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Published on: February 9, 2016
Parallel artificial membrane permeability assay (PAMPA) - Is it better than Caco-2 for human passive permeability
J M Reis1, B Sinkó, C H R Serra
1Department of Pharmacy, School of Pharmaceutical Sciences, São Paulo University, 580 Prof. Lineu Prestes Avenue, Bl. 13, 05508-900 São Paulo, SP, Brazil.
Mini Reviews in Medicinal Chemistry
|November 4, 2010
Summary
This review compares various PAMPA assay techniques against Caco-2 and human jejunum data. It identifies the optimal PAMPA model for predicting drug absorption in humans.
Area of Science:
- Pharmacokinetics and Drug Metabolism
- Membrane Transport Studies
- In vitro ADME Prediction
Background:
- The Parallel Artificial Membrane Permeability Assay (PAMPA) is a widely used in vitro method for predicting drug absorption.
- Variations of the PAMPA assay exist, each with different lipid compositions and incubation conditions, potentially affecting prediction accuracy.
- Comparing these PAMPA variations against established Caco-2 and human jejunum data is crucial for validating their predictive power.
Purpose of the Study:
- To statistically and qualitatively compare major PAMPA assay techniques against experimental Caco-2 and human jejunum data.
- To evaluate the impact of membrane lipid composition and incubation conditions on PAMPA assay performance.
- To identify the most reliable PAMPA model for predicting human intestinal drug absorption and validate prior hypotheses.
Main Methods:
- Review and comparison of prominent PAMPA assay variations.
- Statistical and qualitative analysis of assay results for 16 diverse molecules.
- Correlation of PAMPA data with experimental results from Caco-2 cell monolayers and human jejunum samples.
- Assessment of Biopharmaceutics Classification System (BCS) class prediction accuracy.
Main Results:
- Significant differences were observed in the performance of various PAMPA techniques.
- Membrane lipid composition and incubation conditions were identified as key factors influencing prediction accuracy.
- The study successfully predicted the BCS classification for the tested molecules.
- A specific PAMPA model was identified as superior for predicting human intestinal permeability.
Conclusions:
- The choice of PAMPA assay methodology, including lipid composition and incubation parameters, critically impacts its ability to predict human drug absorption.
- This comparative analysis provides valuable insights for selecting the most appropriate PAMPA model for drug discovery and development.
- The findings support the utility of optimized PAMPA assays as reliable tools for early-stage ADME assessment.
