive nanospheres (1):
  • the radiation prevention layer (32) is applied by physical adsorption method, arc discharge method, plasma polymerization method, laser chemical vapor deposition method, chemical replacement method, emulsion polymerization method, surface deposition method (electroless plating method, heterogeneous precipitation method) or the like. ) coated or plated onto mesoporous radioactive nanospheres (1).
  • Step 3 Cover or plate the radiation protection layer (32) onto the radioactive metal film layer (21C).
  • Step 4 The anti-cancer anti-AIDS anti-inflammatory drug layer (3A) is coated, covered or adsorbed on the radiation protection layer (32) by physical adsorption, chemical infiltration, copolymerization, magnetization, surface modification, and the like.
  • Step 5 A nano-target carrier layer is prepared by compounding a targeting carrier such as lipase by chemical modification and polymerization (6).
  • Step 6 The nano-targeting carrier layer (6) is coated and covered on the anti-cancer anti-AIDS anti-inflammatory drug layer (3A) by modification, magnetization, copolymerization and the like.
  • the molecular ring of the quasi-rotaxane or rim "spool" (5A) in the nano-radiation-proof valve (5) is electrically Or when the magnetic force drives the upward movement, the valve is in an "on” state, and the radiation in the mesoporous radioactive nanosphere (1) passes through the mesoporous radioactive nanospheres to irradiate the mesopores (4) to the target cancer tissue.
  • HIV anti-cancer inflammatory drugs or anti-cancer radiation stopping the flow outwardly inflammatory drugs against AIDS, which is a sustained release anti-cancer radiotherapy and process control HIV anti-inflammatory drugs.
  • bio-directed anti-cancer anti-inflammatory drugs are concentrated in target sites of cancer tissues and cancer cells, HIV and inflammatory cells, killing cancer cells, HIV and inflammation; and anti-cancer, anti-AIDS and anti-inflammatory
  • the drug is killed by the blood cells circulating to the cancer cells of the whole body. This is the process of
  • anticancer drug experimental example 1 ( Figure 1 for the experimental example).
  • an anticancer drug such as a cisplatin drug molecule is successfully grafted on the surface of the mesoporous radioactive nanosphere (1), and the anticancer drug layer (3A) such as cisplatin is coated by copolymerization and self-assembly.
  • the drug molecule is coated with a nano-targeting carrier layer (6) on the surface of the anticancer drug layer (3A), such as a cisplatin drug molecule, and the results show that the drug loading efficiency is 50 due to coordination and superior adsorption performance of the material. %, slow release of the drug lasts for 20 days.
  • the release system has pH-sensitive release characteristics, and at the same drug concentration, the drug delivery system is more effective in inhibiting human cervical cancer cells than conventional drugs, and at the same time, the anticancer drug layer (3A) is treated with chemotherapy.
  • Mesoporous radioactive nanospheres (1) capable of emitting alpha-rays as a radioactive substance through a mesoporous radioactive nanosphere-radiating mesoporous port (4) for radiotherapy of target cancer cells, after 1 hour of treatment, The killing rate of cancer cells at the cervical targeting site reaches 100%.
  • mesoporous radioactive nanospheres (1) mesoporous radioactive nanospheres (1), radiation-proof active metal film layer (21B), metal-proof organic a pollution prevention protective layer (31), an anticancer drug layer (3A), a mesoporous radioactive nanosphere radiation mesopores (4), a nanometer radiation protection valve (5), and a nanotarget carrier layer (6)
  • a nano-anticancer drug with radiotherapy function is
  • Radioactive nanospheres (1) synthesized by chemical methods, such as radium, which is capable of emitting alpha ray as a radioactive substance, successfully grafted an anticancer targeting or conventional drug layer such as doxorubicin internally using a mesoporous surface.
  • the drug molecule is coated with an anticancer drug layer (3 ⁇ ), such as a cisplatin drug molecule, by copolymerization, self-assembly or magnetization, and then coated with an enzyme on the surface of the anticancer drug layer (3 ⁇ ) such as cisplatin drug molecule.
  • the drug delivery system nano-targeted carrier layer (6) which exhibits extremely high doxorubicin loading (800 mg/g) and loading efficiency (60%).
  • the drug-loading system can achieve targeted therapy of liver cancer.
  • the results showed that the synthesized ligand-functionalized drug delivery system was more effectively recognized by liver cancer cells than the unfunctionalized vector, and showed more effective than conventional drugs and unfunctionalized mesoporous nano drug delivery systems.
  • the anticancer drug layer (3A) performs chemotherapy, and the mesoporous radioactive nanospheres (1) that set the radiation ⁇ -rays pass through the mesoporous radioactive nanospheres to irradiate the mesopores (4) to the target cancer cells.
  • the kill rate of cancer cells at the liver-targeted site reached 100%.
  • Nano-targeting carrier layer A nano anti-AIDS or anti-inflammatory drug with radiotherapy function.
  • One DC power supply with 24V voltage with electrodes.
  • the results show that due to coordination
  • the release system has a pH-sensitive release property, and at the same drug concentration, the drug delivery system is more effective in inhibiting cervical HIV than the conventional drug, and at the same time, the anti-AIDS anti-inflammatory drug layer (3A) is treated with chemotherapy.
  • a radioactive nano-sphere (1) capable of emitting alpha-rays as a radioactive substance through a mesoporous radioactive nanosphere-radiating mesoporous (4) combination of target radiotherapy for HIV, from the results of the test
  • 93% of AIDS patients who were simultaneously injected and taken with anti-AIDS targeted drugs containing the novel integrase inhibitors did not detect the virus.
  • anti-AIDS anti-inflammatory drugs experimental example 2 ( Figure 3 for the experimental example).
  • mesoporous radioactive nanospheres (1) mesoporous radioactive nanospheres (1), radiation-proof active metal film layer (22 ⁇ ), metal and organic pollution protection film layer (31), anti-AIDS and anti-inflammatory drug layer (3 ⁇ ), mesoporous radioactive nano-micro A nano-anti-AIDS or anti-inflammatory drug with radiotherapy function consisting of a spherical radiation mesoporous (4), a nano-radiation-proof valve (5), and a nano-targeted carrier layer (6).
  • the surface of the inhibitor molecule is coated with an enzyme-trigger delivery system nano-targeted carrier layer (6) which exhibits a very high new integrase inhibitor loading (800 mg/g) and loading efficiency (60%).
  • the results showed that the synthesized ligand-functionalized drug delivery system was more effectively recognized by hepatic HIV than the unfunctionalized vector, and showed more than conventional drugs and unfunctionalized mesoporous nano drug delivery systems. Effective killing effect on HIV.
  • the anti-AIDS anti-inflammatory drug layer (3A) is treated with the mesoporous radioactive nanospheres (1) that set the radiation beta-rays through the mesoporous radioactive nanospheres to irradiate the mesopores (4) to the target.
  • 90% of AIDS patients who were injected and taken with anti-AIDS targeted drugs containing novel integrase inhibitors were not detected at 48 weeks after treatment.

Abstract

Disclosed are an anti-inflammatory drug against cancer and AIDS with radiotherapy and a preparation method thereof. The drug from inside to outside in sequence consists of radioactive mesoporous nanospheres (1), a radiation-resistant inert metal layer (21A), an optional layer of anti-inflammatory drug against cancer and AIDS (3A), and a nano-targeting carrier layer (6). There are numerous mesoporous radioactive-mesoporous-nanosphere radiation openings (4) and nano radiation-resistant valves (5) on the surface of a radioactive mesoporous nanosphere (1) which are in connection and communication with each other.

Description

说 明 书  Description
一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法 所属技术领域: Anti-cancer anti-AIDS anti-inflammatory drug with radiotherapy and preparation method thereof
一本发明涉及纳米制造、 分子生物抗癌药物和放疗抗癌技术, 具体地说是一 种带放疗的抗癌抗艾滋病抗炎药物及其制备方法。  The invention relates to a nanometer manufacturing, a molecular biological anticancer drug and a radiotherapy anticancer technology, in particular to an anticancer anti-AIDS anti-inflammatory drug with radiotherapy and a preparation method thereof.
技术背景: technical background:
1、 抗癌药物: 目前国内外治疗癌症多采用放疗和化疗、 手术或中医等方法, 医院在肿瘤放射治疗时用的放射性物质, 只是肿瘤病人才会使用, 为了对付肿 瘤, 虽然对身体会有危寄存害, 但两害相权取其轻, 不得不用。 癌症的传统治 疗方法的二次伤害已大于癌症本身, 这一直是困扰现代医学治疗癌症的全球性 难题, 传统抗癌治疗应用一个最大的障碍是在杀灭肿瘤细胞的同时也经常影响 正常组织的细胞, 引起各种各样的并发症。 癌症发病过程癌症亦称恶性肿瘤, 是由控制细胞生长增殖机制失常而引起的疾病。 癌细胞除了生长失控外, 还会 局部侵入周遭正常组织甚至经由体内循环系统或淋巴系统转移到身体其他部 分, 由于癌细胞可发生扩散、 转移或复发, 很多癌症患者往往在花掉大量费用 治疗后换来的一般是 3-5年的存活期, 获得延长的寿命非常有限, 传统抗癌技 术明显存在着对癌症患者治疗的二次伤害大的缺陷和存活期短、 费用高的缺 点,同时,放疗和化疗会导致已经被破坏脏腑功能的癌症患者免疫力大大降低, 为癌症的扩散、 转移和复发埋下了更大隐患, 本技术采用带放疗功能的靶向或 常规抗癌药物, 采用靶向等药物的协同治疗和缓释治疗, 加大治疗的力度, 一 方面, 将传统的放疗造成的皮肤和皮下组织、 器官的损害大大降低, 大大控制 癌细胞的生长速度, 另一方面, 相对地提高患者的免疫力, 为治疗赢得宝贵的 时间, 将扩散或转移的轻度的癌细胞消灭干净的机率大幅度地提高。 1. Anticancer drugs: At present, cancer treatment at home and abroad is often treated by radiotherapy and chemotherapy, surgery or Chinese medicine. The radioactive substances used in hospital radiotherapy are only used by cancer patients. In order to deal with tumors, although there will be Dangerously, but the two evils are light and have to be used. The second treatment of cancer's traditional treatment method is greater than the cancer itself. This has been a global problem that has plagued modern medical treatment of cancer. One of the biggest obstacles to the application of traditional anti-cancer treatment is to kill tumor cells and often affect normal tissues. Cells that cause a variety of complications. Cancer Pathogenesis Cancer, also known as malignant tumor, is a disease caused by the abnormality of the cell growth and proliferation mechanism. In addition to uncontrolled growth, cancer cells can locally invade surrounding normal tissues and even transfer to other parts of the body via the circulatory system or lymphatic system. Because cancer cells can spread, metastasize or recur, many cancer patients often spend a lot of money after treatment. In general, the survival period is 3-5 years, and the extended life expectancy is very limited. Traditional anti-cancer technology has obvious defects of secondary injury to cancer patients, shortcomings of short survival and high cost. Radiotherapy and chemotherapy can lead to greatly reduced immunity of cancer patients who have been destroyed by visceral function, and pose a greater hidden danger for cancer spread, metastasis and recurrence. This technology uses targeted or conventional anticancer drugs with radiotherapy, using targets. Synergistic treatment and sustained-release treatment of other drugs, increasing the intensity of treatment, on the one hand, greatly reducing the damage of skin and subcutaneous tissues and organs caused by traditional radiotherapy, greatly controlling the growth rate of cancer cells, on the other hand, relative Improve the patient's immunity and win valuable for treatment Time, the chance of eradicating the spread or transfer of mild cancer cells is greatly improved.
2、 抗艾滋病和抗炎药物: 目前国内外治疗艾滋病多采用抗艾滋病或抗炎性感 染药物例如: 核苷逆转录酶抑制剂例如齐多夫定、 司他夫定、 去羟肌苷等、 非 核苷逆转录酶抑制剂例如奈韦拉平、 蛋白酶抑制剂例如茚地那韦。 它们以组成 4套国际公认的 "鸡尾酒疗法"方案用来治疗艾滋病, 即齐多夫定 +去羟肌苷 +奈韦拉平、 去羟肌苷 +司他夫定 +奈韦拉平、 齐多夫定 +去羟肌苷+茚地那 韦、 司他夫定 +去羟肌苷 +茚地那韦。 随着研究的深入和发展, 也逐步采用新 型的药物例如侵入和融合抑制剂、 艾滋病中和抗体药物、 整合酶抑制剂、 化学 趋化因子受体拮抗剂和抗艾滋病疫苗等用于艾滋病的治疗, 传统抗艾滋病治疗 应用一个最大的障碍是在艾滋病病毒基因可以发生变异并躲到药物无法杀灭 的地方隐藏起来,那就是即使当抗逆转录病毒药物(antiretroviral drugs , ARVs) 在将体内 HIV清除到血液中难以检邇的水平时,仍有部分病毒在组织中维持了 活性状态, 目前国内外所有的抗艾药物均不能从根本上治愈艾滋病患者, 但可 以有效延长患者的寿命, 这一直是困扰现代医学治疗艾滋病的全球性难题, 本 技术采用带放疗功能的靶向或常规抗艾滋病或抗炎性感染药物, 采用靶向等药 物的协同治疗和缓释治疗, 加大治疗的力度, 一方面, 通过体内循环, 将带放 疗功能的靶向或常规抗艾滋病或抗炎性感染药物输送到含有艾滋病毒的各组 织和器官中, 对艾滋病毒进行杀灭, 另一方面, 通过体液循环杀灭艾滋病毒, 相对地提高患者的免疫力, 为治疗赢得宝贵的时间, 将变异、 扩散、 转移的艾 滋病毒消灭干净的机率大幅度地提高。  2. Anti-AIDS and anti-inflammatory drugs: At present, anti-AIDS or anti-inflammatory drugs such as nucleoside reverse transcriptase inhibitors such as zidovudine, stavudine, didanosine, etc. Non-nucleoside reverse transcriptase inhibitors such as nevirapine, protease inhibitors such as indinavir. They are used to treat AIDS by forming four internationally recognized "cocktail therapies": zidovudine + didanosine + nevirapine, didanosine + stavudine + nevirapine, zidovudine + dehydroxyl Inosine + indinavir, stavudine + didanosine + indinavir. With the deepening and development of research, new drugs such as invasive and fusion inhibitors, AIDS neutralizing antibody drugs, integrase inhibitors, chemical chemokine receptor antagonists and anti-AIDS vaccines are gradually being used for the treatment of AIDS. One of the biggest obstacles to traditional anti-AIDS treatments is that HIV genes can mutate and hide where drugs can't be killed, even when antiretroviral drugs (ARVs) are used to clear HIV in the body. When the level of blood is difficult to detect, some viruses remain active in tissues. At present, all anti-AIDS drugs at home and abroad can not cure AIDS patients fundamentally, but can effectively prolong the life of patients, which has been A global problem that plagues modern medicine for the treatment of AIDS. This technology uses targeted or conventional anti-AIDS or anti-inflammatory infections with radiotherapy, and uses synergistic and sustained-release treatments for targeted drugs to increase the intensity of treatment. In terms of the body, the target with radiotherapy function Transmitting HIV or other anti-inflammatory or anti-inflammatory drugs to HIV-infected tissues and organs to kill HIV. On the other hand, killing HIV through the humoral circulation and relatively improving the patient's immunity, To gain valuable time for treatment, the chances of eliminating variability, spread, and metastasis of HIV have been greatly improved.
发明内容: Summary of the invention:
1、 由内至外依次是介孔放射性纳米微球、 防辐射惰性金属层、 抗癌抗艾滋病 抗炎药物层、 纳米靶向载体层, 也可以取消抗癌抗艾滋病抗炎药物层; 介孔放 射性纳米微球表面有众多的介孔放射性纳米微球辐射介孔口和纳米防辐射阀 门, 纳米防辐射阀门与介孔放射性纳米微球辐射介孔口相连接连通; 介孔放射 性纳米微球可分别采用放射性材料加内部介孔通道添加抗癌抗艾滋病抗炎药 物的方式和纯放射性材料的方式制作。 1. From the inside to the outside, mesoporous radioactive nanospheres, anti-radiation inert metal layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-AIDS anti-inflammatory drug layer can also be eliminated; mesopores Put The surface of the radioactive nanospheres has a plurality of mesoporous radioactive nanospheres radiating mesopores and nano anti-radiation valves, and the nano anti-radiation valve is connected with the mesoporous radioactive nanospheres radiation mesopores; mesoporous radioactive nanospheres It can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
2、 由内至外依次是介孔放射性纳米微球、 吸波膜层、 抗癌抗艾滋病抗炎药物 层、 纳米靶向载体层, 也可以取消抗癌抗艾滋病抗炎药物层; 介孔放射性纳米 微球表面有众多的介孔放射性纳米微球辐射介孔口和纳米防辐射阀门, 纳米防 辐射阔门与介孔放射性纳米微球辐射介孔口相连接连通; 介孔放射性纳米微球 可分别采用放射性材料加内部介孔通道添加抗癌抗艾滋病抗炎药物的方式和 纯放射性材料的方式制作。  2. From the inside to the outside, mesoporous radioactive nanospheres, absorbing membrane layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-AIDS anti-inflammatory drug layer can also be eliminated; mesoporous radioactivity The surface of the nanosphere has a plurality of mesoporous radioactive nanospheres radiating mesopores and a nanometer radiation protection valve, and the nanometer radiation shielding gate is connected with the mesoporous radioactive nanospheres radiation mesopores; the mesoporous radioactive nanospheres can be They were made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
3、 由内至外依次是介孔放射性纳米微球、 防辐射活跃金属膜层、 防金属和有 机物污染保护膜层、 抗癌抗艾滋病抗炎药物层、 纳米靶向载体层, 也可以取消 抗癌抗艾滋病抗炎药物层; 介孔放射性纳米微球表面有众多的介孔放射性纳米 微球辐射介孔口和纳米防辐射阀门, 纳米防辐射阀门与介孔放射性纳米微球辐 射介孔口相连接连通; 介孔放射性纳米微球可分别采用放射性材料加内部介孔 通道添加抗癌抗艾滋病抗炎药物的方式和纯放射性材料的方式制作。  3. From the inside to the outside, there are mesoporous radioactive nanospheres, anti-radiation active metal film layer, metal and organic pollution protection film layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and can also eliminate the anti-antibody Cancer anti-AIDS anti-inflammatory drug layer; mesoporous radioactive nanospheres have numerous mesoporous radioactive nanospheres radiation mesopores and nano anti-radiation valves, nano anti-radiation valves and mesoporous radioactive nanospheres radiation mesoporous phase Connected and connected; mesoporous radioactive nanospheres can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
4、 由内至外依次是介孔放射性纳米微球、 吸波膜层、 防金属和有机物污染保 护膜层、 抗癌抗艾滋病抗炎药物层、 纳米靶向载体层, 也可以取消抗癌抗艾滋 病抗炎药物层; 当吸波膜层采用无毒无生物反应的材料时, 取消防金属和有机 物污染保护膜层; 介孔放射性纳米微球表面有众多的介孔放射性纳米微球辐射 介孔口和纳米防辐射阀门, 纳米防辐射阔门与介孔放射性纳米微球辐射介孔口 相连接连通; 介孔放射性纳米微球可分别采用放射性材料加内部介孔通道添加 抗癌抗艾滋病抗炎药物的方式和纯放射性材料的方式制作。  4. From the inside to the outside, there are mesoporous radioactive nanospheres, absorbing membrane layer, metal and organic pollution protection membrane layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-cancer AIDS anti-inflammatory drug layer; when the absorbing membrane layer adopts non-toxic and non-bioreactive materials, the protective film layer against metal and organic pollution is removed; the mesoporous radioactive nanospheres have numerous mesoporous radioactive nanospheres radiating mesopores The mouth and nano radiation protection valve, the nano radiation protection wide door is connected with the mesoporous radioactive nano microsphere radiation mesoporous mouth; the mesoporous radioactive nano microsphere can be added with anti-cancer anti-AIDS anti-inflammatory by using radioactive material and internal mesoporous channel respectively The way the drug is made and the way the pure radioactive material is made.
5、 由内至外依次是介孔放射性纳米微球、 放射性金属膜层、 防辐射层、 抗癌 抗艾滋病抗炎药物层、纳米靶向载体层,也可以取消抗癌抗艾滋病抗炎药物层; 介孔放射性纳米微球表面有众多的介孔放射性纳米微球辐射介孔口和纳米防 辐射阀门, 纳米防辐射阀门与介孔放射性纳米微球辐射介孔口相连接连通; 介 孔放射性纳米微球可分别采用放射性材料加内部介孔通道添加抗癌抗艾滋病 抗炎药物的方式和纯放射性材料的方式制作。 5. From the inside to the outside, mesoporous radioactive nanospheres, radioactive metal film layer, anti-radiation layer, anti-cancer The anti-AIDS anti-inflammatory drug layer and the nano-targeting carrier layer can also eliminate the anti-cancer anti-AIDS anti-inflammatory drug layer; the mesoporous radioactive nanospheres have numerous mesoporous radioactive nano-microsphere radiation mesopores and nano anti-radiation valves. The nano-radiation-proof valve is connected with the mesoporous radioactive nano-microsphere radiation mesopores; the mesoporous radioactive nano-spheres can be supplemented with radioactive materials and internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials. Way of making.
本发明所要解决的技术问题: Technical problems to be solved by the present invention:
克服现有癌症、艾滋病毒和炎症的治疗方法的二次伤害大和存活期短以及 费用高的不足, 本技术采用带放疗功能的靶向或常规抗癌抗艾滋病抗炎药物, 采用靶向等药物的协同治疗和缓释治疗, 加大治疗的力度, 达到 "将传统的放 疗造成的皮肤和皮下组织、 器官的损害大大降低, 大大控制癌细胞、 艾滋病毒 和炎症的生长速度, 相对地提高患者的免疫力, 为治疗赢得宝贵的时间, 将现 有难治的癌细胞、 艾滋病毒和炎症或扩散或转移的轻度的癌细胞艾滋病毒和炎 症也消灭干净的机率大幅度地提高"的良好效果。  Overcoming the secondary injury, short survival time and high cost of existing cancer, HIV and inflammation treatment methods, this technology uses targeted or conventional anti-cancer anti-inflammatory drugs with radiotherapy function, using targeted drugs Synergistic treatment and sustained-release treatment, increase the intensity of treatment, to achieve "significant reduction of skin and subcutaneous tissues and organs caused by traditional radiotherapy, greatly control the growth rate of cancer cells, HIV and inflammation, and relatively improve patients The immunity, for the treatment to win valuable time, the existing refractory cancer cells, HIV and inflammation or the spread or metastasis of mild cancer cells HIV and inflammation also eliminate the chance of a clean increase "good effect.
本发明的技术要求是这样的: The technical requirements of the present invention are as follows:
1)、 介孔放射性纳米微球可单独采用天然或人造的可以从原子核内部放出粒子 或射线 (如 α射线、 3射线、 Υ射线等) 的放射性材料, 例如放射能量大是铀 (U) 、 钍 (Th) 和镭(Ra) , 或钾- 40 (40K) , 铷(Rb)和铯 (Cs ) 等, 或 放射性材料与陶瓷粉末等的混合, 并根据实际病情需要确定所需的放射性物质 的种类。  1) Mesoporous radioactive nanospheres can be made of natural or artificial radioactive materials that can release particles or rays (such as alpha rays, 3 rays, xenon rays, etc.) from inside the nucleus. For example, the radiant energy is uranium (U).钍 (Th) and radium (Ra), or potassium - 40 (40K), 铷 (Rb) and 铯 (Cs), etc., or a mixture of radioactive materials and ceramic powder, and determine the required radioactive material according to actual conditions. kind of.
3、 为保证本药物在血液和身体中的正常流动和渗透, 药物调制后的比重浓度 最好与血液相吻合, 例如比重最好不超过血液的比重 1. 05, 以免发生沉淀。  3. In order to ensure the normal flow and penetration of the drug in the blood and body, the specific gravity concentration of the drug after preparation is preferably consistent with the blood, for example, the specific gravity does not exceed the specific gravity of the blood 1. 05, so as to avoid precipitation.
4) 、 为达到较好的防辐射效果, 防辐射活跃金属膜层或吸波膜层例如采用铅 材料时, 厚度最好厚于 23微米。 5 ) 、 为避免与身体组织发生反应, 防辐射惰性金属或吸波膜层可采用各种具 有防辐射的惰性金属例如金或银或硅胶吸收波材料。 4) In order to achieve better radiation protection, when the radiation-proof active metal film layer or the absorbing film layer is made of, for example, a lead material, the thickness is preferably thicker than 23 μm. 5) In order to avoid reaction with body tissues, the radiation-proof inert metal or absorbing layer may be made of various radiation-proof inert metals such as gold or silver or silica gel.
6 ) 、 纳米防辐射阀门的准轮垸或轮垸 "阀芯", 最好采用具备防辐射的材料 例如金属或硅材料等。  6), quasi-rim or rim "spool" of nano anti-radiation valve, preferably with radiation-proof materials such as metal or silicon.
7 ) 、 为了防止本药物的体积的均匀以增加疗效, 可以对药物的溶液进行设定 孔径的过滤。  7) In order to prevent the volume of the drug from being uniform to increase the therapeutic effect, the solution of the drug can be filtered by a set aperture.
8 ) 、 为发生个别的药物有可能无法完全在规定时间内通过新陈代谢排出体外, 可以通过血液透析的方法滤除, 必要时, 可以在过滤膜和介孔放射性纳米微球 均增加磁性物质, 通过磁吸等方法更好地滤除。  8), in order to occur, individual drugs may not be completely excreted by metabolism within the specified time, and may be filtered by hemodialysis. If necessary, magnetic substances may be added to both the filter membrane and the mesoporous radioactive nanospheres. Magnetic absorption and other methods are better filtered.
9 ) 、 抗癌抗艾滋病抗炎药物层可以是靶向或常规药物层。  9) The anti-cancer anti-AIDS anti-inflammatory drug layer may be a targeted or conventional drug layer.
本发明解决技术问题所采用的技术方案: The technical solution adopted by the present invention to solve the technical problem:
1、 由内至外依次是介孔放射性纳米微球、 防辐射惰性金属层、 抗癌抗艾滋 病抗炎药物层、 纳米靶向载体层, 也可以取消抗癌抗艾滋病抗炎药物层; 介孔 放射性纳米微球表面有众多的介孔放射性纳米微球辐射介孔口和纳米防辐射 阀门, 纳米防辐射阀门与介孔放射性纳米微球辐射介孔口相连接连通; 介孔放 射性纳米微球可分别采用放射性材料加内部介孔通道添加抗癌抗艾滋病抗炎 药物的方式和纯放射性材料的方式制作。  1. From the inside to the outside, mesoporous radioactive nanospheres, anti-radiation inert metal layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-AIDS anti-inflammatory drug layer can also be eliminated; mesopores The surface of the radioactive nanospheres has a plurality of mesoporous radioactive nanospheres radiating mesopores and nano anti-radiation valves, and the nano anti-radiation valve is connected with the mesoporous radioactive nanospheres radiation mesopores; the mesoporous radioactive nanospheres can be They were made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
2、 由内至外依次是介孔放射性纳米微球、 吸波膜层、 抗癌抗艾滋病抗炎药物 层、 纳米靶向载体层, 也可以取消抗癌抗艾滋病抗炎药物层; 介孔放射性纳米 微球表面有众多的介孔放射性纳米微球辐射介孔口和纳米防辐射阀门, 纳米防 辐射阀门与介孔放射性纳米微球辐射介孔口相连接连通; 介孔放射性纳米微球 可分别采用放射性材料加内部介孔通道添加抗癌抗艾滋病抗炎药物的方式和 纯放射性材料的方式制作。 3、 由内至外依次是介孔放射性纳米微球、 防辐射活跃金属膜层、 防金属和有 机物污染保护膜层、 抗癌抗艾滋病抗炎药物层、 纳米靶向载体层, 也可以取消 抗癌抗艾滋病抗炎药物层; 介孔放射性纳米微球表面有众多的介孔放射性纳米 微球辐射介孔口和纳米防辐射阀门, 纳米防辐射阀门与介孔放射性纳米微球辐 射介孔口相连接连通; 介孔放射性纳米微球可分别采用放射性材料加内部介孔 通道添加抗癌抗艾滋病抗炎药物的方式和纯放射性材料的方式制作。 2. From the inside to the outside, mesoporous radioactive nanospheres, absorbing membrane layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-AIDS anti-inflammatory drug layer can also be eliminated; mesoporous radioactivity The surface of the nanosphere has a plurality of mesoporous radioactive nanospheres radiating mesopores and a nanometer radiation protection valve, and the nanometer radiation protection valve is connected with the mesoporous radioactive nanospheres radiation mesopores; the mesoporous radioactive nanospheres can be separately It is made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials. 3. From the inside to the outside, there are mesoporous radioactive nanospheres, anti-radiation active metal film layer, metal and organic pollution protection film layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and can also eliminate the anti-antibody Cancer anti-AIDS anti-inflammatory drug layer; mesoporous radioactive nanospheres have numerous mesoporous radioactive nanospheres radiation mesopores and nano anti-radiation valves, nano anti-radiation valves and mesoporous radioactive nanospheres radiation mesoporous phase Connected and connected; mesoporous radioactive nanospheres can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
4、 由内至外依次是介孔放射性纳米微球、 吸波膜层、 防金属和有机物污染保 护膜层、 抗癌抗艾滋病抗炎药物层、 纳米靶向载体层, 也可以取消抗癌抗艾滋 病抗炎药物层; 当吸波膜层采用无毒无生物反应的材料时, 取消防金属和有机 物污染保护膜层; 介孔放射性纳米微球表面有众多的介孔放射性纳米微球辐射 介孔口和纳米防辐射阀门, 纳米防辐射阀门与介孔放射性纳米微球辐射介孔口 相连接连通; 介孔放射性纳米微球可分别采用放射性材料加内部介孔通道添加 抗癌抗艾滋病抗炎药物的方式和纯放射性材料的方式制作。  4. From the inside to the outside, there are mesoporous radioactive nanospheres, absorbing membrane layer, metal and organic pollution protection membrane layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-cancer AIDS anti-inflammatory drug layer; when the absorbing membrane layer adopts non-toxic and non-bioreactive materials, the protective film layer against metal and organic pollution is removed; the mesoporous radioactive nanospheres have numerous mesoporous radioactive nanospheres radiating mesopores The mouth and nano anti-radiation valve, the nano anti-radiation valve is connected with the mesoporous radioactive nano-microsphere radiation mesopores; the mesoporous radioactive nano-spheres can be added with anti-cancer anti-inflammatory drugs by radioactive materials and internal mesoporous channels, respectively. The way and the way of purely radioactive materials are produced.
5、 由内至外依次是介孔放射性纳米微球、 放射性金属膜层、 防辐射层、 抗癌 抗艾滋病抗炎药物层、纳米靶向载体层,也可以取消抗癌抗艾滋病抗炎药物层; 介孔放射性纳米微球表面有众多的介孔放射性纳米微球辐射介孔口和纳米防 辐射阀门, 纳米防辐射阀门与介孔放射性纳米微球辐射介孔口相连接连通; 介 孔放射性纳米微球可分别采用放射性材料加内部介孔通道添加抗癌抗艾滋病 抗炎药物的方式和纯放射性材料的方式制作。 5. From the inside to the outside, mesoporous radioactive nanospheres, radioactive metal film layer, radiation protection layer, anti-cancer anti-inflammatory anti-inflammatory drug layer, nano-targeting carrier layer, and anti-cancer anti-AIDS anti-inflammatory drug layer can also be eliminated. The mesoporous radioactive nanospheres have a plurality of mesoporous radioactive nanospheres radiating mesopores and nanometer radiation protection valves, and the nanometer radiation protection valve is connected with the mesoporous radioactive nanospheres radiation mesopores; mesoporous radioactive nanometers; Microspheres can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs and pure radioactive materials.
实现本发明的一些具体方式和要求: Some specific ways and requirements for implementing the invention:
1、 介孔放射性纳米微球的介孔道尺寸最好控制在 2〜50nm范围。  1. The mesoporous size of mesoporous radioactive nanospheres is preferably controlled in the range of 2 to 50 nm.
2、 介孔放射性纳米微球与纳米防辐射阔门的聚合可采用组装或其他化学方法 组装, 但最好采用自组装方式, 以实现大批量生产。 3、 介孔放射性纳米微球可采用放射性材料加内部介孔通道添加抗癌抗艾滋病 抗炎药物的方式或单独采用纯放射性材料的方式制作. 2. The polymerization of mesoporous radioactive nanospheres and nano-radiation-proof wide doors can be assembled by assembly or other chemical methods, but self-assembly is preferred to achieve mass production. 3. Mesoporous radioactive nanospheres can be prepared by adding radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs or pure radioactive materials.
本发明产生的有益效果为: The beneficial effects produced by the present invention are:
克服现有癌症、 艾滋病毒和炎症的治疗方法的二次伤害大和存活期短以及 费用高的不足, 本技术采用带放疗功能的靶向或常规抗癌抗艾滋病抗炎药物, 采用靶向等药物的协同治疗和缓释治疗, 加大治疗的力度, 达到 "将传统的放 疗造成的皮肤和皮下组织、 器官的损害大大降低, 大大控制癌细胞、 艾滋病毒 和炎症的生长速度, 相对地提高患者的免疫力, 为治疗赢得宝贵的时间, 将现 有难治的癌细胞、 艾滋病毒和炎症或扩散或转移的轻度的癌细胞艾滋病毒和炎 症也消灭干净的机率大幅度地提高"的良好效果。  Overcoming the current secondary cancer, HIV and inflammation treatments with secondary damage and short survival and high cost, this technology uses targeted or conventional anti-cancer anti-inflammatory drugs with radiotherapy, targeting drugs Synergistic treatment and sustained-release treatment, increase the intensity of treatment, to achieve "significant reduction of skin and subcutaneous tissues and organs caused by traditional radiotherapy, greatly control the growth rate of cancer cells, HIV and inflammation, and relatively improve patients The immunity, for the treatment to win valuable time, the existing refractory cancer cells, HIV and inflammation or the spread or metastasis of mild cancer cells HIV and inflammation also eliminate the chance of a clean increase "good effect.
附图说明: BRIEF DESCRIPTION OF THE DRAWINGS:
图 1为本实用新型的剖视图和简图。 Figure 1 is a cross-sectional view and a schematic view of the present invention.
如图所示 : 1、 介孔放射性纳米微球, 21A、 防辐射惰性金属层, 3A、 抗癌抗艾 滋病抗炎药物层, 4、 介孔放射性纳米微球辐射介孔口, 5、 纳米防辐射阀门, 5A、 准轮烷或轮垸 "阀芯", 6、 纳米靶向载体层。 As shown in the figure: 1, mesoporous radioactive nanospheres, 21A, radiation-proof inert metal layer, 3A, anti-cancer anti-AIDS anti-inflammatory drug layer, 4, mesoporous radioactive nanospheres radiation mesopores, 5, nano-anti Radiation valve, 5A, quasi-rotaxane or rim "spool", 6, nano-targeting carrier layer.
图 2为本实用新型的剖视图。 Figure 2 is a cross-sectional view of the present invention.
如图所示 : 1、 介孔放射性纳米微球, 21B、 吸波膜层, 3A、 抗癌抗艾滋病抗炎 药物层, 4、 介孔放射性纳米微球辐射介孔口, 5、 纳米防辐射阀门, 5A、 准轮 烷或轮烷"阀芯", 6、 纳米靶向载体层。 As shown in the figure: 1, mesoporous radioactive nanospheres, 21B, absorbing membrane layer, 3A, anti-cancer anti-AIDS anti-inflammatory drug layer, 4, mesoporous radioactive nanospheres radiation mesopores, 5, nano-radiation Valve, 5A, pseudorotaxane or rotaxane "spool", 6, nano-targeting carrier layer.
图 3为本实用新型的剖视图。 Figure 3 is a cross-sectional view of the present invention.
如图所示 : 1、 介孔放射性纳米微球, 22A、 防辐射活跃金属膜层, 31、 防金属 和有机物污染保护膜层, 3A、 抗癌抗艾滋病抗炎药物层, 4、 介孔放射性纳米 微球辐射介孔口, 5、 纳米防辐射阀门, 5A、 准轮烷或轮烷 "阀芯", 6、 纳米靶 向载体层。 As shown in the figure: 1. Mesoporous radioactive nanospheres, 22A, radiation-proof active metal film layer, 31, metal and organic pollution protection film layer, 3A, anti-cancer anti-AIDS anti-inflammatory drug layer, 4. Mesoporous radioactivity Nano Microsphere radiation mesopores, 5, nano anti-radiation valve, 5A, quasi-rotaxane or rotaxane "spool", 6, nano-targeting carrier layer.
图 4为本实用新型的剖视图。 如图所示:1、 介孔放射性纳米微球, 21B、 吸波膜层, 31、 防金属和有机物污 染保护膜层, 3A、 抗癌抗艾滋病抗炎药物层, 4、 介孔放射性纳米微球辐射介 孔口, 5、 纳米防辐射阀门, 5A、 准轮垸或轮烷 "阀芯", 6、 纳米靶向载体层。 图 5为本实用新型的剖视图。 Figure 4 is a cross-sectional view of the present invention. As shown in the figure: 1, mesoporous radioactive nanospheres, 21B, absorbing membrane layer, 31, metal and organic pollution protection membrane layer, 3A, anti-cancer anti-AIDS anti-inflammatory drug layer, 4, mesoporous radioactive nano-micro Ball radiation mesopores, 5, nano anti-radiation valve, 5A, quasi-rim or rotaxane "spool", 6, nano-targeting carrier layer. Figure 5 is a cross-sectional view of the present invention.
如图所示: 1、介孔放射性纳米微球, 23、 放射性金属膜层, 32、 防辐射层, 3A、 抗癌抗艾滋病抗炎药物层, 4、 介孔放射性纳米微球辐射介孔口, 5、 纳米防辐 射阔门, 5A、 准轮烷或轮烷 "阀芯", 6、 纳米靶向载体层。 As shown in the figure: 1. Mesoporous radioactive nanospheres, 23, radioactive metal film layer, 32, radiation protection layer, 3A, anti-cancer anti-AIDS anti-inflammatory drug layer, 4. Mesoporous radioactive nano-microsphere radiation mesopores 5, nano-radiation wide door, 5A, quasi-rotaxane or rotaxane "spool", 6, nano-targeting carrier layer.
图 6是纳米防辐射阀门 (5 )其中之一结构的防辐射金属簇为核心的准轮烷等 超分子结构图。 Fig. 6 is a super-molecular structure diagram of a pseudo-rotaxane in which a radiation-proof metal cluster of one of the structures of the nano-radiation-proof valve (5) is a core.
4、 介孔放射性纳米微球辐射介孔口, 5A、 准轮垸或轮烷 "阔芯"。  4, mesoporous radioactive nanospheres radiation mesopores, 5A, quasi-rims or rotaxes "wide core".
具体实施方式: 下面结合附图和及一个优选实施例叙述本发明实施例 1 : 图 1和图 2分别是一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法的结构剖 视宏观放大图: DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS Hereinafter, Embodiment 1 of the present invention will be described with reference to the accompanying drawings and a preferred embodiment: FIG. 1 and FIG. 2 are respectively a structural enlarged cross-sectional view of an anti-cancer anti-inflammatory anti-inflammatory drug with radiotherapy and a preparation method thereof. Figure:
(一) 、 一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法简略制备过程: 第 1步: 制成表面具有防辐射金属离子的纳米防辐射阀门 (5 ) 功能基的介孔放 射性纳米微球 (1 ) :  (1) An anti-cancer, anti-inflammatory and anti-inflammatory drug with radiotherapy and a preparation method thereof. Brief preparation process: Step 1: Preparation of a nano-radiation-proof valve with a radiation-proof metal ion on the surface (5) Functional mesoporous radioactivity Nanospheres (1):
以放射性材料例如天然或人造的可以从原子核内部放出粒子或射线 (如 d 射线、 β射线、 Υ射线等)的铀(U)、钍(Th)和镭(Ra) , 或钾 -40 (40K) , 铷 (Rb) 和铯(Cs ) 等放射性材料和二氧化硅混合材料或单独的放射性材料为 基材, 采用化学或生物合成或机械等方法例如共沉淀法、 溶胶凝胶法、 分散聚 合法或可控自由基聚合法合成尺寸均一、 较大孔容 (例如 0. 6-5cm3/g) ,高比表 面积 (例如 700- -1500 m2/g), 孔墙壁高密度修饰的放射性介孔放射性纳米微球 ( 1 ) , 例如: 可采用以下几种方法制备, 等等, Radioactive materials such as natural or artificial uranium (U), thorium (Th) and radium (Ra), or potassium-40 (40K) that emit particles or rays (such as d-rays, beta rays, xenon rays, etc.) from inside the nucleus. ) , Radioactive materials such as lanthanum (Rb) and lanthanum (Cs) and silica hybrid materials or individual radioactive materials are used as substrates, by chemical or biosynthetic or mechanical methods such as coprecipitation, sol-gel, dispersion polymerization or Controlled free radical polymerization to synthesize uniform size, large pore volume (for example, 0. 6-5cm3/g), high specific surface area (for example, 700--1500 m2/g), high-density modified radioactive mesoporous radioactive nanometer Microspheres (1), for example: can be prepared by the following methods, etc.
方法 1 ) 、 把碳酸鈣和镭放射性材料混合后机械磨细的粉末达到纳米尺寸 加进去, 凝胶去溶剂后用稀酸洗出来。  Method 1) After mixing the calcium carbonate and radium radioactive materials, the mechanically ground powder is added to the nanometer size, and the gel is desolvated and washed with dilute acid.
方法 2)、 制备方法包括用共沉淀法制备放射性粒子; 再将洗好的放射性 粒子直接分散到含 Si02的水溶性无机盐的水溶液中进行无机硅源包覆或混合; 然后以十六烷基三甲基溴化铵为模板剂、 正硅酸乙酯为硅源进行介孔二氧化硅 包覆或混合。  Method 2), the preparation method comprises: preparing radioactive particles by coprecipitation; then dispersing the washed radioactive particles directly into an aqueous solution of a SiO2-containing water-soluble inorganic salt for coating or mixing with an inorganic silicon source; Trimethylammonium bromide is used as a templating agent, and tetraethyl orthosilicate is a silicon source for mesoporous silica coating or mixing.
方法 3)、 采用次磷酸钠液相还原方法制备了纳米镭溶胶, 再以正硅酸乙 酯为硅源, 十六烷基三甲基溴化铵为模板剂, 采用溶胶-凝胶法, 在制备的纳 米镭溶胶中的镭颗粒表面原位生长二氧化硅球壳, 然后利用溶剂萃取法去除有 机模板剂, 再经超临界干燥后制备出介孔二氧化硅包覆镭纳米颗粒。  Method 3), using a sodium hypophosphite liquid phase reduction method to prepare a nano-ray sol, and then using tetraethyl orthosilicate as a silicon source, cetyltrimethylammonium bromide as a template, using a sol-gel method, The silica spherical shell was grown in situ on the surface of the radium particles in the prepared nano-laser sol, and then the organic template was removed by solvent extraction, and the mesoporous silica-coated radium nanoparticles were prepared by supercritical drying.
方法 4)、 如获得专利号为 03153265, 名称为 "一种微米球形介孔二氧化 硅的制备方法", 专利权人为 "中国科学院理化技术研究所"的授权, 可以采 取如下方法步骤制备, 内容包括: ( 1 )配制酸溶液,酸的浓度为 Q . 0 1〜 1 0摩尔 /升; 2 ) 向步骤( 1 ) 的溶液中加入表面活性剂, 使得混合溶液中 十六烷基三甲基卤化铵的浓度为 0 . 0 0 1〜5摩尔 /升, 聚乙烯醇的浓度为 0 . 0 1〜 2 0克 /升, 聚 (氧乙烯) 一聚 (氧丙烯) 一聚(氧乙烯) 的浓度 为 1 1 0 † [― 6 ] 〜 5 1 0 † [— 3 ]摩尔 /升; ( 3 )将硅酸酯加入步骤 ( 2 )得到的混合溶液中,使混合后的硅酸酯的浓度为 0 . 0 1〜 5摩尔 /升, 继续搅拌, 静置, 得白色沉淀的溶液, 离心分离、 洗涤、 干燥, 焙烧, 得到介 孔二氧化硅, 之后, 再将镭材料纳米粉末化, 然后再混合, 得到含有镭元素的 二氧化硅混合物。 Method 4), if the patent number is 03153265, the name is "a preparation method of a micrometer spherical mesoporous silica", and the patentee is authorized by the "Institute of Physical and Chemical Technology of the Chinese Academy of Sciences", and can be prepared by the following method steps, The method comprises the following steps: (1) preparing an acid solution, the concentration of the acid is Q. 0 1~10 mol/L; 2) adding a surfactant to the solution of the step (1), so that the cetyltrimethyl group in the mixed solution The concentration of ammonium halide is 0. 0 0 1~5 mol / liter, the concentration of polyvinyl alcohol is 0. 0 1~ 2 0 g / liter, poly (oxyethylene) poly(oxypropylene) poly(oxyethylene) The concentration is 1 10 † [― 6 ] ~ 5 1 0 † [-3] mol / liter; (3) the silicate is added to the mixed solution obtained in the step (2) to make the mixed silicate The concentration is 0. 0 1~5 mol / liter, stirring is continued, and the solution is allowed to stand to obtain a white precipitated solution, which is centrifuged, washed, dried, and calcined to obtain a medium. The silica is then pulverized, and then the radium material is nano-pulverized and then mixed to obtain a silica mixture containing radium.
介孔放射性纳米微球(1 ) 制备以后, 再将介孔放射性纳米微球 (1 ) 内 部的介孔表面成功嫁接或物理吸附抗癌抗艾滋病抗炎药物, 制备负载了抗癌抗 艾滋病抗炎药物的孔放射性纳米微球(1 ) ; 介孔放射性纳米微球(1 ) 可釆用 放射性材料加内部介孔通道添加抗癌抗艾滋病抗炎药物的方式或单独采用纯 放射性材料的方式制作。  After preparation of the mesoporous radioactive nanospheres (1), the mesoporous surface inside the mesoporous radioactive nanospheres (1) is successfully grafted or physically adsorbed against the anti-cancer anti-inflammatory drugs, and the anti-cancer, anti-AIDS and anti-inflammatory drugs are prepared. The drug's pore radioactive nanospheres (1); mesoporous radioactive nanospheres (1) can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs or pure radioactive materials.
由于金属离子之间和金属与配位体配位键很强或非常强, 成为驱动超分子 自组装的作用力, 通过共聚、 表面改性和超分子自组装等方法, 将含有银金属 或硅分子等超分子的结构和功能的组分或建筑模块按照设计的方式组装成新 的超分子化合物, 通过金属与金属分子之间相互作用或成键得到表面具有防辐 射金属离子的纳米防辐射阀门 (5 ) 功能基的介孔放射性纳米微球(1 ) , 可 直接结合带有, 也可经过化学修饰后再结合得到。 例如采用统计学缠绕、 化学 转移、 受氢键驱动、 受亲水-疏水相互作用驱动、 受金属配位作用驱动、 和受 π - π堆积相互作用以及电荷转移驱动、 穿线封端法、 快速溶剂挥发法等方法 例如:以下方法得到表面具有防辐射金属离子的纳米防辐射阀门 (5 ) 功能基的 金属轮垸或具有放疗功能的的纳米放射性材料阀门 (5 )功能基的金属轮垸, 例如 (1 ): 以可代替 X射线用来治疗癌症和艾滋病的人工放射性同位素钴 60为 例, 由葫芦脲 cucurbituri l和精胺盐酸盐生成的类轮烷, 与水合烷基钴肟发生 自组装反应后,在水溶液中形成了一种新型的金属轮垸; 再例如 (2 ) : 可参考 中国清华大学化学系王梅祥教授和赵亮副教授课题组成功地发展出一种利用 金属簇作为配位核心开展自组装的新方法(如他们或单位已经申请专利则需要 获得专利权人的许可),具体是:利用防辐射金属簇作为配位核心开展自组装, 即: 利用阴离子型有机配体指导调控防辐射金属簇的合成, 然后用大环化合物 与防辐射金属簇配位, 产生具有特定配位方向的防辐射金属簇组装体, 然后再 以其他的配体作为连接子, 从而获得防辐射金属簇为核心的准轮垸、 锁烃等超 分子结构; 例如 (3): 利用金属离子作为模板或在轮烷、 索烃等超分子体系中 引入金属离子及其配合物,合成了很多种金属轮烷、 索烃等新型超分子。 通过 自组装等方法将银金属等超分子准轮垸或轮垸构筑在介孔放射性纳米微球( 1 ) 表面, 构成以功能化纳米硅或纳米银为线轴分子, 银金属等超分子可在线轴 上滑动的超分子纳米防辐射阀门 (5) , 控制释放与开关的新功能, 从而得到 表面具有防辐射金属离子的纳米防辐射阀门 (5) 功能基的介孔放射性纳米微 球 (1 ) , 通过 pH和竞争结合双通道等驱动银金属等超分子纳米阀的控制释放, 满足设定条件的多种释放和开关需求。 以介孔放射性纳米微球 (1 ) 为纳米容 器, 纳米靶向载体层 (6)例如氨基酸脱羧酶引发的银金属等超分子纳米阀的 控制释放,该输运体系具有生物靶向和开关功能,并且能够多步按需控制释放。 在外界电、 光、 磁、 声的作用和控制下, 纳米防辐射阀门 (5) 的开关被自动 打开, 介孔放射性纳米微球(1 ) 内部的抗癌抗艾滋病抗炎药物通过介孔放射 性纳米微球辐射介孔口 (4) 向外缓释, 对癌组织癌细胞、 艾滋病毒和炎症进 行 "化疗"杀灭; 纳米防辐射阀门 (5) 的开关被自动打开的同时, 介孔放射 性纳米微球(1 )内部的放射线在外界通过介孔放射性纳米微球辐射介孔口(4) 对外辐射, 对靶点的癌组织的癌细胞、 艾滋病毒和炎症进行 "放疗"杀灭; 另 一方面, 抗癌抗艾滋病抗炎药物层 (3A)对靶点的癌组织癌细胞、 艾滋病毒和 炎症化疗或中药治疗进行常规快速杀灭; 上述过程是放疗和化疗单独或同时进 行。 Due to the strong or very strong coordination bond between metal ions and metal and ligand, it becomes the driving force for self-assembly of supramolecules. It will contain silver metal or silicon by copolymerization, surface modification and supramolecular self-assembly. The structural and functional components or building blocks of molecules such as molecules are assembled into new supramolecular compounds in a designed manner, and nano-radiation-proof valves with anti-radiation metal ions on the surface are obtained by interaction or bonding between metal and metal molecules. (5) Functionally based mesoporous radioactive nanospheres (1), which can be directly bound or obtained by chemical modification. For example, using statistical entanglement, chemical transfer, hydrogen bond driving, driven by hydrophilic-hydrophobic interactions, driven by metal coordination, and driven by π-π stacking and charge transfer, threading end capping, fast solvent A method such as a volatilization method, for example, a metal rim having a function of a nano-radiation-proof valve (5) having a radiation-proof metal ion on the surface or a metal rim having a function of a nano-radioactive material (5) having a radiotherapy function, for example, (1): Taking the artificial radioisotope cobalt 60, which can replace X-rays for the treatment of cancer and AIDS, as an example, the rotaxane produced by cucurbituril and spermine hydrochloride is self-assembled with hydrated alkyl cobalt ruthenium. After the reaction, a new type of metal rim is formed in the aqueous solution; for example, (2): Reference can be made to Professor Wang Meixiang and Associate Professor Zhao Liang of the Department of Chemistry, Tsinghua University, China, to develop a metal cluster as a coordination core. New methods of self-assembly (if they or the unit has applied for a patent, they need to obtain the license of the patentee), specifically: use Radiation metal cluster core conduct self-assembly as a ligand, namely: synthetic anionic organic ligand radiation regulatory guidance metal clusters, then macrocycle Coordination with a radiation-proof metal cluster to produce a radiation-proof metal cluster assembly having a specific coordination direction, and then using other ligands as a linker, thereby obtaining a quasi-rim, a hydrocarbon-locking, etc. with a radiation-proof metal cluster as a core Molecular structure; for example, (3): The use of metal ions as a template or the introduction of metal ions and their complexes in supermolecular systems such as rotaxanes and hydrocarbons has synthesized a variety of novel supermolecules such as metal rotaxanes and hydrocarbons. The supermolecular quasi-rim or rim of silver metal is constructed on the surface of mesoporous radioactive nanospheres (1) by means of self-assembly, etc., and functionalized nano-silica or nano-silver is used as a bobbin molecule, and super-molecules such as silver metal can be online. A supramolecular nano-radiation-proof valve (5) that slides on the shaft, controls the release and the new function of the switch, thereby obtaining a mesoporous radioactive nanosphere (1) with a functional anti-radiation metal ion on the surface of the nano-radiation-proof valve (5) Controlled release of supramolecular nanovalves such as silver metal by pH and competition combined with dual channels, etc., to meet various release and switching requirements of the set conditions. The mesoporous radioactive nanospheres (1) are nano-containers, and the nano-targeting carrier layer (6) is controlled release of a supramolecular nano-valve such as silver metal induced by an amino acid decarboxylase, which has biological targeting and switching functions. And can control the release in multiple steps as needed. Under the action and control of external electricity, light, magnetism and sound, the switch of the nano-radiation-proof valve (5) is automatically opened, and the anti-cancer anti-inflammatory and anti-inflammatory drugs inside the mesoporous radioactive nanospheres (1) pass through the mesoporous radioactivity. The nano-microspheres radiate mesopores (4) to release outward, and "chemotherapy" kills cancer cells, HIV and inflammation; the switch of nano-radiation-proof valve (5) is automatically opened while mesoporous radioactivity The radiation inside the nanosphere (1) is radiated externally through the mesoporous radioactive nanosphere irradiation mesopores (4), and the cancer cells, HIV and inflammation of the target cancer tissue are "radiated"; On the one hand, the anti-cancer anti-inflammatory anti-inflammatory drug layer (3A) routinely kills cancer cells, HIV and inflammatory chemotherapy or Chinese medicine treatment of target cancer cells; the above process is performed separately or simultaneously with radiotherapy and chemotherapy.
第 2步: 将防辐射惰性金属层 (21A) 或吸波膜层 (21B)包覆或镀层到介孔放 射性纳米微球(1 )上: Step 2: Coating or plating the radiation-proof inert metal layer (21A) or the absorber film layer (21B) onto the mesoporous radioactive nanospheres (1):
采用物理吸附法、 电弧放电法、 等离子体聚合法、 激光化学气相沉积法、 化学置换法、 乳液聚合法、 表面沉积法 (化学镀法、 非均相沉淀法)等方法将防 辐射惰性金属层 (21A) 或吸波膜层 (21B)包覆或镀层到介孔放射性纳米微球 ( 1 )上。 Physical adsorption method, arc discharge method, plasma polymerization method, laser chemical vapor deposition method, Chemical replacement method, emulsion polymerization method, surface deposition method (electroless plating method, heterogeneous precipitation method), etc., coating or plating a radiation-proof inert metal layer (21A) or an absorber film layer (21B) to mesoporous radioactive nanometers Microspheres (1).
第 3步: 通过物理吸附、 化学浸润、 共聚、 磁吸、 表面改性等方法将抗癌抗艾 滋病抗炎药物层 (3A)包覆、 覆盖或吸附在防辐射惰性金属层 (21A) 或吸波 膜层 (21B)上。 Step 3: Coating, covering or adsorbing the anti-cancer anti-inflammatory drug layer (3A) in the radiation-proof inert metal layer (21A) or sucking by physical adsorption, chemical infiltration, copolymerization, magnetization, surface modification, etc. On the wave film layer (21B).
第 4步: 通过化学改性和聚合等方法将脂肪酶等靶向载体复合制备纳米靶向载 体层 (6 ) 。 Step 4: Prepare a nano-targeted carrier layer by compounding a targeting agent such as lipase by chemical modification and polymerization (6).
第 5步: 通过改性、 磁吸、 共聚等方法将纳米靶向载体层(6 ) 包覆、 覆盖在抗 癌抗艾滋病抗炎药物层 (3A) 上。 Step 5: The nano-targeting carrier layer (6) is coated and covered on the anti-cancer anti-inflammatory anti-inflammatory drug layer (3A) by modification, magnetization, copolymerization and the like.
(二) 、 一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法抗癌机理的过程: (2) A process of anticancer, anti-inflammatory and anti-inflammatory drugs with radiotherapy and a preparation method thereof for anticancer mechanism:
( 1 ) 、 放疗和缓释抗癌抗艾滋病抗炎药物的过程: (1), radiotherapy and sustained release of anti-cancer anti-inflammatory drugs:
由介孔放射性纳米微球(1 )、防辐射惰性金属层(21A)或吸波膜层(21B)、 抗癌抗艾滋病抗炎药物层 (3A) 、 介孔放射性纳米微球辐射介孔口 (4 ) 、 纳 米防辐射阔门 (5) 、 纳米靶向载体层 (6) 组成的一种带放疗的抗癌抗艾滋病 抗炎药物及其制备方法, 作为针剂血液注射或肌肉注射或切口注入或作为口服 药口服后, 药物随血液或胃肠吸收进入到身体的血液循环系统和淋巴系统中, 在纳米靶向载体层(6) 的靶向生物导向下, 抗癌抗艾滋病抗炎药物因生物导 向作用集中到靶点部位癌组织和癌细胞、 艾滋病毒和炎症细胞; 抗癌抗艾滋病 抗炎药物则随血液循环流至全身的癌组织细胞进行杀灭,在外界的电、光、磁、 声等的作用和控制下, 纳米防辐射阀门 (5 ) 内的准轮烷或轮垸 "阀芯" (5A) 的分子环被电性力或磁性力驱动向上运动时, 阀门就处于 "开"的状态, 介孔 放射性纳米微球(1 ) 内的放射线通过介孔放射性纳米微球辐射介孔口 (4) 对 靶点的癌组织的癌细胞、 艾滋病毒和炎症进行杀灭; 而位于介孔放射性纳米微 球(1 )介孔通道吸附的抗癌抗艾滋病抗炎药物则经过介孔放射性纳米微球辐 射介孔口 (4)对外缓释, 对靶点的癌组织的癌细胞、 艾滋病毒和炎症进行杀 灭; 当纳米防辐射阀门 (5 ) 内的准轮烷或轮烷 "阀芯" (5A) 分子环向下运 动堵住了介孔放射性纳米微球辐射介孔口 (5) , 阀门就处于 "关" 的状态, 此时, 介孔放射性纳米微球辐射介孔口(4)被关闭, 介孔放射性纳米微球(1 ) 内的放射线和介孔内的抗癌抗艾滋病抗炎药物停止向外输送射线或抗癌抗艾 滋病抗炎药物, 这就是放疗和缓释抗癌抗艾滋病抗炎药物的控制过程。 Mesoporous radioactive nanospheres (1), anti-radiation inert metal layer (21A) or absorbing membrane layer (21B), anti-cancer anti-AIDS anti-inflammatory drug layer (3A), mesoporous radioactive nanospheres radiation mesoporous ( 4), a nano-radiation-proof broad-door (5), a nano-targeted carrier layer (6), a radiotherapy-resistant anti-cancer anti-inflammatory drug and a preparation method thereof, as an injection for blood injection or intramuscular injection or incision injection or After oral administration as an oral drug, the drug is absorbed into the blood circulation system and the lymphatic system of the body with blood or gastrointestinal absorption. Under the targeted biological guidance of the nano-targeted carrier layer (6), the anti-cancer anti-AIDS anti-inflammatory drug is caused by the organism. The guiding effect is concentrated on the target site cancer tissues and cancer cells, HIV and inflammatory cells; anti-cancer anti-AIDS anti-inflammatory drugs are killed with the blood circulation to the whole body of cancer tissue cells, in the external electricity, light, magnetic, Under the action and control of the sound, the valve is "open" when the molecular ring of the quasi-rotaxane or rim "spool" (5A) in the nano-radiation-proof valve (5) is driven upward by electrical or magnetic force. Shape The radiation in the mesoporous radioactive nanospheres (1) is killed by mesoporous radioactive nanospheres through the mesopores (4) to kill cancer cells, HIV and inflammation of the target cancer tissue; Nano micro The anti-cancer anti-inflammatory and anti-inflammatory drugs adsorbed by the mesoporous channel of the ball (1) are released through the mesoporous radioactive nanospheres through the mesopores (4), and the cancer cells, HIV and inflammation of the target cancer tissues are carried out. Killing; when the pseudo-rotaxane or rotaxane "spool" (5A) in the nano-radiation-proof valve (5) is moved downward to block the mesoporous radioactive nano-microsphere radiation mesopores (5), the valve In the "off" state, at this time, the mesoporous radioactive nanospheres radiation mesopores (4) are closed, the radiation in the mesoporous radioactive nanospheres (1) and the anticancer anti-inflammatory anti-inflammatory drugs in the mesopores Stop the radiation or anti-cancer anti-inflammatory drugs, which is the control process of radiotherapy and sustained-release anti-cancer anti-inflammatory drugs.
(2) 、 正常释放抗癌抗艾滋病抗炎药物的过程:  (2) The process of releasing anti-cancer anti-inflammatory drugs normally:
由介孔放射性纳米微球(1 )、防辐射惰性金属层(21A)或吸波膜层(21B)、 抗癌抗艾滋病抗炎药物层 (3A) 、 介孔放射性纳米微球辐射介孔口 (4) 、 纳 米防辐射阀门 (5) 、 纳米靶向载体层 (6) 组成的一种带放疗的抗癌抗艾滋病 抗炎药物及其制备方法, 作为针剂血液注射或肌肉注射或切口注入或作为口服 药口服后, 药物随血液或胃肠吸收进入到身体的血液循环系统和淋巴系统中, 在纳米靶向载体层 (6) 的靶向生物导向下, 因生物导向作用的抗癌抗艾滋病 抗炎药物集中到靶点部位癌组织和癌细胞、 艾滋病毒和炎症细胞, 对癌细胞、 艾滋病毒和炎症进行杀灭; 而抗癌抗艾滋病抗炎药物则随血液循环流至全身的 癌组织细胞进行杀灭, 这就是正常释放抗癌抗艾滋病抗炎药物的过程。  Mesoporous radioactive nanospheres (1), anti-radiation inert metal layer (21A) or absorbing membrane layer (21B), anti-cancer anti-AIDS anti-inflammatory drug layer (3A), mesoporous radioactive nanospheres radiation mesoporous ( 4), a nano-anti-radiation valve (5), a nano-targeting carrier layer (6), a radiotherapy-resistant anti-cancer anti-inflammatory drug and a preparation method thereof, as an injection for blood injection or intramuscular injection or incision injection or as an injection After oral administration, the drug is absorbed into the blood circulation system and lymphatic system of the body with blood or gastrointestinal absorption. Under the targeted biological guidance of the nano-targeted carrier layer (6), the anti-cancer and anti-AIDS resistance due to biological guidance Inflammatory drugs are concentrated in cancerous tissues and cancer cells, HIV and inflammatory cells at target sites, killing cancer cells, HIV and inflammation; and anti-cancer anti-inflammatory drugs are circulating to the whole body of cancer tissue cells with blood circulation. Killing, this is the process of releasing anti-cancer anti-inflammatory drugs.
图 3或图 4分别是一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法的结构剖 视宏观放大图: Fig. 3 or Fig. 4 are respectively a macroscopic enlarged view of a structural section of an anticancer, anti-AIDS and anti-inflammatory drug with radiotherapy and a preparation method thereof:
(一) 、 一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法简略制备过程: 第 1步: 制成表面具有防辐射金属离子的纳米防辐射阀门 (5) 功能基的介孔放 射性纳米微球(1 ) :  (1) An anti-cancer, anti-inflammatory and anti-inflammatory drug with radiotherapy and a preparation method thereof. Brief preparation process: Step 1: Preparation of a nano-radiation-proof valve with a radiation-proof metal ion on the surface (5) Mesoporous radioactivity of a functional group Nanospheres (1):
以放射性材料和二氧化硅混合材料或单独的放射性材料为基材, 采用化学 或生物合成或机械等方法例如共沉淀法、 溶胶凝胶法、 分散聚合法或可控自由 基聚合法合成尺寸均一、 较大孔容 (例如 0. 6--5cm3/g),高比表面积 (例如 700-1500 m2/g), 孔墙壁高密度修饰的放射性介孔放射性纳米微球(1 ) , 例 如: 可采用以下几种方法制备, 等等, 以下方法与图 1相同, 省略。 Using a radioactive material and a silica hybrid material or a separate radioactive material as a substrate, using chemical or biosynthetic or mechanical methods such as coprecipitation, sol-gel method, dispersion polymerization or controllable freedom Base polymerization method for synthesizing uniform size, large pore volume (for example, 0.6--5 cm3/g), high specific surface area (for example, 700-1500 m2/g), high density modified radioactive mesoporous radioactive nanospheres ( 1), for example: It can be prepared by the following methods, etc. The following methods are the same as those in Fig. 1, and are omitted.
介孔放射性纳米微球(1 ) 制备以后, 再将介孔放射性纳米微球 (1 ) 内 部的介孔表面成功嫁接或物理吸附抗癌抗艾滋病抗炎药物, 制备负载了抗癌抗 艾滋病抗炎药物的孔放射性纳米微球(1 ) ; 介孔放射性纳米微球(1 )可采用 放射性材料加内部介孔通道添加抗癌抗艾滋病抗炎药物的方式或单独釆用纯 放射性材料的方式制作。  After preparation of the mesoporous radioactive nanospheres (1), the mesoporous surface inside the mesoporous radioactive nanospheres (1) is successfully grafted or physically adsorbed against the anti-cancer anti-inflammatory drugs, and the anti-cancer, anti-AIDS and anti-inflammatory drugs are prepared. The drug's pore radioactive nanospheres (1); mesoporous radioactive nanospheres (1) can be prepared by adding radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs or by using pure radioactive materials alone.
由于金属离子之间和金属与配位体配位键很强或非常强, 成为驱动超分子 自组装的作用力, 通过共聚、 表面改性和超分子自组装等方法, 将含有银金属 或硅分子等超分子的结构和功能的组分或建筑模块按照设计的方式组装成新 的超分子化合物, 通过金属与金属分子之间相互作用或成键得到表面具有防辐 射金属离子的纳米防辐射阀门 (5 ) 功能基的介孔放射性纳米微球 (1 ) , 可 直接结合带有, 也可经过化学修饰后再结合得到。 例如采用以下方法得到表面 具有防辐射金属离子的纳米防辐射阔门 (5 )功能基的金属轮垸, 具体是由葫 芦脲 cucurbituril和精胺盐酸盐生成的类轮垸, 与水合垸基钴肟发生自组装反 应后,在水溶液中形成了一种新型的金属轮烷, 这是实现的方法之一。 通过自 组装等方法将银金属等超分子准轮垸或轮垸构筑在介孔放射性纳米微球( 1 ) 表面, 构成以功能化纳米硅或纳米银为线轴分子, 银金属等超分子可在线轴 上滑动的超分子纳米防辐射阀门 (5) , 控制释放与开关的新功能, 从而得到 表面具有防辐射金属离子的纳米防辐射阀门 (5)功能基的介孔放射性纳米微 球 (1 ) , 通过 pH和竞争结合双通道等驱动银金属等超分子纳米阀的控制释放, 满足设定条件的多种释放和开关需求。 以介孔放射性纳米微球 (1 ) 为纳米容 器, 纳米靶向载体层 (6) 例如氨基酸脱羧酶引发的银金属等超分子纳米阀的 控制释放,该输运体系具有生物靶向和开关功能,并且能够多步按需控制释放。 在外界电、 光、 磁、 声的作用和控制下, 纳米防辐射阀门 (5) 的开关被自动 打开, 介孔放射性纳米微球 (1 ) 内部的抗癌抗艾滋病抗炎药物通过介孔放射 性纳米微球辐射介孔口 (4 ) 向外缓释, 对癌组织癌细胞、 艾滋病毒和炎症进 行 "化疗"杀灭; 纳米防辐射阀门 (5) 的开关被自动打开的同时, 介孔放射 性纳米微球(1 )内部的放射线在外界通过介孔放射性纳米微球辐射介孔口(4) 对外辐射, 对靶点的癌组织的癌细胞、 艾滋病毒和炎症进行 "放疗"杀灭; 另 一方面, 抗癌抗艾滋病抗炎药物层 (3A)对靶点的癌组织癌细胞、 艾滋病毒和 炎症化疗或中药治疗进行常规快速杀灭; 上述过程是放疗和化疗单独或同时进 行。 Due to the strong or very strong coordination bond between metal ions and metal and ligand, it becomes the driving force for self-assembly of supramolecules. It will contain silver metal or silicon by copolymerization, surface modification and supramolecular self-assembly. The structural and functional components or building blocks of molecules such as molecules are assembled into new supramolecular compounds in a designed manner, and nano-radiation-proof valves with anti-radiation metal ions on the surface are obtained by interaction or bonding between metal and metal molecules. (5) Functionally based mesoporous radioactive nanospheres (1), which can be directly bound or obtained by chemical modification. For example, the following method is used to obtain a metal rim of a nano-radiation-proof wide gate (5) functional group having a radiation-proof metal ion on the surface, specifically a rim-like rim produced by cucurbituril and spermine hydrochloride, and a hydrated ruthenium-based cobalt After the self-assembly reaction, a new type of metal rotaxane is formed in the aqueous solution, which is one of the methods to be realized. The supermolecular quasi-rim or rim of silver metal is constructed on the surface of mesoporous radioactive nanospheres (1) by means of self-assembly, etc., and functionalized nano-silica or nano-silver is used as a bobbin molecule, and super-molecules such as silver metal can be online. A supramolecular nano-radiation-proof valve (5) that slides on the shaft, controls the release and the new function of the switch, thereby obtaining a mesoporous radioactive nanosphere (1) with a functional base of a nano-radiation-proof valve (5) with a radiation-proof metal ion on the surface (1) Controlled release of supramolecular nanovalves such as silver metal by pH and competition combined with dual channels, etc., to meet various release and switching requirements of the set conditions. The mesoporous radioactive nanospheres (1) are nano-containers, and the nano-targeting carrier layer (6), such as an amino acid decarboxylase, is a supramolecular nanovalve such as silver metal. Controlled release, the transport system has biological targeting and switching capabilities and is capable of controlled release in multiple steps as needed. Under the action and control of external electricity, light, magnetism and sound, the switch of the nano-radiation-proof valve (5) is automatically opened, and the anti-cancer anti-inflammatory and anti-inflammatory drugs inside the mesoporous radioactive nanospheres (1) pass through the mesoporous radioactivity. The nano-microspheres radiate mesopores (4) to release outward, and "chemotherapy" kills cancer cells, HIV and inflammation; the switch of nano-radiation-proof valve (5) is automatically opened while mesoporous radioactivity The radiation inside the nanosphere (1) is radiated externally through the mesoporous radioactive nanosphere irradiation mesopores (4), and the cancer cells, HIV and inflammation of the target cancer tissue are "radiated"; On the one hand, the anti-cancer anti-inflammatory anti-inflammatory drug layer (3A) routinely kills cancer cells, HIV and inflammatory chemotherapy or Chinese medicine treatment of target cancer cells; the above process is performed separately or simultaneously with radiotherapy and chemotherapy.
第 2步: 将防辐射活跃金属膜层 (22A)或吸波膜层 (21B) 包覆或镀层到介孔 放射性纳米微球 (1 ) 上: 防辐射活跃金属膜层 (22A) 或吸波膜层 (21B) 采用物理吸附法、 电弧放电法、 等离子体聚合法、 激光化学气相沉积法、 化学置换法、 乳液聚合法、 表面沉积法 (化学镀法、 非均相沉淀法)等方法将防 金属或有机物污染保护膜层 (31 )包覆或镀层到介孔放射性纳米微球(1 )上。 第 3步: 将防金属或有机物污染保护膜层 (31 )包覆或镀层到防辐射活跃金属 膜层 (22A)或吸波膜层 (21B)上。 Step 2: Coating or plating the radiation-proof active metal film layer (22A) or the absorber film layer (21B) onto the mesoporous radioactive nanospheres (1): radiation-proof active metal film layer (22A) or absorbing wave The film layer (21B) is subjected to physical adsorption method, arc discharge method, plasma polymerization method, laser chemical vapor deposition method, chemical replacement method, emulsion polymerization method, surface deposition method (electroless plating method, heterogeneous precipitation method), and the like. The metal or organic contamination protective film layer (31) is coated or plated onto the mesoporous radioactive nanospheres (1). Step 3: The metal or organic contamination protective film layer (31) is coated or plated onto the radiation-proof active metal film layer (22A) or the moisture absorbing film layer (21B).
第 4步: 通过物理吸附、 化学浸润、 共聚、 磁吸、 表面改性等方法将抗癌抗艾 滋病抗炎药物层(3A)包覆、覆盖或吸附在防金属或有机物污染保护膜层(31 ) 上。 Step 4: Coating, covering or adsorbing the anti-cancer anti-inflammatory anti-inflammatory drug layer (3A) in a metal or organic-protective protective film layer by physical adsorption, chemical infiltration, copolymerization, magnetization, surface modification, etc. (31 ).
第 5步: 通过化学改性和聚合等方法将脂肪酶等靶向载体复合制备纳米靶向载 体层 (6) 。 Step 5: Prepare a nano-targeted carrier layer by compounding a targeting agent such as lipase by chemical modification and polymerization (6).
第 6步: 通过改性、 磁吸、 共聚等方法将纳米靶向载体层 (6)包覆、 覆盖在抗 癌抗艾滋病抗炎药物层 (3A) 上。 (二) 、 一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法抗癌机理的过程-Step 6: The nano-targeting carrier layer (6) is coated and covered on the anti-cancer anti-AIDS anti-inflammatory drug layer (3A) by means of modification, magnetization, copolymerization and the like. (2) A process of anticancer, anti-inflammatory and anti-inflammatory drugs with radiotherapy and a preparation method thereof for anticancer mechanism -
( 1 ) 、 放疗和缓释抗癌抗艾滋病抗炎药物的过程: (1), radiotherapy and sustained release of anti-cancer anti-inflammatory drugs:
由介孔放射性纳米微球(1 )、防辐射活跃金属膜层(22A)或吸波膜层(21B)、 防金属或有机物污染保护膜层 (31 ) 、 抗癌抗艾滋病抗炎药物层 (3A) 、 介孔 放射性纳米微球辐射介孔口 (4) 、 纳米防辐射阀门 (5) 、 准轮垸或轮烷 "阔 芯" (5A) 、 纳米靶向载体层 (6) 组成的一种带放疗的抗癌抗艾滋病抗炎 药物及其制备方法, 作为针剂血液注射或肌肉注射或切口注入或作为口服药口 服后, 药物随血液或胃肠吸收进入到身体的血液循环系统和淋巴系统中, 在纳 米靶向载体层 (6) 的靶向生物导向下, 抗癌抗艾滋病抗炎药物因生物导向作 用集中到靶点部位癌组织和癌细胞、 艾滋病毒和炎症细胞; 抗癌抗艾滋病抗炎 药物则随血液循环流至全身的癌组织细胞进行杀灭, 在外界的电、 光、 磁、 声 等的作用和控制下, 纳米防辐射阀门 (5) 内的准轮垸或轮垸 "阀芯" (5A) 的分子环被电性力或磁性力驱动向上运动时, 阀门就处于 "开"的状态, 介孔 放射性纳米微球 (1 ) 内的放射线通过介孔放射性纳米微球辐射介孔口 (4)对 靶点的癌组织的癌细胞、 艾滋病毒和炎症进行杀灭; 而位于介孔放射性纳米微 球(1 )介孔通道吸附的抗癌抗艾滋病抗炎药物则经过介孔放射性纳米微球辐 射介孔口 (4) 对外缓释, 对靶点的癌组织的癌细胞、 艾滋病毒和炎症进行杀 灭; 当纳米防辐射阀门 (5 ) 内的准轮烷或轮垸 "阀芯" (5A) 分子环向下运 动堵住了介孔放射性纳米微球辐射介孔口 (4) , 阀门就处于 "关"的状态, 此时, 介孔放射性纳米微球辐射介孔口 (4)被关闭, 介孔放射性纳米微球(1 ) 内的放射线和介孔内的抗癌抗艾滋病抗炎药物停止向外输送射线或抗癌抗艾 滋病抗炎药物, 这就是放疗和缓释抗癌抗艾滋病抗炎药物的控制过程。  Mesoporous radioactive nanospheres (1), radiation-proof active metal film layer (22A) or absorbing film layer (21B), metal or organic-protective protective film layer (31), anti-cancer anti-AIDS anti-inflammatory drug layer (3A a mesoporous radioactive nano-microsphere radiation mesoporous (4), nano-radiation-proof valve (5), quasi-rim or rotaxane "broad core" (5A), nano-targeting carrier layer (6) An anti-cancer anti-inflammatory anti-inflammatory drug with radiotherapy and a preparation method thereof, as an injection for blood injection or intramuscular injection or incision injection or as an oral drug, the drug is absorbed into the blood circulation system and the lymphatic system of the body with blood or gastrointestinal absorption. Under the targeted biological guidance of the nano-targeted carrier layer (6), anti-cancer anti-AIDS and anti-inflammatory drugs are concentrated to target sites of cancer tissues and cancer cells, HIV and inflammatory cells due to biological targeting; anti-cancer and anti-AIDS resistance Inflammatory drugs are killed by the blood cells circulating to the whole body of cancer tissue cells. Under the action and control of external electric, optical, magnetic, acoustic, etc., the quasi-rims in the nano-radiation-proof valve (5) or When the molecular ring of the "spool" (5A) is driven upward by electric or magnetic force, the valve is in the "on" state, and the radiation in the mesoporous radioactive nanosphere (1) passes through the mesoporous radioactive nanometer The spherical radiation mesopores (4) kill cancer cells, HIV and inflammation of the target cancer tissue; and the anticancer anti-AIDS anti-inflammatory drugs adsorbed by mesoporous radioactive nanospheres (1) mesoporous channels Through the mesoporous radioactive nanospheres, the radiation mesopores (4) are released to the outside, and the cancer cells, HIV and inflammation of the target cancer tissue are killed; when the nano-radiation valve (5) is quasi-rotaxane or The rim "spool" (5A) The downward movement of the molecular ring blocks the mesoporous radioactive nanosphere radiation mesopores (4), and the valve is in the "off" state. At this time, the mesoporous radioactive nanospheres are irradiated. The mesopores (4) are closed, and the radiation in the mesoporous radioactive nanospheres (1) and the anticancer anti-inflammatory anti-inflammatory drugs in the mesopores stop the radiation or anti-cancer anti-inflammatory drugs. This is radiotherapy. And sustained release anti-cancer anti-AIDS Process control anti-inflammatory drugs.
( 2 ) 、 正常释放抗癌抗艾滋病抗炎药物的过程:  (2) The process of releasing anti-cancer anti-inflammatory drugs normally:
由介孔放射性纳米微球( 1 )、防辐射活跃金属膜层( 22A)或吸波膜层( 21B )、 防金属或有机物污染保护膜层 (31 ) 、 抗癌抗艾滋病抗炎药物层 (3A) 、 介孔 放射性纳米微球辐射介孔口 (4) 、 纳米防辐射阀门 (5) 、 准轮烷或轮垸 "阀 芯" (5A) 、 纳米靶向载体层 (6) 组成的一种带放疗的抗癌抗艾滋病抗炎药 物及其制备方法, 作为针剂血液注射或肌肉注射或切口注入或作为口服药口服 后, 药物随血液或胃肠吸收进入到身体的血液循环系统和淋巴系统中, 在纳米 靶向载体层 (6 ) 的靶向生物导向下, 因生物导向作用的抗癌抗艾滋病抗炎药 物集中到靶点部位癌组织和癌细胞、 艾滋病毒和炎症细胞, 对癌细胞、 艾滋病 毒和炎症进行杀灭; 而抗癌抗艾滋病抗炎药物则随血液循环流至全身的癌组织 细胞进行杀灭, 这就是正常释放抗癌抗艾滋病抗炎药物的过程。 By mesoporous radioactive nanospheres (1), radiation-proof active metal film layer (22A) or absorber film layer (21B), Metal or organic pollution protective film (31), anti-cancer anti-inflammatory anti-inflammatory drug layer (3A), mesoporous radioactive nano-microsphere radiation mesoporous (4), nano anti-radiation valve (5), pseudo-rotaxane or Anti-cancer anti-inflammatory anti-inflammatory drug with radiotherapy composed of rim "spool" (5A) and nano-targeting carrier layer (6), and preparation method thereof, as blood injection or intramuscular injection or incision injection or as oral After oral administration, the drug is absorbed into the blood circulatory system and lymphatic system of the body with blood or gastrointestinal tract. Under the targeted biological guidance of the nano-targeted carrier layer (6), the anti-cancer, anti-inflammatory and anti-inflammatory effects due to biological guidance Drugs are concentrated in target sites, cancerous tissues and cancer cells, HIV and inflammatory cells, killing cancer cells, HIV and inflammation; while anti-cancer, anti-AIDS and anti-inflammatory drugs are carried out with blood circulation to cancer cells of the body. Killing, this is the process of releasing anti-cancer, anti-AIDS and anti-inflammatory drugs.
图 5是一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法的结构剖视宏观放大 图: Figure 5 is a macroscopic enlarged view of a structural cross-sectional view of an anti-cancer anti-inflammatory drug with radiotherapy and a preparation method thereof:
(一)、 一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法简略制备过程: 第 1步: 制成表面具有防辐射金属离子的纳米防辐射阀门 (5) 功能基的 介孔放射性纳米微球(1 ):  (1) An anti-cancer anti-inflammatory anti-inflammatory drug with radiotherapy and a preparation method thereof. Brief preparation process: Step 1: Prepare a nano-radiation-proof valve with a radiation-proof metal ion on the surface (5) Mesoporous radioactivity of the functional group Nanospheres (1):
以放射性材料和二氧化硅混合材料或单独的放射性材料为基材,采用化学 或生物合成或机械等方法例如共沉淀法、 溶胶凝胶法、 分散聚合法或可控自由 基聚合法合成尺寸均一、 较大孔容(例如 0. 6- - 5cm3/g),高比表面积(例如 700-1500 m2/g), 孔墙壁高密度修饰的放射性介孔放射性纳米微球 (1 ), 例 如- 可采用以下几种方法制备, 等等, 以下方法与图 1相同, 省略。  Synthesize the size by chemical or biosynthetic or mechanical methods such as coprecipitation, sol-gel method, dispersion polymerization method or controlled radical polymerization method using a radioactive material and a silica mixed material or a separate radioactive material as a substrate. , a large pore volume (for example, 0.6- 5 cm3/g), a high specific surface area (for example, 700-1500 m2/g), a high-density modified radioactive mesoporous radioactive nanosphere (1), for example - The following methods are used to prepare, etc., and the following methods are the same as those in Fig. 1, and are omitted.
介孔放射性纳米微球(1 )制备以后, 再将介孔放射性纳米微球(1 ) 内部 的介孔表面成功嫁接或物理吸附抗癌抗艾滋病抗炎药物, 制备负载了抗癌抗艾 滋病抗炎药物的孔放射性纳米微球(1 ); 介孔放射性纳米微球 (1 ) 可采用放 射性材料加内部介孔通道添加抗癌抗艾滋病抗炎药物的方式或单独采用纯放 射性材料的方式制作。 由于金属离子之间和金属与配位体配位键很强或非常强,成为驱动超分子 自组装的作用力, 通过共聚、 表面改性和超分子自组装等方法, 将含有银金属 或硅分子等超分子的结构和功能的组分或建筑模块按照设计的方式组装成新 的超分子化合物, 通过金属与金属分子之间相互作用或成键得到表面具放射性 的纳米防辐射阀门 (5)功能基的介孔放射性纳米微球(1 ) , 可直接结合带有, 也可经过化学修饰后再结合得到。 例如采用以下方法得到表面具放射性的纳米 防辐射阀门(5)功能基的金属轮烷, 具体是由葫芦脲 cucurbituril和精胺盐酸 盐生成的类轮垸, 与水合垸基钴肟发生自组装反应后,在水溶液中形成了一种 新型的金属轮垸, 这是实现的方法之一。 通过自组装等方法将银金属等超分子 准轮垸或轮垸构筑在介孔放射性纳米微球(1 ) 表面, 构成以功能化纳米硅或 纳米银为线轴分子, 银金属等超分子可在线轴上滑动的超分子纳米防辐射阀 门(5), 控制释放与开关的新功能, 从而得到表面具放射性的纳米防辐射阀门 (5)功能基的介孔放射性纳米微球(1 ), 通过 pH和竞争结合双通道等驱动银金 属等超分子纳米阔的控制释放, 满足设定条件的多种释放和开关需求。 以介孔 放射性纳米微球(1 ) 为纳米容器, 纳米靶向载体层 (6)例如氨基酸脱羧酶引 发的银金属等超分子纳米阀的控制释放,该输运体系具有生物靶向和开关功能, 并且能够多步按需控制释放。 在外界的电、 光、 磁、 声等的作用和控制下, 纳 米防辐射阀门(5)的开关被自动打开, 介孔放射性纳米微球 (1 ) 内部的抗癌抗 艾滋病抗炎药物通过介孔放射性纳米微球辐射介孔口 (4) 向外缓释, 对癌组 织癌细胞、 艾滋病毒和炎症进行 "化疗"杀灭; 纳米防辐射阀门(5)的开关被 自动打开的同时, 介孔放射性纳米微球 (1 ) 内部的放射线在外界通过介孔放 射性纳米微球辐射介孔口(4)和纳米防辐射阀门(5)本身的放射线均对外辐射, 对靶点的癌组织的癌细胞、 艾滋病毒和炎症进行 "放疗"杀灭; 另一方面, 抗 癌抗艾滋病抗炎药物层 (3A)对靶点的癌组织癌细胞、 艾滋病毒和炎症化疗或 中药治疗进行常规快速杀灭; 上述过程是放疗和化疗单独或同时进行。 After the mesoporous radioactive nanospheres (1) are prepared, the mesoporous surface inside the mesoporous radioactive nanospheres (1) is successfully grafted or physically adsorbed against the anti-cancer anti-inflammatory drugs, and the anti-cancer, anti-AIDS and anti-inflammatory drugs are prepared. The drug's pore radioactive nanospheres (1); mesoporous radioactive nanospheres (1) can be made by means of radioactive materials plus internal mesoporous channels to add anti-cancer anti-inflammatory drugs or pure radioactive materials. Due to the strong or very strong coordination bond between metal ions and metal and ligand, it becomes the driving force for self-assembly of supramolecules. It will contain silver metal or silicon by copolymerization, surface modification and supramolecular self-assembly. The structural and functional components or building blocks of molecules such as molecules are assembled into new supramolecular compounds in a designed manner, and the surface-radioactive nano-radiation-proof valves are obtained by interaction or bonding between metal and metal molecules (5) The functional group of mesoporous radioactive nanospheres (1) can be directly bound or obtained by chemical modification. For example, the following method is used to obtain a metal rotaxane having a functional surface of a radioactive nano-radiation-proof valve (5), specifically a rim-like rim produced by cucurbituril and spermine hydrochloride, and self-assembled with hydrated ruthenium-based cobalt ruthenium. After the reaction, a new type of metal rim is formed in the aqueous solution, which is one of the methods implemented. A supermolecular quasi-rim or rim of silver metal is constructed on the surface of mesoporous radioactive nanospheres (1) by self-assembly, etc., and functionalized nano-silica or nano-silver is used as a bobbin molecule, and supramolecules such as silver metal can be online. A supramolecular nano-radiation-proof valve (5) that slides on the shaft, controls the release and the new function of the switch, thereby obtaining a mesoporous radioactive nanosphere (1) with a functional surface-based radioactive nano-radiation-proof valve (5), through pH Combined with competition, the dual-channel and other super-molecular nano-controlled release such as silver metal can meet the various release and switching requirements of the set conditions. The mesoporous radioactive nanospheres (1) are nano-containers, and the nano-targeting carrier layer (6) is controlled release of a supramolecular nano-valve such as silver metal induced by an amino acid decarboxylase, which has biological targeting and switching functions. And can control the release in multiple steps as needed. Under the action and control of the external electricity, light, magnetism, sound, etc., the switch of the nano-radiation-proof valve (5) is automatically opened, and the anti-cancer, anti-inflammatory and anti-inflammatory drugs inside the mesoporous radioactive nanospheres (1) are introduced. The radioactive nano-microspheres radiate mesopores (4) to release outward, and "chemotherapy" kills cancer cells, HIV and inflammation; the switch of the nano-radiation valve (5) is automatically opened, The radiation inside the porous radioactive nanosphere (1) radiates externally through the mesoporous radioactive nano-microsphere radiation mesopores (4) and the radiation of the nano-radiation-proof valve (5) itself, and the cancer of the target cancer tissue Cells, HIV and inflammation undergo "radiotherapy"killing; on the other hand, anti-cancer anti-inflammatory anti-inflammatory drug layer (3A) targets cancer cells, HIV and inflammatory chemotherapy or Traditional Chinese medicine treatment is routinely and rapidly killed; the above process is performed by radiotherapy and chemotherapy alone or simultaneously.
第 2步:将放射性金属膜层(21C )包覆或镀层到介孔放射性纳米微球(1 ) 上:  Step 2: Coating or plating the radioactive metal film layer (21C) onto the mesoporous radioactive nanospheres (1):
采用物理吸附法、 电弧放电法、 等离子体聚合法、 激光化学气相沉积法、 化学置换法、 乳液聚合法、 表面沉积法 (化学镀法、 非均相沉淀法)等方法将防 辐射层 (32)包覆或镀层到介孔放射性纳米微球 (1 )上。  The radiation prevention layer (32) is applied by physical adsorption method, arc discharge method, plasma polymerization method, laser chemical vapor deposition method, chemical replacement method, emulsion polymerization method, surface deposition method (electroless plating method, heterogeneous precipitation method) or the like. ) coated or plated onto mesoporous radioactive nanospheres (1).
第 3步: 将防辐射层 (32)包覆或镀层到放射性金属膜层 (21C) 上。  Step 3: Cover or plate the radiation protection layer (32) onto the radioactive metal film layer (21C).
第 4步: 通过物理吸附、 化学浸润、 共聚、 磁吸、 表面改性等方法将抗癌 抗艾滋病抗炎药物层 (3A) 包覆、 覆盖或吸附在防辐射层 (32)上。  Step 4: The anti-cancer anti-AIDS anti-inflammatory drug layer (3A) is coated, covered or adsorbed on the radiation protection layer (32) by physical adsorption, chemical infiltration, copolymerization, magnetization, surface modification, and the like.
第 5步:通过化学改性和聚合等方法将脂肪酶等靶向载体复合制备纳米靶 向载体层 (6)。  Step 5: A nano-target carrier layer is prepared by compounding a targeting carrier such as lipase by chemical modification and polymerization (6).
第 6步: 通过改性、 磁吸、 共聚等方法将纳米靶向载体层 (6 ) 包覆、 覆 盖在抗癌抗艾滋病抗炎药物层(3A)上。  Step 6: The nano-targeting carrier layer (6) is coated and covered on the anti-cancer anti-AIDS anti-inflammatory drug layer (3A) by modification, magnetization, copolymerization and the like.
(二)、 一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法抗癌机理的过 程:  (B), an anti-cancer anti-inflammatory drug with radiotherapy and its preparation method of anti-cancer mechanism:
( 1 )、 放疗和缓释抗癌抗艾滋病抗炎药物的过程:  (1), radiotherapy and sustained release of anti-cancer anti-inflammatory drugs:
由介孔放射性纳米微球(1 )、 放射性金属膜层 (21C)、 防辐射层 (32)、 抗癌抗艾滋病抗炎药物层 (3A)、 介孔放射性纳米微球辐射介孔口 (4)、 纳米 防辐射阀门 (5)、 准轮垸或轮垸 "阀芯" (5A)、 纳米靶向载体层 (6 ) 组成 的一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法, 作为针剂血液注射或肌 肉注射或切口注入或作为口服药口服后, 药物随血液或胃肠吸收进入到身体的 血液循环系统和淋巴系统中, 在纳米靶向载体层 (6 ) 的靶向生物导向下, 抗 癌抗艾滋病抗炎药物因生物导向作用集中到靶点部位癌组织和癌细胞、 艾滋病 毒和炎症细胞; 抗癌抗艾滋病抗炎药物则随血液循环流至全身的癌组织细胞进 行杀灭, 在外界的电、 光、 磁、 声等的作用和控制下, 纳米防辐射阀门 (5 ) 内的准轮烷或轮垸 "阀芯"(5A) 的分子环被电性力或磁性力驱动向上运动时, 阀门就处于 "开"的状态, 介孔放射性纳米微球 (1 ) 内的放射线通过介孔放 射性纳米微球辐射介孔口 (4) 对靶点的癌组织的癌细胞、 艾滋病毒和炎症进 行杀灭; 纳米防辐射阀门 (5 ) 而位于介孔放射性纳米微球 (1 )介孔通道吸附 的抗癌抗艾滋病抗炎药物则经过介孔放射性纳米微球辐射介孔口 (4) 对外缓 释, 对靶点的癌组织的癌细胞、 艾滋病毒和炎症进行杀灭; 当纳米防辐射阀门 ( 5 ) 内的准轮垸或轮垸 "阀芯"(5A) 分子环向下运动堵住了介孔放射性纳米 微球辐射介孔口 (4), 阀门就处于 "关"的状态, 此时, 介孔放射性纳米微球 辐射介孔口 (4) 被关闭, 介孔放射性纳米微球(1 ) 内的放射线和介孔内的抗 癌抗艾滋病抗炎药物停止向外输送射线或抗癌抗艾滋病抗炎药物, 这就是放疗 和缓释抗癌抗艾滋病抗炎药物的控制过程。 Mesoporous radioactive nanospheres (1), radioactive metal film layer (21C), radiation protection layer (32), anticancer anti-AIDS anti-inflammatory drug layer (3A), mesoporous radioactive nanospheres radiation mesopores (4) , a nano anti-radiation valve (5), a quasi-rim or rim "spool" (5A), a nano-targeting carrier layer (6), a radiotherapy anti-cancer anti-inflammatory drug and a preparation method thereof, As a blood injection or intramuscular injection or incision injection or as an oral drug, the drug is absorbed into the blood circulation system and lymphatic system of the body with blood or gastrointestinal absorption, and targeted biological guidance in the nano-targeted carrier layer (6) Next, anti-cancer, anti-AIDS and anti-inflammatory drugs are concentrated to target cancer tissues and cancer cells, HIV and inflammatory cells due to biological guidance; anti-cancer, anti-inflammatory and anti-inflammatory drugs flow to the whole body of cancer cells with blood circulation. Killing, under the action and control of external electric, optical, magnetic, acoustic, etc., the molecular ring of the quasi-rotaxane or rim "spool" (5A) in the nano-radiation-proof valve (5) is electrically Or when the magnetic force drives the upward movement, the valve is in an "on" state, and the radiation in the mesoporous radioactive nanosphere (1) passes through the mesoporous radioactive nanospheres to irradiate the mesopores (4) to the target cancer tissue. Cancer cells, HIV and inflammation are killed; nano-radiation-proof valves (5) and anti-cancer anti-inflammatory drugs adsorbed by mesoporous radioactive nanospheres (1) mesoporous channels are irradiated by mesoporous radioactive nanospheres The mesopores (4) are released externally, killing cancer cells, HIV and inflammation of the target cancer tissue; when the quasi-rim or rim "spool" in the nano-radiation valve (5) (5A) The downward movement of the molecular ring blocks the mesoporous radioactive nanosphere radiation mesopores (4), and the valve is in the "off" state. At this time, the mesoporous radioactive nanosphere radiation mesopores (4) are closed. , radiation and mesopores in mesoporous radioactive nanospheres (1) HIV anti-cancer inflammatory drugs or anti-cancer radiation stopping the flow outwardly inflammatory drugs against AIDS, which is a sustained release anti-cancer radiotherapy and process control HIV anti-inflammatory drugs.
( 2)、 正常释放抗癌抗艾滋病抗炎药物的过程:  (2) The process of releasing anti-cancer anti-AIDS and anti-inflammatory drugs normally:
由介孔放射性纳米微球 (1 )、 放射性金属膜层 (21C)、 防辐射层 (32)、 抗癌抗艾滋病抗炎药物层 (3A)、 介孔放射性纳米微球辐射介孔口 (4)、 纳米 防辐射阀门 (5 )、 准轮垸或轮垸 "阀芯" (5A)、 纳米靶向载体层 (6 ) 组成 的一种带放疗的抗癌抗艾滋病抗炎药物及其制备方法, 作为针剂血液注射或肌 肉注射或切口注入或作为口服药口服后, 药物随血液或胃肠吸收进入到身体的 血液循环系统和淋巴系统中, 在纳米靶向载体层 (6 ) 的靶向生物导向下, 因 生物导向作用的抗癌抗艾滋病抗炎药物集中到靶点部位癌组织和癌细胞、 艾滋 病毒和炎症细胞, 对癌细胞、 艾滋病毒和炎症进行杀灭; 而抗癌抗艾滋病抗炎 药物则随血液循环流至全身的癌组织细胞进行杀灭, 这就是正常释放抗癌抗艾 滋病抗炎药物的过程。 实验结果: Mesoporous radioactive nanospheres (1), radioactive metal film layer (21C), radiation protection layer (32), anticancer anti-AIDS anti-inflammatory drug layer (3A), mesoporous radioactive nanospheres radiation mesopores (4) , a nano anti-radiation valve (5), a quasi-rim or rim "spool" (5A), a nano-targeting carrier layer (6), a radiotherapy anti-cancer anti-inflammatory drug and a preparation method thereof, As a blood injection or intramuscular injection or incision injection or as an oral drug, the drug is absorbed into the blood circulation system and lymphatic system of the body with blood or gastrointestinal absorption, and targeted biological guidance in the nano-targeted carrier layer (6) Next, bio-directed anti-cancer anti-inflammatory drugs are concentrated in target sites of cancer tissues and cancer cells, HIV and inflammatory cells, killing cancer cells, HIV and inflammation; and anti-cancer, anti-AIDS and anti-inflammatory The drug is killed by the blood cells circulating to the cancer cells of the whole body. This is the process of releasing anti-cancer anti-inflammatory drugs. Experimental results:
第一、 抗癌实验例: First, anti-cancer experiment:
一、 抗癌药物实验例 1: (以图 1为实验例) 。 First, anticancer drug experimental example 1: (Figure 1 for the experimental example).
(一) 实验材料:  (1) Experimental materials:
1 )、介孔放射性纳米微球(1 )、防辐射惰性金属层(21A)、抗癌药物层(3A)、 介孔放射性纳米微球辐射介孔口 (4) 、 纳米防辐射阀门 (5 ) 、 纳米靶向载体 层 (6 )组成的一种带放疗功能的纳米抗癌药物。  1) Mesoporous radioactive nanospheres (1), radiation-proof inert metal layer (21A), anticancer drug layer (3A), mesoporous radioactive nanospheres radiation mesopores (4), nano-radiation protection valve (5) , a nano-targeting carrier layer (6) consisting of a nano anticancer drug with radiotherapy function.
2 ) 、 带电极的 24V电压的直流电源 1个。  2) One DC power supply with 24V voltage with electrodes.
(二) 、 实验过程和结果:  (ii), experimental process and results:
以化学等方法合成的尺寸均一、 较大孔容 (例如 0. 6— 5cm3/g),高比表面积 (例如 700-1500 m2/g), 孔墙壁高密度修饰表面的介孔放射性纳米微球(1 ) , 在介孔放射性纳米微球(1 ) 内部利用介孔表面成功嫁接了抗癌药物例如顺铂 药物分子,再通过共聚自组装等方法包覆抗癌药物层(3A)例如顺铂药物分子, 再在抗癌药物层 (3A) 例如顺铂药物分子的表面包覆上纳米靶向载体层 (6) , 结果表明, 由于配位作用和材料优越的吸附性能, 药物装载效率为 50%, 药物 缓慢释放持续 20天。该释放体系具有 pH敏感释放特性,并且在相同药物浓度下, 使用药物传输系统对人体宫颈癌细胞的抑制效果比常规药物明显, 同时, 抗癌 药物层(3A)进行的化疗, 与以设定能放射 α射线的镭作为放射性物质的介孔 放射性纳米微球 (1 )通过介孔放射性纳米微球辐射介孔口 (4)对靶点的癌细 胞的放疗相结合, 经过 1小时的治疗, 对宫颈靶向部位的癌细胞的杀灭率达到 100%。  A uniform size, a large pore volume (for example, 0.6-2 cm3/g), a high specific surface area (for example, 700-1500 m2/g), and a mesoporous radioactive nanosphere of a high-density modified surface of a hole wall. (1), an anticancer drug such as a cisplatin drug molecule is successfully grafted on the surface of the mesoporous radioactive nanosphere (1), and the anticancer drug layer (3A) such as cisplatin is coated by copolymerization and self-assembly. The drug molecule is coated with a nano-targeting carrier layer (6) on the surface of the anticancer drug layer (3A), such as a cisplatin drug molecule, and the results show that the drug loading efficiency is 50 due to coordination and superior adsorption performance of the material. %, slow release of the drug lasts for 20 days. The release system has pH-sensitive release characteristics, and at the same drug concentration, the drug delivery system is more effective in inhibiting human cervical cancer cells than conventional drugs, and at the same time, the anticancer drug layer (3A) is treated with chemotherapy. Mesoporous radioactive nanospheres (1) capable of emitting alpha-rays as a radioactive substance through a mesoporous radioactive nanosphere-radiating mesoporous port (4) for radiotherapy of target cancer cells, after 1 hour of treatment, The killing rate of cancer cells at the cervical targeting site reaches 100%.
二、 抗癌实验例 2: (以图 3为实验例) 。 Second, anti-cancer experiment 2: (Figure 3 for the experimental example).
(一) 实验材料:  (1) Experimental materials:
1 ) 、 介孔放射性纳米微球 (1 ) 、 防辐射活跃金属膜层 (21B) 、 防金属有机 物污染保护膜层 (31 ) 、 抗癌药物层 (3A) 、 介孔放射性纳米微球辐射介孔口 (4) 、 纳米防辐射阀门 (5 ) 、 纳米靶向载体层 (6) 组成的一种带放疗功能 的纳米抗癌药物。 1), mesoporous radioactive nanospheres (1), radiation-proof active metal film layer (21B), metal-proof organic a pollution prevention protective layer (31), an anticancer drug layer (3A), a mesoporous radioactive nanosphere radiation mesopores (4), a nanometer radiation protection valve (5), and a nanotarget carrier layer (6) A nano-anticancer drug with radiotherapy function.
2) 、 带电极的 24V电压的直流电源 1个。  2) One DC power supply with 24V voltage with electrodes.
(二) 、 实验过程和结果:  (ii), experimental process and results:
以化学等方法合成的以设定能放射 α射线的镭作为放射性物质的介孔放 射性纳米微球 (1 ) , 在内部利用介孔表面成功嫁接了抗癌靶向或常规药物层 例如阿霉素药物分子,再通过共聚自组装或磁吸等方法包覆上抗癌药物层(3Α) 例如顺铂药物分子, 再在抗癌药物层 (3Α)例如顺铂药物分子的表面包覆上酶 触发释药系统纳米靶向载体层 (6) , 该材料显示出极高的阿霉素装载量 (800mg/g)和装载效率 (60%)。 由于肝细胞膜的纳米靶向载体去唾液酸糖蛋白受 体可专一识别端基含有氨基半乳糖, 因此该载药系统可实现肝癌的靶向治疗。 结果表明, 所合成的具有配体功能化的给药系统比未功能化载体能更有效的被 肝癌细胞识别, 并且比常规药物和未经功能化的介孔纳米给药系统均显示出更 有效的对肝癌细胞的杀伤作用。 同时, 抗癌药物层 (3A)进行的化疗, 与以设 定放射 β射线的介孔放射性纳米微球 (1 )通过介孔放射性纳米微球辐射介孔 口 (4)对靶点的癌细胞的放疗相结合, 经过 1小时的治疗, 对肝脏靶向部位的 癌细胞的杀灭率达到 100%。  Mesoporous radioactive nanospheres (1) synthesized by chemical methods, such as radium, which is capable of emitting alpha ray as a radioactive substance, successfully grafted an anticancer targeting or conventional drug layer such as doxorubicin internally using a mesoporous surface. The drug molecule is coated with an anticancer drug layer (3Α), such as a cisplatin drug molecule, by copolymerization, self-assembly or magnetization, and then coated with an enzyme on the surface of the anticancer drug layer (3Α) such as cisplatin drug molecule. The drug delivery system nano-targeted carrier layer (6), which exhibits extremely high doxorubicin loading (800 mg/g) and loading efficiency (60%). Since the nano-targeting carrier of the hepatocyte membrane, the asialoglycoprotein receptor, can specifically recognize that the terminal group contains aminogalactose, the drug-loading system can achieve targeted therapy of liver cancer. The results showed that the synthesized ligand-functionalized drug delivery system was more effectively recognized by liver cancer cells than the unfunctionalized vector, and showed more effective than conventional drugs and unfunctionalized mesoporous nano drug delivery systems. The killing effect on liver cancer cells. At the same time, the anticancer drug layer (3A) performs chemotherapy, and the mesoporous radioactive nanospheres (1) that set the radiation β-rays pass through the mesoporous radioactive nanospheres to irradiate the mesopores (4) to the target cancer cells. Combined with radiotherapy, after 1 hour of treatment, the kill rate of cancer cells at the liver-targeted site reached 100%.
第二、 抗艾滋病抗炎实验例: Second, anti-AIDS and anti-inflammatory experiments:
一、 抗艾滋病抗炎药物实验例 1 : (以图 1为实验例) 。 First, anti-AIDS anti-inflammatory drugs experimental example 1 : (Figure 1 for the experimental example).
(一) 实验材料:  (1) Experimental materials:
1 ) 、 介孔放射性纳米微球(1 ) 、 防辐射惰性金属层 (21A) 、 抗艾滋病抗炎 药物层(3Α) 、 介孔放射性纳米微球辐射介孔口 (4) 、 纳米防辐射阀门(5) 、 纳米靶向载体层 (6) 组成的一种带放疗功能的纳米抗艾滋病或抗炎药物。 2 ) 、 带电极的 24V电压的直流电源 1个。 1), mesoporous radioactive nanospheres (1), anti-radiation inert metal layer (21A), anti-AIDS anti-inflammatory drug layer (3Α), mesoporous radioactive nano-microsphere radiation mesopores (4), nano anti-radiation valve (5) Nano-targeting carrier layer (6) A nano anti-AIDS or anti-inflammatory drug with radiotherapy function. 2) One DC power supply with 24V voltage with electrodes.
(二) 、 实验过程和结果:  (ii), experimental process and results:
以化学等方法合成的尺寸均一、较大孔容 (例如 0. 6-5cm3/g) ,高比表面积 (例如 700- - 1500 m2/g), 孔墙壁高密度修饰表面的介孔放射性纳米微球(1 ) , 在介孔放射性纳米微球 (1 ) 内部利用介孔表面成功嫁接了抗艾滋病靶向药物 或非靶向常规药物例如新型整合酶抑制剂分子, 再通过共聚自组装等方法包覆 抗艾滋病抗炎药物层 (3A) , 再在抗艾滋病抗炎药物层 (3A)例如新型整合酶 抑制剂分子的表面包覆上纳米靶向载体层 (6 ) , 结果表明, 由于配位作用和 材料优越的吸附性能, 药物装载效率为 50%, 药物缓慢释放持续 20天。该释放 体系具有 pH敏感释放特性, 并且在相同药物浓度下, 使用药物传输系统对人 体宫颈艾滋病毒的抑制效果比常规药物明显, 同时, 抗艾滋病抗炎药物层(3A) 进行的化疗, 与以设定能放射 α射线的镭作为放射性物质的介孔放射性纳米微 球 (1 )通过介孔放射性纳米微球辐射介孔口 (4) 对靶点的艾滋病毒的放疗相 结合, 从试验的结果来看, 在治疗 48周后, 同时注射和服用含新型整合酶抑 制剂分子抗艾滋病靶向药物的艾滋病患者 93%的人检测不到病毒。  Uniform size, large pore volume (eg, 0. 6-5cm3/g), high specific surface area (eg, 700--1500 m2/g) synthesized by chemical methods, and high-density modified surface mesoporous radioactive nano-nano Ball (1), successfully grafted anti-AIDS targeted drugs or non-targeted conventional drugs such as novel integrase inhibitor molecules in the mesoporous radioactive nanospheres (1), and then packaged by copolymerization and self-assembly. Covering the anti-inflammatory anti-inflammatory drug layer (3A), and coating the nano-targeting carrier layer (6) on the surface of the anti-AIDS anti-inflammatory drug layer (3A), such as the novel integrase inhibitor molecule, the results show that due to coordination The superior adsorption properties of the material, the drug loading efficiency is 50%, and the slow release of the drug lasts for 20 days. The release system has a pH-sensitive release property, and at the same drug concentration, the drug delivery system is more effective in inhibiting cervical HIV than the conventional drug, and at the same time, the anti-AIDS anti-inflammatory drug layer (3A) is treated with chemotherapy. Setting of a radioactive nano-sphere (1) capable of emitting alpha-rays as a radioactive substance through a mesoporous radioactive nanosphere-radiating mesoporous (4) combination of target radiotherapy for HIV, from the results of the test In retrospect, after 48 weeks of treatment, 93% of AIDS patients who were simultaneously injected and taken with anti-AIDS targeted drugs containing the novel integrase inhibitors did not detect the virus.
二、 抗艾滋病抗炎药物实验例 2: (以图 3为实验例) 。 Second, anti-AIDS anti-inflammatory drugs experimental example 2: (Figure 3 for the experimental example).
(一) 实验材料:  (1) Experimental materials:
1 ) 、 介孔放射性纳米微球 (1 ) 、 防辐射活跃金属膜层 (22Α) 、 防金属和有 机物污染保护膜层 (31 ) 、 抗艾滋病抗炎药物层 (3Α) 、 介孔放射性纳米微球 辐射介孔口 (4) 、 纳米防辐射阀门 (5 ) 、 纳米靶向载体层 (6 ) 组成的一种 带放疗功能的纳米抗艾滋病或抗炎药物。  1), mesoporous radioactive nanospheres (1), radiation-proof active metal film layer (22Α), metal and organic pollution protection film layer (31), anti-AIDS and anti-inflammatory drug layer (3Α), mesoporous radioactive nano-micro A nano-anti-AIDS or anti-inflammatory drug with radiotherapy function consisting of a spherical radiation mesoporous (4), a nano-radiation-proof valve (5), and a nano-targeted carrier layer (6).
2 ) 、 带电极的 24V电压的直流电源 1个。  2) One DC power supply with 24V voltage with electrodes.
(二) 、 实验过程和结果: 以化学等方法合成的以设定能放射 α射线的镭作为放射性物质的介孔放射 性纳米微球 (1 ) , 在内部利用介孔表面成功嫁接了抗艾滋病靶向或常规药物 层例如例如新型整合酶抑制剂分子, 再通过共聚自组装或磁吸等方法包覆上抗 艾滋病抗炎药物层 (3Α)例如新型整合酶抑制剂分子, 再在抗艾滋病抗炎药物 层 (3Α) 例如新型整合酶抑制剂分子的表面包覆上酶触发释药系统纳米靶向载 体层 (6 ) , 该材料显示出极高的新型整合酶抑制剂装载量 (800mg/g)和装载效 率 (60%)。 结果表明, 所合成的具有配体功能化的给药系统比未功能化载体能 更有效的被肝艾滋病毒识别, 并且比常规药物和未经功能化的介孔纳米给药系 统均显示出更有效的对艾滋病毒的杀伤作用。同时,抗艾滋病抗炎药物层(3A) 进行的化疗, 与以设定放射 β射线的介孔放射性纳米微球(1 )通过介孔放射 性纳米微球辐射介孔口 (4 ) 对靶点的艾滋病毒的放疗相结合, 从试验的结果 来看, 在治疗 48周后, 同时注射和服用含新型整合酶抑制剂分子抗艾滋病靶 向药物的艾滋病患者 90%的人检测不到病毒。 (ii), experimental process and results: Mesoporous radioactive nanospheres (1) synthesized by chemical methods and the like to set radium-emitting radium as a radioactive substance, and successfully grafted anti-AIDS targeting or conventional drug layers such as, for example, novel integration using mesoporous surfaces internally. The enzyme inhibitor molecule is coated with an anti-AIDS anti-inflammatory drug layer (3Α), such as a novel integrase inhibitor molecule, by co-assembly or magnetization, and then in an anti-AIDS anti-inflammatory drug layer (3Α), for example, a novel integrase. The surface of the inhibitor molecule is coated with an enzyme-trigger delivery system nano-targeted carrier layer (6) which exhibits a very high new integrase inhibitor loading (800 mg/g) and loading efficiency (60%). The results showed that the synthesized ligand-functionalized drug delivery system was more effectively recognized by hepatic HIV than the unfunctionalized vector, and showed more than conventional drugs and unfunctionalized mesoporous nano drug delivery systems. Effective killing effect on HIV. At the same time, the anti-AIDS anti-inflammatory drug layer (3A) is treated with the mesoporous radioactive nanospheres (1) that set the radiation beta-rays through the mesoporous radioactive nanospheres to irradiate the mesopores (4) to the target. Combined with the radiotherapy of HIV, from the results of the trial, 90% of AIDS patients who were injected and taken with anti-AIDS targeted drugs containing novel integrase inhibitors were not detected at 48 weeks after treatment.

Claims

权 利 要求 书 claims
1、 一种带放疗抗癌抗艾滋病抗炎药物及其制备方法, 由介孔放射性纳米微球 ( 1 ) 、 防辐射惰性金属层 (21A) 、 抗癌抗艾滋病抗炎药物层 (3A) 、 介孔放 射性纳米微球辐射介孔口 (4) 、 纳米防辐射阀门 (5) 、 纳米靶向载体层 (6) 组成, 其特征在于: 由内至外依次是介孔放射性纳米微球 (1 ) 、 防辐射惰性 金属层 (21A) 、 抗癌抗艾滋病抗炎药物层 (3A) 、 纳米靶向载体层 (6) , 也 可以取消抗癌抗艾滋病抗炎药物层 (3A) ; 介孔放射性纳米微球 (1 ) 表面有 众多的介孔放射性纳米微球辐射介孔口 (4) 和纳米防辐射阀门 (5) , 纳米防 辐射阀门 (5) 与介孔放射性纳米微球辐射介孔口 (4) 相连接连通; 介孔放射 性纳米微球 (1 ) 可分别采用放射性材料加内部介孔通道添加抗癌抗艾滋病抗 炎药物的方式和纯放射性材料的方式制作。 1. An anti-cancer, anti-AIDS, and anti-inflammatory drug with radiotherapy and a preparation method thereof, consisting of mesoporous radioactive nanomicrospheres (1), a radiation-proof inert metal layer (21A), an anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A), It is composed of mesoporous radioactive nano-microsphere radiating mesopores (4), nano-radiation protection valves (5), and nano-targeting carrier layers (6). It is characterized in that: from the inside to the outside, there are mesoporous radioactive nano-microspheres (1). , radiation-proof inert metal layer (21A), anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A), nano-targeting carrier layer (6), the anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A) can also be eliminated; mesoporous radioactive nanometer There are numerous mesoporous radioactive nano-microsphere radiation mesopores (4) and nano-radiation protection valves (5) on the surface of the microsphere (1). The nano-radiation protection valve (5) and the mesoporous radioactive nano-microsphere radiation mesopores (5) 4) Connected; Mesoporous radioactive nanospheres (1) can be made by using radioactive materials plus internal mesoporous channels to add anti-cancer, anti-AIDS, and anti-inflammatory drugs, or by using pure radioactive materials.
2、 一种带放疗抗癌抗艾滋病抗炎药物及其制备方法, 由介孔放射性纳米微球 ( 1 ) 、 吸波膜层 (21B) 、 抗癌抗艾滋病抗炎药物层 (3A) 、 介孔放射性纳米 微球辐射介孔口 (4) 、 纳米防辐射阀门 (5) 、 纳米靶向载体层 (6) 组成, 其特征在于: 由内至外依次是介孔放射性纳米微球 (1 ) 、 吸波膜层 (21B) 、 抗癌抗艾滋病抗炎药物层 (3A) 、 纳米靶向载体层 (6 ) , 也可以取消抗癌抗 艾滋病抗炎药物层 (3A) ; 介孔放射性纳米微球 (1 ) 表面有众多的介孔放射 性纳米微球辐射介孔口 (4) 和纳米防辐射阀门 (5) , 纳米防辐射阀门 (5 ) 与介孔放射性纳米微球辐射介孔口 (4)相连接连通; 介孔放射性纳米微球(1 ) 可分别采用放射性材料加内部介孔通道添加抗癌抗艾滋病抗炎药物的方式和 纯放射性材料的方式制作。 2. An anti-cancer, anti-AIDS, and anti-inflammatory drug with radiotherapy and its preparation method, consisting of mesoporous radioactive nanomicrospheres (1), a wave-absorbing film layer (21B), an anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A), mesoporous It consists of a radioactive nano-microsphere radiation mesopore opening (4), a nano-radiation protection valve (5), and a nano-targeting carrier layer (6). It is characterized by: from the inside to the outside, there are mesoporous radioactive nano-microspheres (1), Wave-absorbing film layer (21B), anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A), nano-targeting carrier layer (6), the anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A) can also be eliminated; mesoporous radioactive nanospheres (1) There are numerous mesoporous radioactive nano-microsphere radiating mesopores (4) and nano-radiation protection valves (5) on the surface. The nano-radiation protection valve (5) and mesoporous radioactive nano-microsphere radiating mesopores (4) Connected and connected; mesoporous radioactive nanospheres (1) can be made by using radioactive materials plus internal mesoporous channels to add anti-cancer, anti-AIDS, and anti-inflammatory drugs, or by using pure radioactive materials.
3、 一种带放疗抗癌抗艾滋病抗炎药物及其制备方法, 由介孔放射性纳米微球 (1) 、 防辐射活跃金属膜层 (22A) 、 防金属和有机物污染保护膜层 (31) 、 抗癌抗艾滋病抗炎药物层 (3A) 、 介孔放射性纳米微球辐射介孔口 (4) 、 纳 米防辐射阀门 (5) 、 纳米靶向载体层 (6) 组成, 其特征在于: 由内至外依次 是介孔放射性纳米微球 (1) 、 防辐射活跃金属膜层 (22A) 、 防金属和有机物 污染保护膜层(31)、抗癌抗艾滋病抗炎药物层(3A)、纳米靶向载体层(6) , 也可以取消抗癌抗艾滋病抗炎药物层 (3A) ; 介孔放射性纳米微球 (1) 表面 有众多的介孔放射性纳米微球辐射介孔口 (4) 和纳米防辐射阀门 (5) , 纳米 防辐射阀门 (5) 与介孔放射性纳米微球辐射介孔口 (4) 相连接连通; 介孔放 射性纳米微球 (1) 可分别采用放射性材料加内部介孔通道添加抗癌抗艾滋病 抗炎药物的方式和纯放射性材料的方式制作。 3. An anti-cancer, anti-AIDS, and anti-inflammatory drug with radiotherapy and its preparation method, consisting of mesoporous radioactive nanometer microspheres (1), anti-radiation active metal film layer (22A), anti-metal and organic pollution protective film layer (31), anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A), mesoporous radioactive nanosphere radiation mesopores (4 ), a nano-radiation protection valve (5), and a nano-targeting carrier layer (6), which are characterized in that: from the inside to the outside, there are mesoporous radioactive nano-microspheres (1), a radiation-proof active metal film layer (22A), Anti-metal and organic pollution protective film layer (31), anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A), nano-targeting carrier layer (6), the anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A) can also be eliminated; mesoporous There are numerous mesoporous radioactive nanosphere radiating mesopores (4) and nano-radiation protection valves (5) on the surface of the radioactive nano-microsphere (1). The nano-radiation protection valve (5) and mesoporous radioactive nano-microsphere radiating mesopores The ports (4) are connected to each other; the mesoporous radioactive nano-microspheres (1) can be made by using radioactive materials plus internal mesoporous channels to add anti-cancer, anti-AIDS, and anti-inflammatory drugs, or by using pure radioactive materials.
4、 一种带放疗抗癌抗艾滋病抗炎药物及其制备方法, 由介孔放射性纳米微球 (1) 、 吸波膜层 (21B) 、 防金属和有机物污染保护膜层 (31) 、 抗癌抗艾滋 病抗炎药物层 (3A) 、 介孔放射性纳米微球辐射介孔口 (4) 、 纳米防辐射阀 门 (5) 、 纳米靶向载体层 (6) 组成, 其特征在于: 由内至外依次是介孔放射 性纳米微球 (1) 、 吸波膜层 (21B) 、 防金属和有机物污染保护膜层 (31) 、 抗癌抗艾滋病抗炎药物层 (3A) 、 纳米靶向载体层 (6) , 也可以取消抗癌抗 艾滋病抗炎药物层 (3A) ; 当吸波膜层 (21B) 采用无毒无生物反应的材料时, 取消防金属和有机物污染保护膜层 (31) ; 介孔放射性纳米微球 (1) 表面有 众多的介孔放射性纳米微球辐射介孔口 (4) 和纳米防辐射阀门 (5) , 纳米防 辐射阔门 (5) 与介孔放射性纳米微球辐射介孔口 (4) 相连接连通; 介孔放射 性纳米微球 (1) 可分别采用放射性材料加内部介孔通道添加抗癌抗艾滋病抗 炎药物的方式和纯放射性材料的方式制作。 4. An anti-cancer, anti-AIDS, and anti-inflammatory drug with radiotherapy and its preparation method, which consists of mesoporous radioactive nanometer microspheres (1), a wave-absorbing film layer (21B), a protective film layer (31) against metal and organic pollution, and an anti-cancer drug. It consists of an anti-AIDS and anti-inflammatory drug layer (3A), a mesoporous radioactive nanosphere radiation mesopore (4), a nano-radiation protection valve (5), and a nano-targeting carrier layer (6). It is characterized by: from the inside to the outside In order, they are mesoporous radioactive nano-microspheres (1), wave-absorbing film layer (21B), anti-metal and organic pollution protective film layer (31), anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A), and nano-targeting carrier layer ( 6), you can also cancel the anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A); when the absorbing film layer (21B) uses non-toxic and non-biologically reactive materials, the anti-metal and organic pollution protective film layer (31) can be cancelled; There are numerous mesoporous radioactive nanospheres radiating mesopores (4) and nanoradiation protection valves (5) on the surface of the pore radioactive nanospheres (1). The mesopore openings (4) are connected to each other; the mesoporous radioactive nanomicrospheres (1) can be made by using radioactive materials plus internal mesoporous channels to add anti-cancer, anti-AIDS, and anti-inflammatory drugs, or by using pure radioactive materials.
5、 一种带放疗抗癌抗艾滋病抗炎药物及其制备方法, 由介孔放射性纳米微球 (1) 、 放射性金属膜层 (23) 、 防辐射层 (32) 、 抗癌抗艾滋病抗炎药物层 (3A) 、 介孔放射性纳米微球辐射介孔口(4)、 纳米防辐射阔门 (5)、 准轮烷或 轮烷"闽芯" (5A)、 纳米靶向载体层 (6)组成, 其特征在于: 由内至外依次是介 孔放射性纳米微球 (1 ) 、 放射性金属膜层 (23) 、 防辐射层 (32 ) 、 抗癌抗 艾滋病抗炎药物层 (3A) 、 纳米靶向载体层 (6) , 也可以取消抗癌抗艾滋病抗 炎药物层 (3A) ; 介孔放射性纳米微球 (1 ) 表面有众多的介孔放射性纳米微 球辐射介孔口 (4) 和纳米防辐射阀门(5), 纳米防辐射阔门(5)与介孔放射性 纳米微球辐射介孔口 (4) 相连接连通; 介孔放射性纳米微球 (1 ) 可分别采用 放射性材料加内部介孔通道添加抗癌抗艾滋病抗炎药物的方式和纯放射性材 料的方式制作。 5. An anti-cancer, anti-AIDS, and anti-inflammatory drug with radiotherapy and a preparation method thereof, which is composed of mesoporous radioactive nanometer microspheres (1), a radioactive metal film layer (23), a radiation protection layer (32), and an anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A), mesoporous radioactive nanosphere radiating mesopores (4), nano radiation-proof wide doors (5), pseudorotaxane or rotaxane "min core" (5A), and nano-targeting carrier layer (6) , which is characterized by: from the inside to the outside, there are mesoporous radioactive nanospheres (1), radioactive metal film layer (23), radiation protection layer (32), anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A), and nano-target To the carrier layer (6), the anti-cancer, anti-AIDS, and anti-inflammatory drug layer (3A) can also be eliminated; the surface of the mesoporous radioactive nanosphere (1) has numerous mesoporous radioactive nanosphere radiating mesopores (4) and nanometer The radiation protection valve (5), the nano-radiation protection wide door (5) are connected with the mesoporous radioactive nano-microsphere radiation mesopore (4); the mesoporous radioactive nano-microsphere (1) can be made of radioactive materials and internal media respectively. The hole channels are made by adding anti-cancer, anti-AIDS, anti-inflammatory drugs and pure radioactive materials.
PCT/CN2013/001069 2012-09-25 2013-09-13 Anti-inflammatory drug against cancer and aids with radiotherapy and preparation method thereof WO2014048060A1 (en)

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