摘要
目的制备多西他赛(DTX)的F127聚合物胶束,对其药剂学特征进行评价。方法薄膜分散法制备胶束,并在单因素考察的基础上,以正交试验优化处方;透射电镜观察胶束形态;粒度分布测定仪测定其粒径、粒度分布;离心过滤法测定胶束的包封率和载药量;以DTX注射液作对照,采用动态膜透析法考察载药胶束的体外释药情况。结果薄膜分散法制备的胶束呈球形或类球形,平均粒径为(30.2±2.56)nm,平均包封率为(86.66±2.46)%,平均载药量为(0.42±0.01)%;体外释放实验结果表明该胶束具有一定的缓释能力。结论该胶束制备工艺简单,成型好,包封率高,具有一定的缓释能力。
Purpose To prepare docetaxel（DTX） loaded pluronic F127 polymeric micelles and to investigate the pharmaceutical characteristics.Methods The DTX loaded polymeric micelles were prepared by film dispersion method using a nonionic surfactant pluronic F127,and based on the results of single-factor experiments,the best formulation of DTX loaded polymeric micelles were optimized by the orthogonal design.The morphology of DTX loaded polymeric micelles was observed under transmission electronic microscopy.The particle sizes and the polydispersity were measured by laser particle size analyzer.The drug loading and entrapment efficiencies were determined by centrifugation-filtration method.The in vitro release kinetics of DTX-micelles was studied by dynamic dialysis system using DTX-injection as control.Results The morphology of DTX-micelles was approximately spherical and the mean particle size was（30.2±2.56） nm.The mean entrapment efficiency and drug loading were（86.66±2.46）% and（0.42±0.01）%,respectively.These release results indicated that DTX-F127 polymeric micelles observed the sustained release capacity.Conclusion DTX-F127 polymeric micelles can be prepared easily by good morphology,high entrapment efficiency and certain restrained release capacity.
出处
《中国生化药物杂志》
CAS
CSCD
北大核心
2011年第2期107-110,114,共5页
Chinese Journal of Biochemical Pharmaceutics
基金
由山东大学大学生创新课题资助
