Caco-2 Uptake/Permeability Assay

Differentiated polarized Caco-2 cells (a human colon carcinoma cell line) express a wide range of transporter proteins on its cell membranes mimicking the intestinal endothelium cells. The Caco-2 uptake/bioavailability investigation utilizes a Caco-2 cell layer grown on a supportive membrane surface that separates two compartments. The Caco-2 uptake study is considered to be the reference standard in pharmaceutical/nutraceutical industries for in vitro prediction of in vivo human intestinal absorption and bioavailability of orally administered substance. In drug discovery field, The FDA recommends that drug-drug interactions should be performed during drug development, and Caco-2 permeability assay is used to predict drug-drug interactions (DDIs) of orally administered drugs.

In this study, test material is added to one side of a confluent monolayer of Caco-2 cells. The degree of biouptake of the test material is then assessed by monitoring the concentration of a major active of the test material on the opposite side of the monolayer.