Dextran carrier macromolecules for colon-specific delivery of 5-aminosalicylic acid

Abstract

Present manuscript describes the sustained and targeted delivery of 5-aminosalicylic acid to the distal ileum and proximal colon, using dextran (40 kDa) as a carrier for targeting 5-aminosalicylic acid at the colonic site by attaching p-aminobenzoic acid and benzoic acid as linkers. Prepared conjugate were characterized by UV, HPLC, FT-IR, and 1 H NMR. The degree of substitution was estimated by complete hydrolysis of conjugates in borate buffer and in vitro hydrolysis study of conjugates was performed in different biological media. It was observed that 5-aminosalicylic acid alone have produced high incidence of gastric ulcer with high ulcer index whereas lower ulcer index was found for the dextran conjugates of 5-aminosalicylic acid. The release pattern of conjugates in 3% w/v rat caecal content was confirmed the colon specificity of 5-aminosalicylic acid conjugates.