Drug Permeability Profiling Using the Novel Permeapad® 96-Well Plate
Ann-Christin Jacobsen1, Sune Nielsen1, Martin Brandl1
1Drug Transport & Delivery Group, Department of Physics, Chemistry & Pharmacy, University of Southern Denmark, 5230, Odense, Denmark.
Pharmaceutical Research
|May 13, 2020
Summary
This study introduces the Permeapad® 96-well plate for high-throughput passive permeability profiling. The tool effectively distinguishes drug absorption levels and correlates well with established methods, showing promise for drug discovery.
Area of Science:
- Pharmacology
- Biophysical Chemistry
- Drug Discovery
Background:
- Passive permeability is crucial for predicting oral drug absorption.
- High-throughput screening methods are needed for efficient drug discovery.
- Existing in vitro models have limitations in speed and reproducibility.
Purpose of the Study:
- To evaluate a novel 96-well plate prototype utilizing the Permeapad® membrane for passive permeability profiling.
- To assess the correlation of permeability data with human oral absorption (Fa) and other in vitro methods.
- To characterize the Permeapad® membrane structure.
Main Methods:
- A 96-well plate system with the artificial phospholipid-based Permeapad® membrane was employed.
- Permeability of 14 model compounds was measured over time to determine apparent permeability (Papp).
- Microscopic analysis was performed on the Permeapad® membrane structure.
Main Results:
- The Permeapad® 96-well plate successfully differentiated high and low absorption drugs.
- Results showed a hyperbolic correlation with human fraction absorbed (Fa).
- Strong correlations were observed with Caco-2 (R2=0.70) and PAMPA (R2=0.89) permeability.
Conclusions:
- The Permeapad® 96-well plate system is a valuable tool for rapid and reproducible passive permeability assessment.
- This high-throughput method aids in early-stage drug discovery and development.
- The findings support the use of Permeapad® for in vitro drug permeability profiling.
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