title: Bioavailability of capsaicin and its implications for drug delivery.
abstract: The dietary compound capsaicin is responsible for the "hot and spicy" taste of chili peppers and pepper extracts. It is a valuable pharmacological agent with several therapeutic applications in controlling pain and inflammation. Emerging studies show that it displays potent anti-tumor activity in several human cancers. On a more basic research level, capsaicin has been used as a ligand to activate several types of ion-channel receptors. The pharmacological activity of capsaicin-like compounds is dependent on several factors like the dose, the route of administration and most importantly on its concentration at target tissues. The present review describes the current knowledge involving the metabolism and bioavailability of capsaicinoids in rodents and humans. Novel drug delivery strategies used to improve the bioavailability and therapeutic index of capsaicin are discussed in detail. The generation of novel capsaicin-mimetics and improved drug delivery methods will foster the hope of innovative applications of capsaicin in human disease.
authors.affiliation: Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA.
authors.forename: William D
authors.initials: WD
authors.lastname: Rollyson
authors.affiliation: Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA.
authors.forename: Cody A
authors.initials: CA
authors.lastname: Stover
authors.affiliation: Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA.
authors.forename: Kathleen C
authors.initials: KC
authors.lastname: Brown
authors.affiliation: Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA.
authors.forename: Haley E
authors.initials: HE
authors.lastname: Perry
authors.affiliation: Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA.
authors.forename: Cathryn D
authors.initials: CD
authors.lastname: Stevenson
authors.affiliation: Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA.
authors.forename: Christopher A
authors.initials: CA
authors.lastname: McNees
authors.affiliation: Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA.
authors.forename: John G
authors.initials: JG
authors.lastname: Ball
authors.affiliation: Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA.
authors.forename: Monica A
authors.initials: MA
authors.lastname: Valentovic
authors.affiliation: Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA. Electronic address: dasgupta@marshall.edu.
authors.forename: Piyali
authors.initials: P
authors.lastname: Dasgupta
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000494:pharmacology; D001682:Biological Availability; D001711:Biotransformation; D002211:Capsaicin / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000494:pharmacology; D016503:Drug Delivery Systems; D006801:Humans
chemical_list: D000893:Anti-Inflammatory Agents; D002211:Capsaicin
keywords: Bioavailability; Capsaicin; Drug carriers; Metabolites