Sinteza konjugata fenoprofena i gemfibrozila s kopolimerom stirena i maleinske kiseline

Two types of polymer-drug conjugates were synthesized starting from styrene-maleic acid anhydride copolymer (SMA). Fenoprofen and gemfibrozil were chosen as model drugs because of their short plasma half lives. Both drugs were first converted to their 2-aminoethylamides, which possess free amino groups capable of reacting with SMA anhydride rings. By modifying the degree and type of substitution, lipophilic and hydrophilic conjugates were obtained. Drug loading in the conjugates was between 17 and 47%.U radu je opisana sinteza polimer-lijek konjugata polazeći od kopolimera stirena i anhidrida maleinske kiseline (SMA) i fenoprofena, odnosno gemfibrozila, ljekovitih tvari s kratkim vremenom zadržavanja u plazmi. Fenoprofen i gemfibrozil su prvo prevedeni u 2-aminoetilamide, koji su zbog slobodne amino skupine mogli reagirati s anhidridnim prstenovima u SMA. Modifikacijom tipa i vrste supstitucije pripravljeni su lipofilni i hidrofilni konjugati. Udio vezanog lijeka u konjugatima bio je između 17 and 47%