Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery

Xiaoyu Chen, Wenhua Huang, Blenda Chi Kwan Wong, Linlin Yin, Yuen Fan Wong, Min Xu, Zhijun YangSchool of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong, Hong KongPurpose: The main objective of this study was to develop a novel aerosolized liposome formulation for pulmonary delivery of...

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Autores principales:	Chen X, Huang W, Kwan Wong BC, Yin L, Wong YF, Xu M, Yang Z
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/f3b9b8c836be479693bf9ca28ffe4554
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spelling	oai:doaj.org-article:f3b9b8c836be479693bf9ca28ffe45542021-12-02T01:04:05ZLiposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery1176-91141178-2013https://doaj.org/article/f3b9b8c836be479693bf9ca28ffe45542012-02-01T00:00:00Zhttp://www.dovepress.com/liposomes-prolong-the-therapeutic-effect-of-anti-asthmatic-medication--a9366https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Xiaoyu Chen, Wenhua Huang, Blenda Chi Kwan Wong, Linlin Yin, Yuen Fan Wong, Min Xu, Zhijun YangSchool of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong, Hong KongPurpose: The main objective of this study was to develop a novel aerosolized liposome formulation for pulmonary delivery of anti-asthmatic medication and to explore the relationship between the bioavailability and anti-asthmatic efficacy of such a formulation. Asthma treatment usually requires frequent administration of medication for sustained bronchodilating response. Liposomes are known for their capability for sustained drug release and thus would be a suitable delivery system for anti-asthmatic medication for prolonged therapeutic effect. Salbutamol sulfate (SBS) was chosen as the model drug in this study because of its high water solubility and fast absorption after administration.Methods: SBS was efficiently encapsulated into liposomes by the vesicular phospholipid gel technique. SBS permeability across the pulmonary membrane of an Asian toad was determined by in vitro study. Intratracheal administration of liposomes labeled with the fluorescent dye 1,1&#39;-dioctadecyltetramethyl indotricarbocyanine iodide (DiR) in a rat model was assessed by a small animal imaging system and pharmacokinetic analysis. Pharmacodynamic analysis was performed in guinea pigs using the Konzett&ndash;R&ouml;ssler method.Results: SBS was efficiently encapsulated into liposomes with encapsulation efficiency as high as 70%. The particle size of the SBS liposome suspension was approximately 57 &plusmn; 21 nm. In the in vitro study of permeability across the pulmonary membrane of Asian toads, SBS from liposomes demonstrated a slower transport rate compared to free SBS solution. Pulmonary delivery of liposomes in a rat model showed that the liposomes were effectively distributed in the respiratory tract and lungs, and that the release of SBS from liposomes was sustained for at least 48 hours. Pharmacodynamic analysis in a guinea pig model showed that the anti-asthmatic effect of SBS liposomes persisted for up to 18 hours, whereas that of free SBS solution was less than 8 hours.Conclusion: The overall results demonstrated that liposomes could increase the concentration and retention time of SBS in the lungs and therefore prolong its therapeutic effect.Keywords: salbutamol sulfate, asthma, intratracheal administration, sustained releaseChen XHuang WKwan Wong BCYin LWong YFXu MYang ZDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 1139-1148 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Chen X Huang W Kwan Wong BC Yin L Wong YF Xu M Yang Z Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery
description	Xiaoyu Chen, Wenhua Huang, Blenda Chi Kwan Wong, Linlin Yin, Yuen Fan Wong, Min Xu, Zhijun YangSchool of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong, Hong KongPurpose: The main objective of this study was to develop a novel aerosolized liposome formulation for pulmonary delivery of anti-asthmatic medication and to explore the relationship between the bioavailability and anti-asthmatic efficacy of such a formulation. Asthma treatment usually requires frequent administration of medication for sustained bronchodilating response. Liposomes are known for their capability for sustained drug release and thus would be a suitable delivery system for anti-asthmatic medication for prolonged therapeutic effect. Salbutamol sulfate (SBS) was chosen as the model drug in this study because of its high water solubility and fast absorption after administration.Methods: SBS was efficiently encapsulated into liposomes by the vesicular phospholipid gel technique. SBS permeability across the pulmonary membrane of an Asian toad was determined by in vitro study. Intratracheal administration of liposomes labeled with the fluorescent dye 1,1&#39;-dioctadecyltetramethyl indotricarbocyanine iodide (DiR) in a rat model was assessed by a small animal imaging system and pharmacokinetic analysis. Pharmacodynamic analysis was performed in guinea pigs using the Konzett&ndash;R&ouml;ssler method.Results: SBS was efficiently encapsulated into liposomes with encapsulation efficiency as high as 70%. The particle size of the SBS liposome suspension was approximately 57 &plusmn; 21 nm. In the in vitro study of permeability across the pulmonary membrane of Asian toads, SBS from liposomes demonstrated a slower transport rate compared to free SBS solution. Pulmonary delivery of liposomes in a rat model showed that the liposomes were effectively distributed in the respiratory tract and lungs, and that the release of SBS from liposomes was sustained for at least 48 hours. Pharmacodynamic analysis in a guinea pig model showed that the anti-asthmatic effect of SBS liposomes persisted for up to 18 hours, whereas that of free SBS solution was less than 8 hours.Conclusion: The overall results demonstrated that liposomes could increase the concentration and retention time of SBS in the lungs and therefore prolong its therapeutic effect.Keywords: salbutamol sulfate, asthma, intratracheal administration, sustained release
format	article
author	Chen X Huang W Kwan Wong BC Yin L Wong YF Xu M Yang Z
author_facet	Chen X Huang W Kwan Wong BC Yin L Wong YF Xu M Yang Z
author_sort	Chen X
title	Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery
title_short	Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery
title_full	Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery
title_fullStr	Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery
title_full_unstemmed	Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery
title_sort	liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/f3b9b8c836be479693bf9ca28ffe4554
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Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery

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