title: The influence of the acyl chain on the transdermal penetration-enhancing effect of synthetic phytoceramides.
abstract: OBJECTIVE
  The skin has become very attractive as a route for drug administration. Optimization of topical drug formulations by the addition of penetration enhancers may facilitate the passage of drugs through the stratum corneum.
  
  
  METHODS
  In this paper, the skin penetration effect of phytosphingosine and 9 derived phytoceramides (PCERs) on 3 transdermal model drugs (i.e. caffeine, testosterone, ibuprofen) was investigated via Franz diffusion cell experiments using split-thickness human skin. Azone was included as a positive control.
  
  
  RESULTS
  The main finding in our study was that the PCERs exerted a compound-dependent penetration-enhancing effect. Some of the investigated PCERs exhibited a penetration-enhancing ratio of more than 2 (mean ± SE): for caffeine PCER1 (2.48 ± 0.44), PCER2 (2.75 ± 0.74), PCER3 (2.62 ± 0.93) and PCER6 (2.70 ± 0.45) and for testosterone PCER1 (2.08 ± 0.56), PCER2 (2.56 ± 0.13), PCER3 (3.48), PCER4 (2.53), PCER5 (2.04 ± 0.14), PCER6 (2.05 ± 0.48) and PCER10 (4.84 ± 0.79), but none of them had an influence on ibuprofen.
  
  
  CONCLUSIONS
  The investigated PCERs exhibited a penetration-enhancing effect on caffeine and testosterone but not on ibuprofen.
authors.affiliation: Drug Quality and Registration Group, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium.
authors.forename: Lieselotte
authors.initials: L
authors.lastname: Veryser
authors.forename: Jente
authors.initials: J
authors.lastname: Boonen
authors.forename: Lien
authors.initials: L
authors.lastname: Taevernier
authors.forename: Joren
authors.initials: J
authors.lastname: Guillaume
authors.forename: Martijn
authors.initials: M
authors.lastname: Risseeuw
authors.forename: Syed Nisar Hussain
authors.initials: SN
authors.lastname: Shah
authors.forename: Nathalie
authors.initials: N
authors.lastname: Roche
authors.forename: Serge
authors.initials: S
authors.lastname: Van Calenbergh
authors.forename: Bart
authors.initials: B
authors.lastname: De Spiegeleer
mesh_terms: D000368:Aged; D002110:Caffeine / Q000494:pharmacology*; D002518:Ceramides / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D006801:Humans; D007052:Ibuprofen / Q000494:pharmacology*; D066298:In Vitro Techniques; D008875:Middle Aged; D015394:Molecular Structure; D010539:Permeability / Q000187:drug effects; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects; D013110:Sphingosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D013739:Testosterone / Q000494:pharmacology*
chemical_list: D002518:Ceramides; D002110:Caffeine; D013739:Testosterone; C012491:phytosphingosine; D013110:Sphingosine; D007052:Ibuprofen