The Caco-2 cell monolayer: usefulness and limitations.
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.


CONCLUSIONS
The catenary model extends the usefulness of Caco-2 monolayer and provides proper mechanistic insight and data interpretation.
Sun
Huadong
H
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.
Chow
Edwin Cy
EC
Liu
Shanjun
S
Du
Yimin
Y
Pang
K Sandy
KS
D001692:Biological Transport; D018938:Caco-2 Cells; D006801:Humans; D008954:Models, Biological; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D010599:Pharmacokinetics
D004364:Pharmaceutical Preparations