Novel pH-sensitive Carriers Containing Naproxen Pendant Groups for Colon-Specific Drug Delivery

摘要

The carboxyl group of naproxen was converted into a vinyl ester group by reacting naproxen with vinyl acetate in the presence of mercuric acetate as a catalyst. Cubane-1, 4-dicarboxylic acid (CDA) was covalently linked with 2-hydroxyethyl methacrylate (HEMA) as the crosslinking agent (CA). Methacrylic-type polymeric prodrugs were synthesized by free radical copolymerization of methacrylic acid, vinyl ester derivative of naproxen (VIN) and polyethylene glycol monomethacrylate (PEGMA) in the presence of a cubane crosslinking agent. In vitro release profiles were established separately in enzyme-free simulated gastric and intestinal fluids (SGF, pH 1 and SIF, pH 7.4).