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Use of simulated intestinal fluid for Caco-2 permeability assay of lipophilic drugs. | LitMetric

Use of simulated intestinal fluid for Caco-2 permeability assay of lipophilic drugs.

Int J Pharm

Preclinical Candidate Selection Unit, Laboratoires Fournier a Solvay Pharmaceuticals Company, 21121 Daix, France.

Published: August 2008

AI Article Synopsis

  • * To improve the solubility and recovery of these compounds, researchers found that using fasted state simulated intestinal fluid (FaSSIF) in the top compartment and Hanks balanced salt solution (HBSS) with bovine serum albumin (BSA) in the bottom compartment gives better results.
  • * Testing showed that this new model aligns well with how lipophilic compounds are absorbed in humans, with only two outliers among 35 tested compounds, making it the preferred method for predicting in vivo absorption of lipoph

Article Abstract

The most commonly used method to assess intestinal permeability is the measurement of compound flux across a Caco-2 cells monolayer by using Hanks balanced salt solution (HBSS)-like buffers. Nevertheless, lipophilic acid drugs are poorly or not at all soluble in these types of buffers and their adsorption on the transwell plate is commonly observed. To reduce adsorption and increase solubility, permeability assays need to be developed in conditions other than classic conditions for lipophilic compounds. The best model to increase recovery of lipophilic compounds was determined as fasted state simulated intestinal fluid (FaSSIF) in the apical compartment and HBSS with 1% bovine serum albumin (BSA) in basolateral compartment. This model allows a correlation between absorption on Caco-2 cells and absorbed fraction in humans. For 35 compounds, only 2 outliers were observed in the Caco-2 assay using the FaSSIF model. These two outliers were the same outlier compounds as those observed with a classic Caco-2 method. Furthermore, a permeability assay of Pgp substrates evidenced efflux transport in both models and addition of a Pgp inhibitor suppressed Pgp efflux transport. FaSSIF in the apical compartment and HBSS with 1% BSA in the basolateral compartment is the model of choice to predict in vivo absorption for lipophilic acid drugs.

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Source
http://dx.doi.org/10.1016/j.ijpharm.2008.04.034DOI Listing

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