Formulation Of Self Micro-emulsifying Drug Delivery System For Ketoconazole

Abstract

The present investigation was undertaken with an objective to prepare the SMEDDS of ketoconazole in order to improve the bioavailability of lipophilic drugs. A ternary phase diagram was constructed in the absence of ketoconazole. The results revealed that span 60 and PEG 600 used in ratios of 2:1 (F17-18) and 3:1 (F23-24) exhibited largest micro-emulsion area and shortest emulsification time (less than 1 min). It was observed that with increase in the ratio of the PEG 600, spontaneity of the self-emulsification process got increased. A fixed ketoconazole concentration of 5% w/w was selected to be loaded in all self-emulsifying formulations. The prepared formulations were kept in closed containers and tested for thermodynamic stability. All the formulations passed the thermodynamic stability studies without any signs of phase separation and precipitation during alternative temperature cycles (4°C and 40°C), freeze thaw cycles (-21°C and +25°C) and centrifugation at 10,000 g indicating good stability of formulations and their emulsions. The in vitro dissolution studies revealed the drug release profiles for the SMEDDS. All the formulations exhibited quick drug release characteristics and almost complete drug release in 15-20 minutes. In contrast, the pure drug exhibited only a maximum of 39.63% release in 60 min duration.