Active transport drug design

One of the main in vitro permeability assays used in the pharmaceutical industry has been for many years the Caco-2 monolayer. Therefore, most of the in silica models developed to predict permeability were based on Caco-2 data. Hou and Johnson produced a couple of reviews that comprehensibly summarizes the recent efforts using Caco-2 permeability data [92, 94]. All those models are designed to predict the influx or apparent permeability of drugs in the same direction as intestinal absorption occurs, that is, from the apical to the basal side of the cell line, regardless of the extent of active transport involved in the permeation process. 

The transport activity of drug carriers can be affected in many different ways. Thus, with respect to drug design, different questions have to be addressed Which transporters can be utilized in the intestine for oral drug absorption Can the expression of these transporters be affected by either disease states or type of nutrition, age, and sex Is it possible that in a population, various genotypes exist with different transport activities and substrate specificities ... 

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