两亲性嵌段共聚物PGMA-b-PMAPEG的制备及其胶束的布洛芬药物控制释放性能

Preparation of an amphiphilic block copolymer PGMA-b-PMAPEG and evaluation of its drug-releasing behavior for controlled release of ibuprofen

利用自由基可逆加成-断链链转移(RAFT)活性/可控聚合法成功合成了两亲性嵌段共聚物聚(甲基丙烯酸缩水甘油酯)-b-聚(甲基丙烯酸聚乙二醇酯)(PGMA-b-PMAPEG).利用傅立叶变换红外光谱、核磁共振谱仪、凝胶渗透色谱仪及透射电镜等分析了所合成聚合物的结构、胶束粒径及形貌.以布洛芬作为模型药物负载于聚合物胶束内,考察了其控制释放行为.结果表明,聚合物胶束呈核/壳结构的球形,粒径在100nm左右;释放介质的pH对载药胶束的药物释放速率影响较大.总体而言,所制备的两亲性嵌段共聚物有望用作药物控释载体.

Amphiphilic block copolymer,poly（glycidyl methacrylate）-block-poly（methacrylic acid ester of polyethylene glycol）,PGMA-b-PMAPEG in short,was synthesized by reversible addition-fragmentation chain transfer（RAFT）-controlled radical polymerization.The structure of as-synthesized block copolymer as well as the morphology and size of its micelle were analyzed by means of Fourier transform infrared spectrometry,nuclear magnetic resonance spectroscopy,gel permeation chromatography,and transmission electron microscopy.Ibuprofen was loaded in the micelle of as-synthesized block copolymer,and its in vitro drug-release behavior was investigated.Results show that the micelles of as-synthesized block copolymer have spherical shape and a diameter of about 100 nm.The pH value of the releasing medium（solution of as-synthesized block copolymer） had significant impact on the release of ibuprofen.In one word,as-synthesized block copolymer could be used as a drug delivery carrier.