L-Serine and glycine based ceramide analogues as transdermal permeation enhancers: polar head size and hydrogen bonding
Language English Country Great Britain, England Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
12824032
DOI
10.1016/s0960-894x(03)00409-8
PII: S0960894X03004098
Knihovny.cz E-resources
- MeSH
- Administration, Cutaneous MeSH
- Azepines pharmacology MeSH
- Ceramides chemical synthesis pharmacology MeSH
- Diffusion Chambers, Culture MeSH
- Glycine chemistry MeSH
- Indicators and Reagents MeSH
- Skin Absorption drug effects MeSH
- Humans MeSH
- Excipients MeSH
- Serine chemistry MeSH
- In Vitro Techniques MeSH
- Theophylline administration & dosage pharmacokinetics MeSH
- Vasodilator Agents administration & dosage pharmacokinetics MeSH
- Hydrogen Bonding MeSH
- Chromatography, High Pressure Liquid MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Azepines MeSH
- Ceramides MeSH
- Glycine MeSH
- Indicators and Reagents MeSH
- laurocapram MeSH Browser
- Excipients MeSH
- Serine MeSH
- Theophylline MeSH
- Vasodilator Agents MeSH
Novel transdermal permeation enhancers related to stratum corneum ceramides were investigated. The synthesis of a series of simple compounds based on two selected amino acids, L-serine and glycine, and their enhancement activities are reported. Glycine derivative 3 enhanced the permeation of theophylline through human skin in vitro 12.5+/-0.5 times. The relationships between properties of the polar head of the compounds and their activity are discussed.
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