Related Experiment Video
Updated: May 29, 2026

An in vivo Assay to Test Blood Vessel Permeability
Published on: March 16, 2013
In situ artificial membrane permeation assay under hydrodynamic control: correlation between drug in vitro
Matěj Velický1, Kin Y Tam, Robert A W Dryfe
1School of Chemistry, University of Manchester, Oxford Road, Manchester M13 9PL, UK.
Abstract:
The purpose of this study was to develop an in vitro permeation model that will predict the fraction of drugs absorbed in humans. A rotating-diffusion cell with two aqueous compartments, separated by a lipid-impregnated artificial membrane, was used to determine the permeability of drugs under conditions of controlled hydrodynamics. The measured effective permeability coefficient was modified to include the paracellular transport derived from a previously reported colorectal adenocarcinoma epithelial cell line (Caco-2) permeability study and the effects of unstirred water layer anticipated in vivo. Permeability data were collected for 31 different marketed drugs with known absolute oral bioavailability and human hepatic clearance data. Literature bioavailability values were corrected for the first pass hepatic clearance thus obtaining the fraction absorbed from intestinal lumen (fraction absorbed), F(a), while assuming that the fraction escaping intestinal extraction, F(g), was approximately ~1. Permeability obtained under conditions of controlled hydrodynamics was compared with the permeability measured under unstirred conditions. It is shown that the optimized effective permeability correlates with the fraction absorbed. In contrast, permeability data obtained under unstirred conditions does not show a good correlation. The in vitro permeation model developed in this study predicts the fraction absorbed of the selected drugs in humans within experimental uncertainty. It has been demonstrated that the correlation with the fraction absorbed is greatly improved using the permeability data obtained under controlled hydrodynamics with paracellular transport included in the model.
More Related Videos
10:33A Method for Determination and Simulation of Permeability and Diffusion in a 3D Tissue Model in a Membrane Insert System for Multi-well Plates
Published on: February 23, 2018
09:35An In Vivo Blood-brain Barrier Permeability Assay in Mice Using Fluorescently Labeled Tracers
Published on: February 26, 2018
Related Concept Videos
Methods for Studying Drug Absorption: In situ
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
Methods for Studying Drug Absorption: In vitro
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
Drug Product Performance: In Vitro–In Vivo Correlation
Drug Absorption Mechanism: Passive Membrane Transport
Bioavailability Enhancement: Drug Permeability Enhancement
Factors Influencing Drug Absorption: Drug Dissolution