Amino acid derivatives as transdermal permeation enhancers

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F13%3A10145630" target="_blank" >RIV/00216208:11160/13:10145630 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0168365912007572" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0168365912007572</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.jconrel.2012.11.003" target="_blank" >10.1016/j.jconrel.2012.11.003</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Amino acid derivatives as transdermal permeation enhancers

Popis výsledku v původním jazyce

Transdermal permeation enhancers are compounds that temporarily decrease skin barrier properties to promote drug flux. In this study, we investigated enhancers with amino acids (proline, sarcosine, alanine, beta-alanine, and glycine) attached to hydrophobic chain(s) via a biodegradable ester link. The double-chain lipid-like substances displayed no enhancing effect, whereas single-chain substances significantly increased skin permeability. The proline derivative L-Pro2 reached enhancement ratios of up to 40 at 1% concentration, which is higher than that of thewell-established and standard enhancers Azone, DDAIP, DDAK, and Transkarbam 12. No stereoselectivity was observed. L-Pro2 acted synergistically with propylene glycol. Infrared studies revealed that L-Pro2 forms a separate liquid ordered phase in the stratum corneum lipids and has no significant effect on proteins. L-Pro2 action was at least partially reversible as measured by skin electrical impedance. Toxicity in keratinocyte (Ha

Název v anglickém jazyce

Amino acid derivatives as transdermal permeation enhancers

Popis výsledku anglicky

Transdermal permeation enhancers are compounds that temporarily decrease skin barrier properties to promote drug flux. In this study, we investigated enhancers with amino acids (proline, sarcosine, alanine, beta-alanine, and glycine) attached to hydrophobic chain(s) via a biodegradable ester link. The double-chain lipid-like substances displayed no enhancing effect, whereas single-chain substances significantly increased skin permeability. The proline derivative L-Pro2 reached enhancement ratios of up to 40 at 1% concentration, which is higher than that of thewell-established and standard enhancers Azone, DDAIP, DDAK, and Transkarbam 12. No stereoselectivity was observed. L-Pro2 acted synergistically with propylene glycol. Infrared studies revealed that L-Pro2 forms a separate liquid ordered phase in the stratum corneum lipids and has no significant effect on proteins. L-Pro2 action was at least partially reversible as measured by skin electrical impedance. Toxicity in keratinocyte (Ha

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

<a href="/cs/project/GAP207%2F11%2F0365" target="_blank" >GAP207/11/0365: Syntéza a studium strukturních závislostí ceramidů v kůži a látek s nimi interagujících</a><br>

Návaznosti

S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2013

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Journal of Controlled Release

ISSN

0168-3659

e-ISSN

—

Svazek periodika

165

Číslo periodika v rámci svazku

2

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

10

Strana od-do

91-100

Kód UT WoS článku

000315679100001

EID výsledku v databázi Scopus

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