Acta Pharm. 55 (2005) 169-176[ Full paper in PDF ]
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%.
Keywords: fenoprofen, gemfibrozil, polymer-drug conjugate, macromolecular prodrug, styrene-maleic acid anhydride copolymer