Development and Characterization of A Nanoemulsion Gel formulation for Transdermal delivery of Carvedilol

The aim of the present study was to develop nanoemulsion formulation for transdermal delivery of carvedilol to enhance the water solubility as well as bioavailability of drug. O/W nanoemulsions were prepared by the spontaneous emulsification method. Pseudoternary phase diagrams were constructed to obtain the nanoemulsion region. Oleic acid and IPM (3:1) was chosen as the oil phase, Tween 20 and carbitol were used as surfactant and cosurfactant respectively, on the basis of solubility studies, in formulation of nanoemulsion. Parameters evaluated included: thermodynamic stability testing, droplet size and in vitro mice skin permeation ware performed. Significant difference in the steady state flux (Jss), permeability coefficient (Kp) and enhancement ratio (Er) was observed in nanoemulsion formulations and control (P*** < 0.001). The composition of optimized formulation NEB1 which shows highest value of flux 211.8123 μg cm-2h-1 at the 24 h. Post application plasma carvedilol was increased 6.41 fold to marketed dosage form. The study suggested that nanoemulsion significantly enhanced bioavailability of transdermally applied carvedilol and eliminated the first pass metabolism.

Author(s): Singh Bhuwanesh Pratap, Kumar Brajesh, Jain S.K, Shafaat Kausar

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