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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
Published on: October 17, 2013
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Principles and Experimental Considerations for In Vitro Transporter Interaction Assays
Sid Bhoopathy1, Chris Bode2, Vatsala Naageshwaran2
1Absorption Systems, Exton, PA, USA. sid.bhoopathy@absorption.com.
Methods in Molecular Biology (Clifton, N.J.)
|July 17, 2021
Summary
Understanding drug transporters is key to predicting drug interactions and toxicity. Optimizing in vitro assays by considering compound characteristics and experimental design improves the accuracy of these predictions.
Area of Science:
- Pharmacology
- Drug Metabolism and Pharmacokinetics
- Biochemistry
Background:
- Drug transporters significantly influence the absorption, distribution, metabolism, and excretion (ADME) of endogenous and exogenous compounds.
- Altered transporter function can lead to variable drug efficacy and toxicity by affecting drug and substrate levels.
- Accurate prediction of clinical drug-drug interactions (DDIs) necessitates robust in vitro test systems.
Purpose of the Study:
- To identify critical variables influencing in vitro drug transporter assay outcomes.
- To provide actionable steps for improving the translatability of in vitro assay results.
- To enhance the prediction of clinical DDIs and avoid unnecessary clinical studies.
Main Methods:
- Review of factors affecting in vitro drug transporter assays.
- Analysis of test compound characteristics.
- Evaluation of test systems, assay formats, and experimental design.
Main Results:
- Experimental outcomes are sensitive to multiple factors including compound properties, assay systems, and design.
- A comprehensive understanding of these variables is crucial for assay optimization.
- Improved in vitro assays can lead to more reliable predictions of clinical DDI risks.
Conclusions:
- Optimizing in vitro assays by carefully considering experimental variables is essential for accurate DDI prediction.
- Enhanced understanding of factors influencing transporter assays aids in avoiding costly clinical trials.
- This work provides a framework for improving the reliability and translatability of drug transporter research.
Keywords:
ABC efflux transportersBCRPBSEPDrug transportersMATEMRP2OATOATPOCTP-gpSLC uptake transportersSLCOMore Related Videos
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