多烯紫杉醇脂质核胶束的制备及性质考察  

Preparation and characterization of docetaxel-loaded lipid-core micelles

作　　者：胡凯莉[1] 贾娜[1] 刘梅[1] 奉建芳[1] 

机构地区：[1]上海中医药大学穆拉德中药现代化研究中心,上海201203

出　　处：《中成药》2014年第6期1181-1186,共6页Chinese Traditional Patent Medicine

基　　金：上海市科学技术委员会纳米专项项目(11nm0506700);上海高校青年教师培养资助计划(shzy004)

摘　　要：目的采用正交试验优化多烯紫杉醇脂质核胶束的处方工艺并考察其质量。方法以二硬脂酰基磷脂酰乙醇胺-聚乙二醇2000（PEG-2000DSPE）为载体材料，通过薄膜水化法制备载多烯紫杉醇的脂质核胶束。通过单因素试验和正交试验优化确立了制剂的最优处方工艺。以透射电镜观察载药胶束的外观形态；动态光散射法测定其粒径；HPLC法测定载药量；以透析法进行体外释放特性考察。结果透射电镜下观察多烯紫杉醇脂质核胶束呈外观圆整的球形，动态光散射法测定其粒径为（18．3±1．8）nm，Zeta电位为（-17．20±6．46）mV，载药量为3．1％～4．1％；体外释放试验表明其具有一定的缓释效应，体外释放曲线符合Higuchi方程。结论通过处方优化制得的多烯紫杉醇脂质核胶束，具有理想的粒径，载药量和体外释放行为，有望提高多烯紫杉醇的抗肿瘤效果。AIM To optimize the preparation of docetaxel-loaded PEG-DSPE lipid-core micelles with orthogo- nal design and study the characteristics of the optimized micelles. METHODS The docetaxel-loaded PEG-DSPE lipid-core micelles were prepared by the thin-film hydration procedure using PEG-DSPE as the carrier material. The optimal formulation was verified by single factor experiment and orthogonal design. The morphologic features of the micelles were examined by transmission electron microscopy. The particle size and Zeta potential of the micelles were determined by dynamic light scattering method. The docetaxel loads were detected by HPLC. The in vitro release property was measured by dialysis method. RESULTS The spherical micelles were found to be with a parti- cle size of （18.3± 1.8） nm and a Zeta potential of （ -17.20 ±6.46） mV. The drug loading capacity was 3.1%～4. 1%. The in vitro release results showed the micelles had a controlled release property, and the release profile was in line with the Higuchi equation. CONCLUSION The optimized docetaxel-loaded PEG-DSPE lipid-core micelles, with ideal particle size, drug loading capacity and release properties, may improve the antitumor efficacy of docetaxel.

关 键 词：多烯紫杉醇 脂质核胶束 正交试验 体外释放 

分 类 号：R944.9[医药卫生—药剂学]