Synthesis and transdermal penetration of NSAID glycoside esters.
The glucoside and mannoside derivatives of the NSAIDs flurbiprofen, ibuprofen, ketoprofen and naproxen were synthesised and their penetration through human skin was determined. Experimental transdermal flux data showed that the parent NSAIDs penetrated human skin to a much higher extent than the glycosides.
Swart
Henk
H
School of Pharmacy, North-West University, Potchefstroom 2520, South Africa.
Breytenbach
Jaco C
JC
Hadgraft
Jonathan
J
du Plessis
Jeanetta
J
D000279:Administration, Cutaneous; D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D002384:Catalysis; D002851:Chromatography, High Pressure Liquid; D004952:Esters / Q000138:chemical synthesis / Q000493:pharmacokinetics; D005260:Female; D005947:Glucose / Q000737:chemistry; D006027:Glycosides / Q000138:chemical synthesis / Q000493:pharmacokinetics; D006801:Humans; D066298:In Vitro Techniques; D008358:Mannose / Q000737:chemistry; D000442:Octanols / Q000737:chemistry; D012869:Skin Absorption / Q000502:physiology*; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship; D014867:Water / Q000737:chemistry
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004952:Esters; D006027:Glycosides; D000442:Octanols; D014867:Water; D005947:Glucose; D008358:Mannose