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Bioreducible Micelles Self-Assembled from Poly(ethylene glycol)-Cholesteryl Conjugate As a Drug Delivery Platform

Title
Bioreducible Micelles Self-Assembled from Poly(ethylene glycol)-Cholesteryl Conjugate As a Drug Delivery Platform
Authors
Baek, C[Baek, Chulsu]Ha, TL[Ha, Tae-Lin]Kim, E[Kim, Eunjoo]Jeong, SW[Jeong, Sang Won]Lee, SG[Lee, Se Guen]Lee, SJ[Lee, Sung Jun]Kim, HC[Kim, Hyun-Chul]
DGIST Authors
Baek, C[Baek, Chulsu]; Ha, TL[Ha, Tae-Lin]; Kim, E[Kim, Eunjoo]Jeong, SW[Jeong, Sang Won]Lee, SG[Lee, Se Guen]; Lee, SJ[Lee, Sung Jun]; Kim, HC[Kim, Hyun-Chul]
Issue Date
2015-11
Citation
Polymers, 7(11), 2245-2258
Type
Article
Article Type
Article
Keywords
Bio-CompatibleBiocompatibilityCell CultureCellsControlled Drug DeliveryCovalent BondsCytologyDisulfide-Thiol ExchangeDisulfide-Thiol ExchangesDrug Delivery SystemDrug ProductsEthylene GlycolMicellesPolyethylene GlycolsPolymeric MicellePolymeric MicellesPolymersPolyolsSolutionsStimulus-Sensitive PolymersSulfur Compounds
ISSN
2073-4360
Abstract
The ability of polymeric micelles to self-assemble into nanosized particles has created interest in their application as potential anticancer drug delivery systems. A poly(ethylene glycol)-cholesteryl conjugate (Chol-ss-PEG-ss-Chol) connected by cleavable disulfide linkages was synthesized and used as a nanocarrier for in vitro release of doxorubicin (DOX). Owing to its amphiphilic structure, Chol-ss-PEG-ss-Chol was able to self-assemble into micelles with an average diameter 18.6 nm in aqueous solution. The micelles formed large aggregates due to the shedding of the PEG shell through cleavage of disulfide bonds in a reductive environment. The in vitro release studies revealed that Chol-ss-PEG-ss-Chol micelles released 80% and approximately 9% of the encapsulated DOX within 6 h under reductive and non-reductive conditions, respectively. The glutathione (GSH)-mediated intracellular drug delivery was investigated in a KB cell line. The cytotoxicity of DOX-loaded micelles indicated a higher cellular anti-proliferative effect against GSH-pretreated than untreated KB cells. Furthermore, confocal laser scanning microscopy (CLSM) measurement demonstrated that Chol-ss-PEG-ss-Chol micelles exhibited faster drug release in GSH-pretreated KB cells than untreated KB cells. These results suggest the potential usefulness of disulfide-based polymeric micelles as controlled drug delivery carriers. © 2015 by the authors.
URI
http://hdl.handle.net/20.500.11750/2582
DOI
10.3390/polym7111511
Publisher
MDPI AG
Related Researcher
Files:
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Collection:
Convergence Research Center for Solar Energy1. Journal Articles
Companion Diagnostics and Medical Technology Research Group1. Journal Articles


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