Abstract:

The objective of the study was to develop a microemulsion based topical gel formulation of Aceclofenac, an oral NSAID with known major complications like dyspepsia, ulcer and bleeding. Topical route overcomes the above complications and provides the additional advantage of site specific delivery. Aceclofenac being BCS class II drug pose the formulation problem because of lower aqueous solubility. Thus development of microemulsion based gel will be of greater benefit as oil phase will aid in drug solubilisation and its smaller size will facilitate higher permeation. The components of the formulation include Labrafac Lipophile WL1349, Cremophor EL and Transcutol P as oil phase, surfactant and cosurfactant, respectively. The effect of oil to surfactant/co-surfactant ratio and carbopol 940 on drug release and viscosity profile of the formulation was studied by 32 factorial design. Dynamic light scattering demonstrate a well defined spherical shape and uniform size (̴90 nm) with narrow poly-dispersity index (0.234) and a zeta potential -7.02 mV. The in vitro drug release from the optimized batch containing oil to surfactant/co-surfactant ratio (1:9) and 1.015 %w/w Carbopol 940 was found to be 73.85±2.07% at 180 min. The in-vitro drug release profile of the optimized formulation was compared with marketed product showing greater drug release with similarity factor (f2) of 34.486 %. The results revealed that the developed microemulsion gel has great potential for topical delivery of Aceclofenac.

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