Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu 610052, China.
J Mater Chem B. 2019 Jan 14;7(2):334-345. doi: 10.1039/c8tb02313a. Epub 2018 Dec 17.
pH-responsive stereocomplexed micelles based on poly(l-lactic acid)-b-polylysine/poly(d-lactic acid)-b-methoxy poly(ethylene glycol) (PLLA-b-PLys/PDLA-b-mPEG) were fabricated by stereocomplexation between enantiomeric PLA segments. The morphology, critical micelle concentration, formation of stereocomplexation and pH sensitivity of the stereocomplexed micelles were investigated by TEM, DLS, fluorescence spectra, DSC, XRD, and the acid-base titration method. Interestingly, it was observed that compared to PLLA-b-PLys micelles, the stereocomplexed micelles showed lower critical micelle concentration. Anticancer drug doxorubicin (DOX) was encapsulated in the stereocomplexed micelles and then they were incubated with Hela cells to study the in vitro anti-tumor effect. The results showed that the DOX-loaded stereocomplexed micelles exhibited a slower drug release behavior and a weaker efficacy of intracellular proliferation inhibition than PLLA-b-PLys micelles. Stereocomplexation would provide a favorable platform to construct stable micelles for cancer therapy.
基于聚（L-丙交酯）-b-聚赖氨酸/聚（D-丙交酯）-b-甲氧基聚（乙二醇）（PLLA-b-PLys/PDLA-b-mPEG）的 pH 响应性立体复合物胶束是通过对映 PLA 段之间的立体复合物形成制备的。通过 TEM、DLS、荧光光谱、DSC、XRD 和酸碱滴定法研究了立体复合物胶束的形态、临界胶束浓度、立体复合物形成和 pH 敏感性。有趣的是，与 PLLA-b-PLys 胶束相比，观察到立体复合物胶束的临界胶束浓度较低。将抗癌药物阿霉素（DOX）包封在立体复合物胶束中，然后用其孵育 Hela 细胞，以研究体外抗肿瘤作用。结果表明，载 DOX 的立体复合物胶束表现出较慢的药物释放行为和较弱的细胞内增殖抑制作用，低于 PLLA-b-PLys 胶束。立体复合物化将为构建用于癌症治疗的稳定胶束提供有利的平台。
