西罗莫司脂质体的制备及处方因素考察

Preparation and study on formulation of sirolimus liposomes

目的制备西罗莫司脂质体并对处方进行筛选,以期得到高包封率的脂质体制剂。方法选用乙醇注入法制备西罗莫司脂质体,微柱离心-HPLC法测定包封率,以包封率为评价指标,考察磷脂浓度、磷脂胆固醇质量比、药脂比、水相介质pH等因素对脂质体的影响,在此基础上运用正交设计对处方进行优化。结果正交试验结果表明磷脂浓度为4%,磷脂与胆固醇质量比例为8:1,药物磷脂质量比为1:20,水相pH为7.4为最佳处方,制得的脂质体包封率为(82.11±2.13)%。结论优选出最佳处方,制得的西罗莫司脂质体包封率高,重现性好。

Objective To optimize the formulation of prepared sirolimus liposomes with high encapsulation efficiency （ EE% ）. Methods Sirolimus liposomes were prepared by ethanol injection method and the encapsulation efficiency was determindated by the minicolumn centrifugation-HPLC method.The single factors such as the concentration of PC,the ratio of PC to cholesterol,the ratio of drug to PC and the pH value of aqueous phase were studied. And the orthogonal design was adopted to obtain the optimized prescription, the main index was entrapment efficiency. Results The best prescription is as follows： the concentration of PC was 4%, the ratio of PC to cholesterol was 8：1, the ratio of PC to drug was 20：1 and the pH value of aqueous phase was 7.4.The encapsulation efficiency of the sirolimus liposomes was （82.11±2.13）%. Conclusion The formulation was optimized and the sirolimus liposome is of high encapsulation efficiency and good reproducibility.