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ID 49557
FullText URL
Author
Candan, Gerile
Michiue, Hiroyuki Kakenhi
Ishikawa, Sanae
Fujimura, Atsushi
Hayashi, Keiichiro
Uneda, Atsuhito
Mori, Akiko
Ohmori, Iori Kakenhi
Nishiki, Tei-ichi Kakenhi
Matsui, Hideki
Tomizawa, Kazuhito
Abstract
Topical therapy is the most favored form of treatment for whitening against hyperpigmentation and sunburn because it lends itself to self-administration, patient compliance, and absence of systemic adverse effects. However, transdermal delivery of hydrophilic chemicals is difficult. The main purpose of this study is to develop a delivering system of hydrophilic drugs and proteins across the skin. Hydroquinone (HQ), a well-known tyrosinase inhibitor and antimelanogenesis compound, and enhanced green fluorescent protein (EGFP) were fused with eleven poly-arginine (11R). Both HQ-11R and EGFP-11R were efficiently delivered in B16 cells, a mouse melanoma cell line. HQ-11R was as effective as HQ alone at inhibiting melanin synthesis in B16 cells. EGFP-11R was efficiently delivered into cells of the epidermis with 4-(1-pyrenyl)-butyric acid (PB), a counteranion bearing an aromatic hydrophobic moiety, in vivo, but EGFP alone or EGFP-11R without PB was not. Finally, topical application of HQ-11R with PB significantly inhibited UV irradiation-induced pigmentation in guinea pigs compared with HQ alone. These results suggest that topical therapy using poly-arginine in combination with PB is useful for the delivery of hydrophilic drugs and proteins by the transdermal route.
Keywords
Transdermal delivery
Protein transduction
Poly-arginine
Tat
Hydroquinone
Tyrosinase inhibitor
Published Date
2012-09
Publication Title
Biomaterials
Volume
volume33
Issue
issue27
Publisher
Elsevier Ltd.
Start Page
6468
End Page
6475
ISSN
0142-9612
NCID
AA11522637
Content Type
Journal Article
Official Url
http://dx.doi.org/10.1016/j.biomaterials.2012.04.056
Related Url
http://ousar.lib.okayama-u.ac.jp/metadata/49124
language
英語
Copyright Holders
(c) 2012 Elsevier Ltd. All rights reserved.
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author
Refereed
True
DOI
Web of Sience KeyUT