In vitro and in vivo antitumor activity of a novel pH-activated polymeric drug delivery system for doxorubicin.

<h4>Background</h4>Conventional chemotherapy agent such as doxorubicin (DOX) is of limited clinical use because of its inherently low selectivity, which can lead to systemic toxicity in normal healthy tissue.<h4>Methods</h4>A pH stimuli-sensitive conjugate based on polyethyle...

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Autores principales:	Menglei Huan, Bangle Zhang, Zenghui Teng, Han Cui, Jieping Wang, Xinyou Liu, Hui Xia, Siyuan Zhou, Qibing Mei
Formato:	article
Lenguaje:	EN
Publicado:	Public Library of Science (PLoS) 2012
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/cc8936b69110404391661108caa659af
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spelling	oai:doaj.org-article:cc8936b69110404391661108caa659af2021-11-18T07:04:26ZIn vitro and in vivo antitumor activity of a novel pH-activated polymeric drug delivery system for doxorubicin.1932-620310.1371/journal.pone.0044116https://doaj.org/article/cc8936b69110404391661108caa659af2012-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/23028490/?tool=EBIhttps://doaj.org/toc/1932-6203<h4>Background</h4>Conventional chemotherapy agent such as doxorubicin (DOX) is of limited clinical use because of its inherently low selectivity, which can lead to systemic toxicity in normal healthy tissue.<h4>Methods</h4>A pH stimuli-sensitive conjugate based on polyethylene glycol (PEG) with covalently attachment doxorubicin via hydrazone bond (PEG-hyd-DOX) was prepared for tumor targeting delivery system. While PEG-DOX conjugates via amid bond (PEG-ami-DOX) was synthesized as control.<h4>Results</h4>The synthetic conjugates were confirmed by proton nuclear magnetic resonance (NMR) spectroscopy, the release profile of DOX from PEG-hyd-DOX was acid-liable for the hydrazone linkage between DOX and PEG, led to different intracellular uptake route; intracellular accumulation of PEG-hyd-DOX was higher than PEG-ami-DOX due to its pH-triggered profile, and thereby more cytotoxicity against MCF-7, MDA-MB-231 (breast cancer models) and HepG2 (hepatocellular carcinoma model) cell lines. Following the in vitro results, we xenografted MDA-MB-231 cell onto SCID mice, PEG-hyd-DOX showed stronger antitumor efficacy than free DOX and was tumor-targeting.<h4>Conclusions</h4>Results from these in vivo experiments were consistent with our in vitro results; suggested this pH-triggered PEG-hyd-DOX conjugate could target DOX to tumor tissues and release free drugs by acidic tumor environment, which would be potent in antitumor drug delivery.Menglei HuanBangle ZhangZenghui TengHan CuiJieping WangXinyou LiuHui XiaSiyuan ZhouQibing MeiPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 7, Iss 9, p e44116 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Menglei Huan Bangle Zhang Zenghui Teng Han Cui Jieping Wang Xinyou Liu Hui Xia Siyuan Zhou Qibing Mei In vitro and in vivo antitumor activity of a novel pH-activated polymeric drug delivery system for doxorubicin.
description	<h4>Background</h4>Conventional chemotherapy agent such as doxorubicin (DOX) is of limited clinical use because of its inherently low selectivity, which can lead to systemic toxicity in normal healthy tissue.<h4>Methods</h4>A pH stimuli-sensitive conjugate based on polyethylene glycol (PEG) with covalently attachment doxorubicin via hydrazone bond (PEG-hyd-DOX) was prepared for tumor targeting delivery system. While PEG-DOX conjugates via amid bond (PEG-ami-DOX) was synthesized as control.<h4>Results</h4>The synthetic conjugates were confirmed by proton nuclear magnetic resonance (NMR) spectroscopy, the release profile of DOX from PEG-hyd-DOX was acid-liable for the hydrazone linkage between DOX and PEG, led to different intracellular uptake route; intracellular accumulation of PEG-hyd-DOX was higher than PEG-ami-DOX due to its pH-triggered profile, and thereby more cytotoxicity against MCF-7, MDA-MB-231 (breast cancer models) and HepG2 (hepatocellular carcinoma model) cell lines. Following the in vitro results, we xenografted MDA-MB-231 cell onto SCID mice, PEG-hyd-DOX showed stronger antitumor efficacy than free DOX and was tumor-targeting.<h4>Conclusions</h4>Results from these in vivo experiments were consistent with our in vitro results; suggested this pH-triggered PEG-hyd-DOX conjugate could target DOX to tumor tissues and release free drugs by acidic tumor environment, which would be potent in antitumor drug delivery.
format	article
author	Menglei Huan Bangle Zhang Zenghui Teng Han Cui Jieping Wang Xinyou Liu Hui Xia Siyuan Zhou Qibing Mei
author_facet	Menglei Huan Bangle Zhang Zenghui Teng Han Cui Jieping Wang Xinyou Liu Hui Xia Siyuan Zhou Qibing Mei
author_sort	Menglei Huan
title	In vitro and in vivo antitumor activity of a novel pH-activated polymeric drug delivery system for doxorubicin.
title_short	In vitro and in vivo antitumor activity of a novel pH-activated polymeric drug delivery system for doxorubicin.
title_full	In vitro and in vivo antitumor activity of a novel pH-activated polymeric drug delivery system for doxorubicin.
title_fullStr	In vitro and in vivo antitumor activity of a novel pH-activated polymeric drug delivery system for doxorubicin.
title_full_unstemmed	In vitro and in vivo antitumor activity of a novel pH-activated polymeric drug delivery system for doxorubicin.
title_sort	in vitro and in vivo antitumor activity of a novel ph-activated polymeric drug delivery system for doxorubicin.
publisher	Public Library of Science (PLoS)
publishDate	2012
url	https://doaj.org/article/cc8936b69110404391661108caa659af
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In vitro and in vivo antitumor activity of a novel pH-activated polymeric drug delivery system for doxorubicin.

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