酮洛芬高分子前药纳米微球的制备及药物释放

Preparation of poly-KVE prodrug loaded by polyvinyl pyrrolidone nanoparticles and Its controlled drug release

高分子前药可以有效控制药物的释放速率,在药物后期性能改善方面发挥重要作用.本研究以酮洛芬为药物模型,利用化学法合成酮洛芬乙烯酯单体,再通过自由基聚合制备具有较高分子量的聚合物前药.为改善酮洛芬高分子前药的缓释行为,在酮洛芬高分子前药中加入亲水性聚乙烯吡咯烷酮进行高压静电喷雾,制备酮洛芬高分子前药的聚合物微球.用FT-IR、NMR、SEM、XRD对前药聚合物的结构和形貌进行表征.结果表明,酮洛芬前药以无定形态形式分布于聚乙烯吡咯烷酮中.电喷法制得的前药聚合物微球的平均粒径约200～400nm.酮洛芬聚合物纳米微球载药量（w/w）为20％,2h内释放的药物总量占总体的48.1％,具有良好的缓释性能.

Polymeric prodrug can controll the release of drug, it improves drugs＇ characters significantly. So we used polymerization process to prepare ketoprofen vinyl ester as the monomer, then polymer＇ized the monomers to get the poly- KVE. Because the hydrophility of polyvinyl pyrrolidon（PVP）, we added it to the prodrug to electrospray together to get microparticles. The chemical characterizations of the drug-loaded particles were investigated by means of FTIR, NMR, SEM and XRD. It showed that the poly-KVE was successfully encapsulated inside the polyvinyl pyrrolidone, and spreaded in it amorphously. The diameter of the particles was about 200~400nm. The drug load was about 20%,and 48. 1% of the total drug was released within 2hs, so the prodrug particles had a better controll in slow-release.