Box-Behnken效应面法优化多西他赛长循环脂质体处方.PDFVIP

·1946 · 中草药 Chinese Traditional and Herbal Drugs 第 43 卷 第 10 期 2012 年 10 月 Box-Behnken 效应面法优化多西他赛长循环脂质体处方 * 程 怡 ，吴 琼，余秋强，赵菊香 广州中医药大学中药学院，广东 广州 510006 摘 要：目的 优化多西他赛长循环脂质体（DLCL ）处方。方法 采用薄膜蒸发法制备 DLCL ，分别以卵磷脂（PC ）与多 西他赛（DOC ）质量比（X 1 ）、PC 与胆固醇（Chol ）质量比（X2 ）、DSPE-PEG 2000 与 PC 物质的量之比（X 3 ）为考察对象， 包封率（Y ）、载药量（Y ）、综合指标 OD 值为评价指标，采用 Box-Behnken 效应面法筛选 DLCL 的最佳处方。结果 最优 1 2 处方为 X 1 ＝0.616 2，X2 ＝1.0，X 3 ＝−1.0；DLCL 的包封率为（94.71 ±1.75）%，载药量为（5.37 ±0.43 ）%，标准偏差均小 于 10%；平均粒径 139.6 nm，分布均匀，体外释放试验结果表明其具有明显的缓释效果。结论 采用 Box-Behnken 效应面 法优化 DLCL 处方是有效、可行的。 关键词：多西他赛；长循环脂质体；Box-Behnken ；效应面法；体外释放 中图分类号：R283.6 文献标志码：A 文章编号：0253 - 2670(2012)10 - 1946 - 05 Formula optimization of Docetaxel long-circulation liposomes by Box-Behnken design and response surface method CHENG Yi, WU Qiong, YU Qiu-qiang, ZHAO Ju-xiang School of Chinese Materica Medica, Guangzhou University of Chinese Medicine, Guangzhou 510006, China Abstract: Objective To optimize the formula of Docetaxel (DOC) long-circulation liposomes (DLCL). Methods DLCL was prepared by the membrane-hydration method. The effects of phosphatidylcholine (PC)-DOC (X ), PC-cholesterol (Chol) (X ), and the 1 2 amount of DSPE-PEG 2000 (X ) were observed. The encapsulation efficiency (Y ), drug loading amount (Y ), and the general 3 1 2 requirements (Y ) were evaluated and the formula was optimized by Box-Behnken design and response surface method. Results The 3 optimal formula was as following: X 1 ＝0.616 2, X2 ＝1.0, and X 3 ＝−1.0; The encapsulation efficiency was (94.71 ± 1.75)%, drug loading amount was (5.37 ± 0.43)%. The standard deviations were all below 10%. Th