Počet záznamů: 1
Dodecyl Amino Glucoside Enhances Transdermal and Topical Drug Delivery via Reversible Interaction with Skin Barrier Lipids
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SYSNO ASEP 0481743 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Dodecyl Amino Glucoside Enhances Transdermal and Topical Drug Delivery via Reversible Interaction with Skin Barrier Lipids Tvůrce(i) Kopečná, M. (CZ)
Macháček, M. (CZ)
Prchalová, Eva (UOCHB-X)
Štěpánek, P. (CZ)
Drašar, P. (CZ)
Kotora, Martin (UOCHB-X) RID, ORCID
Vávrová, K. (CZ)Zdroj.dok. Pharmaceutical Research. - : Springer - ISSN 0724-8741
Roč. 34, č. 3 (2017), s. 640-653Poč.str. 14 s. Jazyk dok. eng - angličtina Země vyd. US - Spojené státy americké Klíč. slova penetration enhancers ; sugar ; topical drug delivery ; transdermal drug delivery Vědní obor RIV FR - Farmakologie a lékárnická chemie Obor OECD Pharmacology and pharmacy Institucionální podpora UOCHB-X - RVO:61388963 UT WOS 000413909600006 EID SCOPUS 85008675526 DOI 10.1007/s11095-016-2093-z Anotace Skin permeation/penetration enhancers are substances that enable drug delivery through or into the skin. To search for new enhancers with high but reversible activity and acceptable toxicity, we synthesized a series of D-glucose derivatives, both hydrophilic and amphiphilic. Initial evaluation of the ability of these sugar derivatives to increase permeation and penetration of theophylline through/ into human skin compared with a control (no enhancer) or sorbitan monolaurate (Span 20, positive control) revealed dodecyl 6-amino-6-deoxy-a-D-glucopyranoside 5 as a promising enhancer. Furthermore, this amino sugar 5 increased epidermal concentration of a highly hydrophilic antiviral cidofovir by a factor of 7. The effect of compound 5 on skin electrical impedance suggested its direct interaction with the skin barrier. Infrared spectroscopy of isolated stratum corneum revealed no effect of enhancer 5 on the stratum corneum proteins but an overall decrease in the lipid chain order. The enhancer showed acceptable toxicity on HaCaT keratinocyte and 3T3 fibroblast cell lines. Finally, transepidermal water loss returned to baseline values after enhancer 5 had been removed from the skin. Compound 5, a dodecyl amino glucoside, is a promising enhancer that acts through a reversible interaction with the stratum corneum lipids. Pracoviště Ústav organické chemie a biochemie Kontakt asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Rok sběru 2018
Počet záznamů: 1