Related Experiment Video
Updated: Jan 20, 2026
The Caco-2 Cell Bioassay for Measurement of Food Iron Bioavailability
Published on: April 28, 2022
Drug-permeability and transporter assays in Caco-2 and MDCK cell lines
1Food & Drug Administration, Center for Drug Evaluation & Research, 10903 New Hampshire Ave. Silver Spring, MD 20993-0002, USA. donna.volpe@fda.hhs.gov
Abstract:
The human colon adenocarcinoma Caco-2 and Madin-Darby canine kidney epithelial cell lines provide in vitro tools to assess a drug's permeability and transporter interactions during discovery and development. The cells, when cultured on semiporous filters, form confluent monolayers that model the intestinal epithelial barrier for permeability, transporter and drug-interaction assays. The applications of these assays in pharmaceutical research include qualitative prediction and ranking of absorption, determining mechanism(s) of permeability, formulation effects on drug permeability, and the potential for transporter-mediated drug-drug interactions. This review focuses on recent examples of Caco-2 and Madin-Darby canine kidney cells assays for drug permeability including transfected and knock-down cells, miniaturization and automation, and assay combinations to better understand and predict intestinal drug absorption.
Insights
Caco-2 and Madin-Darby canine kidney cells are vital in vitro models for predicting drug absorption and interactions. Recent advancements enhance their utility in pharmaceutical research for better drug development.
Area of Science:
- Pharmacology
- Cell Biology
- Drug Development
Background:
- Caco-2 and Madin-Darby canine kidney (MDCK) cells are established in vitro models.
- These cell lines form confluent monolayers on semiporous filters, mimicking the intestinal epithelial barrier.
- They are crucial for assessing drug permeability and transporter interactions.
Purpose of the Study:
- To review recent advancements in Caco-2 and MDCK cell-based assays for drug permeability.
- To highlight applications in predicting drug absorption, transporter mechanisms, and drug-drug interactions.
- To discuss innovative assay formats for improved in silico prediction.
Main Methods:
- Utilizing Caco-2 and MDCK cell monolayers cultured on semiporous filters.
- Employing assays to evaluate drug permeability and transporter interactions.
- Reviewing studies involving transfected/knock-down cells, miniaturization, automation, and assay combinations.
Main Results:
- These assays enable qualitative prediction and ranking of drug absorption.
- They help elucidate mechanisms of drug permeability and formulation effects.
- Recent innovations improve the prediction of transporter-mediated drug-drug interactions.
Conclusions:
- Caco-2 and MDCK cell assays are indispensable tools in pharmaceutical research and development.
- Advancements in assay technology enhance the understanding and prediction of intestinal drug absorption.
- These models are critical for optimizing drug candidates and predicting in vivo behavior.
Related Concept Videos
06:34The Caco-2 Cell Bioassay for Measurement of Food Iron Bioavailability
11:40A Co-culture Method to Investigate the Crosstalk Between X-ray Irradiated Caco-2 Cells and PBMC
11:27Methods to Study Epithelial Transport Protein Function and Expression in Native Intestine and Caco-2 Cells Grown in 3D
07:00Using Caco-2 Cells to Study Lipid Transport by the Intestine
18:57Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
03:56Caco-2 Cell Bioassay: An In Vitro Method for Measuring Iron Bioavailability in Complex Food Sources