Galactosyl Pentadecene Reversibly Enhances Transdermal and Topical Drug Delivery
Identifikátory výsledku
Kód výsledku v 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>
Nalezeny alternativní kódy
RIV/00216208:11160/17:10365075 RIV/00216208:11310/17:10365075 RIV/60461373:22330/17:43913350
Výsledek na webu
<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>
Alternativní jazyky
Jazyk výsledku
angličtina
Název v původním jazyce
Galactosyl Pentadecene Reversibly Enhances Transdermal and Topical Drug Delivery
Popis výsledku v původním jazyce
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.
Název v anglickém jazyce
Galactosyl Pentadecene Reversibly Enhances Transdermal and Topical Drug Delivery
Popis výsledku anglicky
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.
Klasifikace
Druh
J<sub>imp</sub> - Článek v periodiku v databázi Web of Science
CEP obor
—
OECD FORD obor
30104 - Pharmacology and pharmacy
Návaznosti výsledku
Projekt
<a href="/cs/project/GA13-23891S" target="_blank" >GA13-23891S: Modely lipidových membrán - nový nástroj pro studium patofyziologie kožních onemocnění na molekulární úrovni</a><br>
Návaznosti
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Ostatní
Rok uplatnění
2017
Kód důvěrnosti údajů
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Údaje specifické pro druh výsledku
Název periodika
Pharmaceutical Research
ISSN
0724-8741
e-ISSN
—
Svazek periodika
34
Číslo periodika v rámci svazku
10
Stát vydavatele periodika
US - Spojené státy americké
Počet stran výsledku
12
Strana od-do
2097-2108
Kód UT WoS článku
000409050300010
EID výsledku v databázi Scopus
2-s2.0-85021751271