The two faces of capsiate: Nutraceutical and therapeutic potential. (April 2021) - Gupta, Reena
Abstract: Background: Capsiate is a non-pungent analogue of capsaicin. Consumed worldwide, capsiate hitherto remains unexplored despite its proven track record as a food ingredient and recent use for its therapeutic profile. Though possessing a much better safety profile and an equivalent therapeutic potential, the molecule has not been extensively explored in scientific research pertaining to either food or therapeutic sciences. Scope and approach: This comprehensive review summarizes the studies demonstrating the therapeutic potential of capsiate in various pathological conditions. The mechanistic pathways for these pharmacological activities are also deliberated upon. Discussed also are various patents that have been filed for various innovative uses of capsiate. Key findings and conclusions: The molecule has been successfully explored in treatment of obesity, metabolic disorders, cancer, cardiovascular disorders and gastro-intestinal disorders. It, however, faces the challenge of low aqueous solubility and stability. The lack of popularity of this immensely useful therapeutic nutraceutical probably accrues from these two factors. Designing an effective dosage form with complete absence of water is a challenge in itself. The capsules available in the market for its anti-obesity effect are also oily in nature. The challenge further intensifies when topical delivery across the mucous membrane of skin is targeted. The approaches that may be used for exploration of this drug in conditions like weight management, cancer, pain, diabetes, dysphagia, skin diseases and muscle atrophy include solid lipid nanoparticles, polymer nanoparticles, dendrimers, non-aqueous nanoemulsions and even liquid/solid self-nanoemulsifying drug delivery systems that may be reconstituted at the time of injection. Highlights: Conventional and modern methods for isolation of capsiate. Chemical and enzymatic strategies for synthesis of capsiate. Therapeutic benefits of capsiate due to activation of TRPV1 receptors. Patents on the isolation, formulation development and pharmacological actions of capsiate.