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目的制备依托泊苷脂质体并考察其药剂学性质。方法采用薄膜水化-高压均质法制备依托泊苷脂质体,以胆固醇与氢化磷脂的摩尔比(A)、脂质体溶液中的磷脂浓度(B)、依托泊苷与氢化磷脂的质量比(C)为考察因素,以包封率(Y1)、载药量(Y2)、综合指标(Y3)为响应值,经Box-Behnken效应面法(response surface methodology,RSM)进行处方优化,得到最优处方,并测定脂质体的粒径。结果经RSM优化后,A、B、C分别为0.49,4.96%,0.15;制得的依托泊苷脂质体实测包封率为82.6%,载药量为11.4%,平均粒径为132.5 nm。结论利用Box-Behnken效应面法优化依托泊苷脂质体处方,能制备符合药剂学要求的脂质体,可供体内实验研究。
Objective To prepare etoposide liposomes and study their pharmacological properties. Methods Etoposide liposomes were prepared by membrane hydration-high pressure homogenization. The molar ratio of cholesterol to phospholipid (A), phospholipid concentration in liposome solution (B), the mass of etoposide and phospholipid (C) was used as the investigation factor. The optimal formulation was optimized by Box-Behnken response surface methodology (RSM) using the encapsulation efficiency (Y1), drug loading capacity (Y2) and composite index (Y3) Get the best prescription, and determine the size of liposomes. Results After optimized by RSM, A, B and C were 0.49, 4.96% and 0.15, respectively. The measured entrapment efficiency of etoposide liposome was 82.6% and drug loading was 11.4%, and the average particle size was 132.5 nm . Conclusion Box-Behnken effect surface optimization of etoposide liposomal prescription, can meet the requirements of pharmacological liposomes for in vivo experimental study.