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Int. J. Mol. Sci. 2016, 17(11), 1892;

CPP-Assisted Intracellular Drug Delivery, What Is Next?

Collaborative Innovation Center of Chemical Science and Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China
Tianjin Key Laboratory on Technologies Enabling, Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin 300070, China
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinjudaero, Jinju, Gyeongnam 660-751, Korea
Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109-1065, USA
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Academic Editors: Jagdish Singh and Buddhadev Layek
Received: 9 October 2016 / Revised: 8 November 2016 / Accepted: 9 November 2016 / Published: 14 November 2016
(This article belongs to the Special Issue Cell-Penetrating Peptides 2016)
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For the past 20 years, we have witnessed an unprecedented and, indeed, rather miraculous event of how cell-penetrating peptides (CPPs), the naturally originated penetrating enhancers, help overcome the membrane barrier that has hindered the access of bio-macromolecular compounds such as genes and proteins into cells, thereby denying their clinical potential to become potent anti-cancer drugs. By taking the advantage of the unique cell-translocation property of these short peptides, various payloads of proteins, nucleic acids, or even nanoparticle-based carriers were delivered into all cell types with unparalleled efficiency. However, non-specific CPP-mediated cell penetration into normal tissues can lead to widespread organ distribution of the payloads, thereby reducing the therapeutic efficacy of the drug and at the same time increasing the drug-induced toxic effects. In view of these challenges, we present herein a review of the new designs of CPP-linked vehicles and strategies to achieve highly effective yet less toxic chemotherapy in combating tumor oncology. View Full-Text
Keywords: CPPs; intracellular delivery; pH and enzyme triggered drug delivery system CPPs; intracellular delivery; pH and enzyme triggered drug delivery system

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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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Ye, J.; Liu, E.; Yu, Z.; Pei, X.; Chen, S.; Zhang, P.; Shin, M.-C.; Gong, J.; He, H.; Yang, V.C. CPP-Assisted Intracellular Drug Delivery, What Is Next? Int. J. Mol. Sci. 2016, 17, 1892.

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