Octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components to enhance tumor targeting and hepatoma therapy

Ding Qu,1,2 Mingjian Liu,1 Mengmeng Huang,1,2 Lixiang Wang,1 Yan Chen,1,2 Congyan Liu,1,2 Yuping Liu1,2 1Research Center for Multicomponent Traditional Medicine and Microecology, Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, 2Res...

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Autores principales:	Qu D, Liu M, Huang M, Wang L, Chen Y, Liu C, Liu Y
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	Coix seed oil coixan multicomponent-based microemulsion hepatic targeting anti-hepatoma oral drug delivery system Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/7c5f9460a31a4e95bd78eba89ca47139
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spelling	oai:doaj.org-article:7c5f9460a31a4e95bd78eba89ca471392021-12-02T00:07:19ZOctanoyl galactose ester-modified microemulsion system self-assembled by coix seed components to enhance tumor targeting and hepatoma therapy1178-2013https://doaj.org/article/7c5f9460a31a4e95bd78eba89ca471392017-03-01T00:00:00Zhttps://www.dovepress.com/octanoyl-galactose-ester-modified-microemulsion-system-self-assembled--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Ding Qu,1,2 Mingjian Liu,1 Mengmeng Huang,1,2 Lixiang Wang,1 Yan Chen,1,2 Congyan Liu,1,2 Yuping Liu1,2 1Research Center for Multicomponent Traditional Medicine and Microecology, Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, 2Research Center for Multicomponent Traditional Medicine and Microecology, Jiangsu Provincial Academy of Traditional Chinese Medicine, Nanjing, People’s Republic of China Abstract: A nanosized drug delivery platform with a combination of rational components and tumor targeting is significant for enhancement of anticancer therapy and reduction of side effects. In this study, we developed a octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components (Gal(oct)-C-MEs), which improved the tumor accumulation through asialoglycoprotein receptor-mediated endocytosis and promoted the antitumor efficacy through multicomponent-mediated synergistic effect. Octanoyl galactose ester (Gal(oct)) with a yield of 82.3% was synthesized through a green enzymatic reaction and multidimensional characterization. Gal(oct)-C-MEs with a spherical shape had a small and uniform particle size (58.49±1.03 nm), narrow polydispersity index (0.09±0.01) and neutral surface charge (-5.82±0.57 mV). In the cellular uptake studies, the internalized Gal(oct)-C-ME was 2.28-fold higher relative to that of coix seed component-based microemulsions (C-MEs). The half-maximal inhibitory concentration of Gal(oct)-C-MEs against HepG2 cells was 46.5±2.4 µg/mL, which was notably higher than that of C-MEs. Importantly, the intratumor fluorescence of HepG2 xenograft-bearing nude mice treated with Cy5/Gal(oct)-C-MEs was 1.9-fold higher relative to treatment with Cy5/C-MEs. In the study of antitumor efficacy in vivo, HepG2 xenograft-bearing nude mice intragastrically administered Gal(oct)-C-MEs for 14 days exhibited the strongest inhibition of tumor growth and the lowest toxicity against liver and kidney among all the treatments. In summary, Gal(oct)-C-ME, as a highly effective and safe anticancer drug delivery system, showed promising potential for hepatoma therapy. Keywords: coix seed oil, coixan, multicomponent-based microemulsion, hepatic targeting, antihepatoma, oral drug delivery systemQu DLiu MHuang MWang LChen YLiu CLiu YDove Medical PressarticleCoix seed oilcoixanmulticomponent-based microemulsionhepatic targetinganti-hepatomaoral drug delivery systemMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 2045-2059 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Coix seed oil coixan multicomponent-based microemulsion hepatic targeting anti-hepatoma oral drug delivery system Medicine (General) R5-920
spellingShingle	Coix seed oil coixan multicomponent-based microemulsion hepatic targeting anti-hepatoma oral drug delivery system Medicine (General) R5-920 Qu D Liu M Huang M Wang L Chen Y Liu C Liu Y Octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components to enhance tumor targeting and hepatoma therapy
description	Ding Qu,1,2 Mingjian Liu,1 Mengmeng Huang,1,2 Lixiang Wang,1 Yan Chen,1,2 Congyan Liu,1,2 Yuping Liu1,2 1Research Center for Multicomponent Traditional Medicine and Microecology, Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, 2Research Center for Multicomponent Traditional Medicine and Microecology, Jiangsu Provincial Academy of Traditional Chinese Medicine, Nanjing, People’s Republic of China Abstract: A nanosized drug delivery platform with a combination of rational components and tumor targeting is significant for enhancement of anticancer therapy and reduction of side effects. In this study, we developed a octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components (Gal(oct)-C-MEs), which improved the tumor accumulation through asialoglycoprotein receptor-mediated endocytosis and promoted the antitumor efficacy through multicomponent-mediated synergistic effect. Octanoyl galactose ester (Gal(oct)) with a yield of 82.3% was synthesized through a green enzymatic reaction and multidimensional characterization. Gal(oct)-C-MEs with a spherical shape had a small and uniform particle size (58.49±1.03 nm), narrow polydispersity index (0.09±0.01) and neutral surface charge (-5.82±0.57 mV). In the cellular uptake studies, the internalized Gal(oct)-C-ME was 2.28-fold higher relative to that of coix seed component-based microemulsions (C-MEs). The half-maximal inhibitory concentration of Gal(oct)-C-MEs against HepG2 cells was 46.5±2.4 µg/mL, which was notably higher than that of C-MEs. Importantly, the intratumor fluorescence of HepG2 xenograft-bearing nude mice treated with Cy5/Gal(oct)-C-MEs was 1.9-fold higher relative to treatment with Cy5/C-MEs. In the study of antitumor efficacy in vivo, HepG2 xenograft-bearing nude mice intragastrically administered Gal(oct)-C-MEs for 14 days exhibited the strongest inhibition of tumor growth and the lowest toxicity against liver and kidney among all the treatments. In summary, Gal(oct)-C-ME, as a highly effective and safe anticancer drug delivery system, showed promising potential for hepatoma therapy. Keywords: coix seed oil, coixan, multicomponent-based microemulsion, hepatic targeting, antihepatoma, oral drug delivery system
format	article
author	Qu D Liu M Huang M Wang L Chen Y Liu C Liu Y
author_facet	Qu D Liu M Huang M Wang L Chen Y Liu C Liu Y
author_sort	Qu D
title	Octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components to enhance tumor targeting and hepatoma therapy
title_short	Octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components to enhance tumor targeting and hepatoma therapy
title_full	Octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components to enhance tumor targeting and hepatoma therapy
title_fullStr	Octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components to enhance tumor targeting and hepatoma therapy
title_full_unstemmed	Octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components to enhance tumor targeting and hepatoma therapy
title_sort	octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components to enhance tumor targeting and hepatoma therapy
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/7c5f9460a31a4e95bd78eba89ca47139
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Octanoyl galactose ester-modified microemulsion system self-assembled by coix seed components to enhance tumor targeting and hepatoma therapy

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