Laboratory of Polymer Physics and Chemistry, Institute of Chemistry, The Chinese Academy of Sciences, Beijing 100190, China.
J Biomed Mater Res A. 2011 Feb;96(2):330-40. doi: 10.1002/jbm.a.32985. Epub 2010 Nov 29.
Novel micelles from biamphiphilic triblock copolymer poly(ethylene glycol)-b-poly(ε-caprolactone)-b-poly(acrylic acid) (PEG-b-PCL-b-PAA) as new multifunctional nanocarriers to delivery anticancer drugs were evaluated. The well-defined triblock copolymers prepared by controlled polymerizations self-assembled into micelles in aqueous solution with a hydrodynamic radius of 13 nm as obtained by dynamic light scattering (DLS) and a low critical micellization concentration of 2.9 × 10(-4) g/L. The hydrophobic PCL cores of micelles were applied to load hydrophobic drug doxorubicin and the functional PAA subcoronas clung to the micellar core were used to carry cisplatin through covalent interaction. The results indicated that two anticancer drugs had been loaded by different mechanism either separately or simultaneously. Drug loading content and efficiency as well as release profiles were evaluated. Furthermore, internalization and cytotoxicity of the anticancer nanoparticles against human bladder carcinoma EJ cells were studied. The biamphiphilic triblock copolymer micelles provided not only biocompatibility and biodegradability, but also abilities for loading single and dual anticancer drugs, indicating that this was a useful multifunctional platform for anticancer drug delivery.
新型两亲性三嵌段共聚物聚乙二醇-聚己内酯-聚（丙烯酸）（PEG-b-PCL-b-PAA）胶束作为新型多功能纳米载体用于递送抗癌药物。通过控制聚合制备的结构明确的三嵌段共聚物在水溶液中自组装成胶束，动态光散射（DLS）测得胶束的水动力半径为 13nm，临界胶束浓度（CMC）低至 2.9×10(-4)g/L。胶束的疏水性 PCL 内核用于负载疏水性药物阿霉素，而与胶束核心附着的功能化 PAA 亚冠则通过共价相互作用携带顺铂。结果表明，两种抗癌药物可以分别或同时通过不同机制进行负载。评价了载药含量、载药效率和释放曲线。此外，还研究了抗癌纳米粒子对人膀胱癌 EJ 细胞的内化和细胞毒性。两亲性三嵌段共聚物胶束不仅提供了生物相容性和生物降解性，还具有负载单药和双药的能力，表明这是一种用于抗癌药物递送的有用多功能平台。
