CA4P脂质体的制备工艺研究

Preparation process of Combretastatin A4 Prodrug liposome

目的研究CA4P脂质体的处方及制备工艺。方法以包封率为主要评价指标考察制备方法;用透射电镜和粒径测定仪表征脂质体的形态和粒径;用HPLC法测定脂质体中CA4P的包封率和载药量;以正交设计筛选优化最佳处方工艺。结果脂质体的平均粒径为167nm,Zeta电位为-24.3mV,最佳工艺处方的药-脂比为1:12,磷脂-胆固醇为8:1,有机相-水相体积为4:1,水合介质为0.9%NaCl;制备3批脂质体的平均包封率为58%、载药量为4.8%。结论逆相蒸发-探头超声法可制备具有较高包封率的CA4P脂质体。

OBJECTIVE To study the formulation and preparation technique of Combretastin A4 prodrug （CA4P） liposome. METHODS Liposme was prepared with different methods, using entrapment efficiency as the optimized index. The shape and particle size were determined by electronic microscopy and Zetamaster, and the encapsulation efficiencies were determined by HPLC. The orthogonal design method was used to optimize the formulation and preparation technique of CA4P liposome. RESULTS The average size was about 167 nm and Zete -potential of -24.3 inV. The optimal preparation conditions of CA4P liposome were as follows：the proportion of CA4P and lipids in weight was 1 ： 12, soybean phosphatidylcholine ： cholesterol was 8 ： 1, oil ：water was 4 ： 1, the hydration medium was 0.9% NaCl. The average encapsulation efficiency of the optimized liposome was 58.0% and the mean drug - loading efficiency was 4.8%. CONCLUSION The entrapment efficiency of CA4P liposome prepared with reverse evaporation method and probe ultrasonic technique is optimized.