Preparation and characterization of microparticulate systems for oral delivery of genistein
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Genistein, a potential anticancer agent was chosen as a model for poorly water-soluble drugs with low oral bioavailability. The study is based on the hypothesis that encapsulation of genistein in water soluble polymers (e.g. Polyethylene glycol) will enhance its dissolution rate. The objective of the study was to prepare, characterize, and optimize the fast release formulations- microspheres and simple dispersions. In order to achieve this goal, solid dispersions were prepared using two different techniques; solution-solvent evaporation and emulsion-solvent evaporation. Various process parameters such as ratio of drug/polymer, ratio of solvents, and speed of homogenization have been studied. A Box-Behnken experimental design was used for the preparations of simple dispersions by solution-solvent method. The formulations were compared in order to elucidate the effect of preparation methodology. Dissolution studies were performed on the formulations. Further, the solid dispersion systems were characterized using various techniques such as Differential Scanning Calorimetry, ATR-FTIR spectroscopy, in vitro dissolution, and Scanning Electron Microscopy in order to understand the physicochemical properties of the formulations. Dissolution studies showed an increase in the dissolution rate of genistein formulated as dispersion or microspheres as compared to genistein alone. Approximately, up to 5-fold enhancement in the dissolution of genistein could be achieved with the solution based formulation while up to 10-fold enhancement was observed in case of the emulsion based formulation.