A novel, lipid-free nanodispersion formulation of propofol and its characterization.
OBJECTIVE
Propofol is a widely used anesthetic agent with highly desirable fast "on" and "off" effects. It is currently formulated as lipid emulsions, which are known to support microbial growth. In this study, a novel, lipid-free nanodispersion formulation of propofol was characterized.


METHODS
The formulation was evaluated for its physical and chemical stability, in vitro compatibility with red blood cells, and its antimicrobial effectiveness. In vivo pharmacokinetic and pharmacodynamic properties of the formulation were evaluated in rats.


RESULTS
Our data suggest that this lipid-free formulation is physically and chemically stable. Compared to the commercial emulsion formulation Diprivan, it causes less hemolysis with red blood cells and has improved antimicrobial activity. In addition, the lipid-free formulation demonstrates similar pharmacological effects to Diprivan in rats.


CONCLUSIONS
This novel, lipid-free formulation exhibits improved in vitro properties without compromising in vivo effects, therefore representing a promising new alternative for propofol.
Chen
Hongming
H
TransForm Pharmaceuticals, Inc., 29 Hartwell Avenue, Lexington, Massachusetts 02421, USA. chen@transformpharma.com
Zhang
Zhong
Z
Almarsson
Orn
O
Marier
Jean-Francois
JF
Berkovitz
Dina
D
Gardner
Colin R
CR
D000818:Animals; D002626:Chemistry, Pharmaceutical; D006461:Hemolysis / Q000187:drug effects / Q000502:physiology; D006801:Humans; D008297:Male; D009043:Motor Activity / Q000187:drug effects / Q000502:physiology; D049329:Nanostructures / Q000737:chemistry; D015742:Propofol / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
D015742:Propofol