Novel lipid and preservative-free propofol formulation: Properties and pharmacodynamics

François Ravenelle*, Sandra Gori, Dorothée Le Garrec, David Lessard, Laibin Luo, Dana Palusova, J. Robert Sneyd, Damon Smith

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

Purpose. 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.

Original languageEnglish
Pages (from-to)313-319
Number of pages7
JournalPharmaceutical Research
Volume25
Issue number2
DOIs
Publication statusPublished - Feb 2008

ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)

Keywords

  • Anesthesia
  • Micelle
  • Microbial growth
  • PVP-PLA
  • Propofol

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