Novel Lipid and Preservative-free Propofol Formulation: Properties and Pharmacodynamics

Autor: Dana Palusova, Laibin Luo, Dorothée Le Garrec, Sandra Gori, David Lessard, J. Robert Sneyd, Francois Ravenelle, Damon Smith
Rok vydání: 2007
Předmět:
Zdroj: Pharmaceutical Research. 25:313-319
ISSN: 1573-904X
0724-8741
DOI: 10.1007/s11095-007-9471-5
Popis: 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). 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. 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®. 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.
Databáze: OpenAIRE
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