Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble Formulation

Therapeutic applications of coenzyme Q10 (CoQ10) are greatly limited by its lack of solubility in aqueous media. In this study, polyethylene glycol monostearate (stPEG) was used to construct micelles containing CoQ10 as a new formulation. The micellar formulations (stPEG/CoQ10) were prepared using f...

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Main Authors: Kengo Banshoya, Tetsuya Nakamura, Tetsuro Tanaka, Yoshiharu Kaneo
Format: Article
Language:English
Published: MDPI AG 2020-01-01
Series:Antioxidants
Subjects:
Online Access:https://www.mdpi.com/2076-3921/9/1/86
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author Kengo Banshoya
Tetsuya Nakamura
Tetsuro Tanaka
Yoshiharu Kaneo
author_facet Kengo Banshoya
Tetsuya Nakamura
Tetsuro Tanaka
Yoshiharu Kaneo
author_sort Kengo Banshoya
collection DOAJ
description Therapeutic applications of coenzyme Q10 (CoQ10) are greatly limited by its lack of solubility in aqueous media. In this study, polyethylene glycol monostearate (stPEG) was used to construct micelles containing CoQ10 as a new formulation. The micellar formulations (stPEG/CoQ10) were prepared using five types of stPEG with 10, 25, 40, 55, and 140 PEG repeat units, respectively. The micellar preparation was simple, consisting of only stPEG and CoQ10. Next, we compared the physical properties and blood circulation of these micelles. The CoQ10 load of this formulation was approximately 15 <i>w/w</i>%. Based on the dynamic light scattering method, the average molecular size of the stPEG/CoQ10 micelles was approximately 15 to 60 nm. The zeta potentials of these micelles were approximately &#8722;10 to &#8722;25 mV. The micelles using stPEG25, 40, and 55 demonstrated high solubility in water. Furthermore, these micelles had in vitro antioxidant activity. On comparing the blood circulation of micelles using stPEG25, 40, 55, and 140, micelles using stPEG55 had a significantly higher circulation in blood. The stPEG55/CoQ10 micelle demonstrated a protective effect against acetaminophen-induced liver injury in mice. In conclusion, these data indicate that the intravenous administration of the stPEG/CoQ10 micellar aqueous formulation is of great value against oxidant stress.
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spelling doaj.art-fd672b59fab04553b3f5bf59fd1837a32023-09-02T19:48:58ZengMDPI AGAntioxidants2076-39212020-01-01918610.3390/antiox9010086antiox9010086Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble FormulationKengo Banshoya0Tetsuya Nakamura1Tetsuro Tanaka2Yoshiharu Kaneo3Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Gakuen-cho 1, Fukuyama, Hiroshima 729-0292, JapanFaculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Gakuen-cho 1, Fukuyama, Hiroshima 729-0292, JapanFaculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Gakuen-cho 1, Fukuyama, Hiroshima 729-0292, JapanFaculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Gakuen-cho 1, Fukuyama, Hiroshima 729-0292, JapanTherapeutic applications of coenzyme Q10 (CoQ10) are greatly limited by its lack of solubility in aqueous media. In this study, polyethylene glycol monostearate (stPEG) was used to construct micelles containing CoQ10 as a new formulation. The micellar formulations (stPEG/CoQ10) were prepared using five types of stPEG with 10, 25, 40, 55, and 140 PEG repeat units, respectively. The micellar preparation was simple, consisting of only stPEG and CoQ10. Next, we compared the physical properties and blood circulation of these micelles. The CoQ10 load of this formulation was approximately 15 <i>w/w</i>%. Based on the dynamic light scattering method, the average molecular size of the stPEG/CoQ10 micelles was approximately 15 to 60 nm. The zeta potentials of these micelles were approximately &#8722;10 to &#8722;25 mV. The micelles using stPEG25, 40, and 55 demonstrated high solubility in water. Furthermore, these micelles had in vitro antioxidant activity. On comparing the blood circulation of micelles using stPEG25, 40, 55, and 140, micelles using stPEG55 had a significantly higher circulation in blood. The stPEG55/CoQ10 micelle demonstrated a protective effect against acetaminophen-induced liver injury in mice. In conclusion, these data indicate that the intravenous administration of the stPEG/CoQ10 micellar aqueous formulation is of great value against oxidant stress.https://www.mdpi.com/2076-3921/9/1/86coenzyme q10polyethylene glycol monostearatewater-solublemicellar formulationoxidative stress
spellingShingle Kengo Banshoya
Tetsuya Nakamura
Tetsuro Tanaka
Yoshiharu Kaneo
Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble Formulation
Antioxidants
coenzyme q10
polyethylene glycol monostearate
water-soluble
micellar formulation
oxidative stress
title Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble Formulation
title_full Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble Formulation
title_fullStr Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble Formulation
title_full_unstemmed Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble Formulation
title_short Coenzyme Q10-Polyethylene Glycol Monostearate Nanoparticles: An Injectable Water-Soluble Formulation
title_sort coenzyme q10 polyethylene glycol monostearate nanoparticles an injectable water soluble formulation
topic coenzyme q10
polyethylene glycol monostearate
water-soluble
micellar formulation
oxidative stress
url https://www.mdpi.com/2076-3921/9/1/86
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AT tetsuyanakamura coenzymeq10polyethyleneglycolmonostearatenanoparticlesaninjectablewatersolubleformulation
AT tetsurotanaka coenzymeq10polyethyleneglycolmonostearatenanoparticlesaninjectablewatersolubleformulation
AT yoshiharukaneo coenzymeq10polyethyleneglycolmonostearatenanoparticlesaninjectablewatersolubleformulation