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作 者 ：张智舟;姜守刚;祖元刚*;赵冬梅;赵修华;金晓慧

期 刊 ：植物研究 2011年 31卷 (3)期 页码：381-384

关键词：多西紫杉醇；白蛋白微球；去溶剂化—化学交联法；

Keywords:docetaxel, BSA-NPs, desolvation-chemical crosslinking method,

摘 要 ：多西紫杉醇（DT）是唯一应用于临床治疗肿瘤的紫杉醇的衍生物，其水溶性差，制剂中需要加入有机溶剂和助溶剂，而有机溶剂和助溶剂具有刺激性。为减少多西紫杉醇制剂的刺激性，本实验通过去溶剂化—化学交联法制备水溶性多西紫杉醇白蛋白微球。对制备过程中的重要影响因素进行考察，并通过Design-expert软件进行数据优化，最终得优化条件：白蛋白浓度为35 mg·mL^-1，DT浓度为1.03 mg·mL^-1，乙醇和水的比例为3∶1，乙醇的滴加速度为0.73 mL·min^-1，搅拌时间为12 h，0.2%戊二醛与白蛋白的交联比为2∶1。得到的多西紫杉醇白蛋白微球粒径为185 nm，载药量为14.4%，成功的解决了其水溶性，为接下来的动物实验、临床应用提供了良好的基础。

Abstract:Docetaxel (DT), the only derivative of paclitaxel for clinical application in tumor, is mainly used for the treatment of breast cancer, nonsmall-cell lung cancer, oophoroma, etc. Because of its low solubility, organic solvents and solution adjuvants are always added to the preparation. However, organic solvents and solution adjuvants are pungent. Solubility of docetaxel can be increased by the preparation of docetaxel-loaded bovine serum albumin nanoparticles (DT-BSA-NPs) through desolvation-chemical crosslinking method. In this study, the important factors during preparation were tested, and the optimal conditions were obtained according to the optimized data by Design-expert. These data were as follows: the concentration of albumin was 35 mg·mL^-1, the concentration of DT was 1.03 mg·mL^-1, the ratio of ethanol to water was 3∶1, the dripping speed of ethanol was 0.73 mL·min^-1, the stirring time was 12 h, cross-link ratio of glutaraldehyde and BSA was 2∶1. The particle size of the product is 185 nm, and the drug-loading rate is 14.4%. The developed method successfully helped to improve the water-solubility of docetaxel and therefore provided a good foundation for the animal experiments and clinical applications in days to come.

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