{"data":{"id":33,"name":"CACO-2 Permeability Assay","abbreviation":"CACO-2_assay","description":"

Caco-2 cells, derived from human colon adenocarcinoma, are widely used as an in vitro<\/em> model of the intestinal epithelium for assessing drug permeability and absorption. When cultured on permeable supports, Caco-2 cells differentiate into polarized monolayers with brush-border microvilli, tight junctions, and expression of key transporters and metabolic enzymes. This organization mimics many features of the small intestine, allowing quantification of both passive diffusion and transporter-mediated flux.<\/p>

Permeability experiments are performed by applying test compounds to the apical side of the monolayer and measuring appearance in the basolateral compartment. Apparent permeability coefficients (Papp) are calculated from transport rates normalized to surface area and concentration. Bidirectional assays (apical-to-basolateral and basolateral-to-apical) help distinguish passive diffusion from active efflux processes mediated by proteins such as P-glycoprotein or BCRP.<\/p>

Caco-2 permeability data correlate well with human intestinal absorption for passively transported drugs, making the system a gold standard in pharmaceutical research. However, limitations include long culture times (~21 days), variability between laboratories, and differences from the human small intestine in enzyme and transporter expression. Despite these caveats, Caco-2 assays remain a cornerstone of drug development and ADME screening.<\/p>

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source of image: 10.3390\/pharmaceutics15041146<\/a>
<\/p>","categories":[{"id":168,"title":"Permeability","breadcrumb":[{"id":4,"title":"Experimental"},{"id":168,"title":"Permeability"}]}],"url":"https:\/\/molmedb.upol.cz\/api\/v1\/methods\/33","landing_page":"https:\/\/molmedb.upol.cz\/method\/33","created_at":"2018-10-22T07:07:58.000000Z","updated_at":"2026-07-08T09:52:51.000000Z"}}