Abstract
The anticancer drug methotrexate (MTX) was covalently linked to gelatin by the azide coupling-grafting method. Two gelatin-MTX conjugates were prepared by coupling (i) MTX azide to gelatin (GMC-I) and gelatin azide to MTX (GMC-II). The resulting conjugates were separated by gel filtration and characterised by UV and IR spectroscopy. The drug content of GMC-I and GMC-II was 205 μg MTX/mg gelatin and 203 μg MTX/mg gelatin respectively. GMC-I and GMC-II were used to prepare biodegradable hydrophilic gelatin microspheres (GMCM-I and GMCM-II) of different mean particle sizes (1–5, 5–10, 15–20 μm). The in vitro release of MTX from GMCM-1 and GMCM-II was investigated in simulated intestinal fluid. GMCM-I released MTX in zero order manner for 9–11 days in intestinal medium and GMCM-II released MTX in a zero order manner for 7–10 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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