Formulation and Evaluation of Microsponges-loaded Transdermal Gel for the Management of Osteoarthritis.

Abstract

Background: Osteoarthritis (OA) stands as the most widespread form of arthritis, representing a primary source of pain and functional impairment among the elderly. It is often referred to as a degenerative joint disease. OA is more than just wear and tear; it is an aberrant remodelling of joint tissues prompted by a deluge of inflammatory mediators released within the compromised joint. This disease affects 15 million people in India annually.

Objective: Aceclofenac is a COX-2 inhibitor that has anti-inflammatory activity. However, aceclofenac has a short mean plasma elimination half-life and poor water solubility. It requires frequent dosing, which has been linked to a number of negative side effects, including bleeding and gastrointestinal irritation. A potential solution to this problem is the transdermal administration of aceclofenac using microsponges. In order to have a synergistic effect along with the bioenhancer effects, piperine was incorporated into the formulation.

Methods: Microsponges were created using the quasi-emulsion solvent diffusion method. After characterization, the prepared microsponges were incorporated into the Carbopol gel. The in vivo study focused on evaluating the optimized formulation, F1.

Results: All the prepared microsponge formulations underwent assessment based on parameters including yield of production, entrapment efficiency, and in vitro drug release. The outcomes indicated that batches ranging from F1 to F9 showed positive entrapment efficiency and in vitro drug release. From 50.37% to 80.76 % and 71.18% to 91.8% and in vivo studies the results reveal that the inflammatory cells in the best formulation Ace(B) group were reduced hence the formulation's anti-inflammatory impact was achieved.

Conclusion: The findings indicate that Formulation F1 exhibits superior entrapment and enhanced drug release. The kinetics study suggests that the optimized formulation aligns well with the Higuchi model and adheres to the Fickian transport drug release mechanism. Animal study findings suggest that optimized formulation Ace(B) may possess ideal -anti-osteoarthritic activity for osteoarthritic disease. Further clinical trials on humans may be conducted in order to make the research fruitful for society.