CN103656692A - Nano targeted or ordinary anticancer medicament with radiotherapy function and preparation method thereof - Google Patents
Nano targeted or ordinary anticancer medicament with radiotherapy function and preparation method thereof Download PDFInfo
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Abstract
The invention discloses a nano targeted or ordinary anticancer medicament with a radiotherapy function. The medicament consists of a mesoporous radioactivity nano microsphere, a radiation protection inert metal or microwave absorpting film layer, an anticancer or ordinary medicament layer, a mesoporous radioactivity nanoparticle radiation mesoporous opening, a nano radiation prevention valve and a nano target carrier layer, wherein the mesoporous radioactivity nano microsphere, the radiation protection inert metal or microwave absorpting film layer, the anticancer or ordinary medicament layer and the nano target carrier layer are arranged inside to outside in sequence; under the action and control of external electricity, light, magnetism and sound, the nano radiation protection valve can be automatically opened and closed; the anticancer target medicament or non-target ordinary medicament inside the mesoporous radioactivity nano microsphere is slowly released to the outside through the mesoporous radioactivity nanoparticle radiation mesoporous opening, so as to kill the cancer tissues and cancer cells in a radiotherapy mode; and when the nano radiation protection valve is automatically opened, radioactive ray inside the mesoporous radioactivity nano microsphere can be radiated out through the mesoporous radioactivity nanoparticle radiation mesoporous opening outside, so as to kill the cancer tissues and cancer cells at a target point in a radiotherapy mode.
Description
Affiliated technical field:
---the present invention relates to nanometer manufacture, molecular biosciences cancer therapy drug and radiotherapy anti-cancer technology, specifically a kind of nano target with radiotherapy function or conventional cancer therapy drug and preparation method thereof.
Technical background:
Treatment cancer adopts the methods such as radiation and chemotherapy, operation or the traditional Chinese medical science more both at home and abroad at present, the radioactive substance that hospital uses when tumour radiotherapy, and just the oncosis talent can use, in order to tackle tumor, although health is had to danger, deposit evil, choose the light for two of the victims, have to use.The secondary injury of the traditional therapy of cancer has been greater than cancer itself, this is a global difficult problem for puzzlement modern medicine treatment cancer always, a maximum obstacle of tradition anticancer therapy application is in killing off tumor cells, also often to affect the cell of normal structure, causes various complication.Pathogenesis of cancer process cancer also claims malignant tumor, is disease not normal by control growth and proliferation of cell mechanism and that cause.Cancerous cell except grow out of control, arround also can locally invading, normal structure is even transferred to other parts of health via body-internal-circulation system or lymphsystem, because cancerous cell can spread, shift or recurrence, what a lot of cancer patients often brought after using up a large amount of expense treatments is generally the survival period of 3-5, obtain the life-span extending very limited, tradition anti-cancer technology obviously exists the secondary injury of cancer patient's treatment large defect and survival period short, the shortcoming that expense is high, simultaneously, radiation and chemotherapy can cause cancer patient's immunity of destroyed function greatly to reduce, diffusion for cancer, larger hidden danger has been buried in transfer and recurrence, this technology adopts targeting or the conventional cancer therapy drug with radiotherapy function, adopt Synergistic treatment and the slow release treatment of the medicines such as targeting, strengthen the dynamics for the treatment of, on the one hand, the skin that traditional radiotherapy is caused and subcutaneous tissue, the infringement of organ reduces greatly, greatly control the speed of growth of cancerous cell, on the other hand, relatively improve patient's immunity, for treatment tries to gain time precious to one, the probability that the slight cancerous cell of diffusion or transfer is wiped up improves significantly.
Summary of the invention:
1, be successively from the inside to the outside mesoporous radioactive nano microsphere, radioprotective inert metal or suction ripple rete, anti cancer target or conventional medicine layer, nano target carrier layer; Mesoporous radioactive nano microsphere surface has mesoporous mouthful of numerous mesoporous radioactive nano microsphere radiation and nano-antiradiation valve, mesoporous mouthful of connection that is connected of nano-antiradiation valve and the radiation of mesoporous radioactive nano microsphere; Mesoporous radioactive nano microsphere can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make; Anti cancer target or conventional medicine layer are more than 0 layer or 1 layer or 1 layer; Whether mesoporous radioactive nano microsphere is no matter in the situation that adopting active material to add inner mesoporous passage to add anticancer targeting medicine or non-targeted conventional medicine, under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nano-antiradiation valve can be opened automatically, the anticancer targeting medicine of mesoporous radioactive nano microsphere inside or non-targeted conventional medicine be by the mesoporous mouthful outwards slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill; When the switch of nano-antiradiation valve is opened automatically, the lonizing radiation of mesoporous radioactive nano microsphere inside are mesoporous mouthful to external radiation by the radiation of mesoporous radioactive nano microsphere in the external world, the cancerous cell of the cancerous tissue of target spot is carried out to " radiotherapy " and kill; On the other hand, anti cancer target or conventional medicine layer carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast; Said process is the independent or cohesive process of radiation and chemotherapy.
2, be successively from the inside to the outside mesoporous radioactive nano microsphere, radioprotective inert metal or suction ripple rete, anti cancer target or conventional medicine layer, nano target carrier layer; Mesoporous radioactive nano microsphere surface has mesoporous mouthful of numerous mesoporous radioactive nano microsphere radiation and nano-antiradiation valve, mesoporous mouthful of connection that is connected of nano-antiradiation valve and the radiation of mesoporous radioactive nano microsphere; Mesoporous radioactive nano microsphere can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make; Anti cancer target or conventional medicine layer are more than 0 layer or 1 layer or 1 layer; When radioprotective enlivens metallic diaphragm or inhales ripple rete while only using the suction ripple rete of nontoxic inanimate object reaction, anti-metal or Organic Pollution protective film can be 0 layer; Whether mesoporous radioactive nano microsphere is no matter in the situation that adopting active material to add inner mesoporous passage to add anticancer targeting medicine or non-targeted conventional medicine, under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nano-antiradiation valve can be opened automatically, the anticancer targeting medicine of mesoporous radioactive nano microsphere inside or non-targeted conventional medicine be by the mesoporous mouthful outwards slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill; When the switch of nano-antiradiation valve is opened automatically, the lonizing radiation of mesoporous radioactive nano microsphere inside are mesoporous mouthful to external radiation by the radiation of mesoporous radioactive nano microsphere in the external world, the cancerous cell of the cancerous tissue of target spot is carried out to " radiotherapy " and kill; On the other hand, anti cancer target or conventional medicine layer carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast; Said process is the independent or cohesive process of radiation and chemotherapy.
3, be successively from the inside to the outside mesoporous radioactive nano microsphere, radioactive metal rete, radiation protective layer, anti cancer target or conventional medicine layer, nano target carrier layer; Mesoporous radioactive nano microsphere surface has mesoporous mouthful of numerous mesoporous radioactive nano microsphere radiation and nanometer radioactive radiation valve, mesoporous mouthful of connection that is connected of nanometer radioactive radiation valve and the radiation of mesoporous radioactive nano microsphere; Mesoporous radioactive nano microsphere can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make; Anti cancer target or conventional medicine layer are more than 0 layer or 1 layer or 1 layer; Whether mesoporous radioactive nano microsphere (1) is no matter in the situation that adopting active material to add inner mesoporous passage to add anticancer targeting medicine or non-targeted conventional medicine, under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nanometer radioactive radiation valve can be opened automatically, the anticancer targeting medicine of mesoporous radioactive nano microsphere inside or non-targeted conventional medicine be by the mesoporous mouthful outwards slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill; When the switch of nanometer radioactive radiation valve is opened automatically, the lonizing radiation of the lonizing radiation of mesoporous radioactive nano microsphere inside and nanometer radioactive radiation valve mesoporous mouthful by the radiation of mesoporous radioactive nano microsphere in the external world itself, all to external radiation, carry out " radiotherapy " to the cancerous cell of the cancerous tissue of target spot and kill; On the other hand, anti cancer target or conventional medicine layer carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast; Said process is the independent or cohesive process of radiation and chemotherapy.
Technical problem to be solved by this invention:
Overcome the deficiency that secondary injury is large and survival period is short and expense is high of the Therapeutic Method of existing cancer, this technology adopts targeting or the conventional cancer therapy drug with radiotherapy function, adopt Synergistic treatment and the slow release treatment of the medicines such as targeting, strengthen the dynamics for the treatment of, reach " skin that traditional radiotherapy is caused and subcutaneous tissue, the infringement of organ reduces greatly, greatly control the speed of growth of cancerous cell, relatively improve patient's immunity, for treatment tries to gain time precious to one, the probability that the slight cancerous cell of the cancerous cell of existing refractory or diffusion or transfer is also wiped up improves significantly " good result.
Specification requirement of the present invention is such:
1), mesoporous radioactive nano microsphere can adopt separately the natural or artificial active material that can emit from atomic nucleus inside particle or ray (as alpha ray, β ray, gamma-rays etc.), for example radiant is greatly uranium (U), thorium (Th) and radium (Ra), or kalium-40 (40K), rubidium (Rb) and caesium (Cs) etc., or the mixing of active material and ceramic powders etc., and according to the actual state of an illness, need to determine the kind of required radioactive substance.
2), for guaranteeing proper flow and the infiltration of this medicine in blood and health, the proportion concentration after medicine modulation preferably and blood match, for example proportion is preferably no more than the proportion 1.05 of blood, to avoid precipitation.
3), for reaching good radiation-proof effect, radioprotective enlivens metallic diaphragm or inhales ripple rete while for example adopting lead material, thickness is preferably thicker than 23 microns.
4), react with bodily tissue for avoiding, radioprotective inert metal or inhale ripple rete and can adopt and variously there is radiation-resistant inert metal for example gold or silver or silica gel absorb wave materials.
5), pseudorotaxane or the rotaxane " spool " of nano-antiradiation valve, preferably adopt and possess such as metal or silicon materials etc. of radiation-resistant material.
6), for prevent this medicine volume evenly to increase curative effect, can set to the solution of medicine the filtration in aperture.
7), for there is other medicine, likely cannot by metabolism, excrete completely at the appointed time, can be by the method filtering of hemodialysis, if desired, can all increase magnetisable material at filter membrane and mesoporous radioactive nano microsphere, by the filtering better of the methods such as magnetic.
8), preferably targeting, conventional medicine layer are placed on to outermost in the independent assortment layer of the independent assortment layer of radiation protective layer, targeting, conventional medicine layer or plastic foil, radiation protective layer, targeting, conventional medicine layer, with the drug release effect having reached.
9), for guaranteeing that the normal cell of human body does not come to harm, while adopting the third method, the radioactive intensity of nanometer radioactive radiation valve (6) must suitably adopt the active material of lower radioactivities, such as cobalt etc.
The technical scheme that technical solution problem of the present invention adopts:
1, be successively from the inside to the outside mesoporous radioactive nano microsphere, radioprotective inert metal or suction ripple rete, anti cancer target or conventional medicine layer, nano target carrier layer; Mesoporous radioactive nano microsphere surface has mesoporous mouthful of numerous mesoporous radioactive nano microsphere radiation and nano-antiradiation valve, mesoporous mouthful of connection that is connected of nano-antiradiation valve and the radiation of mesoporous radioactive nano microsphere; Mesoporous radioactive nano microsphere can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make; Anti cancer target or conventional medicine layer are more than 0 layer or 1 layer or 1 layer; Whether mesoporous radioactive nano microsphere is no matter in the situation that adopting active material to add inner mesoporous passage to add anticancer targeting medicine or non-targeted conventional medicine, under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nano-antiradiation valve can be opened automatically, the anticancer targeting medicine of mesoporous radioactive nano microsphere inside or non-targeted conventional medicine be by the mesoporous mouthful outwards slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill; When the switch of nano-antiradiation valve is opened automatically, the lonizing radiation of mesoporous radioactive nano microsphere inside are mesoporous mouthful to external radiation by the radiation of mesoporous radioactive nano microsphere in the external world, the cancerous cell of the cancerous tissue of target spot is carried out to " radiotherapy " and kill; On the other hand, anti cancer target or conventional medicine layer carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast; Said process is the independent or cohesive process of radiation and chemotherapy.
2, be successively from the inside to the outside mesoporous radioactive nano microsphere, radioprotective inert metal or suction ripple rete, anti cancer target or conventional medicine layer, nano target carrier layer; Mesoporous radioactive nano microsphere surface has mesoporous mouthful of numerous mesoporous radioactive nano microsphere radiation and nano-antiradiation valve, mesoporous mouthful of connection that is connected of nano-antiradiation valve and the radiation of mesoporous radioactive nano microsphere; Mesoporous radioactive nano microsphere can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make; Anti cancer target or conventional medicine layer are more than 0 layer or 1 layer or 1 layer; When radioprotective enlivens metallic diaphragm or inhales ripple rete while only using the suction ripple rete of nontoxic inanimate object reaction, anti-metal or Organic Pollution protective film can be 0 layer; Whether mesoporous radioactive nano microsphere is no matter in the situation that adopting active material to add inner mesoporous passage to add anticancer targeting medicine or non-targeted conventional medicine, under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nano-antiradiation valve can be opened automatically, the anticancer targeting medicine of mesoporous radioactive nano microsphere inside or non-targeted conventional medicine be by the mesoporous mouthful outwards slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill; When the switch of nano-antiradiation valve is opened automatically, the lonizing radiation of mesoporous radioactive nano microsphere inside are mesoporous mouthful to external radiation by the radiation of mesoporous radioactive nano microsphere in the external world, the cancerous cell of the cancerous tissue of target spot is carried out to " radiotherapy " and kill; On the other hand, anti cancer target or conventional medicine layer carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast; Said process is the independent or cohesive process of radiation and chemotherapy.
3, be successively from the inside to the outside mesoporous radioactive nano microsphere, radioactive metal rete, radiation protective layer, anti cancer target or conventional medicine layer, nano target carrier layer; Mesoporous radioactive nano microsphere surface has mesoporous mouthful of numerous mesoporous radioactive nano microsphere radiation and nanometer radioactive radiation valve, mesoporous mouthful of connection that is connected of nanometer radioactive radiation valve and the radiation of mesoporous radioactive nano microsphere; Mesoporous radioactive nano microsphere can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make; Anti cancer target or conventional medicine layer are more than 0 layer or 1 layer or 1 layer; Whether mesoporous radioactive nano microsphere (1) is no matter in the situation that adopting active material to add inner mesoporous passage to add anticancer targeting medicine or non-targeted conventional medicine, under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nanometer radioactive radiation valve can be opened automatically, the anticancer targeting medicine of mesoporous radioactive nano microsphere inside or non-targeted conventional medicine be by the mesoporous mouthful outwards slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill; When the switch of nanometer radioactive radiation valve is opened automatically, the lonizing radiation of the lonizing radiation of mesoporous radioactive nano microsphere inside and nanometer radioactive radiation valve mesoporous mouthful by the radiation of mesoporous radioactive nano microsphere in the external world itself, all to external radiation, carry out " radiotherapy " to the cancerous cell of the cancerous tissue of target spot and kill; On the other hand, anti cancer target or conventional medicine layer carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast; Said process is the independent or cohesive process of radiation and chemotherapy.
Realize concrete mode and requirements more of the present invention:
1, Jie's pore size of mesoporous radioactive nano microsphere is preferably controlled at 2～50nm scope.
2, the polymerization of mesoporous radioactive nano microsphere and nano-antiradiation valve can adopt assembling or the assembling of other chemical methodes, but preferably adopts self assembly mode, to realize production in enormous quantities.
3, mesoporous radioactive nano microsphere can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make.
The beneficial effect that the present invention produces is:
Overcome the deficiency that secondary injury is large and survival period is short and expense is high of the Therapeutic Method of existing cancer, this technology adopts targeting or the conventional cancer therapy drug with radiotherapy function, adopt Synergistic treatment and the slow release treatment of the medicines such as targeting, strengthen the dynamics for the treatment of, reach " skin that traditional radiotherapy is caused and subcutaneous tissue, the infringement of organ reduces greatly, greatly control the speed of growth of cancerous cell, relatively improve patient's immunity, for treatment tries to gain time precious to one, the probability that the slight cancerous cell of the cancerous cell of existing refractory or diffusion or transfer is also wiped up improves significantly " good result.
Accompanying drawing explanation:
Fig. 1 is cutaway view of the present invention and sketch.
As shown in the figure: 1, mesoporous radioactive nano microsphere, 2, radioprotective inert metal or suction ripple rete, 3, the independent assortment layer of the independent assortment layer of anti cancer target or conventional medicine layer or radiation protective layer, targeting, conventional medicine layer or plastic foil, radiation protective layer, targeting, conventional medicine layer, 4, the radiation of mesoporous radioactive nano microsphere is mesoporous mouthful, 5, nano-antiradiation valve, 5A, pseudorotaxane or rotaxane " spool ", 6, nano target carrier layer.Fig. 2 is cutaway view of the present invention and sketch.
As shown in the figure: 1, mesoporous radioactive nano microsphere; 2, radioprotective enlivens metallic diaphragm or inhales ripple rete; 3, anti-metal or Organic Pollution protective film; 4, anti cancer target or conventional medicine layer; 5, the radiation of mesoporous radioactive nano microsphere is mesoporous mouthful; 6, nano-antiradiation valve, 6A, pseudorotaxane or rotaxane " spool ", 7, nano target carrier layer.
Fig. 3 is cutaway view of the present invention and sketch.
As shown in the figure: 1, mesoporous radioactive nano microsphere, 2, radioactive metal rete, 3, radiation protective layer, 4, anti cancer target or conventional medicine layer, 5, the radiation of mesoporous radioactive nano microsphere is mesoporous mouthful, 6, nanometer radioactive radiation valve, 6A, pseudorotaxane or rotaxane " spool ", 7, nano target carrier layer.
Fig. 4 is the supramolecular structured compositions such as pseudorotaxane that the radioprotective metal cluster of one of them structure of nano-antiradiation valve (5) is core.
4, the radiation of mesoporous radioactive nano microsphere is mesoporous mouthful, 5A, pseudorotaxane or rotaxane " spool ".
The specific embodiment: below in conjunction with accompanying drawing and and preferred embodiment narration embodiment of the present invention 1:
Fig. 1 a kind ofly analyses and observe macroscopical enlarged drawing with the nano target of radiotherapy function or the structure of conventional cancer therapy drug:
(1), a kind of nano target with radiotherapy function or the simple preparation method of conventional cancer therapy drug:
The 1st step: make the mesoporous radioactive nano microsphere (1) that surface has nano-antiradiation valve (5) the function base of radioprotective metal ion:
So that active material is for example natural or artificial, can from atomic nucleus inside, emit particle or ray (as alpha ray, β ray, gamma-rays etc.) uranium (U), thorium (Th) and radium (Ra), or kalium-40 (40K), the active materials such as rubidium (Rb) and caesium (Cs) and silicon dioxide composite material or independent active material are base material, adopt for example coprecipitation of the methods such as chemistry or biosynthesis or machinery, sol-gal process, dispersion copolymerization method or controllable free-radical polymerisation method are synthesized size homogeneous, for example, compared with large pore volume (0.6--5cm3/g), high-specific surface area (for example 700--1500m2/g), the mesoporous radioactive nano microsphere of radioactivity (1) that hole wall high density is modified, for example: can adopt following several method preparation, etc.,
Method 1), calcium carbonate and radium active material are mixed after the powder of mechanical grinding reach nano-scale and add, after gel desolventizing by Diluted Acid Washing out.
Method 2), preparation method comprises by coprecipitation and prepares radioactive particle; Again washed radioactive particle is directly distributed to in the aqueous solution containing the water-soluble inorganic salt of SiO2, to carry out inorganic silicon source coated or mix; Then the cetyl trimethyl ammonium bromide of take is coated or mixes as template, ethyl orthosilicate carry out mesoporous silicon oxide as silicon source.
Method 3), adopt sodium hypophosphite liquid-phase reduction method to prepare nanometer radium colloidal sol, take ethyl orthosilicate as silicon source again, cetyl trimethyl ammonium bromide is template, adopt sol-gel process, radium particle surface growth in situ silicon dioxide spherical shell in the nanometer radium colloidal sol of preparation, then utilize solvent extraction to remove organic formwork agent, then after supercritical drying, prepare the coated radium nano-particle of mesoporous silicon oxide.
Method 4), as patented number is 03153265, name is called " a kind of preparation method of micron spherical mesoporous SiO 2 ", patentee is the mandate of " Physical Chemistry Technology Inst., Chinese Academy of Sciences ", can take following method step preparation, content comprises: (1) preparating acid solution, and the concentration of acid is 0.01～10 mol/L; 2) in the solution of step (1), add surfactant, the concentration that makes cetyl trimethyl ammonium halide in mixed solution is 0.001～5 mol/L, the concentration of polyvinyl alcohol is 0.01～20 grams per liter, and the concentration of poly-(oxygen ethylene)-poly-(oxypropylene)-poly-(oxygen ethylene) is 110 ↑ [6]～510 ↑ [3] mol/L; (3) esters of silicon acis is added in the mixed solution that step (2) obtains, the concentration that makes mixed esters of silicon acis is 0.01～5 mol/L, continues to stir, standing, obtain the solution of white precipitate, centrifugalize, washing, dry, roasting, obtains mesoporous silicon oxide, afterwards, again by radium material nano powdered, and then mix, obtain the silica mixture that contains radium element.
After mesoporous radioactive nano microsphere (1) preparation, again by the inner successful grafting in mesoporous surface or physical absorption anticancer targeting medicine or the non-targeted conventional medicine of mesoporous radioactive nano microsphere (1), preparation load the hole radioactive nano microsphere (1) of anticancer targeting medicine or non-targeted conventional medicine; Mesoporous radioactive nano microsphere (1) can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make.
Due between metal ion and metal and ligand coordinate bond very by force or very strong, become the active force that drives supermolecule self assembly, by copolymerization, the methods such as surface modification and supermolecule self assembly, the component that contains the supramolecular 26S Proteasome Structure and Functions such as silver metal or silicon molecule or building block are assembled into new super molecular compound according to the mode of design, by interaction or Cheng Jian between metal and metallic molecule, obtain the mesoporous radioactive nano microsphere (1) that surface has nano-antiradiation valve (5) the function base of radioprotective metal ion, can be directly in conjunction with, also can be again in conjunction with obtaining after chemical modification.For example adopt statistics to be wound around, chemistry shifts, driven by hydrogen bond, driven by hydrophilic-hydrophobic interaction, driven by metal-complexing effect, with interacted by pi-pi accumulation and charge transfer drives, threading blocking method, fast the method such as solvent evaporation method is for example: following methods obtain surface have radioprotective metal ion nano-antiradiation valve (5) function base metal rotaxane or have radiotherapy function the metal rotaxane of nanometer active material valve (5) function base, for example (1): the artificial radioisotope's Co 60 that can replace X ray to be used for treating cancer of take is example, the class rotaxane being generated by Cucurbituril cucurbituril and spermine hydrochlorate, after hydrated alkyl cobalt oxime generation self-assembling reaction, in aqueous solution, formed a kind of novel metal rotaxane, again for example (2): can successfully develop a kind of metal cluster that utilizes with reference to Chinese department of chemistry, tsinghua university Wang Meixiang professor associate professor He Zhaoliang seminar and as coordination core, carry out the new method (as they or unit have applied for a patent the license that needs patented power people) of self assembly, specifically: utilize radioprotective metal cluster to carry out self assembly as coordination core, that is: utilize anionic organic ligand to instruct the synthetic of regulation and control radioprotective metal cluster, then use macrocyclic compound and the coordination of radioprotective metal cluster, generation has the radioprotective metal cluster assembly of specific coordination direction, and then using other part as connexon, thereby obtain the pseudorotaxane that radioprotective metal cluster is core, the supramolecular structures such as lock hydrocarbon, such as (3): utilize metal ion to introduce metal ion and coordination compound thereof as template or in the supramolecular systems such as rotaxane, catenne, synthesized the novel supermolecules such as a variety of metal rotaxanes, catenne.By methods such as self assemblies, the supermolecule pseudorotaxanes such as silver metal or rotaxane are constructed on mesoporous radioactive nano microsphere (1) surface, it is bobbin molecule that formation be take functionalized nano silicon or nanometer silver, the supermolecule nano radioprotective valve (5) that the supermolecules such as silver metal can slide on bobbin, control the new function discharging with switch, thereby obtain the mesoporous radioactive nano microsphere (1) that surface has nano-antiradiation valve (5) the function base of radioprotective metal ion, by pH, discharge with the control of competition in conjunction with supermolecule nano valves such as driving silver metal such as the dual pathwayss, meet the multiple release and the switch demand that impose a condition.The mesoporous radioactive nano microsphere (1) of take is nano container, the control of the supermolecule nano valves such as silver metal that nano target carrier layer (6) such as amino acid decarboxylases causes discharges, this transports system and has biological targeting and switching function, and can discharge by multistep control on demand.Under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nano-antiradiation valve (5) is opened automatically, the anticancer targeting medicine that mesoporous radioactive nano microsphere (1) is inner or non-targeted conventional medicine be by mesoporous mouthful of (4) outside slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill; When the switch of nano-antiradiation valve (5) is opened automatically, the inner lonizing radiation of mesoporous radioactive nano microsphere (1) in the external world by the mesoporous mouth of mesoporous radioactive nano microsphere radiation (4) to external radiation, the cancerous cell of the cancerous tissue of target spot is carried out to " radiotherapy " and kills; On the other hand, 3, the independent assortment layer (3) of the independent assortment layer of anti cancer target or conventional medicine layer or radiation protective layer, targeting, conventional medicine layer or plastic foil, radiation protective layer, targeting, conventional medicine layer carries out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kills fast; Said process is that radiation and chemotherapy carries out individually or simultaneously.
The 2nd step: by radioprotective inert metal or inhale that ripple rete (2) is coated or coating is upper to mesoporous radioactive nano microsphere (1):
The methods such as employing physisorphtion, arc discharge method, Plasma Polymerization, laser chemical vapor deposition method, electroless plating method, emulsion polymerization, surface deposition method (electroless plating method, heterogeneous precipitation method) are by radioprotective inert metal or suction ripple rete (2) is coated or coating arrives on mesoporous radioactive nano microsphere (1).
The 3rd step: by methods such as physical absorption, chemical infiltration, copolymerization, magnetic, surface modifications by 3, the independent assortment layer (3) of the independent assortment layer of anti cancer target or conventional medicine layer or radiation protective layer, targeting, conventional medicine layer or plastic foil, radiation protective layer, targeting, conventional medicine layer is coated, covers or be adsorbed on radioprotective inert metal or inhale on ripple rete (2).
The 4th step: by methods such as chemical modification and polymerizations by the compound nano target carrier layer (6) of preparing of the targeting vectors such as lipase.
The 5th step: by the methods such as modification, magnetic, copolymerization by nano target carrier layer (6) be coated, cover 3, on the independent assortment layer (3) of the independent assortment layer of anti cancer target or conventional medicine layer or radiation protective layer, targeting, conventional medicine layer or plastic foil, radiation protective layer, targeting, conventional medicine layer.
(2), the process of a kind of nano target with radiotherapy function or conventional cancer therapy drug anticancer mechanism:
(1), the process of radiotherapy and slow release cancer therapy drug:
By mesoporous radioactive nano microsphere (1), radioprotective inert metal or suction ripple rete (2), 3, anti cancer target or conventional medicine layer or radiation protective layer, targeting, independent assortment layer or the plastic foil of conventional medicine layer, radiation protective layer, targeting, the independent assortment layer (3) of conventional medicine layer, mesoporous mouthful of mesoporous radioactive nano microsphere radiation (4), nano-antiradiation valve (5), a kind of nano target with radiotherapy function that nano target carrier layer (6) forms or conventional cancer therapy drug and preparation method thereof, as the injection of injection blood or intramuscular injection or otch inject or oral as oral medicine after, medicine absorbs with blood or gastrointestinal blood circulation and the lymphsystem that enters into health, under the target biology guiding of nano target carrier layer (6), targeted anticancer medicine focuses on target spot position cancerous tissue and cancerous cell because of bio-guide effect, the cancerous tissue cell that conventional cancer therapy drug flow to whole body with blood circulation is killed, under the effect and control of extraneous electricity, light, magnetic, sound, pseudorotaxane in nano-antiradiation valve (5) or rotaxane " spool " the electrical power of Molecular Ring quilt or magnetive attraction (5A) drives while moving upward, valve is just in "open" state, and the lonizing radiation in mesoporous radioactive nano microsphere (1) are killed the cancerous cell of the cancerous tissue of target spot by mesoporous radioactive nano microsphere radiation mesoporous mouthful (4), the cancer therapy drug that is positioned at the mesoporous passage absorption of mesoporous radioactive nano microsphere (1) passes through mesoporous mouthful of (4) external slow release of mesoporous radioactive nano microsphere radiation, and the cancerous cell of the cancerous tissue of target spot is killed, pseudorotaxane in nano-antiradiation valve (5) or rotaxane " spool " (5A) Molecular Ring move downward and have blocked mesoporous radioactive nano microsphere radiation mesoporous mouthful (5), valve is just in "off" state, now, mesoporous radioactive nano microsphere radiation mesoporous mouthful (4) is closed, lonizing radiation in mesoporous radioactive nano microsphere (1) and mesoporous interior cancer therapy drug stop outwards carrying ray or cancer therapy drug, the control procedure of radiotherapy that Here it is and slow release cancer therapy drug.
(2), the process of normal release anti-cancer medicine:
By mesoporous radioactive nano microsphere (1), radioprotective inert metal or suction ripple rete (2), 3, anti cancer target or conventional medicine layer or radiation protective layer, targeting, independent assortment layer or the plastic foil of conventional medicine layer, radiation protective layer, targeting, the independent assortment layer (3) of conventional medicine layer, mesoporous mouthful of mesoporous radioactive nano microsphere radiation (4), nano-antiradiation valve (5), a kind of nano target with radiotherapy function that nano target carrier layer (6) forms or conventional cancer therapy drug and preparation method thereof, as the injection of injection blood or intramuscular injection or otch inject or oral as oral medicine after, medicine absorbs with blood or gastrointestinal blood circulation and the lymphsystem that enters into health, under the target biology guiding of nano target carrier layer (6), because the targeted anticancer medicine of bio-guide effect focuses on target spot position cancerous tissue and cancerous cell, cancerous cell is killed, the cancerous tissue cell that conventional cancer therapy drug flow to whole body with blood circulation is killed, the process of Here it is normal release anti-cancer medicine.
Fig. 2 a kind ofly analyses and observe macroscopical enlarged drawing with the nano target of radiotherapy function or the structure of conventional cancer therapy drug:
(1), a kind of nano target with radiotherapy function or the simple preparation method of conventional cancer therapy drug:
The 1st step: make the mesoporous radioactive nano microsphere (1) that surface has nano-antiradiation valve (5) the function base of radioprotective metal ion:
Take active material and silicon dioxide composite material or independent active material is base material, adopt the methods such as chemistry or biosynthesis or machinery for example the synthetic size homogeneous of coprecipitation, sol-gal process, dispersion copolymerization method or controllable free-radical polymerisation method, for example, compared with large pore volume (0.6--5cm3/g), high-specific surface area (for example 700--1500m2/g), the mesoporous radioactive nano microsphere of radioactivity (1) that hole wall high density is modified, for example: can adopt following several method preparation, etc., following methods is identical with Fig. 1, omits.
After mesoporous radioactive nano microsphere (1) preparation, again by the inner successful grafting in mesoporous surface or physical absorption anticancer targeting medicine or the non-targeted conventional medicine of mesoporous radioactive nano microsphere (1), preparation load the hole radioactive nano microsphere (1) of anticancer targeting medicine or non-targeted conventional medicine; Mesoporous radioactive nano microsphere (1) can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make.
Due between metal ion and metal and ligand coordinate bond very by force or very strong, become the active force that drives supermolecule self assembly, by copolymerization, the methods such as surface modification and supermolecule self assembly, the component that contains the supramolecular 26S Proteasome Structure and Functions such as silver metal or silicon molecule or building block are assembled into new super molecular compound according to the mode of design, by interaction or Cheng Jian between metal and metallic molecule, obtain the mesoporous radioactive nano microsphere (1) that surface has nano-antiradiation valve (6) the function base of radioprotective metal ion, can be directly in conjunction with, also can be again in conjunction with obtaining after chemical modification.For example adopt following methods to obtain the metal rotaxane that surface has nano-antiradiation valve (6) the function base of radioprotective metal ion, the class rotaxane specifically being generated by Cucurbituril cucurbituril and spermine hydrochlorate, after hydrated alkyl cobalt oxime generation self-assembling reaction, in aqueous solution, formed a kind of novel metal rotaxane, this is one of method realizing.By methods such as self assemblies, the supermolecule pseudorotaxanes such as silver metal or rotaxane are constructed on mesoporous radioactive nano microsphere (1) surface, it is bobbin molecule that formation be take functionalized nano silicon or nanometer silver, the supermolecule nano radioprotective valve (6) that the supermolecules such as silver metal can slide on bobbin, control the new function discharging with switch, thereby obtain the mesoporous radioactive nano microsphere (1) that surface has nano-antiradiation valve (6) the function base of radioprotective metal ion, by pH, discharge with the control of competition in conjunction with supermolecule nano valves such as driving silver metal such as the dual pathwayss, meet the multiple release and the switch demand that impose a condition.The mesoporous radioactive nano microsphere (1) of take is nano container, the control of the supermolecule nano valves such as silver metal that nano target carrier layer (7) such as amino acid decarboxylases causes discharges, this transports system and has biological targeting and switching function, and can discharge by multistep control on demand.Under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nano-antiradiation valve (6) is opened automatically, the anticancer targeting medicine that mesoporous radioactive nano microsphere (1) is inner or non-targeted conventional medicine be by mesoporous mouthful of (5) outside slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill; When the switch of nano-antiradiation valve (6) is opened automatically, the inner lonizing radiation of mesoporous radioactive nano microsphere (1) in the external world by the mesoporous mouth of mesoporous radioactive nano microsphere radiation (5) to external radiation, the cancerous cell of the cancerous tissue of target spot is carried out to " radiotherapy " and kills; On the other hand, anti cancer target or conventional medicine layer (4) carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast; Said process is that radiation and chemotherapy carries out individually or simultaneously.
The 2nd step: radioprotective is enlivened to metallic diaphragm or inhale that ripple rete (2) is coated or coating is upper to mesoporous radioactive nano microsphere (1): radioprotective enlivens metallic diaphragm or suction ripple rete (2)
The methods such as employing physisorphtion, arc discharge method, Plasma Polymerization, laser chemical vapor deposition method, electroless plating method, emulsion polymerization, surface deposition method (electroless plating method, heterogeneous precipitation method) are by anti-metal or Organic Pollution protective film (3) is coated or coating arrives on mesoporous radioactive nano microsphere (1).
The 3rd step: coated or coating enlivens on metallic diaphragm or suction ripple rete (2) to radioprotective by anti-metal or Organic Pollution protective film (3).
The 4th step: anti cancer target or conventional medicine layer (4) are coated, are covered or be adsorbed in anti-metal or Organic Pollution protective film (3) by methods such as physical absorption, chemical infiltration, copolymerization, magnetic, surface modifications.The 5th step: by methods such as chemical modification and polymerizations by the compound nano target carrier layer (7) of preparing of the targeting vectors such as lipase.
The 6th step: nano target carrier layer (7) is coated, is covered on anti cancer target or conventional medicine layer (4) by methods such as modification, magnetic, copolymerization.
(2), the process of a kind of nano target with radiotherapy function or conventional cancer therapy drug anticancer mechanism:
(1), the process of radiotherapy and slow release cancer therapy drug:
By mesoporous radioactive nano microsphere (1), radioprotective enlivens metallic diaphragm or inhales ripple rete (2), anti-metal or Organic Pollution protective film (3), anti cancer target or conventional medicine layer (4), mesoporous mouthful of mesoporous radioactive nano microsphere radiation (5), nano-antiradiation valve (6), pseudorotaxane or rotaxane " spool " are (6A), a kind of nano target with radiotherapy function that nano target carrier layer (7) forms or conventional cancer therapy drug and preparation method thereof, as the injection of injection blood or intramuscular injection or otch inject or oral as oral medicine after, medicine absorbs with blood or gastrointestinal blood circulation and the lymphsystem that enters into health, under the target biology guiding of nano target carrier layer (7), targeted anticancer medicine focuses on target spot position cancerous tissue and cancerous cell because of bio-guide effect, the cancerous tissue cell that conventional cancer therapy drug flow to whole body with blood circulation is killed, under the effect and control of extraneous electricity, light, magnetic, sound, pseudorotaxane in nano-antiradiation valve (6) or rotaxane " spool " the electrical power of Molecular Ring quilt or magnetive attraction (6A) drives while moving upward, valve is just in "open" state, and the lonizing radiation in mesoporous radioactive nano microsphere (1) are killed the cancerous cell of the cancerous tissue of target spot by mesoporous radioactive nano microsphere radiation mesoporous mouthful (5), the cancer therapy drug that is positioned at the mesoporous passage absorption of mesoporous radioactive nano microsphere (1) passes through mesoporous mouthful of (5) external slow release of mesoporous radioactive nano microsphere radiation, and the cancerous cell of the cancerous tissue of target spot is killed, pseudorotaxane in nano-antiradiation valve (6) or rotaxane " spool " (6A) Molecular Ring move downward and have blocked mesoporous radioactive nano microsphere radiation mesoporous mouthful (6), valve is just in "off" state, now, mesoporous radioactive nano microsphere radiation mesoporous mouthful (5) is closed, lonizing radiation in mesoporous radioactive nano microsphere (1) and mesoporous interior cancer therapy drug stop outwards carrying ray or cancer therapy drug, the control procedure of radiotherapy that Here it is and slow release cancer therapy drug.
(2), the process of normal release anti-cancer medicine:
By mesoporous radioactive nano microsphere (1), radioprotective enlivens metallic diaphragm or inhales ripple rete (2), anti-metal or Organic Pollution protective film (3), anti cancer target or conventional medicine layer (4), mesoporous mouthful of mesoporous radioactive nano microsphere radiation (5), nano-antiradiation valve (6), pseudorotaxane or rotaxane " spool " are (6A), a kind of nano target with radiotherapy function that nano target carrier layer (7) forms or conventional cancer therapy drug and preparation method thereof, as the injection of injection blood or intramuscular injection or otch inject or oral as oral medicine after, medicine absorbs with blood or gastrointestinal blood circulation and the lymphsystem that enters into health, under the target biology guiding of nano target carrier layer (7), because the targeted anticancer medicine of bio-guide effect focuses on target spot position cancerous tissue and cancerous cell, cancerous cell is killed, the cancerous tissue cell that conventional cancer therapy drug flow to whole body with blood circulation is killed, the process of Here it is normal release anti-cancer medicine.Fig. 3 a kind ofly analyses and observe macroscopical enlarged drawing with the nano target of radiotherapy function or the structure of conventional cancer therapy drug:
(1), a kind of nano target with radiotherapy function or the simple preparation method of conventional cancer therapy drug:
The 1st step: make the mesoporous radioactive nano microsphere (1) that surface has nanometer radioactive radiation valve (5) the function base of radioprotective metal ion:
Take active material and silicon dioxide composite material or independent active material is base material, adopt the methods such as chemistry or biosynthesis or machinery for example the synthetic size homogeneous of coprecipitation, sol-gal process, dispersion copolymerization method or controllable free-radical polymerisation method, for example, compared with large pore volume (0.6--5cm3/g), high-specific surface area (for example 700--1500m2/g), the mesoporous radioactive nano microsphere of radioactivity (1) that hole wall high density is modified, for example: can adopt following several method preparation, etc., following methods is identical with Fig. 1, omits.
After mesoporous radioactive nano microsphere (1) preparation, again by the inner successful grafting in mesoporous surface or physical absorption anticancer targeting medicine or the non-targeted conventional medicine of mesoporous radioactive nano microsphere (1), preparation load the hole radioactive nano microsphere (1) of anticancer targeting medicine or non-targeted conventional medicine; Mesoporous radioactive nano microsphere (1) can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make.
Due between metal ion and metal and ligand coordinate bond very by force or very strong, become the active force that drives supermolecule self assembly, by copolymerization, the methods such as surface modification and supermolecule self assembly, the component that contains the supramolecular 26S Proteasome Structure and Functions such as silver metal or silicon molecule or building block are assembled into new super molecular compound according to the mode of design, by interaction or Cheng Jian between metal and metallic molecule, obtain the mesoporous radioactive nano microsphere (1) of the radioactive nanometer radioactive radiation of surperficial tool valve (6) function base, can be directly in conjunction with, also can be again in conjunction with obtaining after chemical modification.For example adopt following methods to obtain the metal rotaxane of the radioactive nanometer radioactive radiation of surperficial tool valve (6) function base, the class rotaxane specifically being generated by Cucurbituril cucurbituril and spermine hydrochlorate, after hydrated alkyl cobalt oxime generation self-assembling reaction, in aqueous solution, formed a kind of novel metal rotaxane, this is one of method realizing.By methods such as self assemblies, the supermolecule pseudorotaxanes such as silver metal or rotaxane are constructed on mesoporous radioactive nano microsphere (1) surface, it is bobbin molecule that formation be take functionalized nano silicon or nanometer silver, the supermolecule nano radioactive radiation valve (6) that the supermolecules such as silver metal can slide on bobbin, control the new function discharging with switch, thereby obtain the mesoporous radioactive nano microsphere (1) of the radioactive nanometer radioactive radiation of surperficial tool valve (6) function base, by pH, discharge with the control of competition in conjunction with supermolecule nano valves such as driving silver metal such as the dual pathwayss, meet the multiple release and the switch demand that impose a condition.The mesoporous radioactive nano microsphere (1) of take is nano container, the control of the supermolecule nano valves such as silver metal that nano target carrier layer (7) such as amino acid decarboxylases causes discharges, this transports system and has biological targeting and switching function, and can discharge by multistep control on demand.Under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nanometer radioactive radiation valve (6) is opened automatically, the anticancer targeting medicine that mesoporous radioactive nano microsphere (1) is inner or non-targeted conventional medicine be by mesoporous mouthful of (5) outside slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill; When the switch of nanometer radioactive radiation valve (6) is opened automatically, in the external world, the lonizing radiation by the mesoporous mouth of mesoporous radioactive nano microsphere radiation (5) and nanometer radioactive radiation valve (6) itself, all to external radiation, carry out " radiotherapy " to the cancerous cell of the cancerous tissue of target spot and kill the inner lonizing radiation of mesoporous radioactive nano microsphere (1); On the other hand, anti cancer target or conventional medicine layer (4) carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast; Said process is that radiation and chemotherapy carries out individually or simultaneously.
The 2nd step: radioactive metal rete (2) is coated or coating is upper to mesoporous radioactive nano microsphere (1):
Radiation protective layer (3) is coated the methods such as employing physisorphtion, arc discharge method, Plasma Polymerization, laser chemical vapor deposition method, electroless plating method, emulsion polymerization, surface deposition method (electroless plating method, heterogeneous precipitation method) or coating arrives on mesoporous radioactive nano microsphere (1).
The 3rd step: coated or coating is to radioactive metal rete (2) by radiation protective layer (3).
The 4th step: anti cancer target or conventional medicine layer (4) are coated, are covered or be adsorbed in radiation protective layer (3) by methods such as physical absorption, chemical infiltration, copolymerization, magnetic, surface modifications.
The 5th step: by methods such as chemical modification and polymerizations by the compound nano target carrier layer (7) of preparing of the targeting vectors such as lipase.
The 6th step: nano target carrier layer (7) is coated, is covered on anti cancer target or conventional medicine layer (4) by methods such as modification, magnetic, copolymerization.
(2), the process of a kind of nano target with radiotherapy function or conventional cancer therapy drug anticancer mechanism:
(1), the process of radiotherapy and slow release cancer therapy drug:
By mesoporous radioactive nano microsphere (1), radioactive metal rete (2), radiation protective layer (3), anti cancer target or conventional medicine layer (4), mesoporous mouthful of mesoporous radioactive nano microsphere radiation (5), nanometer radioactive radiation valve (6), pseudorotaxane or rotaxane " spool " are (6A), a kind of nano target with radiotherapy function that nano target carrier layer (7) forms or conventional cancer therapy drug and preparation method thereof, as the injection of injection blood or intramuscular injection or otch inject or oral as oral medicine after, medicine absorbs with blood or gastrointestinal blood circulation and the lymphsystem that enters into health, under the target biology guiding of nano target carrier layer (7), targeted anticancer medicine focuses on target spot position cancerous tissue and cancerous cell because of bio-guide effect, the cancerous tissue cell that conventional cancer therapy drug flow to whole body with blood circulation is killed, at extraneous electricity, light, magnetic, under the effect of sound and control, pseudorotaxane in nanometer radioactive radiation valve (6) or rotaxane " spool " the electrical power of Molecular Ring quilt or magnetive attraction (6A) drives while moving upward, valve is just in "open" state, lonizing radiation in mesoporous radioactive nano microsphere (1) and the lonizing radiation of nanometer radioactive radiation valve (6) itself penetrated thinner radiation protective layer (3) simultaneously, by mesoporous radioactive nano microsphere radiation mesoporous mouthful (5), the cancerous cell of the cancerous tissue of target spot is killed, the cancer therapy drug that nanometer radioactive radiation valve (6) is positioned at the mesoporous passage absorption of mesoporous radioactive nano microsphere (1) passes through mesoporous mouthful of (5) external slow release of mesoporous radioactive nano microsphere radiation, and the cancerous cell of the cancerous tissue of target spot is killed, pseudorotaxane in nanometer radioactive radiation valve (6) or rotaxane " spool " (6A) Molecular Ring move downward and have blocked mesoporous radioactive nano microsphere radiation mesoporous mouthful (6), valve is just in "off" state, now, mesoporous radioactive nano microsphere radiation mesoporous mouthful (5) is closed, lonizing radiation in mesoporous radioactive nano microsphere (1) and mesoporous interior cancer therapy drug stop outwards carrying ray or cancer therapy drug, the control procedure of radiotherapy that Here it is and slow release cancer therapy drug.
(2), the process of normal release anti-cancer medicine:
By mesoporous radioactive nano microsphere (1), radioactive metal rete (2), radiation protective layer (3), anti cancer target or conventional medicine layer (4), mesoporous mouthful of mesoporous radioactive nano microsphere radiation (5), nanometer radioactive radiation valve (6), pseudorotaxane or rotaxane " spool " are (6A), a kind of nano target with radiotherapy function that nano target carrier layer (7) forms or conventional cancer therapy drug and preparation method thereof, as the injection of injection blood or intramuscular injection or otch inject or oral as oral medicine after, medicine absorbs with blood or gastrointestinal blood circulation and the lymphsystem that enters into health, under the target biology guiding of nano target carrier layer (7), because the targeted anticancer medicine of bio-guide effect focuses on target spot position cancerous tissue and cancerous cell, cancerous cell is killed, the cancerous tissue cell that conventional cancer therapy drug flow to whole body with blood circulation is killed, and the lonizing radiation of nanometer radioactive radiation valve (6) penetrated thinner radiation protective layer (3) and by sanguimotor process, blood system and lymphoid cancerous cell killed, the process of Here it is normal release anti-cancer medicine.
Experimental result:
One, experimental example 1:(be take Fig. 1 as experimental example).
(1) experiment material:
1) a kind of nano target with radiotherapy function or the conventional cancer therapy drug that, by mesoporous radioactive nano microsphere (1), radioprotective inert metal or suction ripple rete (2), anti cancer target or conventional medicine layer (3), the radiation of mesoporous radioactive nano microsphere mesoporous mouthful of (4), nano-antiradiation valve (5), nano target carrier layer (6), are formed.
2), 1 of the DC source of electroded 24V voltage.
(2), experimentation and result:
With the synthetic size homogeneous of the methods such as chemistry, for example, compared with large pore volume (0.6--5cm3/g), high-specific surface area (for example 700--1500m2/g), the mesoporous radioactive nano microsphere (1) of hole wall high density modification of surfaces, in the successful grafting in mesoporous surface of mesoporous radioactive nano microsphere (1) inner utilization anticancer targeting medicine or non-targeted conventional medicine cisplatin medicine molecule for example, again for example, by the coated anti cancer target of the methods such as copolymerization self assembly or conventional medicine layer (3) cisplatin medicine molecule, at anti cancer target or conventional medicine layer (3), be for example coated upper nano target carrier layer (6) in the surface of cisplatin medicine molecule again, result shows, due to coordination and the superior absorption property of material, medicine efficiency of loading is 50%, sustained release continues 20 days.This delivery systme has the responsive release characteristics of pH, and under same medicine concentration, use drug delivery system more obvious than conventional medicine to the inhibition of human body cervical carcinoma cell, simultaneously, the chemotherapy that anti cancer target or conventional medicine layer (4) carry out, radiate Alpha-ray radium and the radiotherapy of the cancerous cell of target spot is combined by the mesoporous mouth of mesoporous radioactive nano microsphere radiation (5) as the mesoporous radioactive nano microsphere (1) of radioactive substance with usining to set, through the treatment of 1 hour, the killing rate of the cancerous cell of cervix uteri targeting moiety is reached to 100%.
Two, experimental example 2:(be take Fig. 1 as experimental example).
(1) experiment material:
1, by mesoporous radioactive nano microsphere (1), radioprotective, enliven metallic diaphragm or inhale a kind of nano target with radiotherapy function or the conventional cancer therapy drug that ripple rete (2), anti-metal or Organic Pollution protective film (3), anti cancer target or conventional medicine layer (4), the radiation of mesoporous radioactive nano microsphere mesoporous mouthful of (5), nano-antiradiation valve (6), nano target carrier layer (7) form.
2), 1 of the DC source of electroded 24V voltage.
(2), experimentation and result:
With synthetic the usining of the methods such as chemistry, set and can radiate Alpha-ray radium as the mesoporous radioactive nano microsphere (1) of radioactive substance, in the inner utilization successful grafting in mesoporous surface anti cancer target or conventional medicine layer amycin medicine molecule for example, by methods such as copolymerization self assembly or magnetic, be coated again for example cisplatin medicine molecule of anti cancer target or conventional medicine layer (3), at anti cancer target or conventional medicine layer (3), be for example coated upper enzyme triggering medicine-releasing system nano target carrier layer (6) in the surface of cisplatin medicine molecule again, this material demonstrates high amycin useful load (800mg/g) and efficiency of loading (60%).Because the nano target carrier asialoglycoprotein receptor of liver plasma membrane can contain aminogalactose by single-minded identification end group, so this drug-loading system can be realized the targeted therapy of hepatocarcinoma.Result shows, the drug-supplying system with ligand function of synthesized can not more effectively be identified by hepatoma carcinoma cell than functional supports, and all demonstrates the more effective lethal effect to hepatoma carcinoma cell than conventional medicine with without the meso-porous nano drug-supplying system of functionalization.Simultaneously, the chemotherapy that anti cancer target or conventional medicine layer (3) carry out, with to set the Beta-ray mesoporous radioactive nano microsphere of radiation (1), by the mesoporous mouth of mesoporous radioactive nano microsphere radiation (4), the radiotherapy of the cancerous cell of target spot is combined, through the treatment of 1 hour, the killing rate of the cancerous cell at liver target position is reached to 100%.
Claims (3)
1. the nano target with radiotherapy function or conventional cancer therapy drug and preparation method thereof, by mesoporous radioactive nano microsphere (1), radioprotective inert metal or suction ripple rete (2), anti cancer target or conventional medicine layer (3), the radiation of mesoporous radioactive nano microsphere mesoporous mouthful of (4), nano-antiradiation valve (5), nano target carrier layer (6), formed, it is characterized in that: be mesoporous radioactive nano microsphere (1), radioprotective inert metal or suction ripple rete (2), anti cancer target or conventional medicine layer (3), nano target carrier layer (6) from the inside to the outside successively; There are numerous mesoporous radioactive nano microsphere radiation mesoporous mouthful (4) and nano-antiradiation valve (5) in mesoporous radioactive nano microsphere (1) surface, the mesoporous mouth of nano-antiradiation valve (5) and the radiation of mesoporous radioactive nano microsphere (4) connection that is connected; Mesoporous radioactive nano microsphere (1) can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make; Anti cancer target or conventional medicine layer (3) are more than 0 layer or 1 layer or 1 layer; Whether mesoporous radioactive nano microsphere (1) is no matter in the situation that adopting active material to add inner mesoporous passage to add anticancer targeting medicine or non-targeted conventional medicine, under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nano-antiradiation valve (5) can be opened automatically, the anticancer targeting medicine that mesoporous radioactive nano microsphere (1) is inner or non-targeted conventional medicine be by mesoporous mouthful of (4) outside slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill; When the switch of nano-antiradiation valve (5) is opened automatically, the inner lonizing radiation of mesoporous radioactive nano microsphere (1) in the external world by the mesoporous mouth of mesoporous radioactive nano microsphere radiation (4) to external radiation, the cancerous cell of the cancerous tissue of target spot is carried out to " radiotherapy " and kills; On the other hand, anti cancer target or conventional medicine layer (3) carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast; Said process is the independent or cohesive process of radiation and chemotherapy.
2. the nano target with radiotherapy function or conventional cancer therapy drug and preparation method thereof, by mesoporous radioactive nano microsphere (1), radioprotective enlivens metallic diaphragm or inhales ripple rete (2), anti-metal or Organic Pollution protective film (3), anti cancer target or conventional medicine layer (4), mesoporous mouthful of mesoporous radioactive nano microsphere radiation (5), nano-antiradiation valve (6), nano target carrier layer (7) forms, it is characterized in that: be mesoporous radioactive nano microsphere (1) from the inside to the outside successively, radioprotective inert metal or suction ripple rete (3), anti cancer target or conventional medicine layer (4), nano target carrier layer (7), there are numerous mesoporous radioactive nano microsphere radiation mesoporous mouthful (5) and nano-antiradiation valve (6) in mesoporous radioactive nano microsphere (1) surface, the mesoporous mouth of nano-antiradiation valve (6) and the radiation of mesoporous radioactive nano microsphere (5) connection that is connected, mesoporous radioactive nano microsphere (1) can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make, anti cancer target or conventional medicine layer (4) are more than 0 layer or 1 layer or 1 layer, when radioprotective enlivens metallic diaphragm or inhales ripple rete (2) while only using the suction ripple rete (2) of nontoxic inanimate object reaction, anti-metal or Organic Pollution protective film (3) can be 0 layer, whether mesoporous radioactive nano microsphere (1) is no matter in the situation that adopting active material to add inner mesoporous passage to add anticancer targeting medicine or non-targeted conventional medicine, under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nano-antiradiation valve (6) can be opened automatically, the anticancer targeting medicine that mesoporous radioactive nano microsphere (1) is inner or non-targeted conventional medicine be by mesoporous mouthful of (5) outside slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill, when the switch of nano-antiradiation valve (6) is opened automatically, the inner lonizing radiation of mesoporous radioactive nano microsphere (1) in the external world by the mesoporous mouth of mesoporous radioactive nano microsphere radiation (5) to external radiation, the cancerous cell of the cancerous tissue of target spot is carried out to " radiotherapy " and kills, on the other hand, anti cancer target or conventional medicine layer (4) carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast, said process is the independent or cohesive process of radiation and chemotherapy.
3. the nano target with radiotherapy function or conventional cancer therapy drug and preparation method thereof, by mesoporous radioactive nano microsphere (1), radioactive metal rete (2), radiation protective layer (3), anti cancer target or conventional medicine layer (4), mesoporous mouthful of mesoporous radioactive nano microsphere radiation (5), nanometer radioactive radiation valve (6), pseudorotaxane or rotaxane " spool " are (6A), nano target carrier layer (7) forms, it is characterized in that: be mesoporous radioactive nano microsphere (1) from the inside to the outside successively, radioactive metal rete (2), radiation protective layer (3), anti cancer target or conventional medicine layer (4), nano target carrier layer (7), there are numerous mesoporous radioactive nano microsphere radiation mesoporous mouthful (5) and nanometer radioactive radiation valve (6) in mesoporous radioactive nano microsphere (1) surface, the mesoporous mouth of nanometer radioactive radiation valve (6) and the radiation of mesoporous radioactive nano microsphere (5) connection that is connected, mesoporous radioactive nano microsphere (1) can adopt active material add the mode of inner mesoporous passage interpolation anticancer targeting medicine or non-targeted conventional medicine or adopt separately the mode of pure active material to make, anti cancer target or conventional medicine layer (4) are more than 0 layer or 1 layer or 1 layer, whether mesoporous radioactive nano microsphere (1) is no matter in the situation that adopting active material to add inner mesoporous passage to add anticancer targeting medicine or non-targeted conventional medicine, under the effect and control of extraneous electricity, light, magnetic, sound, the switch of nanometer radioactive radiation valve (6) can be opened automatically, the anticancer targeting medicine that mesoporous radioactive nano microsphere (1) is inner or non-targeted conventional medicine be by mesoporous mouthful of (5) outside slow release of mesoporous radioactive nano microsphere radiation, cancerous tissue and cancerous cell carried out to " chemotherapy " and kill, when the switch of nanometer radioactive radiation valve (6) is opened automatically, in the external world, the lonizing radiation by the mesoporous mouth of mesoporous radioactive nano microsphere radiation (5) and nanometer radioactive radiation valve (6) itself, all to external radiation, carry out " radiotherapy " to the cancerous cell of the cancerous tissue of target spot and kill the inner lonizing radiation of mesoporous radioactive nano microsphere (1), on the other hand, anti cancer target or conventional medicine layer (4) carry out routine to the cancerous tissue cancerous cell chemotherapy of target spot or treatment by Chinese herbs and kill fast, said process is the independent or cohesive process of radiation and chemotherapy.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210388401.XA CN103656692A (en) | 2012-09-25 | 2012-09-25 | Nano targeted or ordinary anticancer medicament with radiotherapy function and preparation method thereof |
| PCT/CN2013/001069 WO2014048060A1 (en) | 2012-09-25 | 2013-09-13 | Anti-inflammatory drug against cancer and aids with radiotherapy and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201210388401.XA CN103656692A (en) | 2012-09-25 | 2012-09-25 | Nano targeted or ordinary anticancer medicament with radiotherapy function and preparation method thereof |
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