正交试验优选硫酸铵梯度法制备苦参碱脂质体的工艺研究

目的 以包封率为指标优选苦参碱脂质体的制备工艺.方法 以氢化大豆卵磷脂(HSPC)和胆固醇(Ch)为膜材,采用薄膜超声-硫酸铵梯度法制备脂质体.通过正交设计优化处方工艺,葡聚糖凝胶法分离游离药物,HPLC法测定月旨质体中苦参碱的包封率.结果 最佳工艺为:HSPC:Ch=3∶1,探头超声10 min,药脂比为1:15,包封率均值为50.68％.结论 优化后的工艺可提高苦参碱脂质体的包封率,此工艺条件简单,可操作性强,适于实验室条件下制备苦参碱脂质体.

Optimization of preparation of matrine liposome in ammonium sulfate gradient method by orthogonal experiment

Objective To study the preparation method of matrine liposome and screen the optimal technological conditions by the encapsulation efficiencies.Methods Liposome was made of hydrogenated soybean phosphatidylcholine (HSPC) and cholesterol (Ch) by film ultrasonic-ammonium sulfate gradient method. Then orthogonal design was adopted to screen the optimal conditions. Free drug was separated by Sephadex gel and the encapsulation efficiency of matrine was determined by HPLC. Results The optimum conditions of matrine liposomes were as follows:HSPC:Ch=3:1, the time of probe ultrassonic was 10min, and the ratio of drug to lipid was 1:15. The average entrapment efficiency was 50.68%. Conclusions The entrapment efficiency of liposome could be obviously improved with the optimized condition. The method discussed above was simple, feasible, and easily operated, which could be suitable for laboratory to prepare matrine liposome.