Enhanced antitumor activity of realgar mediated by milling it to nanosize

Ye Tian,1 Xiaobo Wang,1,2 Ronggang Xi,1,2 Weisan Pan,1 Shuang Jiang,2 Zhao Li,1 Yu Zhao,3 Guanghui Gao,4 Dan Liu21Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, 2Department of Pharmacy, 210th Hospital of People's Liberation Army, Dalian, 3Department of Pharmaceut...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Tian Y, Wang XB, Xi RG, Pan WS, Jiang S, Li Z, Zhao Y, Gao GH, Liu D
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/efc211f9e92241cdb0a7dfbd9c1c2627
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:efc211f9e92241cdb0a7dfbd9c1c2627
record_format	dspace
spelling	oai:doaj.org-article:efc211f9e92241cdb0a7dfbd9c1c26272021-12-02T06:50:13ZEnhanced antitumor activity of realgar mediated by milling it to nanosize1178-2013https://doaj.org/article/efc211f9e92241cdb0a7dfbd9c1c26272014-01-01T00:00:00Zhttp://www.dovepress.com/enhanced-antitumor-activity-of-realgar-mediated-by-milling-it-to-nanos-a15688https://doaj.org/toc/1178-2013 Ye Tian,1 Xiaobo Wang,1,2 Ronggang Xi,1,2 Weisan Pan,1 Shuang Jiang,2 Zhao Li,1 Yu Zhao,3 Guanghui Gao,4 Dan Liu21Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, 2Department of Pharmacy, 210th Hospital of People's Liberation Army, Dalian, 3Department of Pharmaceutics, College of Pharmacy, Harbin Medical University, Harbin, 4Department of Laboratory Medicine, Liaoning Institute for Food and Drug Control, Shenyang, People's Republic of ChinaAbstract: Realgar is a poorly water-soluble compound that exhibits poor bioavailability. To improve this, the authors reduced the particle size of realgar to nanoscale by high-energy ball milling and optimized the preparation process under which (realgar weight 40 g, milling time 9 hours, milling speed 38 Hz, milling temperature -20°C) realgar nanoparticles (NPs) with an average size of 78±8.3 nm were prepared. The average particle size of realgar was characterized by laser scattering, and its apparent shape was observed by transmission electron microscopy and scanning electron microscopy. The solubility of realgar was enhanced after milling until the particles were in the nanoscale region without altering its properties, as confirmed by a scanning electron microscopy energy-dispersive spectrometer. Realgar NPs had higher cytotoxicity on the selected cell lines, namely human breast cancer (MCF7), human hepatoma (HepG2), and human lung cancer (A549) cell lines, than coarse realgar. In addition, a pharmacokinetics study performed in rats indicated that the relative bioavailability of realgar NPs was 216.9% compared with coarse realgar; a biodistribution study performed in mice showed that after intragastric administration of realgar NPs, higher arsenic concentration was reached in the tumor, heart, liver, spleen, lung, and kidney compared with the administration of coarse realgar, as confirmed by inductively coupled plasma mass spectrometry to determine the concentration of arsenic. This study indicated that high-energy ball milling is an effective way to reduce the average particle size of realgar, and compared with coarse realgar, the cytotoxicity and bioavailability of realgar NPs were significantly improved.Keywords: realgar nanoparticles, high-energy ball milling, cytotoxicity, pharmacokinetics, biodistributionTian YWang XBXi RGPan WSJiang SLi ZZhao YGao GHLiu DDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 745-757 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Tian Y Wang XB Xi RG Pan WS Jiang S Li Z Zhao Y Gao GH Liu D Enhanced antitumor activity of realgar mediated by milling it to nanosize
description	Ye Tian,1 Xiaobo Wang,1,2 Ronggang Xi,1,2 Weisan Pan,1 Shuang Jiang,2 Zhao Li,1 Yu Zhao,3 Guanghui Gao,4 Dan Liu21Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, 2Department of Pharmacy, 210th Hospital of People's Liberation Army, Dalian, 3Department of Pharmaceutics, College of Pharmacy, Harbin Medical University, Harbin, 4Department of Laboratory Medicine, Liaoning Institute for Food and Drug Control, Shenyang, People's Republic of ChinaAbstract: Realgar is a poorly water-soluble compound that exhibits poor bioavailability. To improve this, the authors reduced the particle size of realgar to nanoscale by high-energy ball milling and optimized the preparation process under which (realgar weight 40 g, milling time 9 hours, milling speed 38 Hz, milling temperature -20°C) realgar nanoparticles (NPs) with an average size of 78±8.3 nm were prepared. The average particle size of realgar was characterized by laser scattering, and its apparent shape was observed by transmission electron microscopy and scanning electron microscopy. The solubility of realgar was enhanced after milling until the particles were in the nanoscale region without altering its properties, as confirmed by a scanning electron microscopy energy-dispersive spectrometer. Realgar NPs had higher cytotoxicity on the selected cell lines, namely human breast cancer (MCF7), human hepatoma (HepG2), and human lung cancer (A549) cell lines, than coarse realgar. In addition, a pharmacokinetics study performed in rats indicated that the relative bioavailability of realgar NPs was 216.9% compared with coarse realgar; a biodistribution study performed in mice showed that after intragastric administration of realgar NPs, higher arsenic concentration was reached in the tumor, heart, liver, spleen, lung, and kidney compared with the administration of coarse realgar, as confirmed by inductively coupled plasma mass spectrometry to determine the concentration of arsenic. This study indicated that high-energy ball milling is an effective way to reduce the average particle size of realgar, and compared with coarse realgar, the cytotoxicity and bioavailability of realgar NPs were significantly improved.Keywords: realgar nanoparticles, high-energy ball milling, cytotoxicity, pharmacokinetics, biodistribution
format	article
author	Tian Y Wang XB Xi RG Pan WS Jiang S Li Z Zhao Y Gao GH Liu D
author_facet	Tian Y Wang XB Xi RG Pan WS Jiang S Li Z Zhao Y Gao GH Liu D
author_sort	Tian Y
title	Enhanced antitumor activity of realgar mediated by milling it to nanosize
title_short	Enhanced antitumor activity of realgar mediated by milling it to nanosize
title_full	Enhanced antitumor activity of realgar mediated by milling it to nanosize
title_fullStr	Enhanced antitumor activity of realgar mediated by milling it to nanosize
title_full_unstemmed	Enhanced antitumor activity of realgar mediated by milling it to nanosize
title_sort	enhanced antitumor activity of realgar mediated by milling it to nanosize
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/efc211f9e92241cdb0a7dfbd9c1c2627
work_keys_str_mv	AT tiany enhancedantitumoractivityofrealgarmediatedbymillingittonanosize AT wangxb enhancedantitumoractivityofrealgarmediatedbymillingittonanosize AT xirg enhancedantitumoractivityofrealgarmediatedbymillingittonanosize AT panws enhancedantitumoractivityofrealgarmediatedbymillingittonanosize AT jiangs enhancedantitumoractivityofrealgarmediatedbymillingittonanosize AT liz enhancedantitumoractivityofrealgarmediatedbymillingittonanosize AT zhaoy enhancedantitumoractivityofrealgarmediatedbymillingittonanosize AT gaogh enhancedantitumoractivityofrealgarmediatedbymillingittonanosize AT liud enhancedantitumoractivityofrealgarmediatedbymillingittonanosize
_version_	1718399727971598336

Enhanced antitumor activity of realgar mediated by milling it to nanosize

Ejemplares similares