目的筛选最佳去甲斑蝥素脂质体的制备方法并研究其理化性质。方法以包封率为测试指标,考察去甲斑蝥素脂质体的制备方法、药-脂比、胆固醇含量、荷电性、水相pH值、离子强度等因素,观察其显微结构并考察其粒径和粒度分布、体外释放特性及初步稳定性。结果采用薄膜分散法,药-脂比为1:20,磷脂-胆固醇比为2:1、水相介质pH为6.8的条件制备去甲斑螫素脂质体的包封率较高,可达47.5%。粒径约为360nm,体外释放度考察表明,在5h释放达到平衡,释放度为36.9%。在低温4℃条件下放置6个月,包封率和粒径基本没有变化。结论通过工艺和处方考察,优选出最佳的制备条件,制得的去甲斑蝥素脂质体包封率较高,比较稳定。

OBJECTIVE To prepare and characterize the liposome containing norcantharidin. METHODS Entrapment efficiency was determined. The ratio of drug to phospholipids, the ratio of phospholipids to cholesterol, the electricity, the pH value of water and the iome. Strength of buffer solution were examined. The physico-chemical properties of norcantharidin encapsulated in liposome were also investigated. RESULTS The entrapped efficiency reached 47.5% by using film hydration method.The ratio of drug to lipids was 1:2.The ratio of phospholipids to cholesterol was 2:1 and pH of water phase was 6. 8. The release rate of norcantharidin from liposome was 36.9% after 5 h and 39.2% after 10 h. The study on the stability showed that norcantharidin liposome was stable at 4℃ for 6 monthes. CONCLUSION Norcantharidin liposome with high entrapped efficiency and stability can be obtained by the optimization of preparation and formulation.