Caco-2 cell implementation

Despite the availability of other cell lines, Caco-2 cells remain the most widely used intestinal cell culture model at present. This model has provided valuable information necessary for lead optimization in the drug discovery process. However, it is important to understand that compounds with high permeability in this model are typically well absorbed, whereas compounds with low solubility and low permeability in this model may not necessarily be poorly absorbed in vivo. Although this type of positive selection limits the usefulness in providing a structure-permeability relationship, the Caco-2 model has the most effect in drug discovery when the screen is implemented early and in conjunction with other types of in vitro and in vivo permeability/absorption screens. 

Inspired by the successful implementation of the intestinal cell line, Caco-2, as a model to predict oral drug absorption, pulmonary-based models are used in a similar manner. The use of pulmonary cells which are covered by a comparatively thick fluid layer (liquid-interfaced deposition, LID) is probably... 

Jewell C, Cashmen KD. The effect of conjugated linoleic acid and medium-chain fatty acids on transepithelial calcium transport in human intestine-like Caco-2 cells. Br J Nutr 2003 89(5) 639-647. Schurer NY. Implementation of fatty acid carriers to skin irritation and the epidermal barrier. Contact Dermatitis 2002 47(4) 199— 205. 

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