Estimating intestinal mucosal permeation of compounds using Caco-2 cell monolayers.

Step-by-step protocols are provided in this unit for the measurement of apparent permeability coefficients of compounds using Caco-2 cell monolayers as an in vitro model of the intestinal mucosa. Procedures for culturing the cells and transmonolayer transport studies are also included. Critical issues for successfully estimating intestinal mucosal permeation of drugs are discussed. Step-by-step protocols are provided in this unit for the measurement of apparent permeability coefficients of compounds using.

[1]  R T Borchardt,et al.  Paracellular diffusion in Caco-2 cell monolayers: effect of perturbation on the transport of hydrophilic compounds that vary in charge and size. , 1997, Journal of pharmaceutical sciences.

[2]  L. Benet,et al.  Active secretion and enterocytic drug metabolism barriers to drug absorption 1 PII of original artic , 1996 .

[3]  Thomas J. Raub,et al.  Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. , 1989, Gastroenterology.

[4]  K. Luthman,et al.  Caco-2 monolayers in experimental and theoretical predictions of drug transport. , 2001, Advanced drug delivery reviews.

[5]  H. Lennernäs,et al.  Comparison between active and passive drug transport in human intestinal epithelial (Caco-2) cells in vitro and human jejunum in vivo , 1996 .

[6]  R. Borchardt,et al.  How structural features influence the biomembrane permeability of peptides. , 1996, Journal of pharmaceutical sciences.

[7]  V. Ganapathy,et al.  Role of pH gradient and membrane potential in dipeptide transport in intestinal and renal brush-border membrane vesicles from the rabbit. Studies with L-carnosine and glycyl-L-proline. , 1983, The Journal of biological chemistry.

[8]  A. Waseem Malick,et al.  The use of the intestinal epithelial cell culture model, Caco-2, in pharmaceutical development , 1996 .

[9]  P. Watkins,et al.  Expression of enzymatically active CYP3A4 by Caco-2 cells grown on extracellular matrix-coated permeable supports in the presence of 1alpha,25-dihydroxyvitamin D3. , 1997, Molecular pharmacology.

[10]  R. Borchardt.  The application of cell culture systems in drug discovery and development. , 1995, Journal of drug targeting.

[11]  J. Goodwin,et al.  In vitro permeability of peptidomimetic drugs : the role of polarized efflux pathways as additional barriers to absorption , 1997 .

[12]  T. Walle,et al.  Taxol transport by human intestinal epithelial Caco-2 cells. , 1998, Drug metabolism and disposition: the biological fate of chemicals.

[13]  K. Hillgren,et al.  In vitro systems for studying intestinal drug absorption , 1995, Medicinal research reviews.

[14]  P Langguth,et al.  P-Glycoprotein (P-gp) mediated efflux in Caco-2 cell monolayers: the influence of culturing conditions and drug exposure on P-gp expression levels. , 1998, Journal of pharmaceutical sciences.

[15]  Ismael J. Hidalgo,et al.  Carrier-mediated transport and efflux mechanisms in Caco-2 cells , 1996 .

[16]  R T Borchardt,et al.  General principles in the characterization and use of model systems for biopharmaceutical studies. , 1996, Pharmaceutical biotechnology.

[17]  P. Artursson,et al.  Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. , 1991, Biochemical and biophysical research communications.

[18]  D. Thakker,et al.  Applications of the Caco-2 model in the design and development of orally active drugs: elucidation of biochemical and physical barriers posed by the intestinal epithelium , 1997 .

[19]  Pravin Chaturvedi,et al.  Design principles for orally bioavailable drugs , 1996 .

[20]  V. Ganapathy,et al.  Peptide transporters in the intestine and the kidney. , 1996, Annual review of nutrition.

[21]  L. Benet,et al.  Active secretion and enterocytic drug metabolism barriers to drug absorption. , 2001, Advanced drug delivery reviews.