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

Authors :
Dana Palusova
Laibin Luo
Dorothée Le Garrec
Sandra Gori
David Lessard
J. Robert Sneyd
Francois Ravenelle
Damon Smith
Source :
Pharmaceutical Research. 25:313-319
Publication Year :
2007
Publisher :
Springer Science and Business Media LLC, 2007.

Abstract

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.

Details

ISSN :
1573904X and 07248741
Volume :
25
Database :
OpenAIRE
Journal :
Pharmaceutical Research
Accession number :
edsair.doi.dedup.....f14c62d4e076c8cd0791e646a22a442e
Full Text :
https://doi.org/10.1007/s11095-007-9471-5