title: Characterization and skin permeation of ketoprofen-loaded vesicular systems.
abstract: OBJECTIVE
  To determine the effect of elasticity on the skin permeation of ketoprofen from surfactant-based vesicular formulations and elastic liposomes.
  
  
  METHODS
  Ketoprofen-loaded surfactant-based vesicles and elastic liposomes were prepared by sonication. Citric buffer (at pH 3.0) was used as rehydration buffer. Characterization studies of the prepared liposomal formulations were performed by dynamic light scattering, extrusion, and (1)H and (31)P nuclear magnetic resonance (NMR) spectroscopy. Ketoprofen transport studies across human skin were performed for all formulations.
  
  
  RESULTS
  Stable ketoprofen-loaded formulations were prepared. Addition of an edge activator, in the absence of the drug, increased the elasticity of the vesicles and liposomes. Ketoprofen loading reduced the elasticity of the liposomes and surfactant-based-vesicles. However, at saturation, the elasticity was still higher than that in the absence of the edge activator and ketoprofen, except for ketoprofen-loaded liposomes with Span 80. NMR studies revealed that the ketoprofen molecules were entrapped in a vesicle bilayer in all vesicular formulations and that the ketoprofen molecules affected the phosphate mobility in the liposomal formulations. Ketoprofen transport studies across human skin clearly showed that the surfactant-based vesicular formulations were superior to the elastic liposomal formulations.
  
  
  CONCLUSIONS
  Surfactant-based vesicles enhance ketoprofen transport across human skin, while no enhancement of ketoprofen was observed when loaded in elastic liposomes.
authors.affiliation: Department of Pharmacy, Faculty of Medicine, The University of Tokyo Hospital, The University of Tokyo, Tokyo, Japan; Leiden/Amsterdam Center for Drug Research, Gorlaeus Laboratories, Leiden University, Leiden, The Netherlands; Department of Clinical Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan. Electronic address: uchinot@u-shizuoka-ken.ac.jp.
authors.forename: Tomonobu
authors.initials: T
authors.lastname: Uchino
authors.affiliation: Division of NMR, Institute of Chemistry, Gorlaeus Laboratories, Leiden, The Netherlands.
authors.forename: Fons
authors.initials: F
authors.lastname: Lefeber
authors.affiliation: Leiden/Amsterdam Center for Drug Research, Gorlaeus Laboratories, Leiden University, Leiden, The Netherlands.
authors.forename: Gert
authors.initials: G
authors.lastname: Gooris
authors.affiliation: Leiden/Amsterdam Center for Drug Research, Gorlaeus Laboratories, Leiden University, Leiden, The Netherlands.
authors.forename: Joke
authors.initials: J
authors.lastname: Bouwstra
mesh_terms: D000279:Administration, Cutaneous; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry* / Q000378:metabolism; D004548:Elasticity; D006801:Humans; D007660:Ketoprofen / Q000008:administration & dosage* / Q000737:chemistry* / Q000378:metabolism; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D010316:Particle Size; D010539:Permeability; D012867:Skin / Q000378:metabolism*; D013501:Surface-Active Agents / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism
chemical_list: D004337:Drug Carriers; D008081:Liposomes; D013501:Surface-Active Agents; D007660:Ketoprofen
keywords: (1)H NMR; (31)P NMR; Elastic liposome; Ketoprofen; Surfactant-based vesicle; Transdermal delivery