Enhancement of paracellular transport of heparin disaccharide across Caco-2 cell monolayers

Yean Cho So, Sik Kim Jong, Hong Li, Changkoo Shim, Robert J. Linhardt, Shik Kim Yeong

Research output: Contribution to journalArticlepeer-review

20 Scopus citations

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, 18β-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, 18β-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.

Original languageEnglish
Pages (from-to)86-92
Number of pages7
JournalArchives of Pharmacal Research
Volume25
Issue number1
DOIs
StatePublished - 28 Feb 2002
Externally publishedYes

Keywords

  • Absorption enhancers
  • Caco-2 cell monolayers
  • Heparin disaccharide
  • Paracellular transport
  • Tight junction

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