DEVELOPMENT AND EVALUATION OF NANOEMULSION FORMULATIONS FOR IMPROVED ORAL DELIVERY OF CARVEDILOL

Abstract

The aim of the presentinvestigation was to develop, optimize and evaluate nanoemulsion system of carvedilol to improve its solubility, and oral bioavailability. Carvedilol is a non-selective beta blocker used in the treatment of mild to moderate congestive heart failure and mild to moderate essential hypertension. It has both poor water solubility (0.583 mg/L) and oral bioavailability (23%) because of significant first-pass hepatic metabolism. Based on solubility testing, clove oil was used as oil, tween 20 was used as surfactants and PEG 400 was used as cosurfactants in construction of phase diagrams. Carvedilol nanoemulsions were prepared by aqueous phase titration method. Out of twelve formulations, eight thermodynamically stable formulations were selected for preparation of carvedilol loaded nanoemulsions and these nanoemulsions were subjected forcharacterization i.e. particle size, viscosity, polydispersity, zeta potential. A 12 hrs in-vitro release release study was performed on selected nanoemulsion formulations of carvedilol. Study concludes, nanoemulsion formulation of batch NEC4 (S mix Ratio 1:3) was found to be optimum formulation.