Фармацевтика Аналитика Акта

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Formulation Design of Indomethacin-Loaded Nanoemulsion For Transdermal Delivery

Nahla Barakat, Ehab Fouad and Azza Elmedany

The aim of the present study was to investigate the potential of nanoemulsion formulations for transdermal delivery of indomethacin (IND). Nanoemulsions formulations with different Surfactant: co surfactant ratios (S mix); F1-F6 (1:1, 2:2, 3:1, 4:1, 1:2 and 3:2) were prepared by the spontaneous emulsification method, and characterized for morphology using transmission electron microscopy (TEM), droplet size, and rheological characteristics. The ex vivo skin permeation studies were performed using Franz diffusion cell with rabbit skin as permeation membrane. A significant increase in the permeability parameters such as steady-state flux (Jss), permeability coefficient (Kp), and enhancement ratio (Er) was observed in nanoemulsion formulations compared with the conventional IND gel. The anti-inflammatory effects of nanoemulsion formulations showed a significant increase in percent inhibition value after 4 hours when compared with conventional IND gel on carrageenan-induced paw edema in rats. Significant increase in permeability parameters was observed in nanoemulsion formulations (P< 0.05). The steady-state flux (Jss) and permeability coefficient (Kp) for optimized nanoemulsion formulation (F1, 1:1 S mix were found to be 22.61±3.45 μg/ cm2/h and 0.22x10− 2 ±0.0003 cm/h, respectively), which were significant compared with conventional IND gel and (P< 0.001). Enhancement ratio (Er) was found to be 8.939 in optimized formulation F1 compared with IND gel. These results suggested that nanoemulsions can be used as potential vehicles for improved transdermal delivery of indomethacin as an approach to eliminate the side effect of the oral dose.