Pharmaceutical Research

, Volume 25, Issue 2, pp 313–319

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
Research Paper

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.

Key words

anesthesia micelle microbial growth propofol PVP–PLA 

Copyright information

© Springer Science+Business Media, LLC 2007

Authors and Affiliations

  • François Ravenelle
    • 1
  • Sandra Gori
    • 1
  • Dorothée Le Garrec
    • 1
  • David Lessard
    • 1
  • Laibin Luo
    • 1
  • Dana Palusova
    • 1
  • J. Robert Sneyd
    • 2
  • Damon Smith
    • 1
  1. 1.Labopharm Inc.LavalCanada
  2. 2.Peninsula Medical SchoolUniversity of PlymouthPlymouthUK

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