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Critical Reviews™ in Therapeutic Drug Carrier Systems
IF: 2.9 5-Year IF: 3.72 SJR: 0.736 SNIP: 0.551 CiteScore™: 2.43

ISSN Print: 0743-4863
ISSN Online: 2162-660X

Volumes:
Volume 36, 2019 Volume 35, 2018 Volume 34, 2017 Volume 33, 2016 Volume 32, 2015 Volume 31, 2014 Volume 30, 2013 Volume 29, 2012 Volume 28, 2011 Volume 27, 2010 Volume 26, 2009 Volume 25, 2008 Volume 24, 2007 Volume 23, 2006 Volume 22, 2005 Volume 21, 2004 Volume 20, 2003 Volume 19, 2002 Volume 18, 2001 Volume 17, 2000 Volume 16, 1999 Volume 15, 1998 Volume 14, 1997 Volume 13, 1996 Volume 12, 1995

Critical Reviews™ in Therapeutic Drug Carrier Systems

DOI: 10.1615/CritRevTherDrugCarrierSyst.v14.i3.20
66 pages

A Human Colonic Cell Line Sharing Similarities With Enterocytes as a Model to Examine Oral Absorption: Advantages and Limitations of the Caco-2 Model

Florence Delie
Genentech, Inc., IDNA Way, South San Francisco, CA 94080
Werner Rubas
Genentech, Inc., IDNA Way, South San Francisco, CA 94080

ABSTRACT

Caco-2 cell monolayers mimic intestinal absorptive epithelium and represent a very useful tool for studying transepithelial transport. The literature on Caco-2 cells is controversial regarding transepithelial resistance and permeabilities of different marker compounds across monolayers. This paper discusses probable causes for these discrepancies. First, we present the role of culture conditions, such as the nature of the support or the passage number, on cell biology and transport properties. Further, we compare the presence of transport proteins in Caco-2 cells to mammalian intestinal tissue and discuss their implication for drug absorption. We also examine the advantages and disadvantages of systems such as Transwell® and side-by-side diffusion chambers. A summary of comparisons between permeabilities across Caco-2 monolayers and mammalian intestinal tissues is provided. We conclude that the origin of Caco-2 cells and the culture conditions are in part responsible for the discrepancies encountered in the literature.