Gelatin-methotrexate conjugate microspheres as a potential drug delivery system.

Gelatin-methotrexate microspheres for intra-tumor administration have possibilities for minimizing systemic toxicities of methotrexate (MTX) and overcoming its resistance. Gelatin-MTX conjugates prepared by a carbodiimide reaction were crosslinked with glutaraldehyde to form microspheres (MTX:gelatin molar ratios of 2:1, 15:1, and 21:1). Microspheres were evaluated under in vitro tumor conditions at pH 6.

Growth inhibition, drug load, and degradation studies of gelatin/methotrexate conjugates.

Macromolecular gelatin-methotrexate conjugates have potential therapeutic advantages over the free drug. Conjugates with MTX:gelatin molar ratios (MR) ranging from 1:1 to 27:1 were examined for cell growth inhibition, stability, degradation, and methotrexate (MTX) release. Conjugate growth inhibition was less than that of free MTX whose IC(50) value of 1.