还原响应型高载药量普朗尼克F127聚合物胶束的制备
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篇名: 还原响应型高载药量普朗尼克F127聚合物胶束的制备
TITLE:
摘要: 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。
ABSTRACT: 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 10 mmol/L dithiothreitol. CONCLUSIONS: The redox-responsive pluronic F127 micelles with high drug-loading efficiency are prepared successfully.
期刊: 2016年第27卷第19期
作者: 串星星,印亚双1,王学清
AUTHORS: CHUAN Xingxing,YIN Yashuang,WANG Xueqing
关键字: 还原响应;载药量;聚合物胶束;普朗尼克F127;紫杉醇
KEYWORDS: Redox-responsive; Drug-loading amount; Polymeric micelles; Pluronic F127; Paclitaxel
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