Preparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug delivery

Xiwei Yu,1 Jiahui Hou,1 Yijie Shi,1 Chang Su,2 Liang Zhao1 1School of Pharmacy, 2School of Veterinary Medicine, Jinzhou Medical University, Jinzhou, People’s Republic of China Abstract: It is well known that most anticancer drugs commonly show high toxicity to the DNA of tumor cells and...

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Autores principales:	Yu X, Hou J, Shi Y, Su C, Zhao L
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	nucleus nanoparticles chitosan protamine cytotoxicity Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/d982641cecfd4eef94244dfd2eb4ff7c
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spelling	oai:doaj.org-article:d982641cecfd4eef94244dfd2eb4ff7c2021-12-02T05:40:44ZPreparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug delivery1178-2013https://doaj.org/article/d982641cecfd4eef94244dfd2eb4ff7c2016-11-01T00:00:00Zhttps://www.dovepress.com/preparation-and-characterization-of-novel-chitosan-protamine-nanoparti-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Xiwei Yu,1 Jiahui Hou,1 Yijie Shi,1 Chang Su,2 Liang Zhao1 1School of Pharmacy, 2School of Veterinary Medicine, Jinzhou Medical University, Jinzhou, People’s Republic of China Abstract: It is well known that most anticancer drugs commonly show high toxicity to the DNA of tumor cells and exert effects by combining with the DNA or associated enzymes in the nucleus. Most developed drugs are first delivered into the cytoplasm and then transferred to the nucleus through the membrane pores. Sometimes, the transportation of drugs from cytoplasm to nucleus is not efficient and often results in poor therapeutic effects. In this study, we developed special and novel nanoparticles (NPs) made of chitosan and protamine for targeted nuclear capture of drugs to enhance anticancer effects. The anticancer effects of nuclear targeted-delivery of drugs in NPs were also evaluated by investigating cytotoxicity, cellular uptake mechanism, and cell apoptosis on cells. Chitosan–protamine NPs were characterized by good drug entrapment, sustained release, small average particle size, low polydispersity index, and high encapsulation efficiency; and accomplished the efficient nuclear delivery of fluorouracil (5-Fu). Compared with free 5-Fu and 5-Fu-loaded chitosan NPs, treatment of A549 cells and HeLa cells with 5-Fu-loaded chitosan–protamine NPs showed the highest cytotoxicity and further induced the significant apoptosis of cells. In addition, 5-Fu-loaded chitosan–protamine NPs exhibited the best efficiency in inhibiting tumor growth than the other three formulations. 5-Fu-loaded chitosan–protamine NPs enhanced antitumor efficacy through the targeted nuclear capture of drugs and showed promising potential as a nanodelivery system for quickly locating drugs in the nucleus of cells. Keywords: nucleus, nanoparticles, chitosan, protamine, cytotoxicityYu XHou JShi YSu CZhao LDove Medical PressarticlenucleusnanoparticleschitosanprotaminecytotoxicityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 11, Pp 6035-6046 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	nucleus nanoparticles chitosan protamine cytotoxicity Medicine (General) R5-920
spellingShingle	nucleus nanoparticles chitosan protamine cytotoxicity Medicine (General) R5-920 Yu X Hou J Shi Y Su C Zhao L Preparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug delivery
description	Xiwei Yu,1 Jiahui Hou,1 Yijie Shi,1 Chang Su,2 Liang Zhao1 1School of Pharmacy, 2School of Veterinary Medicine, Jinzhou Medical University, Jinzhou, People’s Republic of China Abstract: It is well known that most anticancer drugs commonly show high toxicity to the DNA of tumor cells and exert effects by combining with the DNA or associated enzymes in the nucleus. Most developed drugs are first delivered into the cytoplasm and then transferred to the nucleus through the membrane pores. Sometimes, the transportation of drugs from cytoplasm to nucleus is not efficient and often results in poor therapeutic effects. In this study, we developed special and novel nanoparticles (NPs) made of chitosan and protamine for targeted nuclear capture of drugs to enhance anticancer effects. The anticancer effects of nuclear targeted-delivery of drugs in NPs were also evaluated by investigating cytotoxicity, cellular uptake mechanism, and cell apoptosis on cells. Chitosan–protamine NPs were characterized by good drug entrapment, sustained release, small average particle size, low polydispersity index, and high encapsulation efficiency; and accomplished the efficient nuclear delivery of fluorouracil (5-Fu). Compared with free 5-Fu and 5-Fu-loaded chitosan NPs, treatment of A549 cells and HeLa cells with 5-Fu-loaded chitosan–protamine NPs showed the highest cytotoxicity and further induced the significant apoptosis of cells. In addition, 5-Fu-loaded chitosan–protamine NPs exhibited the best efficiency in inhibiting tumor growth than the other three formulations. 5-Fu-loaded chitosan–protamine NPs enhanced antitumor efficacy through the targeted nuclear capture of drugs and showed promising potential as a nanodelivery system for quickly locating drugs in the nucleus of cells. Keywords: nucleus, nanoparticles, chitosan, protamine, cytotoxicity
format	article
author	Yu X Hou J Shi Y Su C Zhao L
author_facet	Yu X Hou J Shi Y Su C Zhao L
author_sort	Yu X
title	Preparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug delivery
title_short	Preparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug delivery
title_full	Preparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug delivery
title_fullStr	Preparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug delivery
title_full_unstemmed	Preparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug delivery
title_sort	preparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug delivery
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/d982641cecfd4eef94244dfd2eb4ff7c
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Preparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug delivery

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