Development and Characterization of Flutamide Containing Self-microemulsifying Drug Delivery System (smedds)

The present work was aimed at formulating a SMEDDS (Self-microemulsifying drug delivery system) for oral drug delivery system containing flutamide. The solubility of flutamide was determined in various vehicles. Pseudo ternary phase diagram was constructed to identify the micro emulsification existence area. SMEDDS formulations were tested for microemulsifying properties, and the resultant formulations loaded with flutamide (ME1, ME2, ME3, ME4 & ME5) were investigated for clarity, phase separation, globule size and shape, zeta potential, effect of various diluents and dilutions, thermodynamic and thermal stability. From the results it is concluded that increase in droplet size is proportional to the concentration of oil in SMEDDS formulation. The optimized formulation’s study was composed of Caproyl PGMC (50%), Cremophore RH 40 (37.5%) and PEG-300 (12.5%). Minor difference in the droplet size and zeta potential was observed by varying the diluents (deionized water and 0.1N HCl) and dilutions (1:10, 1:50 and 1:100). Formulations, which were found to be thermodynamically stable (ME1, ME2, ME3 & ME4), were subjected to stability studies as per International Conference on Harmonization (ICH) guidelines. No significant variations were observed in the formulations over a period of three months at accelerated and long-term conditions. TEM photographs of microemulsions formulations further conformed the spherical shape of globules. Among the various SMEDDS formulations, ME4 offer the advantages of good clarity systems at high oil content and thus offer good solubilization of flutamide. Thus this study illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as flutamide by oral route.