正交试验优选哈西奈德脂质体制备工艺

Preparation Process of Halcinonide Liposomes by Orthogonal Design

目的优选哈西奈德脂质体的最佳制备工艺。方法以胆固醇、卵磷脂为载体，采用薄膜分散法制备哈西奈德脂质体，以包封率为评价指标，采用正交试验进行系统研究，筛选哈西奈德脂质体的最佳制备工艺。结果哈西奈德脂质体的最佳制备工艺为：卵磷脂与胆固醇质量之比为6：1，氯仿与甲醇体积之比为1：1，水化温度为60℃，磷酸盐缓冲液的pH为6．5。优化后制备3批脂质体，平均包封率为93．29％±0．77％，粒径范围为98．26～102．54nm。结论选工艺制备的脂质体包封率高，粒径较均匀，形态较好，结构完整，该方法简单可行。

Objective To optimize the best preparation method of halcinonide liposomes. Methods The liposomes were prepared by thin film dispersion method by using cholesterin and soybean lecithin as carriers. The envelope efficiency of halcinonide liposomes was taken as the evaluation index to optimize the preparation by orthogonal design. The best preparation method of halcinonide liposomes was optimized. Results The optimal proportion and composition of halcinonide liposomes were as follows： the amount of cholesterin to phospholipid was 6： 1, the volume of chloroform to methanol was 1 ： 1, the hydration temperature was 60 ℃ and the phosphate buffer pH was 6.5. The average encapsulation efficiency of the optimized liposomes was 93.29% ± 0.77%, and their size was in the range of 98.26 - 102.54 nm. Conclusion Selected liposome preparation process of coating rate is high, uniform particle size, morphology, structural integrit, the method is simple and feasible.