Title: Implementation of the caco-2 cell culture model as a predictive tool for the oral absorption of drugs. In-house evaluation procedures
Authors: Ingels, F ×
Deferme, S
Delbar, N
Oth, M
Augustijns, Patrick #
Issue Date: Nov-2002
Series Title: Journal de pharmacie de Belgique vol:57 issue:6 pages:153-8
Abstract: The Caco-2 cell culture model is widely used during drug development and lead optimization as a predictive tool for the oral absorption of drugs. In order to improve the reliability and quality of the results of Caco-2 experiments and to ensure that the system being used is functionally and enzymatically representative for the intestinal mucosa, it is important to perform a validation of the implemented Caco-2 system. In this paper, we summarize evaluation techniques to guarantee the in-house validity of the model. Theophyllin and sodium fluorescein are used as model compounds to evaluate passive transcellular and passive paracellular transport, respectively. Phenylalanine serves as a substrate to demonstrate active carrier mechanisms. Aminopeptidase and dipeptidyl peptidase are two brush border enzymes present in an active form in the Caco-2 culture model. The presence of an active efflux carrier mechanism is demonstrated with cyclosporin A as a substrate.
ISSN: 0047-2166
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Drug Delivery and Disposition
× corresponding author
# (joint) last author

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