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Open AccessCommunication
Molecules 2017, 22(11), 1916; doi:10.3390/molecules22111916

Non-Covalent Loading of Anti-Cancer Doxorubicin by Modularizable Peptide Self-Assemblies for a Nanoscale Drug Carrier

1
Department of Materials Chemistry, Ryukoku University, 1-5 Yokotani, Seta-Oe, Otsu 520-2194, Japan
2
Innovative Materials and Processing Research Center, Ryukoku University, 1-5 Yokotani, Seta-Oe, Otsu 520-2194, Japan
3
Faculty of Frontiers of Innovative Research in Science and Technology (FIRST), Konan University, 7-1-20 Minatojima-Minami, Chuo, Kobe 650-0047, Japan
*
Authors to whom correspondence should be addressed.
Received: 4 October 2017 / Accepted: 30 October 2017 / Published: 6 November 2017
(This article belongs to the Special Issue Peptide Therapeutics)
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Abstract

We prepared nanoscale, modularizable, self-assembled peptide nanoarchitectures with diameters less of than 20 nm by combining β-sheet-forming peptides tethering a cell-penetrating peptide or a nuclear localization signal sequence. We also found that doxorubicin (Dox), an anti-cancer drug, was non-covalently accommodated by the assemblies at a ratio of one Dox molecule per ten peptides. The Dox-loaded peptide assemblies facilitated cellular uptake and subsequent nuclear localization in HeLa cells, and induced cell death even at low Dox concentrations. This peptide nanocarrier motif is a promising platform for a biocompatible drug delivery system by altering the targeting head groups of the carrier peptides. View Full-Text
Keywords: peptide self-assembly; drug delivery system; cell-penetrating peptide; nuclear-localization signal; anti-cancer doxorubicin peptide self-assembly; drug delivery system; cell-penetrating peptide; nuclear-localization signal; anti-cancer doxorubicin
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Tomizaki, K.-Y.; Kishioka, K.; Kataoka, S.; Miyatani, M.; Ikeda, T.; Komada, M.; Imai, T.; Usui, K. Non-Covalent Loading of Anti-Cancer Doxorubicin by Modularizable Peptide Self-Assemblies for a Nanoscale Drug Carrier. Molecules 2017, 22, 1916.

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