Nebulized coenzyme Q<inf>10</inf> nanosuspensions: A versatile approach for pulmonary antioxidant therapy

Rossi, I; Sonvico, F; McConville, JT; Rossi, F; Fröhlich, E; Zellnitz, S; Rossi, A; Del Favero, E; Bettini, R; Buttini, F

Nebulized coenzyme Q<inf>10</inf> nanosuspensions: A versatile approach for pulmonary antioxidant therapy

Rossi, I Sonvico, F

McConville, JT Rossi, F Fröhlich, E Zellnitz, S Rossi, A Del Favero, E Bettini, R Buttini, F

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Publication Type:: Journal Article
Citation:: European Journal of Pharmaceutical Sciences, 2018, 113 pp. 159 - 170
Issue Date:: 2018-02-15

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Field	Value	Language
dc.contributor.author	Rossi, I	en_US
dc.contributor.author	Sonvico, F https://orcid.org/0000-0001-7372-1456	en_US
dc.contributor.author	McConville, JT	en_US
dc.contributor.author	Rossi, F	en_US
dc.contributor.author	Fröhlich, E	en_US
dc.contributor.author	Zellnitz, S	en_US
dc.contributor.author	Rossi, A	en_US
dc.contributor.author	Del Favero, E	en_US
dc.contributor.author	Bettini, R	en_US
dc.contributor.author	Buttini, F	en_US
dc.date.available	2017-10-16	en_US
dc.date.issued	2018-02-15	en_US
dc.identifier.citation	European Journal of Pharmaceutical Sciences, 2018, 113 pp. 159 - 170	en_US
dc.identifier.issn	0928-0987	en_US
dc.identifier.uri	http://hdl.handle.net/10453/128321
dc.description.abstract	© 2017 Elsevier B.V. Coenzyme Q10 (CoQ10) is an antioxidant substance indicated as a dietary supplement which has been proposed as adjuvant in the treatment of cardiovascular disorders and cancer for its protective and immunostimulating activities. The aim of this work was the production by high-pressure homogenization, characterization and stability investigation of three different CoQ10 nanosuspensions designed to be administered to the lungs by nebulization. Three surfactants, i.e. lecithin, PEG32 stearate and vitamin-E TPGS, were selected to stabilize CoQ10 formulations. Preparations were identified as nanosuspensions (particle size in the range 35–60 nm): the smallest particles were obtained with vitamin-E TPGS and denoted a core-shell structure. The CoQ10 delivered from a commercial air-jet nebulizer was in all the cases around 30% of the loaded dose. The nanosuspension containing PEG32 stearate presented the highest respirable fraction (70.6%) and smallest MMAD (3.02 μm). Stability tests showed that the most stable formulation, after 90 days, was the one containing vitamin-E TPGS, followed by the CoQ10-lecithin formulation. Interestingly, those formulations were demonstrated to be suitable also for nebulizers using other mechanisms of aerosol production such as ultrasound and vibrating mesh nebulizers. Studies focused on in vitro cellular toxicity of the formulations and their single components using A549 human lung cells showed no obvious cytotoxicity for the formulations containing lecithin and PEG 32 stearate. Vitamin-E TPGS alone was shown to be able to damage the plasma membrane, nevertheless, cell damage was decreased when vitamin-E TPGS was present in the formulation with CoQ10.	en_US
dc.relation.ispartof	European Journal of Pharmaceutical Sciences	en_US
dc.relation.isbasedon	10.1016/j.ejps.2017.10.024	en_US
dc.subject.classification	Pharmacology & Pharmacy	en_US
dc.subject.mesh	Lung	en_US
dc.subject.mesh	Humans	en_US
dc.subject.mesh	Ubiquinone	en_US
dc.subject.mesh	Vitamin E	en_US
dc.subject.mesh	Stearates	en_US
dc.subject.mesh	Aerosols	en_US
dc.subject.mesh	Antioxidants	en_US
dc.subject.mesh	Drug Delivery Systems	en_US
dc.subject.mesh	Calibration	en_US
dc.subject.mesh	Drug Stability	en_US
dc.subject.mesh	Nebulizers and Vaporizers	en_US
dc.subject.mesh	Cell Survival	en_US
dc.subject.mesh	Biological Transport	en_US
dc.subject.mesh	Chemistry, Pharmaceutical	en_US
dc.subject.mesh	Particle Size	en_US
dc.subject.mesh	Surface Properties	en_US
dc.subject.mesh	Viscosity	en_US
dc.subject.mesh	Nanoparticles	en_US
dc.subject.mesh	Lecithins	en_US
dc.subject.mesh	Drug Liberation	en_US
dc.subject.mesh	A549 Cells	en_US
dc.title	Nebulized coenzyme Q<inf>10</inf> nanosuspensions: A versatile approach for pulmonary antioxidant therapy	en_US
dc.type	Journal Article
utslib.citation.volume	113	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/Graduate School of Health
utslib.copyright.status	closed_access
pubs.publication-status	Published	en_US
pubs.volume	113	en_US

Abstract:

© 2017 Elsevier B.V. Coenzyme Q10 (CoQ10) is an antioxidant substance indicated as a dietary supplement which has been proposed as adjuvant in the treatment of cardiovascular disorders and cancer for its protective and immunostimulating activities. The aim of this work was the production by high-pressure homogenization, characterization and stability investigation of three different CoQ10 nanosuspensions designed to be administered to the lungs by nebulization. Three surfactants, i.e. lecithin, PEG32 stearate and vitamin-E TPGS, were selected to stabilize CoQ10 formulations. Preparations were identified as nanosuspensions (particle size in the range 35–60 nm): the smallest particles were obtained with vitamin-E TPGS and denoted a core-shell structure. The CoQ10 delivered from a commercial air-jet nebulizer was in all the cases around 30% of the loaded dose. The nanosuspension containing PEG32 stearate presented the highest respirable fraction (70.6%) and smallest MMAD (3.02 μm). Stability tests showed that the most stable formulation, after 90 days, was the one containing vitamin-E TPGS, followed by the CoQ10-lecithin formulation. Interestingly, those formulations were demonstrated to be suitable also for nebulizers using other mechanisms of aerosol production such as ultrasound and vibrating mesh nebulizers. Studies focused on in vitro cellular toxicity of the formulations and their single components using A549 human lung cells showed no obvious cytotoxicity for the formulations containing lecithin and PEG 32 stearate. Vitamin-E TPGS alone was shown to be able to damage the plasma membrane, nevertheless, cell damage was decreased when vitamin-E TPGS was present in the formulation with CoQ10.

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http://hdl.handle.net/10453/128321