Galactosyl Pentadecene Reversibly Enhances Transdermal and Topical Drug Delivery
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F17%3A00479473" target="_blank" >RIV/61388963:_____/17:00479473 - isvavai.cz</a>
Alternative codes found
RIV/00216208:11160/17:10365075 RIV/00216208:11310/17:10365075 RIV/60461373:22330/17:43913350
Result on the web
<a href="http://dx.doi.org/10.1007/s11095-017-2214-3" target="_blank" >http://dx.doi.org/10.1007/s11095-017-2214-3</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1007/s11095-017-2214-3" target="_blank" >10.1007/s11095-017-2214-3</a>
Alternative languages
Result language
angličtina
Original language name
Galactosyl Pentadecene Reversibly Enhances Transdermal and Topical Drug Delivery
Original language description
To study new skin penetration/permeation enhancers based on amphiphilic galactose derivatives. Two series of alkyl and alkenyl galactosides were synthesized and evaluated for their enhancing effect on transdermal/topical delivery of theophylline (TH), hydrocortisone (HC) and cidofovir (CDV), reversibility of their effects on transepidermal water loss (TEWL) and skin impedance, interaction with the stratum corneum using infrared spectroscopy, and cytotoxicity on keratinocytes and fibroblasts. Initial evaluation identified 1-(alpha-d-galactopyranosyl)-(2E)-pentadec-2-ene A15 as a highly potent enhancer - it increased TH and HC flux through human skin 8.5 and 5 times, respectively. Compound A15 increased the epidermal concentration of a potent antiviral CDV 7 times over that reached by control and Span 20 (an established sugar-based enhancer). Infrared spectroscopy of human stratum corneum indicated interaction of A15 with skin barrier lipids but not proteins. These effects of A15 on the skin barrier were reversible (both TEWL and skin impedance returned to baseline values within 24 h after A15 had been removed from skin). In vitro toxicity of A15 on HaCaT keratinocytes and 3T3 fibroblasts was acceptable, with IC50 values over 60 mu M. Galactosyl pentadecene A15 is a potent enhancer with low toxicity and reversible action.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30104 - Pharmacology and pharmacy
Result continuities
Project
<a href="/en/project/GA13-23891S" target="_blank" >GA13-23891S: Lipid membrane models – a new tool for studying pathophysiology of skin diseases at a molecular level</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Pharmaceutical Research
ISSN
0724-8741
e-ISSN
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Volume of the periodical
34
Issue of the periodical within the volume
10
Country of publishing house
US - UNITED STATES
Number of pages
12
Pages from-to
2097-2108
UT code for WoS article
000409050300010
EID of the result in the Scopus database
2-s2.0-85021751271