In vivo biodistribution, biocompatibility, and efficacy of sorafenib-loaded lipid-based nanosuspensions evaluated experimentally in cancer

Shaomei Yang,1 Bo Zhang,1 Xiaowei Gong,2 Tianqi Wang,1 Yongjun Liu,1 Na Zhang1 1Department of Pharmaceutics, College of Pharmacy, Shandong University, 2Shandong Provincial Key Laboratory of Neuroprotective Drug, Jinan, Shandong Province, People’s Republic of China Abstract: Hepatocellula...

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Autores principales:	Yang S, Zhang B, Gong X, Wang T, Liu Y, Zhang N
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	sorafenib lipid-based nanosuspensions Hepatocellular carcinoma biodistribution anti-tumor efficacy Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/928e5e17bd84474e8549624cf573794f
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spelling	oai:doaj.org-article:928e5e17bd84474e8549624cf573794f2021-12-02T02:42:21ZIn vivo biodistribution, biocompatibility, and efficacy of sorafenib-loaded lipid-based nanosuspensions evaluated experimentally in cancer1178-2013https://doaj.org/article/928e5e17bd84474e8549624cf573794f2016-05-01T00:00:00Zhttps://www.dovepress.com/in-vivo-biodistribution-biocompatibility-and-efficacy-of-sorafenib-loa-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Shaomei Yang,1 Bo Zhang,1 Xiaowei Gong,2 Tianqi Wang,1 Yongjun Liu,1 Na Zhang1 1Department of Pharmaceutics, College of Pharmacy, Shandong University, 2Shandong Provincial Key Laboratory of Neuroprotective Drug, Jinan, Shandong Province, People’s Republic of China Abstract: Hepatocellular carcinoma (HCC) is one of the most common malignant tumors worldwide. In this study, sorafenib-loaded lipid-based nanosuspensions (sorafenib-LNS) were first developed as an intravenous injectable formulation to increase the efficacy of sorafenib against HCC. LNS were used as nanocarriers for sorafenib owing to their desired features in increasing the solubility and dissolution velocity, improving the bioavailability of sorafenib. Sorafenib-LNS were prepared by nanoprecipitation and consisted of spherical particles with a uniform size distribution (164.5 nm, polydispersity index =0.202) and negative zeta potential (-11.0 mV). The drug loading (DL) was 10.55%±0.16%. Sorafenib-LNS showed higher in vitro cytotoxicity than sorafenib against HepG2 cells (P<0.05) and Bel-7402 cells (P<0.05). The in vivo biodistribution, biocompatibility, and antitumor efficacy of sorafenib-LNS were evaluated in H22-bearing liver cancer xenograft murine model. The results showed that sorafenib-LNS (9 mg/kg) exhibited significantly higher antitumor efficacy by reducing the tumor volume compared with the sorafenib oral group (18 mg/kg, P<0.05) and sorafenib injection group (9 mg/kg, P<0.05). Furthermore, the results of the in vivo biodistribution experiments demonstrated that sorafenib-LNS injected into H22 tumor-bearing mice exhibited increased accumulation in the tumor tissue, which was confirmed by in vivo imaging. In the current experimental conditions, sorafenib-LNS did not show significant toxicity both in vitro and in vivo. These results suggest that sorafenib-LNS are a promising nanomedicine for treating HCC. Keywords: sorafenib, lipid-based nanosuspensions, HCC, distribution, antitumor effectYang SZhang BGong XWang TLiu YZhang NDove Medical Pressarticlesorafeniblipid-based nanosuspensionsHepatocellular carcinomabiodistributionanti-tumor efficacyMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 2329-2343 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	sorafenib lipid-based nanosuspensions Hepatocellular carcinoma biodistribution anti-tumor efficacy Medicine (General) R5-920
spellingShingle	sorafenib lipid-based nanosuspensions Hepatocellular carcinoma biodistribution anti-tumor efficacy Medicine (General) R5-920 Yang S Zhang B Gong X Wang T Liu Y Zhang N In vivo biodistribution, biocompatibility, and efficacy of sorafenib-loaded lipid-based nanosuspensions evaluated experimentally in cancer
description	Shaomei Yang,1 Bo Zhang,1 Xiaowei Gong,2 Tianqi Wang,1 Yongjun Liu,1 Na Zhang1 1Department of Pharmaceutics, College of Pharmacy, Shandong University, 2Shandong Provincial Key Laboratory of Neuroprotective Drug, Jinan, Shandong Province, People’s Republic of China Abstract: Hepatocellular carcinoma (HCC) is one of the most common malignant tumors worldwide. In this study, sorafenib-loaded lipid-based nanosuspensions (sorafenib-LNS) were first developed as an intravenous injectable formulation to increase the efficacy of sorafenib against HCC. LNS were used as nanocarriers for sorafenib owing to their desired features in increasing the solubility and dissolution velocity, improving the bioavailability of sorafenib. Sorafenib-LNS were prepared by nanoprecipitation and consisted of spherical particles with a uniform size distribution (164.5 nm, polydispersity index =0.202) and negative zeta potential (-11.0 mV). The drug loading (DL) was 10.55%±0.16%. Sorafenib-LNS showed higher in vitro cytotoxicity than sorafenib against HepG2 cells (P<0.05) and Bel-7402 cells (P<0.05). The in vivo biodistribution, biocompatibility, and antitumor efficacy of sorafenib-LNS were evaluated in H22-bearing liver cancer xenograft murine model. The results showed that sorafenib-LNS (9 mg/kg) exhibited significantly higher antitumor efficacy by reducing the tumor volume compared with the sorafenib oral group (18 mg/kg, P<0.05) and sorafenib injection group (9 mg/kg, P<0.05). Furthermore, the results of the in vivo biodistribution experiments demonstrated that sorafenib-LNS injected into H22 tumor-bearing mice exhibited increased accumulation in the tumor tissue, which was confirmed by in vivo imaging. In the current experimental conditions, sorafenib-LNS did not show significant toxicity both in vitro and in vivo. These results suggest that sorafenib-LNS are a promising nanomedicine for treating HCC. Keywords: sorafenib, lipid-based nanosuspensions, HCC, distribution, antitumor effect
format	article
author	Yang S Zhang B Gong X Wang T Liu Y Zhang N
author_facet	Yang S Zhang B Gong X Wang T Liu Y Zhang N
author_sort	Yang S
title	In vivo biodistribution, biocompatibility, and efficacy of sorafenib-loaded lipid-based nanosuspensions evaluated experimentally in cancer
title_short	In vivo biodistribution, biocompatibility, and efficacy of sorafenib-loaded lipid-based nanosuspensions evaluated experimentally in cancer
title_full	In vivo biodistribution, biocompatibility, and efficacy of sorafenib-loaded lipid-based nanosuspensions evaluated experimentally in cancer
title_fullStr	In vivo biodistribution, biocompatibility, and efficacy of sorafenib-loaded lipid-based nanosuspensions evaluated experimentally in cancer
title_full_unstemmed	In vivo biodistribution, biocompatibility, and efficacy of sorafenib-loaded lipid-based nanosuspensions evaluated experimentally in cancer
title_sort	in vivo biodistribution, biocompatibility, and efficacy of sorafenib-loaded lipid-based nanosuspensions evaluated experimentally in cancer
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/928e5e17bd84474e8549624cf573794f
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In vivo biodistribution, biocompatibility, and efficacy of sorafenib-loaded lipid-based nanosuspensions evaluated experimentally in cancer

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