CN101358383A - Alkanna tinctoria drug loading nano fiber, preparation and application thereof - Google Patents
Alkanna tinctoria drug loading nano fiber, preparation and application thereof Download PDFInfo
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- CN101358383A CN101358383A CNA2008100426899A CN200810042689A CN101358383A CN 101358383 A CN101358383 A CN 101358383A CN A2008100426899 A CNA2008100426899 A CN A2008100426899A CN 200810042689 A CN200810042689 A CN 200810042689A CN 101358383 A CN101358383 A CN 101358383A
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Abstract
The invention relates to lithospermum medicinal nano fiber, and a preparation method and an application thereof; the fiber is a kind of nano fiber with the effective components of lithospermum; the effective components of lithospermum are evenly distributed in the fiber and account for 0.001 weight percent to 30 weight percent of the fiber; the preparation method comprises the following steps: the effective components of lithospermum are dissolved in organic solvent together with polymeric materials to prepare spinning solution, and then prepare the lithospermum nano fiber through an electrospinning process; application: depending on different curing parts or curing purposes, the fiber is processed and prepared to be taken orally, skin penetrative or implanted into a drug delivery system to cure injuries, cancer or resist oxidation. The lithospermum medicinal fiber has the advantages of simple preparation process, medicine release, good biological compatibility and the like.
Description
Technical field
The invention belongs to the medicament-carrying nano-fiber field, particularly relate to a kind of alkanna tinctoria drug loading nano fiber and preparation thereof and application.
Background technology
Asian puccoon is Boraginaceae (boraginacese) herbaceos perennial, and is just on the books in Shennong's Herbal." Chinese pharmacopoeia version in 2005 is recorded its dry root for comfrey lithospermum euchromum Royle [Arnebia euchroma (Royle) Johnst] or arnebia guttata Bunge (Arnebia guttata Bunge).Cool blood is arranged, invigorate blood circulation, the effect of detoxifcation promoting eruption is mainly used in the blood-head poison and contains, and macula is purple black, measles without adequate eruption, sore, eczema, diseases such as scald.It is one of China's conventional Chinese medicine for the treatment of disease of skin clinically.Asian puccoon contains the number of chemical composition, wherein naphthoquinone compound content is the highest and have a multiple biologically active, as anti-inflammation, anticancer and anti-oxidant etc., they also have stable dyeability in addition, thereby obtain extensive concern in medicine, foods and cosmetics field.
Along with the extensive use of new technology, new auxiliary material, some traditional Chinese medicine scholars are doing a lot of work aspect Study on Modernization such as Asian puccoon modified form as problem in recent years.The beautiful grade of Pang show [Chinese patent drug .2001,23 (1): 5] has prepared the solid dispersion of Asian puccoon medicinal extract, has effectively improved the dissolution in vitro of Asian puccoon active ingredient, and then improves bioavilability in its body.Then, they have also prepared the Asian puccoon vagina effervescence, so that the treatment of vaginal disease more convenient effectively [Chinese patent drug .2004,26 (3): 181].Assimopoulou etc. [J Microcapsulation.2004,2:161] have prepared the microcapsule formulation that contains alkannin, thereby have improved its hydrophobicity and made it have slow release effect.Fiber is original owing to it at present, as has very big specific area, superior mechanical performance etc., and become a kind of ideal carrier of adorning the envelope medicine, obtaining many progress and achievement aspect the loading of effectively realizing medicine and the release.And the fiber preparation type of Asian puccoon also never has and appears in the newspapers.
Summary of the invention
The purpose of this invention is to provide a kind of alkanna tinctoria drug loading nano fiber and preparation thereof and application, by Asian puccoon active ingredient and polymer base material are total to the molten spinning solution of making, utilize method of electrostatic spinning, be prepared into Asian puccoon nanofiber or fibrofelt, Asian puccoon active ingredient evenly distributes in fiber.This fiber has excellent biological compatibility and degradability, according to therapentic part or therapeutic purposes difference, further processing and preparing becomes delivery systems such as oral, transdermal or implantation, to reach anti-oxidant, to treat medical purposes such as wound or cancer, this also provides a new approach for the development of Chinese medicine delivery system.
Alkanna tinctoria drug loading nano fiber of the present invention is a kind of nanofiber that is loaded with Asian puccoon active ingredient, and Asian puccoon active ingredient evenly distributes in fiber, and wherein the content of Asian puccoon active ingredient in fiber is 0.001wt.%～30wt.%.
Described Asian puccoon active ingredient is alkannin (shikonin), β, beta-dimethyl-acryloyl alkannin (β, one or more mixtures in β-dimethylacrylshikonin), Acetylshikonin (acetylshikonin), deoxyshikonin (deoxyshikonin), isobutyryl shikonin (isobutylshikonin), isovaleryl alkannin (isovalerylshikonin), the 2-methylbutyryl alkannin (2-methyl-n-butyrylshikonin).
Described alkanna tinctoria drug loading nano fiber, its fibre diameter are 2 μ m～15 μ m, and its fiber base material is one or more mixtures in macromolecular material poly epsilon caprolactone lactone (PCL), poly (l-lactic acid) (PLLA), the polylactic acid-polyglycolic acid copolymer (PLGA).
The preparation method of alkanna tinctoria drug loading nano fiber of the present invention comprises:
Be dissolved in Asian puccoon active ingredient and fiber base material macromolecular material in the organic solvent altogether, make spinning solution, utilize method of electrostatic spinning, preparation Asian puccoon nanofiber, wherein, the mass concentration of macromolecular material is 1%～20% in the spinning solution, and the mass concentration of Asian puccoon active ingredient is 0.001%～30% in the spinning solution.
Described fiber base material macromolecular material, itself and Asian puccoon active ingredient compatibility are good, are the high molecular polymers with biodegradable and biocompatibility, are one or more mixtures in poly epsilon caprolactone lactone, poly (l-lactic acid), the polylactic acid-polyglycolic acid copolymer.
Described organic solvent is chloroform, acetone, dimethylbenzene, carrene, dioxane, chloroform/N, a kind of or its mixture of dinethylformamide (DMF) mixed solvent, carrene/DMF mixed solvent.
The parameter of described electrostatic spinning is voltage 10～30kv, and two die openings are from being 10～20cm, and the flow velocity of spinning solution at the spinning nozzle place is 0.5mL/h～1.5mL/h.
The application of alkanna tinctoria drug loading nano fiber of the present invention is according to therapentic part or therapeutic purposes difference, and further processing and preparing becomes delivery systems such as oral, transdermal or implantation, reaches medical purposes such as anti-oxidant, treatment wound or cancer.
Beneficial effect of the present invention:
(1) the naphthoquinones constituents in the Asian puccoon is a class hydrophobicity chemical substance, and the polymer base material that adopts is and the good Biodegradable Polymers of Asian puccoon naphthoquinones composition compatibility, so the Asian puccoon naphthoquinones is evenly distributed in now being;
(2) the electrospinning technology that is adopted makes polymer be cured as fiber condition from solution state rapidly, also makes the Asian puccoon naphthoquinones have little time to grow up to crystal grain, forms molecular state and is distributed in the fiber, can avoid the prominent phenomenon of releasing of medicine, reduces the toxic and side effect of medicine;
(3) the prepared fibre diameter of electrospinning in nanometer between the micron, thereby can avoid the drug slow phenomenon that stagnates;
(4) because the Asian puccoon naphthoquinones has multiple pharmacologically active, has multiple medical effect;
(5) simple, the medicament slow release of preparation technology of the present invention, good biocompatibility.
Description of drawings
Fig. 1 is the electrostatic spinning apparatus schematic diagram;
Fig. 2 is poly epsilon caprolactone lactone (PCL) fiber that is loaded with 1% alkannin;
Fig. 3 is the chemical constitution of naphthoquinone compound in the Asian puccoon.
The specific embodiment
Below in conjunction with specific embodiment, further set forth the present invention.Should be understood that these embodiment only to be used to the present invention is described and be not used in and limit the scope of the invention.Should be understood that in addition those skilled in the art can make various changes or modifications the present invention after the content of having read the present invention's instruction, these equivalent form of values fall within the application's appended claims institute restricted portion equally.
Embodiment 1
(shikonin) is dissolved in the 5mL chloroform with the 0.0043g alkannin, adds 0.4045g poly epsilon caprolactone lactone (PCL) (Mw ≈ 100,000) under stirring condition, and sonicated makes it become homogeneous solution.The solution that configures is poured in the 5mL syringe into the flat mouthful spinning head in the right angle that adopts No. 9 syringe needles to make.The flow velocity of solution at the spinning nozzle place is 0.6mL/h, and the voltage that is applied is 20kV, and two die openings are from being 20cm.
The result as shown in Figure 1, about gained alkannin/PCL drug-loading fibre diameter 10 μ m.Fiber surface is smooth smooth, and the medicine high degree of dispersion is among fiber base material PCL.
With 0.0204g β, beta-dimethyl-acryloyl alkannin (β, β-dimethylacrylshikonin) is dissolved in the mixed solution (3: 1 of 4mL chloroform and acetone, v/v), under stirring condition, add 0.4080g PLGA (lactide: glycolide=75: 25, Mw ≈ 100,000), sonicated makes it become homogeneous solution.The solution that configures is poured in the 5mL syringe into the flat mouthful spinning head in the right angle that adopts No. 8 syringe needles to make.The flow velocity of solution at the spinning nozzle place is 0.8mL/h, and the voltage that is applied is 22kV, and two die openings are from being 15cm.
The β of gained is about beta-dimethyl-acryloyl alkannin/PLGA drug-loading fibre diameter 12 μ m.Fiber surface is smooth smooth, and the medicine high degree of dispersion is among fiber base material PLGA.
Embodiment 3
(acetylshikonin) is dissolved in the 13.8mL chloroform with the 0.0412g Acetylshikonin, adds 0.4136g PLLA (Mw ≈ 100,000) under stirring condition, and sonicated makes it become homogeneous solution.The solution that configures is poured in the 5mL syringe into the flat mouthful spinning head in the right angle that adopts No. 9 syringe needles to make.The flow velocity of solution at the spinning nozzle place is 1.0mL/h, and the voltage that is applied is 25kV, and two die openings are from being 15cm.
About the Acetylshikonin of gained/PLLA drug-loading fibre diameter 3 μ m.Fiber surface is smooth smooth, and the medicine high degree of dispersion is among fiber base material PLLA.
Embodiment 4
Alkannin/PCL drug-loading fibre/the fibrofelt that obtains among the embodiment 1, further processing and preparing becomes oral formulations, to satisfy the anti-oxidant needs of human body.
Embodiment 5
The β that obtains among the embodiment 2, beta-dimethyl-acryloyl alkannin/PLGA drug-loading fibre/fibrofelt, further processing and preparing becomes the adhesive bandage that the surface of a wound covers, to quicken the healing at skin damage place.
Embodiment 6
Acetylshikonin/PLLA drug-loading fibre/the fibrofelt that obtains among the embodiment 3, further processing and preparing becomes implant, reaches the purpose of local treatment of tumor, and after implantation, polymer base material is degraded gradually, and drug slow discharges, finally the two exhausts at affected area, does not need second operation to take out.
Claims (8)
1. alkanna tinctoria drug loading nano fiber, it is characterized in that: this fiber is a kind of nanofiber that is loaded with Asian puccoon active ingredient, and Asian puccoon active ingredient evenly distributes in fiber, and wherein the content of Asian puccoon active ingredient in fiber is 0.001wt.%～30wt.%.
2. alkanna tinctoria drug loading nano fiber according to claim 1, it is characterized in that: described Asian puccoon active ingredient is alkannin, β, one or more mixtures in beta-dimethyl-acryloyl alkannin, Acetylshikonin, deoxyshikonin, isobutyryl shikonin, isovaleryl alkannin, the 2-methylbutyryl alkannin.
3. alkanna tinctoria drug loading nano fiber according to claim 1, it is characterized in that: described alkanna tinctoria drug loading nano fiber, its fibre diameter is 2 μ m～15 μ m, and its fiber base material is one or more mixtures in poly epsilon caprolactone lactone, poly (l-lactic acid), the polylactic acid-polyglycolic acid copolymer.
4. the preparation method of alkanna tinctoria drug loading nano fiber according to claim 1 comprises:
Be dissolved in Asian puccoon active ingredient and fiber base material macromolecular material in the organic solvent altogether, make spinning solution, utilize method of electrostatic spinning, preparation Asian puccoon nanofiber, wherein, the mass concentration of macromolecular material is 1%～20% in the spinning solution, and the mass concentration of Asian puccoon active ingredient is 0.001%～30% in the spinning solution.
5. the preparation method of alkanna tinctoria drug loading nano fiber according to claim 4, it is characterized in that: described fiber base material macromolecular material is one or more mixtures in poly epsilon caprolactone lactone, poly (l-lactic acid), the polylactic acid-polyglycolic acid copolymer.
6. the preparation method of alkanna tinctoria drug loading nano fiber according to claim 4, it is characterized in that: described organic solvent is chloroform, acetone, dimethylbenzene, carrene, dioxane, chloroform/N, a kind of or its mixture in dinethylformamide (DMF) mixed solvent, the carrene/DMF mixed solvent.
7. the preparation method of alkanna tinctoria drug loading nano fiber according to claim 4, it is characterized in that: the parameter of described electrostatic spinning is voltage 10～30kv, and two die openings are from being 10～20cm, and the flow velocity of spinning solution at the spinning nozzle place is 0.5mL/h～1.5mL/h.
8. the application of alkanna tinctoria drug loading nano fiber according to claim 1 is according to therapentic part or therapeutic purposes difference, and that processing and preparing becomes is oral, transdermal or drug delivery implant system, treatment wound, cancer or anti-oxidant.
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| CNA2008100426899A CN101358383A (en) | 2008-09-09 | 2008-09-09 | Alkanna tinctoria drug loading nano fiber, preparation and application thereof |
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Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102266282A (en) * | 2011-07-28 | 2011-12-07 | 上海交通大学 | Micro/nanometer fiber slow release preparation for treating cicatrices and preparation method thereof |
| CN103156824A (en) * | 2011-12-14 | 2013-06-19 | 国家纳米科学中心 | Three-dimensional drug sustained release stent transdermal drug delivery preparation, its preparation method and application |
| CN106074361A (en) * | 2016-07-14 | 2016-11-09 | 何伟 | A kind of anti-intraocular inflammation implant and its preparation method and application |
| CN106637591A (en) * | 2016-08-31 | 2017-05-10 | 浙江兆新织造有限公司 | Antibacterial skin-smoothing lining with natural faint scent |
| CN106758347A (en) * | 2016-12-01 | 2017-05-31 | 西南大学 | Colouring method of the Acetylshikonin to silk fabric |
| CN106730028A (en) * | 2016-11-17 | 2017-05-31 | 中国医学科学院生物医学工程研究所 | Carrier of controlled release resveratrol and/or Verakanol derivative and preparation method and application |
| CN107157960A (en) * | 2017-04-19 | 2017-09-15 | 苏州大学 | A kind of preparation method of medicament-carrying nano-fiber membrane |
| CN107970229A (en) * | 2018-01-23 | 2018-05-01 | 哈尔滨工业大学 | A kind of shape memory of energy intelligent control insoluble drug release carries medicine micro nanometer fiber film and preparation method thereof |
| CN110029443A (en) * | 2019-05-24 | 2019-07-19 | 华南协同创新研究院 | A kind of camellia seed oil fiber coating materials and the preparation method and application thereof |
| CN111407771A (en) * | 2020-04-02 | 2020-07-14 | 北京化工大学 | Antibacterial alum ice fiber membrane and preparation method thereof |
| CN115381778A (en) * | 2022-08-29 | 2022-11-25 | 成都紫旺药业有限责任公司 | Lithospermum naphthoquinone water-soluble solid dispersion, water-soluble preparation and preparation method |
-
2008
- 2008-09-09 CN CNA2008100426899A patent/CN101358383A/en active Pending
Cited By (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102266282A (en) * | 2011-07-28 | 2011-12-07 | 上海交通大学 | Micro/nanometer fiber slow release preparation for treating cicatrices and preparation method thereof |
| CN102266282B (en) * | 2011-07-28 | 2013-02-27 | 上海交通大学 | Micro/nanometer fiber slow release preparation for treating cicatrices and preparation method thereof |
| CN103156824A (en) * | 2011-12-14 | 2013-06-19 | 国家纳米科学中心 | Three-dimensional drug sustained release stent transdermal drug delivery preparation, its preparation method and application |
| CN106074361B (en) * | 2016-07-14 | 2018-10-19 | 何伟 | A kind of anti-intraocular inflammation implant and its preparation method and application |
| CN106074361A (en) * | 2016-07-14 | 2016-11-09 | 何伟 | A kind of anti-intraocular inflammation implant and its preparation method and application |
| CN106637591A (en) * | 2016-08-31 | 2017-05-10 | 浙江兆新织造有限公司 | Antibacterial skin-smoothing lining with natural faint scent |
| CN106730028A (en) * | 2016-11-17 | 2017-05-31 | 中国医学科学院生物医学工程研究所 | Carrier of controlled release resveratrol and/or Verakanol derivative and preparation method and application |
| CN106730028B (en) * | 2016-11-17 | 2020-01-31 | 中国医学科学院生物医学工程研究所 | Carrier capable of controllably releasing resveratrol and/or resveratrol derivative and preparation method and application thereof |
| CN106758347A (en) * | 2016-12-01 | 2017-05-31 | 西南大学 | Colouring method of the Acetylshikonin to silk fabric |
| CN107157960A (en) * | 2017-04-19 | 2017-09-15 | 苏州大学 | A kind of preparation method of medicament-carrying nano-fiber membrane |
| CN107970229A (en) * | 2018-01-23 | 2018-05-01 | 哈尔滨工业大学 | A kind of shape memory of energy intelligent control insoluble drug release carries medicine micro nanometer fiber film and preparation method thereof |
| CN110029443A (en) * | 2019-05-24 | 2019-07-19 | 华南协同创新研究院 | A kind of camellia seed oil fiber coating materials and the preparation method and application thereof |
| CN111407771A (en) * | 2020-04-02 | 2020-07-14 | 北京化工大学 | Antibacterial alum ice fiber membrane and preparation method thereof |
| CN115381778A (en) * | 2022-08-29 | 2022-11-25 | 成都紫旺药业有限责任公司 | Lithospermum naphthoquinone water-soluble solid dispersion, water-soluble preparation and preparation method |
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Open date: 20090204 |