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Whereas most drugs are absorbed by simple diffusion across biological barriers, the absorption of some therapeutic agents proceeds through carrier-mediated transport. Evolutionary speaking, the transporters that facilitate the absorption of drugs have emerged to mediate the traffic and compartmentalization of physiologic compounds that, due to their physicochemical features (hydrophilicity and/or size) would otherwise not be able to permeate through lipophilic membranes. Amino acids, peptides, nucleosides, sugars, and vitamins are among the physiological compounds that use carrier-mediated transport. Consequently, only drugs that in some way mimic or resemble such physiological compounds can “hijack” (be recognized by) those transporters to get absorbed (see Fig. 1for some examples). Reasonably, active transport and facilitated diffusion will be particularly significant for oral medications, as high levels of relevant transporters that...
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Talevi, A., Bellera, C.L. (2022). Active and Facilitated Transport in Drug Absorption. In: Talevi, A. (eds) The ADME Encyclopedia. Springer, Cham. https://doi.org/10.1007/978-3-030-84860-6_46
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