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Open AccessArticle

Oxidation-Triggerable Liposome Incorporating Poly(Hydroxyethyl Acrylate-co-Allyl methyl sulfide) as an Anticancer Carrier of Doxorubicin

Department of Medical Biomaterials Engineering, College of Biomedical Science and Institute of Bioscience and Biotechnology, Kangwon National University, 192-1, Hyoja 2 dong, Chuncheon, Kangwon-do 200-701, Korea
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Author to whom correspondence should be addressed.
Cancers 2020, 12(1), 180; https://doi.org/10.3390/cancers12010180 (registering DOI)
Received: 30 October 2019 / Revised: 27 December 2019 / Accepted: 8 January 2020 / Published: 10 January 2020
(This article belongs to the Special Issue Cancer Nanomedicine)
Since cancer cells are oxidative in nature, anti-cancer agents can be delivered to cancer cells specifically without causing severe normal cell toxicity if the drug carriers are designed to be sensitive to the intrinsic characteristic. Oxidation-sensitive liposomes were developed by stabilizing dioleoylphosphatidyl ethanolamine (DOPE) bilayers with folate-conjugated poly(hydroxyethyl acrylate-co-allyl methyl sulfide) (F-P(HEA-AMS)). The copolymer, synthesized by a free radical polymerization, was surface-active but lost its surface activity after AMS unit was oxidized by H2O2 treatment. The liposomes with F-P(HEA-AMS) were sensitive to H2O2 concentration (0%, 0.5%, 1.0%, and 2.0%) in terms of release, possibly because the copolymer lost its surface activity and its bilayer-stabilizing ability upon oxidation. Fluorescence-activated cell sorting (FACS) and confocal laser scanning microscopy (CLSM) revealed that doxorubicin (DOX)-loaded liposomes stabilized with folate-conjugated copolymers markedly promoted the transport of the anti-cancer drug to cancer cells. This was possible because the liposomes were readily translocated into the cancer cells via receptor-mediated endocytosis. This liposome would be applicable to the delivery carrier of anticancer drugs. View Full-Text
Keywords: dioleoylphosphatidylethanolamine; liposomes; poly(hydroxyethyl acrylate-co-allyl methyl sulfide) copolymer; folate; oxidation-sensitive release; doxorubicin; cellular interaction; in vitro anti-cancer activity dioleoylphosphatidylethanolamine; liposomes; poly(hydroxyethyl acrylate-co-allyl methyl sulfide) copolymer; folate; oxidation-sensitive release; doxorubicin; cellular interaction; in vitro anti-cancer activity
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Kim, J.A.; Yoon, D.Y.; Kim, J.-C. Oxidation-Triggerable Liposome Incorporating Poly(Hydroxyethyl Acrylate-co-Allyl methyl sulfide) as an Anticancer Carrier of Doxorubicin. Cancers 2020, 12, 180.

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