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The in vitro Caco-2 permeability assay has become a very useful tool for investigating the effects of pharmaceutical excipients on improving permeation of compounds with poor lipophilicity and/or excessive efflux by P-glycoprotein (P-gp) and/or Breast Cancer Resistance Protein (BCRP). Therefore, elucidating the mechanisms of enhanced permeation by pharmaceutical excipients can provide strategies for the development of drug formulations. The purpose of this study is to investigate the cytotoxic potential and the effects of 14 pharmaceutical excipients on the monolayer integrity, P-gp and BCRP activities in Caco- 2 cells.
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