均匀设计法优化塔斯品碱脂质体处方

Application of Uniform Design for Preparation of Taspine Liposomes

目的优化塔斯品碱脂质体的制备处方。方法采用薄膜挤压法制备塔斯品碱脂质体,根据均匀实验设计,以外观、脂质体粒径、复溶情况及包封率为指标综合评价。结果塔斯品碱脂质体的最佳制备处方为:蛋黄卵磷脂与胆固醇摩尔比50:50;水合介质用量10 mL;冻干保护剂选用蔗糖,用量为13%。所得塔斯品碱脂质体的平均粒径为186.4 nm,包封率为(88.29±4.2)%。结论由最佳处方制备的塔斯品碱脂质体,粒径均匀,包封率较高。

OBJECTIVE To optimize the preparation formulation of the taspine liposomes. METHODS The taspine liposomes were prepared by the film evaporation-extrusion. The technology was optimized by uniform design, and evaluated by taspine liposomal appearance, partical size distribution, redissolution and entrapment efficiency. RESULTS The results demonstrated that the best formulation of the taspine liposomes was as follows ： the mol ratio of egg phosphatidylcholine to cholesterol was 50： 50, the volume of the hydration solution was 10 ml, and the eoncentration of sucrose as a lyoprotectant was 13%. The mean size of liposomes determined by the particle size analyzer was 186.4 nm and the entrapment efficiency was （ 88.29±4. 2） %. CONCLUSION The taspine liposome prepared according to the best formulation has good morphological characteristics and high entrapment efficiency.