Exploring Micellar Systems for Intra-Articular Delivery of Vanillic Acid in Management of Osteoarthritis.

Abstract

The current research investigates a new therapeutic strategy for the management of knee osteoarthritis (KOA). For this purpose, we developed mixed polymeric micelles (MPM) encapsulating a natural phytotherapeutic drug, vanillic acid (VA), for intra-articular (IA) delivery. The developed systems were characterized by their particle size profile, zeta potential, morphology, physical stability, and in vitro drug release. Cremophor was found to be an essential component for the production of MPM with optimum particle size profile, as well as maintaining an F127/Cremophor/TPGS weight ratio of 3:2:1. Coating the optimized formulation with hyaluronic acid (HA) provided a dual benefit of sustaining VA release and providing synergistic anti-osteoarthritic activity in an monosodiumiodoacetate-induced KOA model in rats. The proposed HA-coated MPM system encapsulating VA provides a promising strategy for the inhibition of KOA progression.