Evaluation of Optimized Caco-2 Permeability Measurements

Purpose.  To optimize pH conditions for Caco-2 assay that allow de-convoluting and understanding various contributions to passive transport of drugs through the cell membrane. The pH and concentration effects on carrier-mediated/active transport were also studied.

Conclusion.  A novel approach of optimizing Caco-2 conditions based on predicted results enables the interpretation of difficult measurements with greater level of confidence. The developed approach saves costs, by avoiding poorly-designed assay protocols, and in some cases, avoiding the need for costly measurements.