Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake

Xiuying Li1, Dan Chen1, Chaoyi Le2, Chunliu Zhu1, Yong Gan1, Lars Hovgaard3, Mingshi Yang41Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China; 2University of Toronto Mississauga Campus, Ontario, Canada; 3Oral Formulation Development, Novo Nordisk A/S, Maalov; 4Departm...

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Autores principales:	Li X, Chen D, Le C, Zhu C, Gan Y, Hovgaard L, Yang M
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/8620bf8784e74021a35c8af127dac6f6
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spelling	oai:doaj.org-article:8620bf8784e74021a35c8af127dac6f62021-12-02T01:07:53ZNovel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake1176-91141178-2013https://doaj.org/article/8620bf8784e74021a35c8af127dac6f62011-12-01T00:00:00Zhttp://www.dovepress.com/novel-mucus-penetrating-liposomes-as-a-potential-oral-drug-delivery-sy-a8787https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Xiuying Li1, Dan Chen1, Chaoyi Le2, Chunliu Zhu1, Yong Gan1, Lars Hovgaard3, Mingshi Yang41Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China; 2University of Toronto Mississauga Campus, Ontario, Canada; 3Oral Formulation Development, Novo Nordisk A/S, Maalov; 4Department of Pharmaceutics and Analytical Chemistry, University of Copenhagen, Copenhagen, DenmarkBackground: The aim of this study was to investigate the intestinal mucus-penetrating properties and intestinal cellular uptake of two types of liposomes modified by Pluronic F127 (PF127).Methods: The two types of liposomes, ie, PF127-inlaid liposomes and PF127-adsorbed liposomes, were prepared by a thin-film hydration method followed by extrusion, in which coumarin 6 was loaded as a fluorescence marker. A modified Franz diffusion cell mounted with the intestinal mucus of rats was used to study the diffusion characteristics of the two types of PF127 liposomes. Cell uptake studies were conducted in Caco-2 cells and analyzed using confocal laser scanning microcopy as well as flow cytometry.Results: The diffusion efficiency of the two types of PF127-modified liposomes through intestinal rat mucus was 5&ndash;7-fold higher than that of unmodified liposomes. Compared with unmodified liposomes, PF127-inlaid liposomes showed significantly higher cellular uptake of courmarin 6. PF127-adsorbed liposomes showed a lower cellular uptake. Moreover, and interestingly, the two types of PF127-modified liposomes showed different cellular uptake mechanisms in Caco-2 cells.Conclusion: PF127-inlaid liposomes with improved intestinal mucus-penetrating ability and enhanced cellular uptake might be a potential carrier candidate for oral drug delivery.Keywords: Pluronic F127, mucus-penetrating, particles, liposomes, oral drug deliveryLi XChen DLe CZhu CGan YHovgaard LYang MDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 3151-3162 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Li X Chen D Le C Zhu C Gan Y Hovgaard L Yang M Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake
description	Xiuying Li1, Dan Chen1, Chaoyi Le2, Chunliu Zhu1, Yong Gan1, Lars Hovgaard3, Mingshi Yang41Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China; 2University of Toronto Mississauga Campus, Ontario, Canada; 3Oral Formulation Development, Novo Nordisk A/S, Maalov; 4Department of Pharmaceutics and Analytical Chemistry, University of Copenhagen, Copenhagen, DenmarkBackground: The aim of this study was to investigate the intestinal mucus-penetrating properties and intestinal cellular uptake of two types of liposomes modified by Pluronic F127 (PF127).Methods: The two types of liposomes, ie, PF127-inlaid liposomes and PF127-adsorbed liposomes, were prepared by a thin-film hydration method followed by extrusion, in which coumarin 6 was loaded as a fluorescence marker. A modified Franz diffusion cell mounted with the intestinal mucus of rats was used to study the diffusion characteristics of the two types of PF127 liposomes. Cell uptake studies were conducted in Caco-2 cells and analyzed using confocal laser scanning microcopy as well as flow cytometry.Results: The diffusion efficiency of the two types of PF127-modified liposomes through intestinal rat mucus was 5&ndash;7-fold higher than that of unmodified liposomes. Compared with unmodified liposomes, PF127-inlaid liposomes showed significantly higher cellular uptake of courmarin 6. PF127-adsorbed liposomes showed a lower cellular uptake. Moreover, and interestingly, the two types of PF127-modified liposomes showed different cellular uptake mechanisms in Caco-2 cells.Conclusion: PF127-inlaid liposomes with improved intestinal mucus-penetrating ability and enhanced cellular uptake might be a potential carrier candidate for oral drug delivery.Keywords: Pluronic F127, mucus-penetrating, particles, liposomes, oral drug delivery
format	article
author	Li X Chen D Le C Zhu C Gan Y Hovgaard L Yang M
author_facet	Li X Chen D Le C Zhu C Gan Y Hovgaard L Yang M
author_sort	Li X
title	Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake
title_short	Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake
title_full	Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake
title_fullStr	Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake
title_full_unstemmed	Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake
title_sort	novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/8620bf8784e74021a35c8af127dac6f6
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Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake

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