Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers

Chaemin Lim,1,* Yu Seok Youn,2,* Kyung Soo Lee,1 Ngoc Ha Hoang,1 Taehoon Sim,1 Eun Seong Lee,3 Kyung Taek Oh1 1Department of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University, Seoul, 2Department of Pharmaceutical Sciences, School of Pharmacy, Sungkyunkwan University, Suwon, 3Divisi...

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Autores principales:	Lim CM, Youn YS, Lee KS, Hoang NH, Sim TH, Lee ES, Oh KT
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	Polyelectrolyte ionomer complex PEI-PLA-PEG nanomedicine pH-sensitive animal imaging. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/027842e6fcd940489be3dd1ab65d5355
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spelling	oai:doaj.org-article:027842e6fcd940489be3dd1ab65d53552021-12-02T05:10:45ZDevelopment of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers1178-2013https://doaj.org/article/027842e6fcd940489be3dd1ab65d53552016-02-01T00:00:00Zhttps://www.dovepress.com/development-of-a-robust-ph-sensitive-polyelectrolyte-ionomer-complex-f-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Chaemin Lim,1,* Yu Seok Youn,2,* Kyung Soo Lee,1 Ngoc Ha Hoang,1 Taehoon Sim,1 Eun Seong Lee,3 Kyung Taek Oh1 1Department of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University, Seoul, 2Department of Pharmaceutical Sciences, School of Pharmacy, Sungkyunkwan University, Suwon, 3Division of Biotechnology, The Catholic University of Korea, Gyeonggi-do, South Korea *These authors contributed equally to this work Abstract: A polyelectrolyte ionomer complex (PIC) composed of cationic and anionic polymers was developed for nanomedical applications. Here, a poly(ethylene glycol)–poly(lactic acid)–poly(ethylene imine) triblock copolymer (PEG–PLA–PEI) and a poly(aspartic acid) (P[Asp]) homopolymer were synthesized. These polyelectrolytes formed stable aggregates through electrostatic interactions between the cationic PEI and the anionic P(Asp) blocks. In particular, the addition of a hydrophobic PLA and a hydrophilic PEG to triblock copolyelectrolytes provided colloidal aggregation stability by forming a tight hydrophobic core and steric hindrance on the surface of PIC, respectively. The PIC showed different particle sizes and zeta potentials depending on the ratio of cationic PEI and anionic P(Asp) blocks (C/A ratio). The doxorubicin (dox)-loaded PIC, prepared with a C/A ratio of 8, demonstrated pH-dependent behavior by the deprotonation/protonation of polyelectrolyte blocks. The drug release and the cytotoxicity of the dox-loaded PIC (C/A ratio: 8) increased under acidic conditions compared with physiological pH, due to the destabilization of the formation of the electrostatic core. In vivo animal imaging revealed that the prepared PIC accumulated at the targeted tumor site for 24 hours. Therefore, the prepared pH-sensitive PIC could have considerable potential as a nanomedicinal platform for anticancer therapy. Keywords: polyelectrolyte ionomer complex, PEG–PLA–PEI, nanomedicine, pH-sensitive, animal imagingLim CMYoun YSLee KSHoang NHSim THLee ESOh KTDove Medical PressarticlePolyelectrolyte ionomer complexPEI-PLA-PEGnanomedicinepH-sensitiveanimal imaging.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss Issue 1, Pp 703-713 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Polyelectrolyte ionomer complex PEI-PLA-PEG nanomedicine pH-sensitive animal imaging. Medicine (General) R5-920
spellingShingle	Polyelectrolyte ionomer complex PEI-PLA-PEG nanomedicine pH-sensitive animal imaging. Medicine (General) R5-920 Lim CM Youn YS Lee KS Hoang NH Sim TH Lee ES Oh KT Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers
description	Chaemin Lim,1,* Yu Seok Youn,2,* Kyung Soo Lee,1 Ngoc Ha Hoang,1 Taehoon Sim,1 Eun Seong Lee,3 Kyung Taek Oh1 1Department of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University, Seoul, 2Department of Pharmaceutical Sciences, School of Pharmacy, Sungkyunkwan University, Suwon, 3Division of Biotechnology, The Catholic University of Korea, Gyeonggi-do, South Korea *These authors contributed equally to this work Abstract: A polyelectrolyte ionomer complex (PIC) composed of cationic and anionic polymers was developed for nanomedical applications. Here, a poly(ethylene glycol)–poly(lactic acid)–poly(ethylene imine) triblock copolymer (PEG–PLA–PEI) and a poly(aspartic acid) (P[Asp]) homopolymer were synthesized. These polyelectrolytes formed stable aggregates through electrostatic interactions between the cationic PEI and the anionic P(Asp) blocks. In particular, the addition of a hydrophobic PLA and a hydrophilic PEG to triblock copolyelectrolytes provided colloidal aggregation stability by forming a tight hydrophobic core and steric hindrance on the surface of PIC, respectively. The PIC showed different particle sizes and zeta potentials depending on the ratio of cationic PEI and anionic P(Asp) blocks (C/A ratio). The doxorubicin (dox)-loaded PIC, prepared with a C/A ratio of 8, demonstrated pH-dependent behavior by the deprotonation/protonation of polyelectrolyte blocks. The drug release and the cytotoxicity of the dox-loaded PIC (C/A ratio: 8) increased under acidic conditions compared with physiological pH, due to the destabilization of the formation of the electrostatic core. In vivo animal imaging revealed that the prepared PIC accumulated at the targeted tumor site for 24 hours. Therefore, the prepared pH-sensitive PIC could have considerable potential as a nanomedicinal platform for anticancer therapy. Keywords: polyelectrolyte ionomer complex, PEG–PLA–PEI, nanomedicine, pH-sensitive, animal imaging
format	article
author	Lim CM Youn YS Lee KS Hoang NH Sim TH Lee ES Oh KT
author_facet	Lim CM Youn YS Lee KS Hoang NH Sim TH Lee ES Oh KT
author_sort	Lim CM
title	Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers
title_short	Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers
title_full	Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers
title_fullStr	Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers
title_full_unstemmed	Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers
title_sort	development of a robust ph-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/027842e6fcd940489be3dd1ab65d5355
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Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers

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