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

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 p...

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Autores principales: Lim, Chaemin, Youn, Yu Seok, Lee, Kyung Soo, Hoang, Ngoc Ha, Sim, Taehoon, Lee, Eun Seong, Oh, Kyung Taek
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4768899/
https://www.ncbi.nlm.nih.gov/pubmed/26955270
http://dx.doi.org/10.2147/IJN.S99271
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author Lim, Chaemin
Youn, Yu Seok
Lee, Kyung Soo
Hoang, Ngoc Ha
Sim, Taehoon
Lee, Eun Seong
Oh, Kyung Taek
author_facet Lim, Chaemin
Youn, Yu Seok
Lee, Kyung Soo
Hoang, Ngoc Ha
Sim, Taehoon
Lee, Eun Seong
Oh, Kyung Taek
author_sort Lim, Chaemin
collection PubMed
description 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.
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spelling pubmed-47688992016-03-07 Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers Lim, Chaemin Youn, Yu Seok Lee, Kyung Soo Hoang, Ngoc Ha Sim, Taehoon Lee, Eun Seong Oh, Kyung Taek Int J Nanomedicine Original Research 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. Dove Medical Press 2016-02-22 /pmc/articles/PMC4768899/ /pubmed/26955270 http://dx.doi.org/10.2147/IJN.S99271 Text en © 2016 Lim et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Original Research
Lim, Chaemin
Youn, Yu Seok
Lee, Kyung Soo
Hoang, Ngoc Ha
Sim, Taehoon
Lee, Eun Seong
Oh, Kyung Taek
Development of a robust pH-sensitive polyelectrolyte ionomer complex for anticancer nanocarriers
title 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_short 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
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4768899/
https://www.ncbi.nlm.nih.gov/pubmed/26955270
http://dx.doi.org/10.2147/IJN.S99271
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