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Expert Opin Drug Metab Toxicol. 2008 Apr;4(4):395-411. doi: 10.1517/17425255.4.4.395 .

The Caco-2 cell monolayer: usefulness and limitations.

Author information

1
University of Toronto, Department of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, Toronto, M5S 3M2, Canada +1 416 978 6164 ; +1 416 978 8511 ; ks.pang@utoronto.ca.

Abstract

BACKGROUND:

The Caco-2 monolayer has been used extensively for the high-throughput screening of drug permeability and identification of substrates, inhibitors, and inducers of intestinal transporters, especially P-glycoprotein (P-gp). Traditionally, the Caco-2 monolayer is viewed as a single barrier rather than a polarized cell monolayer consisting of metabolic enzymes that are sandwiched between two membrane barriers with distinctly different transporters.

OBJECTIVE:

This review addressed the usefulness and limitations of the Caco-2 cell monolayer in drug discovery and mechanistic studies.

METHODS:

This mini-review covered applications of the Caco-2 monolayer, clarified misconceptions, and critically addressed issues on data interpretation.

CONCLUSION:

The catenary model extends the usefulness of Caco-2 monolayer and provides proper mechanistic insight and data interpretation.

PMID:
18433344
DOI:
10.1517/17425255.4.4.395
[Indexed for MEDLINE]

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