Key Laboratory of Green Chemistry & Technology, Ministry of Education, College of Chemistry, Sichuan University, Chengdu 610064, PR China.
Biomacromolecules. 2010 Dec 13;11(12):3290-3. doi: 10.1021/bm100712k. Epub 2010 Nov 5.
Enzyme-catalyzed polycondensation for the synthesis of polyester prodrugs of ketoprofen was reported. Lipase acrylic resin from Candida antarctica (CAL-B) was used to synthesize the linear polyesters with pendent ketoprofen groups based on ketoprofen glycerol ester, poly(ethylene glycol), and divinyl sebacate. The products were characterized by GPC and (1)H NMR. The results indicated that the molecular weight and yields of the polyesters depend on experimental conditions such as temperature and feed ratio. The in vitro study showed that the drug release from the polyester was slow under physiological conditions, which indicated that the polyester could be a promising prodrug with extended pharmacological effects by delayed release of ketoprofen.
报道了一种酶催化缩聚反应，用于合成酮洛芬的聚酯前药。使用南极假丝酵母脂肪酶（CAL-B），基于酮洛芬甘油酯、聚乙二醇和癸二酸二乙烯酯，合成带有酮洛芬侧基的线性聚酯。通过 GPC 和 1H NMR 对产物进行了表征。结果表明，聚酯的分子量和产率取决于实验条件，如温度和进料比。体外研究表明，聚酯在生理条件下药物释放缓慢，这表明聚酯可以作为一种有前途的前药，通过延迟释放酮洛芬来延长其药理作用。
