共载伊立替康-顺铂复合脂质体的制备及质量评价

Preparation and Quality Evaluation of Compound Liposomes of Irinotecan and Cis-platinum

目的:制备共载伊立替康-顺铂复合脂质体,并对其关键质量指标进行评价。方法:采用薄膜分散和主动载药技术制备目标产品,建立高效液相法测定共载复合脂质体含量及包封率,采用动态光散射法测定粒度和粒度分布。结果:共载伊立替康-顺铂复合脂质体中伊立替康、顺铂包封率分别为(99.51±0.79)%,(98.47±0.91)%(n=3),平均粒径为(129.9±1.9)nm(n=3),多项分散系数(PdI)小于0.20,Zeta电位为(-8.60±0.56)m V(n=3);所制得样品于低温(2~8℃)条件下放置6个月,各项关键指标均未发生明显变化。结论:该方法适合共载伊立替康-顺铂复合脂质体的制备,所建立质控方法简单、准确,适合对该共载复合脂质体质量进行评价。

Objective:To prepare compound liposomes loading irinotecan and cis-platinum,and evaluate the pharmaceutical properties.Methods:Film dispersion-active drug-loading technology was used to load irinotecan and cis-platinum for preparing the compound liposomes.An HPLC method was established for determining irinotecan and cis-platinum.The mean diameter of liposomes was determined by dynamic light scattering(DLS)technique.Results:The encapsulation efficiency of compound liposomes loading irinotecan and cis-platinum was 99.51%±0.79%and 98.47%±0.91%(n=3),respectively.The mean diameter of the compound liposome was(129.9±1.9)nm(n=3)with PdI below 0.20 and its zeta potential was(-8.60±0.56)m V(n=3).The inspection indices of the compound liposomes did not change significantly in 6 months of long-term storage test(2℃~8℃).Conclusion:The method is suitable to prepare compound liposomes of irinotecan and cis-platinum.The analysis method is simple and accurate,which can be used to evaluate the properties of the compound liposomes.