Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect

Juntao Yin,1 Yantao Hou,2 Xiaoyong Song,3 Peiqing Wang,1 Yang Li11Department of Pharmaceutics, Huaihe Hospital Affiliated to Henan University, Kaifeng, People’s Republic of China; 2Henan Vocational College of Applied Technology, Kaifeng, People’s Republic of China; 3School of Pha...

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Autores principales:	Yin J, Hou Y, Song X, Wang P, Li Y
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Quercetin polymer-lipid hybrid nanoparticles bile salt bioavailability leukemia Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/32b890ad8d694a898e78fbaf171553a3
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spelling	oai:doaj.org-article:32b890ad8d694a898e78fbaf171553a32021-12-02T04:33:55ZCholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect1178-2013https://doaj.org/article/32b890ad8d694a898e78fbaf171553a32019-05-01T00:00:00Zhttps://www.dovepress.com/cholate-modified-polymer-lipid-hybrid-nanoparticles-for-oral-delivery--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Juntao Yin,1 Yantao Hou,2 Xiaoyong Song,3 Peiqing Wang,1 Yang Li11Department of Pharmaceutics, Huaihe Hospital Affiliated to Henan University, Kaifeng, People’s Republic of China; 2Henan Vocational College of Applied Technology, Kaifeng, People’s Republic of China; 3School of Pharmacy, Henan University, Kaifeng, People’s Republic of ChinaBackground: Quercetin (QUE) shows a potential antileukemic activity, but possesses poor solubility and low bioavailability.Purpose: This article explored the bile salt transport pathway for oral deliver of QUE using cholate-modified polymer-lipid hybrid nanoparticles (cPLNs) aiming to enhance its antileukemic effect.Methods: QUE-loaded cPLNs (QUE-cPLNs) were developed through a nanoprecipitation technique and characterized by particle size, entrapment efficiency (EE), microscopic morphology and in vitro drug release. In vitro cellular uptake and cytotoxicity of QUE-cPLNs were examined on Caco-2 and P388 cells; in vivo pharmacokinetics and antileukemic effect were evaluated using Sprague Dawley rats and leukemic model mice, respectively.Results: The prepared QUE-cPLNs possessed a particle size of 110 nm around with an EE of 96.22%. QUE-cPLNs resulted in significantly enhanced bioavailability of QUE, up to 375.12% relative to the formulation of suspensions. In addition, QUE-cPLNs exhibited excellent cellular uptake and internalization capability compared to cholate-free QUE-PLNs. The in vitro cytotoxic and in vivo antileukemic effects of QUE-cPLNs were also signally superior to free QUE and QUE-PLNs.Conclusion: These findings indicate that cPLNs are a promising nanocarrier able to improve the oral bioavailability and therapeutic index of QUE.Keywords: quercetin, polymer-lipid hybrid nanoparticles, bile salt, bioavailability, leukemiaYin JHou YSong XWang PLi YDove Medical PressarticleQuercetinpolymer-lipid hybrid nanoparticlesbile saltbioavailabilityleukemiaMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 4045-4057 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Quercetin polymer-lipid hybrid nanoparticles bile salt bioavailability leukemia Medicine (General) R5-920
spellingShingle	Quercetin polymer-lipid hybrid nanoparticles bile salt bioavailability leukemia Medicine (General) R5-920 Yin J Hou Y Song X Wang P Li Y Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect
description	Juntao Yin,1 Yantao Hou,2 Xiaoyong Song,3 Peiqing Wang,1 Yang Li11Department of Pharmaceutics, Huaihe Hospital Affiliated to Henan University, Kaifeng, People’s Republic of China; 2Henan Vocational College of Applied Technology, Kaifeng, People’s Republic of China; 3School of Pharmacy, Henan University, Kaifeng, People’s Republic of ChinaBackground: Quercetin (QUE) shows a potential antileukemic activity, but possesses poor solubility and low bioavailability.Purpose: This article explored the bile salt transport pathway for oral deliver of QUE using cholate-modified polymer-lipid hybrid nanoparticles (cPLNs) aiming to enhance its antileukemic effect.Methods: QUE-loaded cPLNs (QUE-cPLNs) were developed through a nanoprecipitation technique and characterized by particle size, entrapment efficiency (EE), microscopic morphology and in vitro drug release. In vitro cellular uptake and cytotoxicity of QUE-cPLNs were examined on Caco-2 and P388 cells; in vivo pharmacokinetics and antileukemic effect were evaluated using Sprague Dawley rats and leukemic model mice, respectively.Results: The prepared QUE-cPLNs possessed a particle size of 110 nm around with an EE of 96.22%. QUE-cPLNs resulted in significantly enhanced bioavailability of QUE, up to 375.12% relative to the formulation of suspensions. In addition, QUE-cPLNs exhibited excellent cellular uptake and internalization capability compared to cholate-free QUE-PLNs. The in vitro cytotoxic and in vivo antileukemic effects of QUE-cPLNs were also signally superior to free QUE and QUE-PLNs.Conclusion: These findings indicate that cPLNs are a promising nanocarrier able to improve the oral bioavailability and therapeutic index of QUE.Keywords: quercetin, polymer-lipid hybrid nanoparticles, bile salt, bioavailability, leukemia
format	article
author	Yin J Hou Y Song X Wang P Li Y
author_facet	Yin J Hou Y Song X Wang P Li Y
author_sort	Yin J
title	Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect
title_short	Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect
title_full	Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect
title_fullStr	Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect
title_full_unstemmed	Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect
title_sort	cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/32b890ad8d694a898e78fbaf171553a3
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Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect

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