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Passive Permeability And Active Transport Models For The Prediction Of Oral Absorption
P. Artursson, S. Neuhoff, S. Tavelin, P. Matsson
Published 2007 · Engineering
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A variety of cell culture models, including Caco-2 cells, are used to provide better pharmacokinetic decision grounds in drug discovery. This article examines the properties of such cell culture models and discusses their roles during the various stages in the drug discovery process. The strengths and weaknesses of different models for the assessment of passive drug permeability, active drug transport, and for the prediction of oral drug absorption are reviewed. The performance of the cell culture models as compared to emerging alternatives is also discussed. Further, the influence of the quality of the data and data sets used in permeability and transport assessment is investigated. We conclude that cell culture models can be used both as qualitative tools in higher-throughput modes and as quantitative tools for the selection of druglike compounds with optimal permeability and transport properties in later stages of the drug discovery process.
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A Tri-Functionalized Oral Core-Melt Tablet (OCMT) for enhanced delivery of gastro-sensitive proteins and synthetic peptides
Bibi F Choonara (2017)
Oral delivery of natural compounds by phospholipid vesicles.
M. Manconi (2020)
Membrane Permeability – Measurement and Prediction in Drug Discovery
Kiyohiko Sugano (2009)
A review of advanced oral drug delivery technologies facilitating the protection and absorption of protein and peptide molecules.
Bibi F Choonara (2014)
Metabolism in Drug Development
B. Testa (2014)
Organic stereochemistry. Part 5 : Stereoselectivity in molecular and clinical pharmacology
B. Testa (2013)
New sustained release of Zidovudine Matrix tablets − cytotoxicity toward Caco-2 cells
J. V. Santos (2013)