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Caco-2 monolayers in experimental and theoretical predictions of drug transport
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
2012 (English)In: Advanced Drug Delivery Reviews, ISSN 0169-409X, E-ISSN 1872-8294, Vol. 64, no S, 280-289 p.Article, review/survey (Refereed) Published
Abstract [en]

This review examines the use of Caco-2 monolayers in the prediction of intestinal drug absorption. First, the different routes of drug transport in Caco-2 monolayers are compared with those seen in vivo. Second, the prediction of drug absorption in vivo from transport experiments in cell monolayers is discussed for different classes of drugs. Finally, the use of Caco-2 monolayers as a reference model in physico-chemical and theoretical predictions of drug absorption is discussed. We conclude that Caco-2 monolayers can be used to identify drugs with potential absorption problems, and possibly also to select drugs with optimal passive absorption characteristics from series of pharmacologically active molecules generated in drug discovery programs.

Place, publisher, year, edition, pages
2012. Vol. 64, no S, 280-289 p.
Keyword [en]
Drug transport, Drug absorption, Intestinal epithelium, Caco-2, Cell monolayer, Partition coefficient, Hydrogen bonding potential, Desolvation energy, Molecular surface area, In vitro-in vivo correlation
National Category
Medical and Health Sciences
Identifiers
URN: urn:nbn:se:uu:diva-193709DOI: 10.1016/j.addr.2012.09.005ISI: 000312616700025OAI: oai:DiVA.org:uu-193709DiVA: diva2:603528
Available from: 2013-02-06 Created: 2013-02-06 Last updated: 2017-12-06Bibliographically approved

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Artursson, Per

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