Enhancement of Paracellular Transport of Heparin Disaccharide Across Caco-2 Cell Monolayers

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Authors
So, Yean Cho
Jong, Sik Kim
Li, Hong
Shim, Changkoo
Linhardt, Robert J.
Yeong, Shik Kim
Issue Date
2002-02-28
Type
Article
Language
ENG
Keywords
Biology , Chemistry and chemical biology , Chemical and biological engineering , Biomedical engineering
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Abstract
The enhancement of paracellular transport of heparin disaccharide using several absorption enhancers across Caco-2 cell monolayers was tested. The cytotoxicity of these enhancers was also examined. The enhancing effects by Quillaja saponin, dipotassium glycyrrhizinate, 18beta-glycyrrhetinic acid, sodium caprate and taurine were determined by changes in transepithelial electrical resistance (TEER) and the amount of heparin disaccharide transported across Caco-2 cell monolayers. Among the absorption enhancers, 18beta-glycyrrhetinic acid and taurine decreased TEER and increased the permeability of heparin disaccharide in a dose-dependent and time-dependent manner with little or negligible cytotoxicity. Our results indicate that these absorption enhancers can widen the tight junction, which is a dominant paracellular absorption route of hydrophilic compounds. It is highly possible that these absorption enhancers can be applied as pharmaceutical excipients to improve the transport of macromolecules and hydrophilic drugs having difficulty in permeability across the intestinal epithelium.
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Archives Pharmacal Research, 25, 86-92
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Full Citation
Enhancement of Paracellular Transport of Heparin Disaccharide Across Caco-2 Cell Monolayers, S. Y. Cho, J. S. Kim, H. Li, C. Shim, R. J. Linhardt, Y. S. Kim, Archives Pharmacal Research, 25, 86-92 2002.
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2536269
2536269
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