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Related Experiment Video

Updated: Jun 18, 2026

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers

Published on: October 17, 2013

Transporters in absorption, distribution, and elimination.

Jean-Michel Scherrmann¹

¹University Paris Descartes, Department of Pharmaceutical Sciences, Faculty of Pharmacy, 4, avenue de l'Observatoire, FR-75006 Paris. jean-michel.scherrmann@inserm.fr

Chemistry & Biodiversity

|November 26, 2009

Summary

Drug transporters significantly impact drug absorption, distribution, metabolism, and excretion (ADME), shifting pharmacokinetics from diffusion-based to transporter-mediated processes. Understanding transporters is crucial for predicting drug efficacy, toxicity, and interactions.

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Area of Science:

Pharmacology
Biochemistry
Drug Metabolism

Background:

Pharmacokinetics traditionally focuses on drug absorption, distribution, metabolism, and excretion (ADME) via diffusion.
Drug transporters are increasingly recognized as critical factors influencing ADME processes.
The role of transporters challenges the established 'diffusional pharmacokinetics' model.

Purpose of the Study:

To highlight the evolving understanding of pharmacokinetics with the inclusion of drug transporters.
To emphasize the clinical significance of drug transporters in modulating drug effects and toxicity.
To underscore the importance of transporters in drug-drug interactions.

Main Methods:

Review of existing literature on drug transporters and their impact on ADME.
Analysis of the shift from diffusional to vectorial pharmacokinetics.
Discussion of clinical implications and drug interaction mechanisms.

Main Results:

Drug transporters introduce non-diffusional mechanisms for drug permeation across membranes.
Transporters influence intracellular drug concentrations, affecting pharmacological activity and organ-specific toxicity.
Drug transporters play a pivotal role in drug-drug interactions, comparable to drug-metabolizing enzymes.

Conclusions:

Pharmacokinetics is evolving towards 'vectorial pharmacokinetics' due to the influence of drug transporters.
Drug transporters are essential determinants of drug efficacy, safety, and interactions.
Further research into transporter-mediated processes is vital for optimizing drug therapy.