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Open AccessArticle

Dual pH- and GSH-Responsive Degradable PEGylated Graphene Quantum Dot-Based Nanoparticles for Enhanced HER2-Positive Breast Cancer Therapy

1
Biomedical Research Center, Asan Institute for Life Sciences, 88 Olympic-ro 43-gil, Songpa-gu, Seoul 05505, Korea
2
Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine, 88 Olympic-ro 43-gil, Songpa-gu, Seoul 05505, Korea
3
Department of Chemical Engineering and Applied Chemistry, University of Toronto, 200 College Street, Toronto, ON M5S 3E5, Canada
4
Department of Convergence Medicine, University of Ulsan College of Medicine, 88 Olympic-ro 43-gil, Songpa-gu, Seoul 05505, Korea
5
Department of Dental Materials, School of Dentistry, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 02447, Korea
6
Department of Chemical & Biological Engineering, Korea National University of Transportation, 50 Daehak-ro, Chungcheongbuk-do, Cheongju 27469, Korea
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Nanomaterials 2020, 10(1), 91; https://doi.org/10.3390/nano10010091
Received: 28 November 2019 / Revised: 24 December 2019 / Accepted: 29 December 2019 / Published: 2 January 2020
(This article belongs to the Special Issue Graphene-Based Materials for Cancer Therapy)
Dual stimuli-responsive degradable carbon-based nanoparticles (DS-CNPs) conjugated with Herceptin (HER) and polyethylene glycol (PEG) have been designed for the treatment of HER2-positive breast cancer. Each component has been linked through disulfide linkages that are sensitive to glutathione in a cancer microenvironment. β-cyclodextrin (β-CD) on the surface of DS-CNPs formed an inclusion complex (DL-CNPs) with doxorubicin (DOX) at a high loading capacity of 5.3 ± 0.4%. In response to a high level of glutathione (GSH) and low pH in a tumor environment, DL-CNPs were rapidly degraded and released DOX in a controlled manner via disruption of host–guest inclusion. These novel DL-CNPs exhibited high cellular uptake with low toxicity, which induced the efficient inhibition of antitumor activity both in vitro and in vivo. Cell viability, confocal laser scanning microscopy, and animal studies indicate that DL-CNPs are a great platform with a synergistically enhanced antitumor effect from the dual delivery of HER and DOX in DL-CNPs. View Full-Text
Keywords: stimuli-responsive degradation system; glutathione; breast cancer; Herceptin; active targeting; PEGylation stimuli-responsive degradation system; glutathione; breast cancer; Herceptin; active targeting; PEGylation
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MDPI and ACS Style

Ko, N.R.; Van, S.Y.; Hong, S.H.; Kim, S.-Y.; Kim, M.; Lee, J.S.; Lee, S.J.; Lee, Y.-K.; Kwon, I.K.; Oh, S.J. Dual pH- and GSH-Responsive Degradable PEGylated Graphene Quantum Dot-Based Nanoparticles for Enhanced HER2-Positive Breast Cancer Therapy. Nanomaterials 2020, 10, 91.

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