• MeSH
• aminokapronáty MeSH
• kožní absorpce účinky léků   MeSH
• kyselina 6-aminokapronová farmakologie   chemie   MeSH
• lidé MeSH
• pomocné látky chemie   MeSH
• techniky in vitro MeSH
• theofylin farmakokinetika   MeSH
• vazodilatancia farmakokinetika   MeSH
• vztahy mezi strukturou a aktivitou MeSH
• Check Tag
• lidé MeSH
• Geografické názvy
• Česká republika MeSH

Adefovir (9-(2-phosphonomethoxyethyl)adenine) is an acyclic nucleoside phosphonate currently used for the treatment of hepatitis B. The aim of this study was to evaluate the effect of permeation enhancer DDAK (6-dimethylaminohexanoic acid dodecyl ester) on the transdermal and topical delivery of adefovir. In porcine skin, DDAK enhanced adefovir flux 42 times with maximum at pH 5.8 suggesting ion pair formation. DDAK increased thermodynamic activity and stratum corneum/vehicle distribution coefficient of adefovir, as well as it directly decreased the skin barrier resistance. Maximal flux was observed already at 2% adefovir+1% DDAK. The results were confirmed in freshly excised human skin where DDAK enhanced adefovir flux 179 times to 8.9 microg/cm(2)/h. This rate of percutaneous absorption would allow for reaching effective plasma concentrations. After the topical application, adefovir concentrated in the stratum corneum with low penetration into the deeper skin layers from either aqueous or isopropyl myristate vehicle without the enhancer. With 1% DDAK, adefovir concentrations in the viable epidermis and dermis were 33-61 times higher. These results offer an attractive alternative to established routes of administration of adefovir and other acyclic nucleoside phosphonates.

• MeSH
• adenin analogy a deriváty   aplikace a dávkování   chemie   metabolismus   MeSH
• antivirové látky chemie   metabolismus   MeSH
• aplikace kožní MeSH
• chemie farmaceutická MeSH
• difuzní komory kultivační MeSH
• druhová specificita MeSH
• farmaceutická vehikula chemie   MeSH
• kapronáty farmakologie   chemie   MeSH
• kinetika MeSH
• koncentrace vodíkových iontů MeSH
• kožní absorpce účinky léků   MeSH
• kůže metabolismus   účinky léků   MeSH
• lidé MeSH
• methylaminy farmakologie   chemie   MeSH
• organofosfonáty aplikace a dávkování   chemie   metabolismus   MeSH
• permeabilita MeSH
• prasata MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• práce podpořená grantem MeSH