Physicochemical and drug delivery aspects of lipid-based liquid crystalline nanoparticles: a case study of intravenously administered propofol.
Liquid crystalline nanoparticles (LCNP) formed through lipid self-assembly have a range of attractive properties as in vivo drug delivery carriers. In particular they offer: a wide solubilization spectrum, and consequently high drug payloads; effective encapsulation; stabilization and protection of sensitive drug substances. Here we present basic physicochemical features of non-lamellar LCNP systems with a focus on intravenous drug applications. This is exemplified by the formulation properties and in vivo behavior using the drug substance propofol; a well-known anesthetic agent currently used in clinical practice in the form of a stable emulsion. In order to appraise the drug delivery features of the LCNP system the current study was carried out with a marketed propofol emulsion product as reference. In this comparison the propofol-LCNP formulation shows several useful features including: higher drug-loading capacity, lower fat-load, excellent stability, modified pharmacokinetics, and an indication of increased effect duration.
Johnsson
Markus
M
Physical Chemistry 1, Lund University, P.O. Box 124, SE-221 00 Lund, Sweden.
Barauskas
Justas
J
Norlin
Andreas
A
Tiberg
Fredrik
F
D000818:Animals; D004058:Diffusion; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D006993:Hypnotics and Sedatives / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics; D007275:Injections, Intravenous; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes / Q000737:chemistry*; D050866:Liquid Crystals / Q000737:chemistry*; D008297:Male; D008422:Materials Testing; D008657:Metabolic Clearance Rate; D049329:Nanostructures / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D015742:Propofol / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley
D004337:Drug Carriers; D006993:Hypnotics and Sedatives; D008055:Lipids; D008081:Liposomes; D015742:Propofol