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Caco-2 Culture and Transport Experiments

Drug absorption experiments are easy to perform in the cell culture model. The drug is added to the apical (mucosal) side, and the appearance of the drug on the basolateral side (serosal) is followed by time. The model also permits experiments to be carried out in the reverse direction, i.e., from the basolateral side to the apical side. [Pg.100]

The experiments should preferably be performed under sink conditions (e.g., the drug concentration on the receiver side should be less than 10% of the concentration on the donor side during an experiment) in order to avoid bias by back-diffusion of significant amount of compound from the receiver chamber and to [Pg.100]

This equation for calculation of Papp is easily improved by taking into account the change of donor concentration (Q) during the experiment, which affects the concentration gradient and the driving force for passive diffusion [74]  [Pg.101]

Culture protocols have been published which describes an accelerated differentiation process where monolayers are ready to be used after 3-7 days of culture [90-92]. One of these systems, the so-called BD BioCoat Intestinal Epithelium Differentiation Environment, is commercially available through BD Bioscience. This system is described to produce monolayers of a quality that are comparable with the typical Caco-2 cells with respect to permeability for drugs transported transcellularly. The paracellular barrier function is however low, as indicated by high mannitol permeability and low TER. The functional capacity for active uptake and efflux is not as thoroughly characterized as for the standard Caco-2 mono-layers. [Pg.101]


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