Amino acid derivatives as transdermal permeation enhancers

Result code in 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>
Result on the web
<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>

Result language
angličtina
Original language name
Amino acid derivatives as transdermal permeation enhancers
Original language description
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
Czech name
—
Czech description
—

Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
—

Project
<a href="/en/project/GAP207%2F11%2F0365" target="_blank" >GAP207/11/0365: Synthesis and structure-activity relationships of skin ceramides and agents targeting them</a><br>
Continuities
S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2013
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Similar results(10)