Quality by Design (QbD) Approach for Optimization of Microemulsion based Topical Gel

Abstract

This study aimed 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 LabrafacLipophile 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 3 2 factorial design. Dynamic light scattering showed that this formulation had a well defined spherical shape and uniform size ( 90 nm) with narrow polydispersity index (0.234) and a zeta potential -7.02 mV. The drug release from the optimized batch containing 1:9 oil to surfactant/co-surfactant ratio and 1.015 %w/w Carbopol 940 was found to be 73.85±2.07% at 180 min. The results revealed that the developed microemulsion gel has great potential for topical delivery of Aceclofenac.