Transdermal and dermal delivery of adefovir: effects of pH and permeation enhancers
Jazyk angličtina Země Nizozemsko Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
18248973
DOI
10.1016/j.ejpb.2007.12.005
PII: S0939-6411(07)00410-9
Knihovny.cz E-zdroje
- MeSH
- adenin aplikace a dávkování analogy a deriváty farmakokinetika MeSH
- antivirové látky aplikace a dávkování farmakokinetika MeSH
- aplikace kožní MeSH
- koncentrace vodíkových iontů MeSH
- kožní absorpce účinky léků MeSH
- lidé MeSH
- organofosfonáty aplikace a dávkování farmakokinetika MeSH
- permeabilita MeSH
- pomocné látky MeSH
- rozpouštědla MeSH
- systémy cílené aplikace léků MeSH
- techniky in vitro MeSH
- vysokoúčinná kapalinová chromatografie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- adefovir MeSH Prohlížeč
- adenin MeSH
- antivirové látky MeSH
- organofosfonáty MeSH
- pomocné látky MeSH
- rozpouštědla MeSH
The objective of this work was to investigate feasibility of transdermal and dermal delivery of adefovir (9-(2-phosphonomethoxyethyl)adenine), a broad-spectrum antiviral from the class of acyclic nucleoside phosphonates. Transport of 2% adefovir through and into porcine skin and effects of various solvents, pH, and permeation enhancers were studied in vitro using Franz diffusion cell. From aqueous donor samples, adefovir flux through the skin was 0.2-5.4 microg/cm2/h with greatest permeation rate at pH 7.8. The corresponding adefovir skin concentrations reached values of 120-350 microg/g of tissue. Increased solvent lipophilicity resulted in higher skin concentration but had only minor effect on adefovir flux. A significant influence of counter ions on both transdermal and dermal transport of adefovir zwitterion was observed at pH 3.4. Permeation enhancer dodecanol was ineffective, 1-dodecylazepan-2-one (Azone) and dodecyl 2-(dimethylamino)propionate (DDAIP) showed moderate activity. The highest adefovir flux (11.3+/-3.6 microg/cm2/h) and skin concentration (1549+/-416 microg/g) were achieved with 1% Transkarbam 12 (5-(dodecyloxycarbonyl)pentylammonium 5-(dodecyloxycarbonyl)pentylcarbamate) at pH 4. This study suggests that, despite its hydrophilic and ionizable nature, adefovir can be successfully delivered through the skin.
Citace poskytuje Crossref.org
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