Caco-2 cell is a human colon epithelial cancer cell line. Under specific culture conditions, the Caco-2 cells become differentiated and polarized with intercellular tight junctions, a well-differentiated brush border, and typical small-intestinal nutrient transporters, resembling the enterocytes lining the small intestine, making it ideal for intestinal absorption simulations.
Caco-2 permeability assay is one of the recommended in vitro methods to evaluate drug permeability. It has become the gold standard method to evaluate both the passive and active transport and the absorption of orally administered drugs.