Design and Evaluation of Topical Hydrogel Formulation of Aceclofenac for Improved Therapy

Abstract

Aceclofenac, a non-steroidal anti-inflammatory drug has been used in the treatment of rheumatoid arthritis and osteoarthritis. In order to decrease the gastric ulcerogenic effects, aceclofenac hydrogel have been developed. Topical gel preparations are intended for skin application or to certain mucosal surfaces for local action or transdermal penetration of medicament or for their emollient or protective action. Topical delivery of drugs can be achieved by incorporating drug into the gel matrix for effective delivery of drugs, thus avoiding first pass metabolism and for increased local action in pain management and skin diseases. NSAID’s are non-steroidal drugs having excellent anti-inflammatory and analgesic activity but NSAID’s produces GIT ulceration, liver and kidney trouble especially in case of oral administration. In view of adverse drug reaction associated with oral formulations, many NSAID’s are increasingly administered by topical route. Hydrophilic polymers like Guar gum and Carbopol 940 of varying concentrations were used in an attempt to develop topical hydrogel formulations of aceclofenac. Evaluation tests for visual appearance, pH, viscosity, spreadability, assay, in vitro drug release were carried out. In vitro diffusion study was carried out in a Franz diffusion cell using cellophane membrane. No prominent changes in physicochemical properties of formulation were observed after exposure to accelerated conditions of temperature (40 ± 2^oC) and humidity conditions (75 ± 5%RH). The gel formulation consisting of 1% w/v Guar gum 1% w/v Carbopol 940 at 1:1 ratio was found to be suitable for topical application based on in vitro evaluation. These results suggest the feasibility of the topical gel formulation of aceclofenac.

Keywords: Aceclofenac, Guar gum, Carbopol 940, Topical hydrogel, Franz diffusion cell