Permeability Of Hydrophilic

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more
accurately between the molecules of intermediate molecular weight compared to
Caco-2 cells.

These results indicated that 2/4/A1 cells could be used as a model for
hydrophilic drug absorption.

INTRODUCTION

The small intestine plays a crucial role in the absorption of drugs and
nutrients. Exogenous substances cross a series of barriers during the process
of intestinal absorption: (1) the aqueous boundary/mucus layer, (2) a single
layer of epithelial cells, and (3) the lamina propria, which contains the blood
and lymph vessels that then transport the absorbed drugs to other parts of the
body (Artursson 1991).

The cell monolayer is comprised of two parallel barriers: the cell membrane and
the tight junctions. Most drugs are absorbed by a passive diffusion across the
cell membrane by the transcellular route, or across the tight junctions between
the cells - the paracellular route. Drug transport can also be carrier mediated,
when the drug utilizes transporters located in ...

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allows an
opportunity to use human rather than animal tissues; (d) it can minimize
expensive and sometimes controversial animal studies.

Human colorectal carcinoma cell line Caco-2 is nowadays the most widely used and
the best explored model for drug intestinal transport (Hidalgo et al. 1989;
Artursson 1990; Artursson & Karlsson 1991). This cell line displays spontaneous
enterocytic differentiation in culture and forms a polarized monolayer with
apical brush borders and well differentiated tight junctions (Hidalgo, 1989).
Drug transport studies across the Caco-2 cell monolayers showed a satisfactory
correlation with other in vitro absorption models, e.g. rat intestinal segments
(Artursson ...

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