还原响应型高载药量普朗尼克F127聚合物胶束的制备

Preparation of Redox-responsive Pluronic F127 Micelles with High Drug-loading Efficiency

目的:制备还原响应型高载药量普朗尼克F127聚合物胶束。方法:对普朗尼克F127的疏水段引入甲基丙烯酸叔丁酯和半胱胺,合成强疏水性的巯基化衍生物F127-SH。利用薄膜水化法和巯基的氧化反应,制备载紫杉醇(PTX)的还原响应型高载药量普朗尼克F127聚合物胶束(F127-SS/PTX),检测其粒径、包封率、载药量,考察其在还原和非还原环境下的粒径变化和释药行为。结果:该胶束的平均粒径为(77.87±1.79)nm,包封率为(92.73±2.35)%,载药量为(16.25±0.99)%;在10 mmol/L二硫苏糖醇作用下,其粒径迅速增大,PTX释药速度显著增加。结论:成功制得还原响应型高载药量普朗尼克F127聚合物胶束。

OBJECTIVE：To prepare redox-responsive pluronic F127 micelles with high drug-loading efficiency.METHODS：The thiol derivative F127-SH with strong hydrophobicity was synthesized by introducing tert-butyl methacrylate and cysteamine to the hydrophobic segments of F127.Paclitaxel（PTX）-loaded redox-responsive pluronic F127 micelles with high drug-loading efficiency（F127-SS/PTX）were prepared by film-hydration method as well as oxidation reaction of thiol groups.The diameter,encapsulation efficiency and drug-loading amount were detected,and the change of diameter and drug release behavior of micelles were investaged under reducing environment or non-reducing environment.RESULTS：Mean diameter of F127-SS/PTX micelles was about（77.87±1.79）nm,and encapsulation efficiency and drug-loading amount were（92.73±2.35）% and（16.25±0.99）%,respectively.The diameter of the micelles increased rapidly and drug release rate of PTX increased significantly in the presence of 10mmol/L dithiothreitol.CONCLUSIONS：The redox-responsive pluronic F127 micelles with high drug-loading efficiency are prepared successfully.