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Caco-2 Permeability Assay


Creative Bioarray is offering Caco-2 permeability assay to help determine the absorption and the bioavailability of drug candidates, facilitating the lead optimization process in drug discovery.

Caco-2 permeability assay is one of the recommended in vitro methods in the United States FDA guidelines 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. The method can be used to assess the bidirectional permeability of a test compound (from the apical to the basolateral side or vice versa).  By measuring the transport rate of a compound across a Caco-2 cell monolayer membrane, the in vivo absorption of the compound across the gut wall can be well predicted.

Under specific culture condition, the Caco-2 cells, although derived from a human colon carcinoma, 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 and making it ideal for intestinal absorption simulations.   As an in vitro model of the human small intestinal mucosa, Caco-2 monolayers have been widely used in the pharmaceutical industry to predict drug absorption. There is also a well-established correlation between the in vitro apparent permeability across Caco-2 monolayers and the in vivo fraction absorbed.

Caco-2 Permeability Assay  

In this assay, confluent Caco-2 cell monolayers, cultured on a permeable surface, are placed in a cell culture plate to form donor-receiver compartments. Test compounds are added to either the apical or the basolateral compartment. To evaluate the apical-to-basolateral (A-B) transport of a compound, the test compound is added to the apical side with fresh medium in the basolateral compartment. The transport of the compound across the Caco-2 cell monolayer is monitored for 2 hours. To study drug efflux, the basolateral-to-apical (B-A) transport of the compound also needs to be evaluated.

Creative Bioarray has accumulated extensive knowledge and experience in assay designing and data analyzing. We are dedicated to assisting drug developers reduce cost and save time by providing reliable and reproducible data. Our experienced scientific team are capable of designing and providing high-quality in vitro ADME profiling services. If you have any special needs, please contact us at or 1-631-626-9181 for support. We will try our best to accommodate you and help you achieve your goal.

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