Simplified stratum corneum model membranes for studying the effects of permeation enhancers
Jazyk angličtina Země Nizozemsko Médium print-electronic
Typ dokumentu časopisecké články
PubMed
29061325
DOI
10.1016/j.ijpharm.2017.10.038
PII: S0378-5173(17)31017-7
Knihovny.cz E-zdroje
- Klíčová slova
- Artificial model membranes, Franz diffusion cell, Permeation enhancers, Skin lipids, Transdermal absorption,
- MeSH
- aplikace kožní MeSH
- azepiny farmakologie MeSH
- ceramidy metabolismus MeSH
- cholesterol metabolismus MeSH
- indomethacin farmakologie MeSH
- kožní absorpce účinky léků MeSH
- kůže metabolismus MeSH
- kyseliny stearové metabolismus MeSH
- lidé MeSH
- membránové lipidy metabolismus MeSH
- membrány umělé MeSH
- permeabilita účinky léků MeSH
- prasata MeSH
- theofylin farmakologie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- azepiny MeSH
- ceramidy MeSH
- cholesterol MeSH
- indomethacin MeSH
- kyseliny stearové MeSH
- laurocapram MeSH Prohlížeč
- membránové lipidy MeSH
- membrány umělé MeSH
- stearic acid MeSH Prohlížeč
- theofylin MeSH
The activity of transdermal permeation enhancers is usually evaluated in vitro on human or animal skin, but skin samples can be hard to source and highly variable. To provide a more consistent basis for evaluating the activity of permeation enhancers, we prepared relatively simple and inexpensive artificial membranes that imitate the stratum corneum (SC) lipid matrix. Our membranes were composed of stearic acid, cholesterol, cholesterol sulfate and a ceramide (CER) component consisting of N-2-hydroxystearoyl phytosphingosine (CER[AP]) and/or N-stearoyl phytosphingosine (CER[NP]). First, the permeation of theophylline (TH) and indomethacin (IND) through these membranes was compared with their permeation through porcine skin. Because the mixed CER[AP]/[NP] membrane gave the closest results to skin, this membrane was then used to test the effects of two permeation enhancers: N-dodecyl azepan-2-one (Azone) and (S)-N-acetylproline dodecyl ester (L-Pro2). Both enhancers significantly increased the flux of TH and IND through the skin and, even more markedly, through the lipid membrane, L-Pro2 having a stronger effect than Azone. Thus, our simplified model of the SC lipid membrane based on phytosphingosine CERs appears to be suitable for mimicking skin permeation.
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