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A kind of preparation method of chitosan photosensitive microsphere
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A technology of chitosan and chitosan solution, applied in the field of preparation of chitosan photosensitive microspheres, can solve problems such as few research reports, and achieve the effect of improving drug stability and bioavailability
Active Publication Date: 2016-02-03
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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Problems solved by technology
[0006] At present, there is no report on the use of porphyrin-modified chitosan to prepare new photosensitive materials; there are few research reports on the preparation of chitosan microspheres from traditional Chinese medicine ingredients with anti-tumor activity; especially those that focus on improving the targeted sustained-release effect Photosensitive microspheres, the effective substance of traditional Chinese medicine, have not been reported
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Embodiment 1
[0030] A preparation method of chitosan photosensitive microspheres, comprising the steps of:
[0031] (1) Add 50mg chitosan into a three-necked flask, add 150mg K 2 CO 3 , drop 2ml of chloroform, and stir at 40°C for 0.5h; add 20mg of tetrabutylammonium bromide, and then add 50mg of 5-p-(6-bromohexylaminophenyl)-10,15,20-triphenylporphyrin (BHP ) was dissolved in 15ml of chloroform, added dropwise to the flask, and refluxed at 60°C for 6h; the reaction was stopped, cooled to room temperature, filtered with suction, washed with chloroform until the filtrate was colorless, then washed with water for 3 times, and the product was vacuum-dried to obtain porphyrin side groups Chitosan derivatives; porphyrin grafting rate up to 36.20%;
[0033] (2) Weigh 33 mg of chitosan derivatives with porphyrin side groups and add it to 5% acetic acid solution until it swells, stir to dissolve, filter with suction, ...
Embodiment 2
[0036]Change the tetrabutylammonium bromide in step (1) in Example 1 to dodecyltrimethylammonium chloride, and keep other conditions constant, to obtain porphyrin side group chitosan derivatives, porphyrin The grafting rate is 31.01%.
Embodiment 3
[0038] K in the step (1) in the embodiment 1 2 CO 3 , changed to NaOH, and other conditions remain unchanged, the porphyrin side group chitosan derivatives can be obtained, and the grafting rate of porphyrin is 18.4%.
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Abstract
The invention relates to a preparation method of chitosan photosensitive microspheres. The preparation method comprises the following steps: reacting 5-p(6-bromoaminobenzene)-10,15,20-triphenylporphyrin (BHP) serving as a raw material with chitosan under the catalysis of a phase transfer catalyst to generate a new porphyrin side group chitosan photosensitive material, carrying out an emulsification crosslinking method to the selected Chinese herbal medicinal components with anti-tumor activity and the synthesized porphyrin side group chitosan derivatives to obtain the chitosan photosensitive microspheres. According to the preparation method, the original anti-tumor Chinese herbal medicinal ingredient with single action mechanism is combined with photodynamic cell lethality so as to achieve the synergistic effect of the original anti-tumor Chinese herbal medicinal ingredient and the photodynamic cell lethality, and therefore the stability and bioavailability of the drug can be improved, the drug can be enriched and administrated under illumination, and can be slowly, controllably and directionally released so as to reach the high-efficiency and low-toxicity purposes; the invention can provide a new method for researching and developing novel anti-tumor targeted drug forms.
Description
technical field [0001] The invention relates to a preparation method of a sustained-release drug preparation, in particular to a preparation method of chitosan photosensitive microspheres. Background technique [0002] Sustained-release drug preparation is a new dosage form developed in recent years. It is prepared by encapsulating drugs in natural or synthetic polymer materials, which can improve drug stability and bioavailability. To release drugs, etc. There are many types of this class of drugs, including liposomes, solid lipid nanoparticles, polymer micelles, and magnetic nanoparticles. After the traditional Chinese medicine ingredients with anti-tumor activity are prepared into a sustained-release drug delivery system, they have obvious effects in improving solubility and bioavailability, and enhancing anti-tumor activity, which is a successful dosage form improvement. [0003] Chitosan is a kind of amino polymer polysaccharide extracted from chitin in crustaceans su...
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