Development and Characterization of Apremilast Transethosomal Gel for Transdermal Delivery

Abstract

The apremilast is anti-inflammatory drug and PDE-4 inhibitor, used in treatment of psoriasis. The oral route of apremilast has limitation of GI irritation and frequent dosage regimen.The objective of the present work was aimed to prepare transethosomal gel of apremilast to achieve more skin permeation, more drug entrapment efficiency and sustained release. The transethosome vesicle containing apremilast was prepared by using Rotary vacuum evaporator, followed by probe sonication. The Box-Behnken design was used to optimize the formulation by taking quantity of lipoid        S 100, sodium cholate and ethanol as independent variable and vesicle size, entrapment efficiency and cumulative drug release as dependent variable. The optimized batch of transethosome vesicle was incorporated in 1 % of Carbopol gel base. The prepared optimized batch was evaluated for size, zeta potential, surface morphology, pH, viscosity, spreadability, extrudability, drug content and ex-vivo permeation studies. The result showed that optimized batch of transethosome was found to have vesicle size of 130.8 nm, entrapment efficiency of 62.83 % and cumulative drug release of gel 73.13 %. The transethosome vesicles were found to be spherical and uniform in size based on TEM analysis. The ex-vivo permeation studies were performed for 24 hrs through the rat skin. The formulation was found to show better skin permeation and sustained release. The formulation showed satisfactory result with respect to pH, gel characteristics and stability. Thus, can concluded that transethosomal gel containing apremilast could be an effective option for treatment of psoriasis.