Abstract

The anticancer drug methotrexate (MTX) was covalently linked to gelatin using carbodiimide as the coupling agent. The resulting gelatin-methotrexate conjugate (GMC) was separated by gel filtration and characterised by UV and IR spectroscopy. The drug content of the conjugate was 200 μg MTX/mg gelatin. The GMC was used to prepare biodegradable hydrophilic gelatin microspheres (GMCM) of different mean particle sizes (1–5, 5–10 and 15–20 μm). The in vitro release of MTX from GMCM was investigated in simulated gastric and intestinal fluids. GMCM released MTX in a zero-order manner for 7–9 days in gastric medium and for 8–10 days in intestinal medium. The release data also indicated that the rate of release of MTX decreased with increase in particle size of GMCM. Release of MTX was faster in gastric medium when compared to intestinal medium.

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