紫杉醇微胶囊的制备及其靶向释放性能评价

Preparation and Targeted Release Evaluation Studies on Micro-Encapsulation of Paclitaxel

DOI：10.3969/j.issn.1673-1689.2017.01.015

中文关键词: 银杏辛烯基琥珀酸淀粉酯 紫杉醇 微胶囊 喷雾干燥 靶向释放

英文关键词: Octenyl Succinic Anhydride Modified Ginkgo starch,paclitaxel,microcapsule,spray- drying,targeted release

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中文摘要:

以银杏辛烯基琥珀酸淀粉酯为壁材，紫杉醇为芯材，采用喷雾干燥法制备微胶囊。通过正交试验确定了喷雾干燥法制备紫杉醇微胶囊的最优工艺组合：紫杉醇与银杏辛烯基琥珀酸淀粉酯质量比例1∶8，乳状液固形物质量分数15.0%，均质压力40.0 MPa，喷雾干燥进风温度200 ℃。在此工艺条件下，紫杉醇包埋率为96.82%，微胶囊中紫杉醇质量分数为10.63%。产品气味纯正，没有明显的苦味，颗粒表面平整光滑，细小均匀，具有良好的流散性，包埋效果好。在模拟人工胃液中，90.0 min，累积溶出率4.27%，基本不释药；在模拟人工小肠液中，紫杉醇4.0 h 的累积溶出率25.6%；在模拟人工大肠环境中，12.0 h 的体外累积溶出率达89.26%，24.0 h的体外累积溶出率达95.34%。表明紫杉醇微胶囊具有抗酸、抗消化、在大肠中易降解等特性，达到了大肠定位释药的效果，且其制备工艺简单、可行，是一种有潜力用于提高紫杉醇的药效并且降低不良反应的缓释新剂型。

英文摘要:

The paper studies the technological conditions of the spray-drying method for the preparation of targeted delivery microcapsule with octenyl succinic anhydride modified ginkgo starch as wall material，paclitaxel as core，respectively. With microencapsulating efficiency as the main evaluating index，the processing technology for preparing paclitaxel micro-encapsulation by spray-drying was investigated and optimized by the orthogonal experiments as followed：the proportion of core material and wall material is 1∶8，the solid concentration of emulsion is 15.0%，the homogeneous pressure is 40.0 MPa，and the temperature of inlet wind for the spray-drying is 200 ℃. Encapsulating rate of micro-encapsulation under the optimized technology is 96.82%，content of paclitaxel is 10.63% and its quality is good. The micro-encapsule was really stabe. The encapsulated paclitaxel released 4.27% after it was disposed in simulated gastric fluid and the accumulative drug-release percent in vitro at 240 min was 25.60% in simulated intestinal fluid；But in the simulated colonic fluid，the accumulated drug release percent reached 89.26% within 12.0 h，95.34% at 24.0 h，nearly perfectly released. These results indicate that the paclitaxel of micro-encapsulation had the characteristics higher resistance to digestibility and as a colon-specific delivery system. The preparation process is simple and feasible，it would be a novel paclitaxel preparation in clinic for the treatment of tumor.

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