Back to Journals » International Journal of Nanomedicine » Volume 9 » Issue 1

Enhanced antitumor activity of realgar mediated by milling it to nanosize

Authors Tian Y, Wang XB, Xi RG, Pan WS, Jiang S, Li Z, Zhao Y, Gao GH, Liu D

Received 22 October 2013

Accepted for publication 12 December 2013

Published 31 January 2014 Volume 2014:9(1) Pages 745—757

DOI https://doi.org/10.2147/IJN.S56391

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 4

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 Liu2

1Department 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 China

Abstract: 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

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]

 

Readers of this article also read:

Green synthesis of water-soluble nontoxic polymeric nanocomposites containing silver nanoparticles

Prozorova GF, Pozdnyakov AS, Kuznetsova NP, Korzhova SA, Emel’yanov AI, Ermakova TG, Fadeeva TV, Sosedova LM

International Journal of Nanomedicine 2014, 9:1883-1889

Published Date: 16 April 2014

Enhancement of immunogenicity and efficacy of a plasmid DNA rabies vaccine by nanoformulation with a fourth-generation amine-terminated poly(ether imine) dendrimer

Ullas PT, Madhusudana SN, Desai A, Sagar BKC, Jayamurugan G, Rajesh YBRD, Jayaraman N

International Journal of Nanomedicine 2014, 9:627-634

Published Date: 28 January 2014

Methacrylic-based nanogels for the pH-sensitive delivery of 5-Fluorouracil in the colon

Ashwanikumar N, Kumar NA, Nair SA, Kumar GS

International Journal of Nanomedicine 2012, 7:5769-5779

Published Date: 15 November 2012

A novel preparation method for silicone oil nanoemulsions and its application for coating hair with silicone

Hu Z, Liao M, Chen Y, Cai Y, Meng L, Liu Y, Lv N, Liu Z, Yuan W

International Journal of Nanomedicine 2012, 7:5719-5724

Published Date: 12 November 2012

Cross-linked acrylic hydrogel for the controlled delivery of hydrophobic drugs in cancer therapy

Deepa G, Thulasidasan AK, Anto RJ, Pillai JJ, Kumar GS

International Journal of Nanomedicine 2012, 7:4077-4088

Published Date: 27 July 2012

Servant leadership: a case study of a Canadian health care innovator

Vanderpyl TH

Journal of Healthcare Leadership 2012, 4:9-16

Published Date: 16 February 2012

Crystallization after intravitreal ganciclovir injection

Pitipol Choopong, Nattaporn Tesavibul, Nattawut Rodanant

Clinical Ophthalmology 2010, 4:709-711

Published Date: 14 July 2010