New formulation for management of pain and inflammation related disorders: development, characterization and pharmacological evaluation

Amit Bhatia, Bhupinder Singh, O P Katare
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India

Non-steroidal anti-inflammatory drugs (NSAIDs) are the “Gold Standards” in the treatment of various pain and inflammation related disorders like arthritis. However, oral administration and newer selective COX-2 NSAIDs are known to induce severe intolerance. Thus, the present work aims to develop and evaluate a novel carrier for targeted epicutaneous delivery of a potent NSAID, diclofenac. Flexible-Vesicles (FVs) are new generation liposomes designed to deliver drug to deep-seated inflamed and painful locations through topical route. Various formulations with different compositions were prepared and characterized to select the best formulation. The selected vesicular system was characterized and evaluated for ex-vivo drug permeation and drug deposition employing suitable membranes. The biological activity of final optimized formulation was evaluated using the carrageenan induced rat paw edema model with simultaneous radiographic analysis. FVs selected were found have best desired characteristics among all the prepared FVs. The ex-vivo permeation and skin-deposition of the diclofenac loaded FVs were found to be higher compared to other tested formulations. The in-vivo pharmacodynamic result was found to be in agreement with the ex-vivo findings as FVs have shown faster onset and prolonged anti-inflammatory effect, while radiographic analysis ratifies the above result. The results of present study demonstrated superior efficacy and safety of topically applied FVs loaded formulation. Hence, it can be concluded that diclofenac containing FVs can be a very good proposition for management of pain and inflammation related disorders