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P-Glycoprotein in skin contributes to transdermal absorption of topical corticosteroids
http://hdl.handle.net/2297/47881
http://hdl.handle.net/2297/47881ef91ea93-b2d0-42b8-845b-21a17c24fe12
名前 / ファイル | ライセンス | アクション |
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PH-PR-KATO-Y-365.pdf (288.7 kB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2017-12-05 | |||||
タイトル | ||||||
タイトル | P-Glycoprotein in skin contributes to transdermal absorption of topical corticosteroids | |||||
言語 | ||||||
言語 | eng | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
著者 |
Hashimoto, Naoto
× Hashimoto, Naoto× Nakamichi, Noritaka× Yamazaki, Erina× Oikawa, Masashi× Masuo, Yusuke× Schinkel, Alfred H.× Kato, Yukio |
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書誌情報 |
International Journal of Pharmaceutics 巻 521, 号 1-2, p. 365-373, 発行日 2017-04-15 |
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ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0378-5173 | |||||
NCID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA00680771 | |||||
DOI | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.ijpharm.2017.02.064 | |||||
出版者 | ||||||
出版者 | Elsevier B.V. | |||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | ATP binding cassette transporters, P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), are expressed in skin, but their involvement in transdermal absorption of clinically used drugs remains unknown. Here, we examined their role in transdermal absorption of corticosteroids. Skin and plasma concentrations of dexamethasone after dermal application were reduced in P-gp and BCRP triple-knockout (Mdr1a/1b/Bcrp−/−) mice. The skin concentration in Mdr1a/1b/Bcrp−/− mice was reduced in the dermis, but not in the epidermis, indicating that functional expression of these transporters in skin is compartmentalized. Involvement of these transporters in dermal transport of dexamethasone was also supported by the observation of a higher epidermal concentration in Mdr1a/1b/Bcrp−/− than wild-type mice during intravenous infusion. Transdermal absorption after dermal application of prednisolone, but not methylprednisolone or ethinyl estradiol, was also lower in Mdr1a/1b/Bcrp−/− than in wild-type mice. Transport studies in epithelial cell lines transfected with P-gp or BCRP showed that dexamethasone and prednisolone are substrates of P-gp, but are minimally transported by BCRP. Thus, our findings suggest that P-gp is involved in transdermal absorption of at least some corticosteroids in vivo. P-gp might be available as a target for inhibition in order to deliver topically applied drugs and cosmetics in a manner that minimizes systemic exposure. © 2017 Elsevier B.V. | |||||
内容記述 | ||||||
内容記述タイプ | Other | |||||
内容記述 | Embargo Period 12 months | |||||
権利 | ||||||
権利情報 | Copyright © Elsevier B.V. (CCC-BY NC ND) | |||||
著者版フラグ | ||||||
出版タイプ | AM | |||||
出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa | |||||
関連URI | ||||||
識別子タイプ | URI | |||||
関連識別子 | http://www.elsevier.com/locate/issn/03785173 |