Effect of cationized gelatins on the paracellular transport of drugs through caco-2 cell monolayers

Journal of Pharmaceutical Sciences
Toshinobu SekiKazuhiro Morimoto

Abstract

Cationized gelatins, candidate absorption enhancers, were prepared by addition of ethylenediamine or spermine to gelatin and the effects of the resulting ethylenediaminated gelatin (EG) and sperminated gelatin (SG) on the paracellular transport of 5(6)-carboxyfluorescein (CF), FITC-dextran-4 (FD4), and insulin through caco-2 cell monolayers were examined. The Renkin function was used for characterization of the paracellular pathway and changes in the pore radius (R) and pore occupancy/length ratio (epsilon/L) calculated from the apparent permeability coefficients (P(app)) of CF and FD4 are discussed. Ethylenediaminetetraacetic acid (EDTA) increased the R of the caco-2 cell monolayer and the P(app) of all compounds examined was markedly increased by the addition of EDTA. On the other hand, EG and SG did not increase R and their enhancing effects were not as strong as those of EDTA. The increase in epsilon/L could be the enhancing mechanism for the cationized gelatins. The number of pathways for water-soluble drugs, such as CF and FD4, in the caco-2 monolayers could be increased by the addition of the cationized gelatins. The ratios of the permeability coefficients of insulin (observed/calculated based on the Renkin function) sug...Continue Reading

References

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Citations

Nov 5, 2010·Biological & Pharmaceutical Bulletin·Toshinobu SekiYasunori Morimoto
Sep 9, 2010·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Toshinobu Seki
Feb 8, 2011·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Toshinobu SekiYasunori Morimoto
Aug 19, 2007·Expert Opinion on Drug Metabolism & Toxicology·Florian NigschSilvia Miret
Jan 1, 2013·In Silico Pharmacology·Nadia Quignot
Sep 11, 2007·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Sumio Chono
Nov 23, 2007·Journal of Controlled Release : Official Journal of the Controlled Release Society·Toshinobu SekiKazuhiro Morimoto
Oct 16, 2007·Clinical Gastroenterology and Hepatology : the Official Clinical Practice Journal of the American Gastroenterological Association·Thomas D WangChristopher H Contag
Mar 10, 2007·International Journal of Pharmaceutics·Toshinobu SekiKazuhiro Morimoto
Nov 6, 2012·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Toshinobu Seki
Feb 11, 2015·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Sarah DugganHelen Hughes

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