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Membrane transporters are important determinants of cellular and tissue distribution of charged molecules. In the intestine, uptake transporters expressed at the apical membrane of enterocytes contribute to the dietary absorption of endogenous molecules, such as peptides, vitamins or bile acids. Transporters accommodate molecules with a wide range of chemical properties and can be actively targeted to improve oral exposure of therapeutic molecules. This chapter summarises current knowledge of relevant intestinal uptake transporters, describes their characteristics and illustrates approaches taken to target drugs to these transporters.

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