Caco-2 cell culture model

LIU Y and HU m (2002) Absorption and metabolism of flavonoids in the caco-2 cell culture model and a perfused rat intestinal model. Drug Metab Dispos. 30 (4) 370-77. 

Liu, C.S., Glahn, R.P., and Liu R.H., Assessment of carotenoid bioavailability of whole foods using a Caco-2 cell culture model coupled with an in vitro digestion, J. Agric. Food Chem., 52, 4330, 2004. 

Garrett, D.A., Failla, M.L., and Sarama, R.J., Estimation of carotenoid bioavailability from fresh stir-fried vegetables using an in vitro digestion/Caco-2 cell culture model, J. Nutr. Biochem., 11, 574, 2000. 

Pade, V., Stavchansky, S., Estimation of the relative contribution of the transcellular and paracellular pathway to the transport of passively absorbed drugs in the Caco-2 cell culture model, Pharm. Res. 1997, 34, 1210-1215. 

Ingels F, Deferme S, Destexhe E, Oth M, Van den Mooter G, Augustijns P (2002) Simulated intestinal fluid as transport medium in the Caco-2 cell culture model. Int JPharm 232 183-192. 

Marino AM, Yarde M, Patel H, Chong S, Balimane PV (2005) Validation of the 96 well Caco-2 cell culture model for high throughput permeability assessment of discovery compounds. Int J Pharm 297 235-241. 

Biganzoli E, Cavenaghi LA, Rossi R, Brunati MC, Nolli ML (1999) Use of a Caco-2 cell culture model for the characterization of intestinal absorption of antibiotics. Farmaco 54 594-599. 

Rothen-Rutishauser, B., Braun, A., Gunthert, M., and Wunderli-Allenspach, H., Formation of multilayers in the Caco-2 cell culture model a confocal laser scanning microscopy study, Pharm. Res., 17, 460, 2000. 

Demirbas, S. and Stavchansky, S., Effects of citicholine and dimethylsulfoxide on transepithe-lial transport of passively diffused drugs in the Caco-2 cell culture model, Int.. Pharm., 251, 107, 2003. 

Mattar, A. F., Teitelbaum, D. H., Drongowski, R. A., Yongyi, F., Harmon, C. M., and Coran, A. G. (2002). Probiotics up-regulate MUC-2 mucin gene expression in a Caco-2 cell-culture model. Pediatr. Surg. Int. 18, 586-590. 

Glahn, R.P., Lai, C., Hus, J., Thompson, J.F., Guo, M.R.,Van Campen, D.R. 1998. Decreased citrate improves iron availability from infant formula application of an in vitro digestion/ caco-2 cell culture model. J. Nutr. 128, 257-264. 

Liu, Y. and Hu, M., Absorption and metabolism of flavonoids in the caco-2 cell culture model and a perused rat intestinal model. Drug Metab. Dispos., 30, 370, 2002. Sfakianos, J., Coward, L., Kirk, M. and Barnes, S., Intestinal uptake and biliary excretion of the isoflavone genistein in the rat, J. Nutr., 127, 1260, 1997. 

Meaney CM, O Driscoll CM. Comparison of the permeation enhancement potential of simple bile salt and mixed bile salt fatty acid micellar systems using the Caco-2 cell culture model. Int J Pharm 2000 207(10) 21-30. 

The pH in the cellular interstitial space and blood compartment is known to be about 7.4. The pH present in the G1 tract will not only have an impact on the ionization of drugs, and thus on their partitioning capacity, but it will also affect the pH-dependent functionality of various carriers located in the intestinal mucosa (Tsuji and Tamai, 1996). Many of these carriers are also expressed and functionally active in the Caco-2 cell culture model (Hidalgo and Li, 1996 Ogi-hara et al., 1999 Friedrichsen et al., 2002 Putman et al., 2002a,b). Therefore, the pH of the apical medium can have a critical effect on ionization and transport of drugs, ft has for instance been shown that the absorption of w eak bases, like beta-blockers, are absorbed better in the ileum region, where the pH is around... 

A drug is absorbed through diffusion across a series of separate barriers where the single layer of epithelial cells is the most significant barrier to absorption. Many in vitro methods have been developed for the study of this phenomenon. These methods include small animal gut studies, cell culture (i.e., Caco-2 cell culture model), octanol-water partition coefficients, measures of hydrogen bonding and desolvation energies, immobilized artificial membranes, and retention time on reversed-phase HPLC columns. 

Among these testing methods, the small animal GI model and the Caco-2 cell culture model have shown the best correlation with oral absorption in vivo. The Caco-2 culture system consists of a monolayer of human intestinal epithelial cells grown on semipermeable supports such as polycarbonate membranes. Because the cells are human in origin, they exhibit many characteristics of the human small intestinal epithelium. The permeability coefficients relative to the extents of human drug absorption are listed here ... 

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