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Updated: May 25, 2026
10:22
In Vitro and In Vivo Approaches to Determine Intestinal Epithelial Cell Permeability
Published on: October 19, 2018
Estimating intestinal mucosal permeation of compounds using Caco-2 cell monolayers
J Gao1, E D Hugger, M S Beck-Westermeyer
1University of Kansas, Lawrence, Kansas, USA.
Current Protocols in Pharmacology
|February 2, 2012
Summary
This study provides protocols for measuring compound permeability using Caco-2 cell monolayers, an in vitro model for intestinal absorption. These methods aid in estimating drug permeation through the intestinal mucosa.
Area of Science:
- Pharmacology
- Cell Biology
- Drug Discovery
Background:
- Caco-2 cell monolayers serve as a validated in vitro model for the intestinal epithelium.
- Accurate prediction of drug absorption requires reliable methods to assess intestinal permeability.
Purpose of the Study:
- To provide detailed protocols for measuring apparent permeability coefficients of compounds.
- To outline procedures for Caco-2 cell culture and transmonolayer transport studies.
- To discuss critical factors for estimating intestinal mucosal permeation of drugs.
Main Methods:
- Step-by-step protocols for Caco-2 cell culture.
- Transmonolayer transport assays to determine apparent permeability coefficients.
- Discussion of key considerations for in vitro to in vivo extrapolation.
Main Results:
- Established protocols for reproducible measurement of apparent permeability coefficients.
- Demonstrated the utility of Caco-2 cell monolayers for intestinal drug permeation studies.
- Identified critical parameters influencing the accuracy of permeability estimations.
Conclusions:
- The provided protocols enable robust assessment of compound permeability using Caco-2 cells.
- This methodology is crucial for early-stage drug discovery and development.
- Optimized Caco-2 cell-based assays facilitate the prediction of intestinal drug absorption.
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