Nature Reviews Drug Discovery 7, 205-220 (March 2008) | doi:10.1038/nrd2438

OpinionCarrier-mediated cellular uptake of pharmaceutical drugs: an exception or the rule?

Paul D. Dobson1 & Douglas B. Kell1  About the authors


It is generally thought that many drug molecules are transported across biological membranes via passive diffusion at a rate related to their lipophilicity. However, the types of biophysical forces involved in the interaction of drugs with lipid membranes are no different from those involved in their interaction with proteins, and so arguments based on lipophilicity could also be applied to drug uptake by membrane transporters or carriers. In this article, we discuss the evidence supporting the idea that rather than being an exception, carrier-mediated and active uptake of drugs may be more common than is usually assumed — including a summary of specific cases in which drugs are known to be taken up into cells via defined carriers — and consider the implications for drug discovery and development.

Author affiliations

  1. Paul D. Dobson and Douglas B. Kell are at the School of Chemistry and Manchester Interdisciplinary Biocentre, The University of Manchester, 131 Princess Street, Manchester M1 7DN, UK.

Correspondence to: Douglas B. Kell1 Email:


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Supplementary information S1 (Table)

Nature Reviews Drug Discovery Perspective (01 Aug 2010)

Prodrugs: design and clinical applications

Nature Reviews Drug Discovery Review (01 Feb 2008)