pH敏感新型嵌段共聚物的合成及其对叶酸的运载与释放

Preparation of a new type of polymeric micelles with p H/fluorescence properties and the control-release of anti-cancer drug folic acid

采用可逆加成-断裂链转移(RAFT)法,成功合成了一种具有荧光性能的新型p H敏感两亲性嵌段共聚物聚(甲基丙烯酰氧喹啉-co-甲基丙烯酸-2-二甲氨基乙酯)-b-聚(甲基丙烯酸聚乙二醇酯)(P(MAQ-co-DMAEMA)-b-PMAPEG),用红外光谱(FT-IR)、核磁共振(1H NMR)、凝胶渗透色谱(GPC)对其结构进行表征.此共聚物在水溶液中可自组装形成胶束,由扫描电子显微镜(SEM)、动态光散射(DLS)、紫外光谱(UV)和荧光光谱(FL)对聚合物胶束溶液表征可知胶束为尺寸约80 nm的球形颗粒,且胶束溶液具有良好的荧光性.以叶酸(FA)为模型药物,研究载药胶束在模拟人体环境中的控释行为.结果表明:P(MAQ-co-DMAEMA)-b-PMAPEG可作为包载药物的一种新型纳米材料,载药胶束的体外释放呈明显p H依赖性,且具有较好的荧光性,该聚合物有望成为具有荧光性的理想药物载体.

A novel of amphiphilic diblock copolymer,poly(8-methacryloyloxyquinoline-co-(N,N-dimethylamino) ethylmethacrylate)-b-poly(methylacrylic acid polyethylene glycol ester)(P(MAQ-coDMAEMA)-b-PMAPEG) with p H/fluorescent properties,was designed and synthesized by reversible addition fragmentation chain transfer(RAFT) polymerization.Subsequently,the structure of the copolymer was confirmed by fourier transform infrared spectroscopy(FT-IR),1 H nuclear magnetic resonance spectroscopy(1 H NMR) and gel permeation chromatography(GPC).The results of the scanning electron microscopy(SEM) and dynamic laser light scattering(DLS) showed that the prepared polymer micelles exhibited spherical core-shell structure with a mean diameter around 80 nm and narrow size distribution,and unique fluorescent properties and remarkable p H-responsive.Meanwhile,the control-release of anti-cancer drug folic acid(FA) behaviors of the polymer micelles was studied with the drug-loading content and efficiency of 37% and 52%,respectively.