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Review
. 2014 Dec 28:196:96-105.
doi: 10.1016/j.jconrel.2014.09.027. Epub 2014 Oct 12.

Bioavailability of capsaicin and its implications for drug delivery

William D Rollyson  1 , Cody A Stover  1 , Kathleen C Brown  1 , Haley E Perry  1 , Cathryn D Stevenson  1 , Christopher A McNees  1 , John G Ball  1 , Monica A Valentovic  1 , Piyali Dasgupta  2
Affiliations
Review

Bioavailability of capsaicin and its implications for drug delivery

William D Rollyson et al. J Control Release. .

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.

Keywords: Bioavailability; Capsaicin; Drug carriers; Metabolites.

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Conflict of interest statement

The authors declare that they have no conflict of interest.

Figures

Fig. 1
Fig. 1
Structure of capsaicin and capsaicinoids.
Fig. 2
Fig. 2
A schematic diagram showing the metabolites of capsaicin in rodent and human liver.
Fig. 3
Fig. 3
A schematic diagram showing the metabolites of capsaicin in human skin.
Fig. 4
Fig. 4
(A) A flow-chart representing the experiment involving the bioavailability of capsaicin in nude mouse (B). A table summarizing the tissue distribution of orally administered capsaicin in nude mouse.
See this image and copyright information in PMC

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