Formulation and In-Vivo Evaluation of Aceclofenac and Quercetin Nanoemulsion-Based Gel Against Rheumatoid Arthritis

Rheumatoid arthritis (RA) is a chronic inflammatory, T cell-mediated autoimmune disorder which commonly affects the tiny joints of the hands and feet.

To develop and evaluate novel topical gel containing combinatorial aceclofenac (ACF) and quercetin (QCT) nanoemulsion (NE) for management of RA.

NE components (oil, surfactant, and cosurfactant) were selected based on solubility. Pseudo ternary phase diagrams were constructed using titration method. Carbopol bases were screened to produce NE-gel. Drug loaded NE-gels were characterized for transmission electron microscopy and in-vitro drug release. Further evaluated for ex-vivo drug release, retention-permeation studies, in-vivo studies using Wistar rat model.

Optimized NE showed approximate globule size 79nm, zeta potential of -28.1 ± 1.20 mV and polydispersity index 0.22. The NE-gel showed in-vitro drug release of ACF=75.56 ± 0.318% and QCT=74.72 ± 0.715% after 12h, depicting sustained zero order release kinetics in contrast to marketed gel (release of ACF=95.33 ± 0.449% after 9h). Ex-vivo study on porcine ear skin revealed improved permeation and minimum retention. In-vivo studies showed 50.89% reduction in paw volume (p<0.0001) with better anti-arthritic effects.  .

The study substantiated combinatorial NE-gel formulation with advanced permeation characteristics which can be an efficient alternative for topical delivery in RA.