Han Yang, Liang Na, Yan Pengfei, Kawashima Yoshiaki, Cui Fude, Sun Shaoping
Department of Pharmaceutical Engineering, School of Chemistry and Material Science, Heilongjiang University, Harbin 150080, China.
College of Chemistry & Chemical Engineering, Harbin Normal University, Harbin 150025, China.
Polymers (Basel). 2020 Feb 8;12(2):380. doi: 10.3390/polym12020380.
In this study, a redox-sensitive chitosan derivative with modifications by cholesterol, sulfhydryl, and mPEG (mPEG-CS(SH)-CHO) was successfully synthesized and characterized. Due to its amphiphilicity, the conjugate could spontaneously form micelles in an aqueous environment. The optimized paclitaxel (PTX)-loaded mPEG-CS(SH)-CHO micelles, with a mean diameter of 158 nm, zeta potential of +26.9 mV, drug loading of 11.7%, and entrapment efficiency of 88.3%, were successfully prepared. The results of an XRD study demonstrated that PTX was loaded in the core of the micelles in a non-crystalline state. Inspiringly, the PTX-loaded micelles possessed excellent anticancer effect but low toxicity to the body. It can be concluded that the mPEG-CS(SH)-CHO micellar system is a promising drug delivery carrier for the controlled release of PTX.
在本研究中，成功合成并表征了一种经胆固醇、巯基和甲氧基聚乙二醇（mPEG）修饰的氧化还原敏感型壳聚糖衍生物（mPEG-CS(SH)-CHO）。由于其两亲性，该共轭物可在水性环境中自发形成胶束。成功制备了优化的载紫杉醇（PTX）的mPEG-CS(SH)-CHO胶束，其平均直径为158 nm，ζ电位为+26.9 mV，载药量为11.7%，包封率为88.3%。X射线衍射（XRD）研究结果表明，PTX以非晶态形式负载于胶束核心。令人鼓舞的是，载PTX的胶束具有优异的抗癌效果，但对机体毒性较低。可以得出结论，mPEG-CS(SH)-CHO胶束系统是一种用于PTX控释的有前景的药物递送载体。
