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

François Ravenelle1, Sandra Gori, Dorothée Le Garrec

  • 1Labopharm Inc., 480 Blvd. Armand-Frappier, Laval, Québec, Canada, H7V 4B4. fravenelle@labopharm.com

Pharmaceutical Research
|November 22, 2007
PubMed
Abstract

Insights

New propofol formulations in polymeric micelles (Propofol-PM) show no microbial growth and similar pharmacodynamics to Diprivan. This offers potential for reduced pain on injection and improved stability for the anesthetic agent.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Anesthesiology

Background:

  • Propofol, a common intravenous anesthetic, is formulated as a water-in-oil emulsion.
  • Current propofol formulations present drawbacks including pain on injection, susceptibility to microbial contamination, and stability issues.

Purpose of the Study:

  • To evaluate novel propofol formulations using poly (N-vinyl-2-pyrrolidone)-block-poly(D,L-lactide) (PVP-PLA) polymeric micelles, termed Propofol-PM.
  • To assess the microbiological and pharmacodynamic properties of Propofol-PM compared to a commercial propofol emulsion.

Main Methods:

  • Microbial growth inhibition was tested against Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, and Candida albicans.
  • Pharmacodynamic profiles were assessed in female Sprague-Dawley rats, comparing Propofol-PM with Diprivan at a 10mg/kg dose, focusing on sleep and recovery parameters.

Main Results:

  • Propofol-PM formulations demonstrated no support for microbial growth.
  • No significant differences were found in the times to unconsciousness, awakening, righting reflex recovery, or full recovery between Propofol-PM and Diprivan.

Conclusions:

  • Propofol-PM exhibits no microbial growth support and improved stability compared to conventional formulations.
  • These findings suggest Propofol-PM as a promising alternative for propofol delivery, potentially mitigating pain on injection.

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