Formulation and Evaluations of Methotrexate Loaded Multiparticulate System for Colon Targeting: In vitro and Surface Morphology

Abstract

Present study was investigated to prepare and evaluate multiparticulate system based microspheres of methotrexate (MTX) for the purpose of targeting to colonic region, reduce dosing frequency and improve patient compliances. In the present study we have used emulsifying agent and polymer (Eudragit S100) by solvent evaporation method, Polymer concentration and steering speed was used to formulate the microspheres by emulsion solvent evaporation technique. The particle size, shape, and surface morphology were investigated for prepared formulation. Further the percentage yield, DSC, XRD and in vitro drug release behavior were studied. The findings of particle size, surface morphology, entrapment efficiency and %yield of prepared microsphere were appreciable. The release study was done in simulated gastrointestinal fluids for 2 hrs in SGF (pH 1.2), for 3 hrs in SIF (pH 6.8) and up to 14 hrs in SCF (pH 7.4) and have shown that the drug was protected from being released in the physiological environment of the stomach and small intestine and efficiently released in colon. Among all the formulations it was observed that R2 value of formulation SS 3b was more near to one than other formulations. On the basis of this parameter, SS 3b was selected for further study. It is concluded from the present study that pH sensitive Eudragit microspheres are promising carriers for oral colon-targeted delivery of MTX for treatment of colorectal cancer.