title: Novel lipid and preservative-free propofol formulation: properties and pharmacodynamics.
abstract: OBJECTIVE
  Propofol is a water-insoluble intravenous anesthetic agent that is actually formulated as a water-in-oil emulsion with known drawbacks such as pain on injection, microorganism growth support and stability. We report on the properties of formulations of propofol in poly (N-vinyl-2-pyrrolidone)-block-poly(D,L-lactide), PVP-PLA, polymeric micelles (Propofol-PM).
  
  
  METHODS
  Microbial growth in these formulations was evaluated with Pseudomonas aeruginosa (ATCC 9027), Staphylococcus aureus (ATCC 6538), Escherichia coli (ATCC 25922) and Candida albicans (ATCC 10231). Sleep-recovery studies in female Sprague-Dawley rats, at a dose of 10mg/kg were performed to compare pharmacodynamic profiles of the new Propofol-PM formulations with those of Diprivan, a commercially available lipid based propofol formulation.
  
  
  RESULTS
  Growth of microorganisms was not supported in the Propofol-PM formulations tested. No significant differences in times to unconsciousness, awakening, recovery of righting reflex and full recovery were observed between Propofol-PM formulations and Diprivan.
  
  
  CONCLUSIONS
  Propofol loaded in PVP-PLA micelles (Propofol-PM) is not significantly different in terms of pharmacodynamic but demonstrates no microorganism growth support and improved stability that opens up the door to pain on injection reduction strategy.
authors.affiliation: Labopharm Inc., 480 Blvd. Armand-Frappier, Laval, Québec, Canada, H7V 4B4. fravenelle@labopharm.com
authors.forename: François
authors.initials: F
authors.lastname: Ravenelle
authors.forename: Sandra
authors.initials: S
authors.lastname: Gori
authors.forename: Dorothée
authors.initials: D
authors.lastname: Le Garrec
authors.forename: David
authors.initials: D
authors.lastname: Lessard
authors.forename: Laibin
authors.initials: L
authors.lastname: Luo
authors.forename: Dana
authors.initials: D
authors.lastname: Palusova
authors.forename: J Robert
authors.initials: JR
authors.lastname: Sneyd
authors.forename: Damon
authors.initials: D
authors.lastname: Smith
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D015169:Colony Count, Microbial; D004355:Drug Stability; D005260:Female; D010316:Particle Size; D015742:Propofol / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012890:Sleep / Q000187:drug effects
chemical_list: D015742:Propofol