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The Pharmaceutical Society of Korea (대한약학회)
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Enhancement of Paracellular Transport of Heparin Disaccharide Across Caco-2 Cell Monolayers

  • Kim, Yeong-Shik (National Products Research Institute, Seoul National University) ;
  • Cho, So-Yean (National Products Research Institute, Seoul National University) ;
  • Kim, Jong-Sik (National Products Research Institute, Seoul National University) ;
  • Li, Hong (College of Pharmacy, Seoul National University) ;
  • Shim, Chang-Koo (College of Pharmacy, Seoul National University) ;
  • Linhardt, Robert-J. (Division of Medicinal and Natural Products Chemistry, Department of Chemistry and Department of Chemical and Biochemical Engineering, University of lowa.)
  • Published : 2002.02.01
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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, diponin glycyrrhizinate, $18{\beta}-glycyrrhetinic$ 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, $18{\beta}-glycyrrhetinic$ acid arid 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.

Keywords

References

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