In vivo evaluation of an oral delivery system for P-gp substrates based on thiolated chitosan

Biomaterials
Florian FögerAndreas Bernkop-Schnürch

Abstract

Recently, thiolated polymers, so called thiomers, have been reported to modulate drug absorption by inhibition of intestinal P-glycoprotein (P-gp). The aim of the present study was to provide a proof-of-principle for a delivery system based on thiolated chitosan in vivo in rats, using rhodamine-123 (Rho-123) as representative P-gp substrate. In vitro, the permeation enhancing effect of unmodified chitosan, chitosan-4 thiobutylamidine (Ch-TBA) and the combination of Ch-TBA with reduced glutathione (GSH) was evaluated by using freshly excised rat intestinal mucosa mounted in Ussing-type chambers. In comparison to buffer only, Rho-123 transport in presence of 0.5% (w/v) chitosan, 0.5% (w/v) Ch-TBA and the combination of 0.5% (w/v) Ch-TBA/0.5% (w/v) GSH, was 1.8-fold, 2.6-fold, 3.8-fold improved, respectively. Furthermore, enteric-coated tablets based on unmodified chitosan or Ch-TBA/GSH, were investigated in vivo. In rats, the Ch-TBA/GSH tablets increased the area under the plasma concentration time curve (AUC0-12) of Rho-123 by 217% in comparison to buffer control and by 58% in comparison to unmodified chitosan. This in vivo study showed that a delivery system based on thiolated chitosan significantly increased the oral bioavaila...Continue Reading

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Citations

Sep 27, 2007·Pharmaceutical Research·Martin Werle
Apr 6, 2012·Archives of Pharmacal Research·Yu Kyung LeeYoung Hee Choi
Nov 30, 2012·Future Medicinal Chemistry·Flavia Laffleur, Andreas Bernkop-Schnürch
Jul 27, 2012·Therapeutic Delivery·Colin Thompson, Chidinma Ibie
Aug 25, 2007·Nanomedicine·Karin Albrecht, Andreas Bernkop-Schnürch
Dec 12, 2012·Advanced Drug Delivery Reviews·Taslim A Al-HilalYoungro Byun
Nov 20, 2012·Advanced Drug Delivery Reviews·Mei-Chin ChenHsing-Wen Sung
Oct 23, 2013·Future Medicinal Chemistry·Masoom YasinzaiGul Shahnaz
May 1, 2008·Expert Review of Clinical Pharmacology·Martin WerleAndreas Bernkop-Schnürch
Mar 17, 2007·Journal of Drug Targeting·Florian FögerAndreas Bernkop-Schnürch
May 29, 2012·Journal of Drug Targeting·Seung Woo ChungYoungro Byun
May 13, 2011·Drug Development and Industrial Pharmacy·Duangkamon SakloetsakunAndreas Bernkop-Schnürch
Feb 16, 2008·Journal of Drug Targeting·Florian FögerMartin Werle
Aug 21, 2015·Drug Development and Industrial Pharmacy·Kesinee NetsomboonA Bernkop-Schnürch
Nov 19, 2008·Drug Development and Industrial Pharmacy·Martin WerleHerbert Hoyer
Jun 19, 2012·Expert Opinion on Drug Delivery·Sabine Hauptstein, Andreas Bernkop-Schnürch
Aug 28, 2007·Journal of Pharmaceutical Sciences·Martin Werle
Sep 11, 2008·Journal of Pharmaceutical Sciences·Martin WerleAndreas Bernkop-Schnürch
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May 9, 2012·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Andreas Bernkop-Schnürch, Sarah Dünnhaupt
Jul 7, 2009·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Ylenia ZambitoGiacomo Di Colo
Apr 7, 2009·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Melanie GreindlAndreas Bernkop-Schnürch
Nov 6, 2007·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Juliane HombachAndreas Bernkop-Schnürch
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Oct 6, 2012·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Yu Kyung LeeYoung Hee Choi
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Feb 21, 2008·The Journal of Pharmacy and Pharmacology·Martin Werle, Andreas Bernkop-Schnürch
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Aug 11, 2015·Drug Development and Industrial Pharmacy·Kesinee NetsomboonA Bernkop-Schnürch

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