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

• Published in: Archives of pharmacal research Vol. 25; no. 1; pp. 86 - 92
• Main Authors: Kim, Yeong-Shik, Cho, So-Yean, Kim, Jong-Sik, Li, Hong, Shim, Chang-Koo, Linhardt, Robert-J
• Format: Journal Article
• Language: Korean
• Published: 대한약학회 01.02.2002
• Subjects: 약학; Caco-2 cell monolayers; Tight junction; Heparin disaccharide; Absorption enhancers, Paracellular transport
• ISSN: 0253-6269; 1976-3786

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.