Provided are nutraceutical or dietary supplemental compositions comprising esterified capsaicinoids. The esterified capsaicinoids may converted to the active parent capsaicinoid compound following enzymatic or chemical hydrolysis. In various embodiments, these esterified capsaicinoids have a higher lipophilicity, lipid solubility and result in less irritation to the stomach than the parent capsaicinoid, and hence may be included in certain dietary supplement formulations, including capsules, pills and tablets dietary supplement formulations. The dietary supplement compositions may be used for pain management in mammals in vivo and/or in the treatment of various pathological conditions in humans.