Advances in Drug Delivery Science for Diacerein: Strategies to Enhance Solubility, Bioavailability, and Pharmacokinetic Performance

Diacerein is known as a disease-modifying anti-inflammatory drug, primarily used for the treatment of osteoarthritis. Despite its therapeutic potential, the clinical use of diacerein is hindered by poor aqueous solubility, low bioavailability, liver issues, and gastrointestinal side effects, particularly diarrhea. To address these limitations, various innovative pharmaceutical formulation approaches have been explored, including physical modifications, chemical complexation, nanotechnology-based drug delivery systems, and synergistic combination therapies. This review highlights progress in formulation approaches aimed at enhancing the solubility and therapeutic profile of diacerein. Special emphasis is placed on lipid-based carriers, vesicular systems, pH-responsive hydrogels, and dissolving microneedles. Together, these strategies provide a comprehensive platform for the rational design of diacerein formulations, offering promising avenues to overcome its clinical limitations and improve patient outcomes. The insights presented here may also guide the development of more effective delivery systems for other poorly soluble anti-inflammatory agents.