In vitro and in vivo evaluation of novel NGR-modified liposomes containing brucine

Shu Li, Xi-Peng Wang Shanghai First Maternity and Infant Hospital, Tongji University School of Medicine, Shanghai, People’s Republic of China Abstract: In this study, a novel NGR (Asn-Gly-Arg) peptide-modified liposomal brucine was prepared by using spray-drying method. The surface morph...

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Autores principales:	Li S, Wang X
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	Brucine Liposome NGR HepG2 Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/625cdacdee5f48f991e6182a3e349023
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spelling	oai:doaj.org-article:625cdacdee5f48f991e6182a3e3490232021-12-02T04:33:06ZIn vitro and in vivo evaluation of novel NGR-modified liposomes containing brucine1178-2013https://doaj.org/article/625cdacdee5f48f991e6182a3e3490232017-08-01T00:00:00Zhttps://www.dovepress.com/in-vitro-and-in-vivo-evaluation-of-novel-ngr-modified-liposomes-contai-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Shu Li, Xi-Peng Wang Shanghai First Maternity and Infant Hospital, Tongji University School of Medicine, Shanghai, People’s Republic of China Abstract: In this study, a novel NGR (Asn-Gly-Arg) peptide-modified liposomal brucine was prepared by using spray-drying method. The surface morphology of the liposomes, encapsulation efficiency and particle size were investigated. The data showed that the addition of NGR did not produce any significant influence on brucine liposomes in terms of particle size or zeta potential. In addition, after 3 months of storage, no dramatic change such as visible aggregation, drug content changes or precipitation in the appearance of NGR-brucine liposomes occurred. The in vitro release results indicated that the release of brucine from NGR liposomes was similar to that of liposomes, demonstrating that the NGR modification did not affect brucine release. The in vitro drug-release kinetic model of NGR-brucine liposomes fitted well with the Weibull’s equation. In vivo, NGR-brucine liposomes could significantly extend the bioavailability of brucine; however, there was no significant difference observed in the pharmacokinetic parameters between liposomes and NGR liposomes after intravenous administration. Antitumor activity results showed that NGR-modified liposomes exhibited less toxicity and much higher efficacy in HepG2-bearing mice compared with non-modified liposomes. The enhanced antitumor activity might have occurred because brucine was specifically recognized by NGR receptor on the surface of tumor cells, which enhanced the intracellular uptake of drugs. Keywords: brucine, liposome, NGR, HepG2, in vivo, in vitroLi SWang XDove Medical PressarticleBrucineLiposomeNGRHepG2Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 5797-5804 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Brucine Liposome NGR HepG2 Medicine (General) R5-920
spellingShingle	Brucine Liposome NGR HepG2 Medicine (General) R5-920 Li S Wang X In vitro and in vivo evaluation of novel NGR-modified liposomes containing brucine
description	Shu Li, Xi-Peng Wang Shanghai First Maternity and Infant Hospital, Tongji University School of Medicine, Shanghai, People’s Republic of China Abstract: In this study, a novel NGR (Asn-Gly-Arg) peptide-modified liposomal brucine was prepared by using spray-drying method. The surface morphology of the liposomes, encapsulation efficiency and particle size were investigated. The data showed that the addition of NGR did not produce any significant influence on brucine liposomes in terms of particle size or zeta potential. In addition, after 3 months of storage, no dramatic change such as visible aggregation, drug content changes or precipitation in the appearance of NGR-brucine liposomes occurred. The in vitro release results indicated that the release of brucine from NGR liposomes was similar to that of liposomes, demonstrating that the NGR modification did not affect brucine release. The in vitro drug-release kinetic model of NGR-brucine liposomes fitted well with the Weibull’s equation. In vivo, NGR-brucine liposomes could significantly extend the bioavailability of brucine; however, there was no significant difference observed in the pharmacokinetic parameters between liposomes and NGR liposomes after intravenous administration. Antitumor activity results showed that NGR-modified liposomes exhibited less toxicity and much higher efficacy in HepG2-bearing mice compared with non-modified liposomes. The enhanced antitumor activity might have occurred because brucine was specifically recognized by NGR receptor on the surface of tumor cells, which enhanced the intracellular uptake of drugs. Keywords: brucine, liposome, NGR, HepG2, in vivo, in vitro
format	article
author	Li S Wang X
author_facet	Li S Wang X
author_sort	Li S
title	In vitro and in vivo evaluation of novel NGR-modified liposomes containing brucine
title_short	In vitro and in vivo evaluation of novel NGR-modified liposomes containing brucine
title_full	In vitro and in vivo evaluation of novel NGR-modified liposomes containing brucine
title_fullStr	In vitro and in vivo evaluation of novel NGR-modified liposomes containing brucine
title_full_unstemmed	In vitro and in vivo evaluation of novel NGR-modified liposomes containing brucine
title_sort	in vitro and in vivo evaluation of novel ngr-modified liposomes containing brucine
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/625cdacdee5f48f991e6182a3e349023
work_keys_str_mv	AT lis invitroandinvivoevaluationofnovelngrmodifiedliposomescontainingbrucine AT wangx invitroandinvivoevaluationofnovelngrmodifiedliposomescontainingbrucine
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In vitro and in vivo evaluation of novel NGR-modified liposomes containing brucine

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