正交试验法优选盐酸小檗碱脂质体制备工艺

Study on the Preparation Process of Berberine Hydrochloride Liposomes by Orthogonal Design

目的:优选盐酸小檗碱脂质体的制备工艺。方法:采用主动加药法制备盐酸小檗碱脂质体,在单因素考察基础上采用正交试验设计,以包封率为评价指标,筛选脂质体制备的最佳工艺条件。结果:最佳制备工艺为A2B1C1D1,即卵磷脂与胆固醇之质量比为3∶1,药脂质量比1∶30,孵化时间为20min,孵化温度60℃。制备3批脂质体,平均包封率为(78.51±2.45)%,粒径范围为2.2μm～3.5μm。结论:所选工艺制备的脂质体包封率较高,粒径分布较均匀。

Objective To optimize the preparation process of berberine hydrochloride liposomes. Methods Liposomes were prepared by active loading method,. Orthogonal design was adopted to screen the preparation of berberine hydrochloride liposomes after the study of different single variables. The optimal technological conditions were acquired by the evaluation of the encapsulation efficiencies. Results The optimal preparation conditions of berberine hydrochloride liposome were as follows： the proportion of berberine hydrochloride and lipids in weight was 1：30, soybean phosphatidylcholine： cholesterol = 3： 1, incubation time was 20 minutes and incubation temperature was 60 %. The average encapsulation efficiency of the optimized liposomes was （78.51 ± 2.45 ） % and their size range was 2.2 μm- 3.5 μm. Conclusion The entrapment efficiency and partide size of the optimized berberine hydrochloride liposomes are satisfactory.