Integrative Insights into Ursolic Acid: From Physicochemical Properties to Drug Delivery Approaches, Clinical Applications and Patent Landscape

Ursolic acid (UA), a plant-based pentacyclic triterpenoid with diverse pharmacological activities, is used as a nutritional supplement to improve body composition and address metabolic disturbances. Despite its benefits, UA's clinical application is hindered by its poor physicochemical and pharmacokinetic properties. A thorough literature review indicates that while substantial research has been conducted on UA's pharmacological effects, only a limited number of studies (14 out of 3367 articles) had concentrated on improving its solubility and bioavailability. As UA belongs to BCS class IV, it needs a specific delivery approach that can solve both permeability and solubility issues for better clinical performance. This review explores the relationship between physicochemical properties and pharmacokinetics using dimensionless numbers. It also examines the role of supersaturated drug delivery systems in bypassing these limitations and enhancing UA potential. A brief overview of existing patents related to UA is also provided to highlight the current research gap and future opportunities. The findings underscore the necessity for continued research into formulation advancements to fully unlock UA's therapeutic potential. Future investigations should focus on multifunctional delivery systems to enhance solubility, permeability and modify the P-gp efflux for improved pharmacokinetics and pharmacodynamics. This review serves as a foundation for the scientific community to pursue innovative solutions that address existing challenges in delivering UA for its effective clinical application.