Quercetin solid lipid microparticles: A flavonoid for inhalation lung delivery

Scalia, S; Haghi, M; Losi, V; Trotta, V; Young, PM; Traini, D

Quercetin solid lipid microparticles: A flavonoid for inhalation lung delivery

Scalia, S Haghi, M

Losi, V Trotta, V Young, PM

Traini, D

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Publication Type:: Journal Article
Citation:: European Journal of Pharmaceutical Sciences, 2013, 49 (2), pp. 278 - 285
Issue Date:: 2013-05-13

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Field	Value	Language
dc.contributor.author	Scalia, S	en_US
dc.contributor.author	Haghi, M https://orcid.org/0000-0002-3362-1845	en_US
dc.contributor.author	Losi, V	en_US
dc.contributor.author	Trotta, V	en_US
dc.contributor.author	Young, PM https://orcid.org/0000-0002-4357-7999	en_US
dc.contributor.author	Traini, D https://orcid.org/0000-0002-7173-017X	en_US
dc.date.available	2013-03-13	en_US
dc.date.issued	2013-05-13	en_US
dc.identifier.citation	European Journal of Pharmaceutical Sciences, 2013, 49 (2), pp. 278 - 285	en_US
dc.identifier.issn	0928-0987	en_US
dc.identifier.uri	http://hdl.handle.net/10453/115785
dc.description.abstract	Purpose The aim of the present work was to develop solid lipid microparticles (SLMs), as dry powders containing quercetin for direct administration to the lung. Methods Quercetin microparticles were prepared by o/w emulsification via a phase inversion technique, using tristearin as the lipid component and phosphatidylcholine as an emulsifier. The quercetin SLMs were characterised for morphology, drug loading (15.5% ± 0.6, which corresponded to an encapsulation efficiency of 71.4%), particle size distribution, response to humidity, crystallinity, thermal behaviour and in vitro respirable fraction. Furthermore, the toxicity and the in vitro transport of the SLMs on an air liquid interface model of the Calu-3 cell line were also investigated using a modified twin-stage impinger apparatus. Results Results showed that quercetin SLMs could be formulated as dry powder suitable for inhalation drug delivery (20.5 ± 3.3% fine particle fraction ≤4.46 μm) that was absorbed, via a linear kinetic model across the Calu-3 monolayer (22.32 ± 1.51% over 4 h). In addition, quercetin SLMs were shown to be non-toxic at the concentrations investigated. Interestingly, no apical to basolateral transport of the micronised quercetin was observed over the period of study. Conclusions These observations suggest quercetin diffusion was enhanced by the presence of the lipid/emulsifying excipients in the SLMs; however further studies are necessary to elucidate the exact mechanisms. © 2013 Elsevier B.V. All rights reserved.	en_US
dc.relation.ispartof	European Journal of Pharmaceutical Sciences	en_US
dc.relation.isbasedon	10.1016/j.ejps.2013.03.009	en_US
dc.subject.classification	Pharmacology & Pharmacy	en_US
dc.subject.mesh	Lung	en_US
dc.subject.mesh	Cell Line, Tumor	en_US
dc.subject.mesh	Humans	en_US
dc.subject.mesh	Quercetin	en_US
dc.subject.mesh	Triglycerides	en_US
dc.subject.mesh	Antioxidants	en_US
dc.subject.mesh	Drug Delivery Systems	en_US
dc.subject.mesh	Administration, Inhalation	en_US
dc.subject.mesh	Cell Survival	en_US
dc.subject.mesh	Biological Transport	en_US
dc.subject.mesh	Dry Powder Inhalers	en_US
dc.title	Quercetin solid lipid microparticles: A flavonoid for inhalation lung delivery	en_US
dc.type	Journal Article
utslib.citation.volume	2	en_US
utslib.citation.volume	49	en_US
utslib.for	1115 Pharmacology and Pharmaceutical Sciences	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Faculty of Science
pubs.organisational-group	/University of Technology Sydney/Faculty of Science/School of Mathematical and Physical Sciences
pubs.organisational-group	/University of Technology Sydney/Graduate School of Health
utslib.copyright.status	closed_access
pubs.issue	2	en_US
pubs.publication-status	Published	en_US
pubs.volume	49	en_US

Abstract:

Purpose The aim of the present work was to develop solid lipid microparticles (SLMs), as dry powders containing quercetin for direct administration to the lung. Methods Quercetin microparticles were prepared by o/w emulsification via a phase inversion technique, using tristearin as the lipid component and phosphatidylcholine as an emulsifier. The quercetin SLMs were characterised for morphology, drug loading (15.5% ± 0.6, which corresponded to an encapsulation efficiency of 71.4%), particle size distribution, response to humidity, crystallinity, thermal behaviour and in vitro respirable fraction. Furthermore, the toxicity and the in vitro transport of the SLMs on an air liquid interface model of the Calu-3 cell line were also investigated using a modified twin-stage impinger apparatus. Results Results showed that quercetin SLMs could be formulated as dry powder suitable for inhalation drug delivery (20.5 ± 3.3% fine particle fraction ≤4.46 μm) that was absorbed, via a linear kinetic model across the Calu-3 monolayer (22.32 ± 1.51% over 4 h). In addition, quercetin SLMs were shown to be non-toxic at the concentrations investigated. Interestingly, no apical to basolateral transport of the micronised quercetin was observed over the period of study. Conclusions These observations suggest quercetin diffusion was enhanced by the presence of the lipid/emulsifying excipients in the SLMs; however further studies are necessary to elucidate the exact mechanisms. © 2013 Elsevier B.V. All rights reserved.

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http://hdl.handle.net/10453/115785