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Drug Delivery Systems using Self-aggregated Chitosan Derivatives

使用自聚集壳聚糖衍生物的药物输送系统

基本信息

批准号：
14580820
负责人：
SHIGEMASA Yoshihiro
金额：
$ 1.73万
依托单位：
Tottori University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2002
资助国家：
日本
起止时间：
2002 至 2004
项目状态：
已结题

项目摘要

Our object is application of chitosan derivatives possessed cell attracting effects to drug delivery systems. In this study, we obtained following results :1)Hydrothermal reaction is useful for decomposition of chitosan and the other acetals. Using this treatment, we can obtain chitosan with low molecular weight easily.2)New chitosan derivatives with hydrophobic, phenolic and carboxyl groups were synthesized. w by reductive alkylation reaction of chitosan with aldehyds and oxidization of chitosan. The hyrophobized chitosan derivatives is advantageous for self-aggregation effect and emulsion formation. The oxidized chitosan derivatives show a unique biological effect.3)Chitosan and hydrophobized chitosan derivatives act as a surfactant and stabilize O/W emulsion. In this situation, the organic phase in the emulsion should be encapsulated by the chitosan derivatives. The emulsion was formed by vigorous stirring of a hydrophobic drug in an organic solvent and chitosan in aqueous acetic acid and the chitosan containing the emulsion was solidified by addition of alkaline. Encapsulated drug into chitosan was released by re-dissolution of yielded chitosan containing the organic phase in acidic solution.4)Biodegradability is key-step for drug releasing in the system. Blend materials with chitosan derivatives and other biodegradable polymers were prepared. The blend materials composed chitosan enhanced chemical properties and kept biodegradability of chitosan.

本论文的研究目的是将具有细胞吸引作用的壳聚糖衍生物应用于药物释放系统。本研究得到以下结果：1）水热反应有利于壳聚糖等缩醛的分解。利用该方法可以得到低分子量的壳聚糖。2）合成了具有疏水性、酚性和羧基的新型壳聚糖衍生物。通过壳聚糖与壳聚糖的还原烷基化反应和壳聚糖的氧化反应，疏水化壳聚糖衍生物有利于自聚集效应和乳液形成。氧化壳聚糖衍生物显示出独特的生物学效应。3）壳聚糖和疏水化壳聚糖衍生物作为表面活性剂，稳定O/W乳状液。在这种情况下，乳液中的有机相应该被壳聚糖衍生物包封。通过剧烈搅拌有机溶剂中的疏水性药物和乙酸水溶液中的壳聚糖形成乳液，并通过加入碱固化含有乳液的壳聚糖。药物在壳聚糖中的释放主要是通过壳聚糖有机相在酸性溶液中的溶解来实现的。制备了壳聚糖衍生物与其他可生物降解聚合物的共混材料。壳聚糖的加入提高了材料的化学性能，同时保持了壳聚糖的生物降解性能。