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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 |
| 阅读数： | 666 次 |
| 本月下载数： | 8 次 |
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