Ma Boxuan, Zhuang Weihua, Liu Gongyan, Wang Yunbing
National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China and.
National Engineering Laboratory of Clean Technology of Leather Manufacture, Department of Biomass Chemistry, Sichuan University, Chengdu 610064, China.
Regen Biomater. 2018 Feb;5(1):15-24. doi: 10.1093/rb/rbx023. Epub 2017 Aug 16.
As nano-scale drug delivery systems, smart micelles that are sensitive to specific biological environment and allowed for target site-triggered drug release by reversible stabilization of micelle structure are attractive. In this work, a biocompatible and pH-sensitive copolymer is synthesized through bridging poly (2-methacryloyloxyethyl phosphorylcholine) (PMPC) block and poly (-lactide) (PLA) block by a benzoyl imine linkage (). Biomimetic micelles with excellent biocompatibility based on such PLA--PMPC copolymer are prepared as carriers for paclitaxel (PTX) delivery. Due to the rapid breakage of the benzoyl imine linkage under acidic condition, the micelle structure is disrupted with accelerated PTX release. Such pH-sensitive triggered drug release behavior in synchronization with acidic conditions at tumor site is helpful for improving the utilization of drug and facilitating antitumor efficacy. These micelles can be used as promising drug delivery systems due to their biocompatible and smart properties.
作为纳米级药物递送系统，对特定生物环境敏感且能通过胶束结构的可逆稳定实现靶位点触发药物释放的智能胶束颇具吸引力。在本工作中，通过苯甲酰亚胺键连接聚（2-甲基丙烯酰氧基乙基磷酰胆碱）（PMPC）嵌段和聚（-丙交酯）（PLA）嵌段，合成了一种生物相容性且对pH敏感的共聚物。基于这种PLA-PMPC共聚物制备了具有优异生物相容性的仿生胶束作为紫杉醇（PTX）递送载体。由于苯甲酰亚胺键在酸性条件下快速断裂，胶束结构被破坏，PTX释放加速。这种在肿瘤部位与酸性条件同步的pH敏感触发药物释放行为有助于提高药物利用率并促进抗肿瘤疗效。由于其生物相容性和智能特性，这些胶束可作为有前景的药物递送系统。
