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Enhanced skin permeation of a novel peptide via structural modification, chemical enhancement, and microneedles

Jungen Chen, Junxing Bian, Basil M. Hantash, David E. Hibbs, Chunyong Wu, View ORCID ProfileLifeng Kang
doi: https://doi.org/10.1101/2020.10.07.312850
Jungen Chen
aDepartment of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, JS 210009, China
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Junxing Bian
bSchool of Pharmacy, Faculty of Medicine and Health, University of Sydney, Sydney, NSW 2006, Australia
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Basil M. Hantash
cEscape Therapeutics Inc., 3800 Geer Road, Suite 200, Turlock, CA 95382, USA
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David E. Hibbs
bSchool of Pharmacy, Faculty of Medicine and Health, University of Sydney, Sydney, NSW 2006, Australia
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Chunyong Wu
aDepartment of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, JS 210009, China
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  • For correspondence: cywu@cpu.edu.cn lifeng.kang@sydney.edu.au
Lifeng Kang
bSchool of Pharmacy, Faculty of Medicine and Health, University of Sydney, Sydney, NSW 2006, Australia
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  • ORCID record for Lifeng Kang
  • For correspondence: cywu@cpu.edu.cn lifeng.kang@sydney.edu.au
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Abstract

Hyperpigmentation is a common skin condition with serious psychosocial consequences. Decapeptide-12, a novel peptide, has been found to be safer than hydroquinone in reducing content of melanin, with efficacy up to more than 50% upon 16 weeks of twice daily treatment. However, the peptide suffers from limited transcutaneous penetration due to its hydrophilicity and large molecular weight. Therefore, decapeptide-12 was modified by adding a palmitate chain in an attempt to overcome this limitation. We also tested the effects of chemical penetration enhancers and microneedles to deliver two peptides through skin. Enhanced skin permeation was found using an in vitro human skin permeation model. Moreover, we examined peptide retention of different formulations in skin. Our data showed that palm-peptides in microneedle patch was the most effective.

Competing Interest Statement

The authors have declared no competing interest.

Copyright 
The copyright holder for this preprint is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. All rights reserved. No reuse allowed without permission.
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Posted October 08, 2020.
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Enhanced skin permeation of a novel peptide via structural modification, chemical enhancement, and microneedles
Jungen Chen, Junxing Bian, Basil M. Hantash, David E. Hibbs, Chunyong Wu, Lifeng Kang
bioRxiv 2020.10.07.312850; doi: https://doi.org/10.1101/2020.10.07.312850
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Enhanced skin permeation of a novel peptide via structural modification, chemical enhancement, and microneedles
Jungen Chen, Junxing Bian, Basil M. Hantash, David E. Hibbs, Chunyong Wu, Lifeng Kang
bioRxiv 2020.10.07.312850; doi: https://doi.org/10.1101/2020.10.07.312850

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