Abstract

The aim of the present study was to investigate the nanoemulsion system for enhanced percutaneous penetration of domperidone. Pseudoternary phase diagrams were constructed in order to optimize the surfactant, cosurfactant and surfactant: cosurfactant weight ratios (Smix). Nine nanoemulsion formulations were selected, characterized and their ex-vivo permeation studies using rat skin were performed. The nanoemulsion formulations had small droplet size ( < 90 nm), uniform size distribution (PI, < 0.2) and low viscosity ( < 160 mP). The results demonstrated that the droplet size and viscosity of nanoemulsion decreased following decrease in the concentration of polysorbate 20, whereas transdermal flux was increased. The optimized formulation NE-B1, which contained oleic acid (4 % w/w), polysorbate 20 (10 % w/w), diethylene glycol monoethyl ether (20 % w/w) and water (64 % w/w) showed significant increase (P < 0.01) in the transdermal flux (169.32 ± 8.33 μg.h-1cm-2). The in vivo studies revealed a 3.5 fold increase in relative bioavailability through transdermal application of NE-B1 formulation compared to oral drug suspension. Moreover, the effective drug plasma concentration was maintained for 16 hour after the transdermal application indicated that the developed nanoemulsion systems could be a promising carrier for the transdermal delivery of domperidone for prolonged period.

Keywords: Nanoemulsions, transdermal delivery, pseudo ternary phase diagrams, domperidone, steady state flux, oleic acid