Abstract
AbstractN‐(2‐hydroxypropyl)methacrylamide (HPMA) copolymers (11a, b) containing side chains terminating in 5‐aminosalicylic acid (5‐ASA) and fucosylamine (10) were synthesized. A reactive polymeric precursor (9), a copolymer of HPMA (7) and N‐methacryloylglycylglycine p‐nitrophenyl ester (8), was consecutively aminolyzed with 5‐[4‐(2‐aminoethylcarbamoyl)phenylazo]‐salicylic acid (6) and fucosylamine (10). The latter renders the copolymers bioadhesive in the gastrointestinal tract. The release of 5‐ASA from 11a, b was studied in vitro by incubation with cell‐free extracts isolated from rat cecum, and factors influencing the degradation were determined. The rate of azo bond cleavage of 11a, b was similar to the rate of cleavage of low‐molecular‐weight substrates, methyl orange and compound 6. Addition of benzyl viologen, a low potential electron carrier, increased the rate of cleavage. At optimal benzyl viologen and substrate concentration ratios, a zero order release was observed. At higher substrate concentration, the rate of 5‐ASA release decreased.
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