Ch-PCL-b-PVP生物可降解胶束的制备及其对布洛芬的控制释放

Preparation of Ch-PCL-b-PVP Biodegradable Micelles for Controlled Release of Ibuprofen

以胆固醇(Ch)引发ε-己内酯(ε-CL)开环聚合,制备了端胆固醇基聚己内酯(Ch-PCL),然后与端羧基聚乙烯基吡咯烷酮(PVP-COOH)偶合制备了两亲性嵌段共聚物端胆固醇基聚己内酯-b-聚乙烯吡咯烷酮(Ch-PCL-b-PVP)。利用红外(FT-IR)、核磁(1 H-NMR)及凝胶渗透色谱(GPC)对其进行了结构和组成表征。透射电镜(TEM)和动态激光光散射(DLS)测试结果表明:该共聚物在水溶液中自组装形成粒径在150nm左右的球形胶束,其临界胶束-质量浓度(CMC)为2.6mg/L。采用布洛芬(IBUPROFEN)为药物模型,测得其载药量(DLC)为32.4%,药物负载率(EE)为70.1%,具有较好的缓释功效。

Cholesterol-terminated polycaprolactone （Ch-PCL） was synthesized by the ring-opening polymerization of ε-caprolactone （ε-CL） using cholesterol（Ch） as the macro-initiator. Then, the amphiphilic block copolymer cholesterol-terminated polycaprolactone-b-polyvinyl pyrrolidone （Ch-PCL-b-PVP） was prepared by coupling reaction of the Ch-PCL and carboxyl-terminated polyvinylpyrrolidone （PVP-COOH）, and its structure and composition were confirmed by Gel Permeation Chromatography（GPC）, 1H-Nuclear Magnetic Resonance （1H-NMR ） spectroscopy and FT-IR spectroscopy. The Transmission Electron Microscopy （TEM） and Dynamic Laser Light Scattering （DLS） results showed that the copolymers could self-assemble into spherical micelles with the diameter about 150 nm. The critical micelle concentration （CMC） was 2.6 mg/L. Using the ibuprofen as drug model, the drug loading （DLC） and encapsulation efficiency （EE） were 32.4% and 70.1%,respectively.