Zhuang Weihua, Ma Boxuan, Liu Gongyan, Chen Xiaobing, Wang Yunbing
National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
Department of Biomass Chemistry, National Engineering Laboratory of Clean Technology of Leather Manufacture, Sichuan University, Chengdu 610064, China.
Regen Biomater. 2018 Feb;5(1):1-8. doi: 10.1093/rb/rbx012. Epub 2017 Apr 19.
cis-dichlorodiammineplatinum(II) (CDDP)-loaded polymeric micelles for cancer therapy have been developed to reduce the serious side effects of cisplatin CDDP. Herein, polymeric micelles incorporated with cisplatin are prepared based on the complexation between CDDP and hydrophilic poly (-glutamic acid)-b-poly (2-methacryloyloxyethyl phosphorylcholine) (PLG-b-PMPC) diblock copolymers. These CDDP-loaded micelles possess an average size of 91 nm with narrow distribution, providing remarkable stability in media containing proteins. The release of CDDP from the micelles is faster at pH 5.0 and pH 6.0 than that at pH 7.4 and in a sustained manner without initial burst release. In addition, there is almost no difference in cellular uptake between these CDDP-loaded micelles and free CDDP. Moreover, in vitro cytotoxicity test shows they possess high efficacy to kill 4T1 cells as compared with free drug. Thus, PLG-b-PMPC copolymer might be a promising carrier for CDDP incorporating in cancer therapy.
用于癌症治疗的顺式二氯二氨铂（II）（CDDP）负载型聚合物胶束已被开发出来，以减少顺铂CDDP的严重副作用。在此，基于CDDP与亲水性聚（γ-谷氨酸）-b-聚（2-甲基丙烯酰氧基乙基磷酰胆碱）（PLG-b-PMPC）二嵌段共聚物之间的络合作用，制备了负载顺铂的聚合物胶束。这些负载CDDP的胶束平均尺寸为91nm，分布狭窄，在含蛋白质的介质中具有显著的稳定性。CDDP从胶束中的释放在pH 5.0和pH 6.0时比在pH 7.4时更快，且以持续方式释放，无初始突释。此外，这些负载CDDP的胶束与游离CDDP之间的细胞摄取几乎没有差异。而且，体外细胞毒性试验表明，与游离药物相比，它们对杀死4T1细胞具有高效性。因此，PLG-b-PMPC共聚物可能是一种用于癌症治疗中负载CDDP的有前景的载体。
