capsaicin palmitate

Capsaicin palmitate is a synthetic ester formed from capsaicin and palmitic acid. It is designed as a topical analgesic for the relief of pain, particularly osteoarthritic and neuropathic pain, in a formulation that aims to reduce the burning sensation typically associated with standard capsaicin products. Upon topical administration, capsaicin palmitate is absorbed into the skin and enzymatically hydrolyzed to release free capsaicin. The released capsaicin acts primarily by activating the transient receptor potential vanilloid 1 (TRPV1) receptor—a nonselective cation channel highly permeable to calcium—on nociceptive nerve fibers. This activation leads to an initial excitation followed by desensitization or "defunctionalization" of these sensory neurons, resulting in reduced transmission of pain signals. Capsaicin also depletes substance P from sensory nerve endings and can block synaptic transmission in the spinal cord dorsal horn[5]. Capsaicin palmitate has been considered for compounding into creams or gels at concentrations delivering 1.5%–3% free capsaicin[5].

Other names

hexadecanoic acid, 2-methoxy-4-(2-propenyl)phenyl estercapsaicin palmitate