Wang Yu-Cai, Li Yang, Sun Tian-Meng, Xiong Meng-Hua, Wu Juan, Yang Yi-Yan, Wang Jun
Department of Polymer Science and Engineering and CAS Key Laboratory of Soft Matter Chemistry, University of Science and Technology of China, Hefei, Anhui 230026, P. R. China.
Macromol Rapid Commun. 2010 Jul 1;31(13):1201-6. doi: 10.1002/marc.200900863. Epub 2010 Mar 19.
Reversibly cross-linked core-shell-corona micelles based on a triblock copolymer composed of poly(aliphatic ester), polyphosphoester, and poly(ethylene glycol) are reported. The triblock copolymer is synthesized through consecutive ring-opening polymerization of ε-caprolactone and 2,4-dinitrophenylthioethyl ethylene phosphate, followed by conjugation of poly(ethylene glycol). After deprotection under mild conditions, the amphiphilic polymer forms core-shell-corona micelles with free thiols in the shell. Cross-linking of the micelles within the shell reduces their critical micellization concentration and enhances their stability against severe conditions. The redox-sensitive cross-linkage allows the facilitated release of entrapped anticancer drugs in the cytoplasm in response to the intracellular reductive environment. With enhanced stability during circulation after administration, and accelerated intracellular drug release at the target site, the biocompatible and biodegradable shell-cross-linked polymeric micelle is promising as a drug vehicle for cancer chemotherapy.
报道了基于由聚（脂肪族酯）、聚磷酸酯和聚（乙二醇）组成的三嵌段共聚物的可逆交联核壳-冠层胶束。通过ε-己内酯和2,4-二硝基苯硫基乙基磷酸乙烯酯的连续开环聚合，随后与聚（乙二醇）共轭来合成三嵌段共聚物。在温和条件下脱保护后，两亲性聚合物形成壳层带有游离硫醇的核壳-冠层胶束。壳层内胶束的交联降低了它们的临界胶束浓度，并增强了它们在苛刻条件下的稳定性。氧化还原敏感的交联使得在细胞内还原环境下能够促进包裹的抗癌药物在细胞质中释放。由于给药后循环过程中稳定性增强，且在靶部位细胞内药物释放加速，这种生物相容性和可生物降解的壳交联聚合物胶束有望作为癌症化疗的药物载体。
