IN VITRO AND IN SILICO APPROACHES FOR SCREENING INTESTINAL PERMEABILITY AND ABSORPTION OF DRUGS.

Document Type : Review Article

Authors

1 Department of Pharmaceutics, Faculty of Pharmacy, Al-Baha University, Al-Baha, Saudi Arabia

2 Department of Pharmaceutical Sciences, Philadelphia College of Pharmacy, Saint Joseph's University, Philadelphia, Pennsylvania, 19131, USA

3 Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt

4 Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt

Abstract

Because the oral route of drug delivery is incomparable, screening of intestinal permeability and absorption of drug candidates is a critical stage before clinical trials for time and cost reasons. Permeability assessment of drugs after oral administration have been investigated using different in-vitro approaches. Fast, reliable, and non-invasive in-vitro techniques are crucial in the early stages of the drug discovery process as primary screening tools to assess intestinal permeability of lead compounds. In-vitro techniques are either experimental based or computer assisted (in-silico) methods. Experimental methods to predict intestinal permeability of drugs are mainly partitioning based physicochemical models and direct measurement based models that depend on using laborious techniques of isolated human/animal cells or tissues. In this work, partitioning based physicochemical models that can predict a compound/drug permeability potential across intestinal membrane will be elaborated. In addition, in silico models that could be of value in scaling up feasible hit compounds and throwing away possible losers will also be overviewed.

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