Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia

Laurent Salade,1 Nathalie Wauthoz,1 Magali Deleu,2 Marjorie Vermeersch,3 Carine De Vriese,1 Karim Amighi,1 Jonathan Goole1 1Laboratoire de Pharmacie Galénique et de Biopharmacie, Université libre de Bruxelles (ULB), Brussels, 2Laboratoire de Biophysique Moléculaire...

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Autores principales:	Salade L, Wauthoz N, Deleu M, Vermeersch M, De Vriese C, Amighi K, Goole J
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	nasal delivery peptide liposome cachexia brain targeting enzyme Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/43df0d7b81cf490ea7e7369108916880
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spelling	oai:doaj.org-article:43df0d7b81cf490ea7e73691089168802021-12-02T03:03:56ZDevelopment of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia1178-2013https://doaj.org/article/43df0d7b81cf490ea7e73691089168802017-11-01T00:00:00Zhttps://www.dovepress.com/development-of-coated-liposomes-loaded-with-ghrelin-for-nose-to-brain--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Laurent Salade,1 Nathalie Wauthoz,1 Magali Deleu,2 Marjorie Vermeersch,3 Carine De Vriese,1 Karim Amighi,1 Jonathan Goole1 1Laboratoire de Pharmacie Galénique et de Biopharmacie, Université libre de Bruxelles (ULB), Brussels, 2Laboratoire de Biophysique Moléculaire aux Interfaces, Gembloux Agro-Bio Tech, Université de Liège, Gembloux, 3Centre for Microscopy and Molecular Imaging (CMMI), Charleroi, Belgium Abstract: The aim of the present study was to develop a ghrelin-containing formulation based on liposomes coated with chitosan intended for nose–brain delivery for the treatment of cachexia. Among the three types of liposomes developed, anionic liposomes provided the best results in terms of encapsulation efficiency (56%) and enzymatic protection against trypsin (20.6% vs 0% for ghrelin alone) and carboxylesterase (81.6% vs 17.2% for ghrelin alone). Ghrelin presented both electrostatic and hydrophobic interactions with the anionic lipid bilayer, as demonstrated by isothermal titration calorimetry. Then, anionic liposomes were coated with N-(2-hydroxy)propyl-3-trimethyl ammonium chitosan chloride. The coating involved a size increment from 146.9±2.7 to 194±6.1 nm, for uncoated and coated liposomes, respectively. The ζ-potential was similarly increased from -0.3±1.2 mV to 6±0.4 mV before and after coating, respectively. Chitosan provided mucoadhesion, with an increase in mucin adsorption of 22.9%. Enhancement of permeation through the Calu3 epithelial monolayer was also observed with 10.8% of ghrelin recovered in the basal compartment in comparison to 0% for ghrelin alone. Finally, aerosols generated from two nasal devices (VP3 and SP270) intended for aqueous dispersion were characterized with either coated or uncoated liposomes. Contrarily to the SP270 device, VP3 device showed minor changes between coated and uncoated liposome aerosols, as shown by their median volume diameters of 38.4±5.76 and 37.6±5.74 µm, respectively. Overall, the results obtained in this study show that the developed formulation delivered by the VP3 device can be considered as a potential candidate for nose–brain delivery of ghrelin. Keywords: nasal delivery, peptide, liposome, cachexia, brain targeting, enzymeSalade LWauthoz NDeleu MVermeersch MDe Vriese CAmighi KGoole JDove Medical Pressarticlenasal deliverypeptideliposomecachexiabrain targetingenzymeMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 8531-8543 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	nasal delivery peptide liposome cachexia brain targeting enzyme Medicine (General) R5-920
spellingShingle	nasal delivery peptide liposome cachexia brain targeting enzyme Medicine (General) R5-920 Salade L Wauthoz N Deleu M Vermeersch M De Vriese C Amighi K Goole J Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia
description	Laurent Salade,1 Nathalie Wauthoz,1 Magali Deleu,2 Marjorie Vermeersch,3 Carine De Vriese,1 Karim Amighi,1 Jonathan Goole1 1Laboratoire de Pharmacie Galénique et de Biopharmacie, Université libre de Bruxelles (ULB), Brussels, 2Laboratoire de Biophysique Moléculaire aux Interfaces, Gembloux Agro-Bio Tech, Université de Liège, Gembloux, 3Centre for Microscopy and Molecular Imaging (CMMI), Charleroi, Belgium Abstract: The aim of the present study was to develop a ghrelin-containing formulation based on liposomes coated with chitosan intended for nose–brain delivery for the treatment of cachexia. Among the three types of liposomes developed, anionic liposomes provided the best results in terms of encapsulation efficiency (56%) and enzymatic protection against trypsin (20.6% vs 0% for ghrelin alone) and carboxylesterase (81.6% vs 17.2% for ghrelin alone). Ghrelin presented both electrostatic and hydrophobic interactions with the anionic lipid bilayer, as demonstrated by isothermal titration calorimetry. Then, anionic liposomes were coated with N-(2-hydroxy)propyl-3-trimethyl ammonium chitosan chloride. The coating involved a size increment from 146.9±2.7 to 194±6.1 nm, for uncoated and coated liposomes, respectively. The ζ-potential was similarly increased from -0.3±1.2 mV to 6±0.4 mV before and after coating, respectively. Chitosan provided mucoadhesion, with an increase in mucin adsorption of 22.9%. Enhancement of permeation through the Calu3 epithelial monolayer was also observed with 10.8% of ghrelin recovered in the basal compartment in comparison to 0% for ghrelin alone. Finally, aerosols generated from two nasal devices (VP3 and SP270) intended for aqueous dispersion were characterized with either coated or uncoated liposomes. Contrarily to the SP270 device, VP3 device showed minor changes between coated and uncoated liposome aerosols, as shown by their median volume diameters of 38.4±5.76 and 37.6±5.74 µm, respectively. Overall, the results obtained in this study show that the developed formulation delivered by the VP3 device can be considered as a potential candidate for nose–brain delivery of ghrelin. Keywords: nasal delivery, peptide, liposome, cachexia, brain targeting, enzyme
format	article
author	Salade L Wauthoz N Deleu M Vermeersch M De Vriese C Amighi K Goole J
author_facet	Salade L Wauthoz N Deleu M Vermeersch M De Vriese C Amighi K Goole J
author_sort	Salade L
title	Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia
title_short	Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia
title_full	Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia
title_fullStr	Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia
title_full_unstemmed	Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia
title_sort	development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/43df0d7b81cf490ea7e7369108916880
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Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia

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