Development and evaluation of diacerein and aceclofenac loaded topical nanoemulgel for osteoarthritis an experimental study

Abstract

ABSTRACT Background Osteoarthritis (OA) affects millions globally, causing chronic pain and disability. Current oral therapies, like nonsteroidal anti-inflammatory drugs and cyclooxygenase-2 enzyme inhibitors, have limited effectiveness and significant side effects. Nowadays, the focus of OA treatment has shifted towards modifying and slowing disease progression along with symptomatic management. Diacerein (DCN) and aceclofenac (ACE), frequently prescribed for OA treatment due to their disease-modifying and analgesic properties, are available in fixed-dose combination tablets (DCN 50 mg/ACE 100 mg) for OA and rheumatoid arthritis. However, the chronic oral delivery of DCN and ACE remains challenging due to their poor aqueous solubility, low bioavailability (BA), and undesirable side effects, which collectively cause patient noncompliance and decreased adherence to their oral regimens. Hence, it is essential to develop a new formulation that can increase the rate and extent of DCN and ACE absorption, resulting in enhanced BA and a significant reduction in side effects. Since poor BA and side effects may occur due to oral administration, novel, non-oral DCN and ACE formulations have been proposed to overcome these problems. Objectives The objectives of the study are: (i) To develop, optimize, and evaluate diacerein- and aceclofenac-loaded topical nanoemulgel for osteoarthritis. (ii) To study the effect of diacerein and aceclofenac-loaded nanoemulgel as anti-inflammatory and anti-osteoarthritis by topical route.