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Updated: Jul 10, 2026
18:57
Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
Published on: October 17, 2013
Transporter-mediated uptake into cellular compartments.
S Oswald1, M Grube, W Siegmund
1Research Center of Pharmacology and Experimental Therapeutics, University of Greifswald, Greifswald, Germany.
Xenobiotica; the Fate of Foreign Compounds in Biological Systems
|October 31, 2007
Summary
Drug transporters like P-glycoprotein (P-gp) influence drug absorption and excretion. This review explores their impact on drug levels within cells and tissues, affecting drug efficacy and clinical outcomes.
Area of Science:
- Pharmacology
- Biochemistry
- Cell Biology
Background:
- Active transport proteins, including P-glycoprotein (P-gp), multidrug resistance-associated proteins (MRPs), and organic anion transporting polypeptides (OATPs), are crucial for drug disposition.
- These transporters are primarily located at absorption and elimination sites, impacting drug bioavailability and excretion.
- While their role in blood-organ barriers is recognized, their influence on intracellular drug concentrations remains less understood.
Purpose of the Study:
- To review the current understanding of how transporter proteins affect drug concentrations within pharmacologically relevant cellular compartments and tissues.
- To highlight the potential clinical significance of these transporters in modulating drug effects at the site of action.
Main Methods:
- Literature review of existing research on drug transporters.
- Analysis of studies investigating transporter function in various tissues and cellular compartments.
- Synthesis of data on the impact of transporters on drug pharmacokinetics and pharmacodynamics.
Main Results:
- Drug transporters significantly influence drug absorption, distribution, metabolism, and excretion (ADME).
- Transporter activity can alter drug concentrations at the subcellular level, affecting target engagement and therapeutic efficacy.
- Specific transporters play critical roles in hepatocytes, enterocytes, blood cells, brain, and heart.
Conclusions:
- Transporter proteins are key determinants of drug availability and efficacy within tissues and cellular compartments.
- Understanding transporter function is essential for predicting drug response and optimizing therapeutic strategies.
- Further research into transporter-mediated drug disposition at the cellular level holds significant clinical implications.
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