Chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties

Kerstin Gradauer,1 Caroline Vonach,1 Gerd Leitinger,2,3 Dagmar Kolb,2,3 Eleonore Fr&ouml;hlich,3 Eva Roblegg,4 Andreas Bernkop-Schn&uuml;rch,5 Ruth Prassl1,61Institute of Biophysics and Nanosystems Research, Austrian Academy of Sciences, Graz, Austria; 2Institute of Cell Biology, His...

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Autores principales:	Gradauer K, Vonach C, Leitinger G, Kolb D, Fr&ouml;hlich E, Roblegg E, Bernkop-Schn&uuml;rch A, Prassl R
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/e18309ade76a40a9b9e6118cadcb4d76
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spelling	oai:doaj.org-article:e18309ade76a40a9b9e6118cadcb4d762021-12-02T01:50:40ZChemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties1176-91141178-2013https://doaj.org/article/e18309ade76a40a9b9e6118cadcb4d762012-05-01T00:00:00Zhttp://www.dovepress.com/chemical-coupling-of-thiolated-chitosan-to-preformed-liposomes-improve-a9926https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Kerstin Gradauer,1 Caroline Vonach,1 Gerd Leitinger,2,3 Dagmar Kolb,2,3 Eleonore Fr&ouml;hlich,3 Eva Roblegg,4 Andreas Bernkop-Schn&uuml;rch,5 Ruth Prassl1,61Institute of Biophysics and Nanosystems Research, Austrian Academy of Sciences, Graz, Austria; 2Institute of Cell Biology, Histology, and Embryology, Medical University of Graz, Graz, Austria; 3Center for Medical Research, Medical University of Graz, Graz, Austria; 4Institute of Pharmaceutical Sciences/Pharmaceutical Technology, Karl-Franzens University, Graz, Austria; 5Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innsbruck, Austria; 6Ludwig Boltzmann Institute for Lung Vascular Research, Graz, AustriaAim: To develop mucoadhesive liposomes by anchoring the polymer chitosan-thioglycolic acid (chitosan-TGA) to the liposomal surface to target intestinal mucosal membranes.Methods: Liposomes consisting of phosphatidylcholine (POPC) and a maleimide-functionalized lipid were incubated with chitosan-TGA, leading to the formation of a thioether bond between free SH-groups of the polymer and maleimide groups of the liposome. Uncoated and newly generated thiomer-coated liposomes were characterized according to their size, zeta potential, and morphology using photon correlation spectroscopy and transmission electron microscopy. The release behavior of calcitonin and the fluorophore/quencher-couple ANTS/DPX (8-aminonaphthalene-1,3,6-trisulfonic acid/p-xylene-bis- pyridinium bromide) from coated and uncoated liposomes, was investigated over 24 hours in simulated gastric and intestinal fluids. To test the mucoadhesive properties of thiomer-coated and uncoated liposomes in-vitro, we used freshly excised porcine small intestine.Results: Liposomes showed a concentration-dependent increase in size &ndash; from approximately 167 nm for uncoated liposomes to 439 nm for the highest thiomer concentration used in this study. Likewise, their zeta potentials gradually increased from about &ndash;38 mV to +20 mV, clearly indicating an effective coupling of chitosan-TGA to the surface of liposomes. As a result of mucoadhesion tests, we found an almost two-fold increase in the mucoadhesion of coupled liposomes relative to uncoupled ones. With fluorescence microscopy, we saw a tight adherence of coated particles to the intestinal mucus.Conclusion: Taken together, our current results indicate that thiomer-coated liposomes possess a high potential to be used as an oral drug-delivery system.Keywords: thiomer, liposome, mucoadhesion, chitosan-thioglycolic acid, oral drug deliveryGradauer KVonach CLeitinger GKolb DFr&ouml;hlich ERoblegg EBernkop-Schn&uuml;rch APrassl RDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 2523-2534 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Gradauer K Vonach C Leitinger G Kolb D Fr&ouml;hlich E Roblegg E Bernkop-Schn&uuml;rch A Prassl R Chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties
description	Kerstin Gradauer,1 Caroline Vonach,1 Gerd Leitinger,2,3 Dagmar Kolb,2,3 Eleonore Fr&ouml;hlich,3 Eva Roblegg,4 Andreas Bernkop-Schn&uuml;rch,5 Ruth Prassl1,61Institute of Biophysics and Nanosystems Research, Austrian Academy of Sciences, Graz, Austria; 2Institute of Cell Biology, Histology, and Embryology, Medical University of Graz, Graz, Austria; 3Center for Medical Research, Medical University of Graz, Graz, Austria; 4Institute of Pharmaceutical Sciences/Pharmaceutical Technology, Karl-Franzens University, Graz, Austria; 5Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innsbruck, Austria; 6Ludwig Boltzmann Institute for Lung Vascular Research, Graz, AustriaAim: To develop mucoadhesive liposomes by anchoring the polymer chitosan-thioglycolic acid (chitosan-TGA) to the liposomal surface to target intestinal mucosal membranes.Methods: Liposomes consisting of phosphatidylcholine (POPC) and a maleimide-functionalized lipid were incubated with chitosan-TGA, leading to the formation of a thioether bond between free SH-groups of the polymer and maleimide groups of the liposome. Uncoated and newly generated thiomer-coated liposomes were characterized according to their size, zeta potential, and morphology using photon correlation spectroscopy and transmission electron microscopy. The release behavior of calcitonin and the fluorophore/quencher-couple ANTS/DPX (8-aminonaphthalene-1,3,6-trisulfonic acid/p-xylene-bis- pyridinium bromide) from coated and uncoated liposomes, was investigated over 24 hours in simulated gastric and intestinal fluids. To test the mucoadhesive properties of thiomer-coated and uncoated liposomes in-vitro, we used freshly excised porcine small intestine.Results: Liposomes showed a concentration-dependent increase in size &ndash; from approximately 167 nm for uncoated liposomes to 439 nm for the highest thiomer concentration used in this study. Likewise, their zeta potentials gradually increased from about &ndash;38 mV to +20 mV, clearly indicating an effective coupling of chitosan-TGA to the surface of liposomes. As a result of mucoadhesion tests, we found an almost two-fold increase in the mucoadhesion of coupled liposomes relative to uncoupled ones. With fluorescence microscopy, we saw a tight adherence of coated particles to the intestinal mucus.Conclusion: Taken together, our current results indicate that thiomer-coated liposomes possess a high potential to be used as an oral drug-delivery system.Keywords: thiomer, liposome, mucoadhesion, chitosan-thioglycolic acid, oral drug delivery
format	article
author	Gradauer K Vonach C Leitinger G Kolb D Fr&ouml;hlich E Roblegg E Bernkop-Schn&uuml;rch A Prassl R
author_facet	Gradauer K Vonach C Leitinger G Kolb D Fr&ouml;hlich E Roblegg E Bernkop-Schn&uuml;rch A Prassl R
author_sort	Gradauer K
title	Chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties
title_short	Chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties
title_full	Chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties
title_fullStr	Chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties
title_full_unstemmed	Chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties
title_sort	chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/e18309ade76a40a9b9e6118cadcb4d76
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Chemical coupling of thiolated chitosan to preformed liposomes improves mucoadhesive properties

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