Formulation and In Vitro Evaluation of Ethosomes as Vesicular Carrier for Enhanced Topical Delivery of Isotretinoin

Sheba Rani Nakka David, Mah Si Hui, Chong Fui Pin, Foo Yun Ci, Rajan Rajabalaya

Abstract


Purpose: The purpose of the present research was to evaluate the ability of ethosomes for topical delivery of isotretinoin. The ethosomal vesicles were prepared with various concentrations of lecithin and ethanol by using hot method. The ethosomal based isotretinoin gel (GEL-ES) was compared to that of marketed formulations isotretinoin (GEL-MF) by using hydrophobic hydroxyl propyl methyl cellulose as gel base. The physicochemical and stability of ethosomal based isotretinoin and a marketed gel (control) were evaluated for organoleptic properties, drug entrapment, drug content uniformity and in vitro drug release and skin permeation studies. F2 ethosomal vesicles containing 2%w/w lecithin and 30%w/w ethanol was found to have shown the best entrapment percentage (99.21%) and also showed suitable physicochemical characteristics for topical administration. Physical stability studies were also conducted for 45 days at 4°C and 25°C. GEL-ES and GEL-MF were applied to rat skin and penetration was assessed by Franz diffusion cells. In vitro release studies showed that less than 10% of isotretinoin reached the receptor compartment compared to GEL-MF till 8 h. On comparing F2 and F4 gel formulations, F2 gel has shown better controlled release by in vitro drug release and in vitro skin permeation profile than F4 gel. However, the in vitro skin permeation was increased with the addition of enhancers. From the experimental data, it may be concluded that the ethosomal vesicles and enhancers increased the skin permeation and depot formation of drug in the skin.


Keywords


, topical delivery, isotretinoin, N-methyl-2-pyrrolidone, eugenol

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References


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