Extended in vivo blood circulation time of fluorinated liposomes.
The clearance from blood circulation of fluorinated liposomes made with perfluoroalkylated phosphatidylcholines was investigated in mice using liposome-entrapped 5(6)-carboxyfluorescein. The presence of a fluorinated core inside the membrane strongly retards their blood clearance. The fluorinated vesicles showed circulation half-lives of up to 8.6 h, which are 6-13 and 3-6 times larger than those of similarly sized conventional distearoylphosphatidylcholine and distearoylphosphatidylcholine/cholesterol liposomes, respectively. Their blood clearance was similar to that of some polyethylene glycol (PEG)-labelled 'stealth' liposomes and was dose-independent in a 3.3-330 mumol/kg body weight dose range.
Santaella
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C
Laboratoire de Chimie Moléculaire, URA 426 au CNRS, Faculté des Sciences, Université de Nice-Sophia Antipolis, France.
Frézard
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F
Vierling
P
P
Riess
J G
JG
D000818:Animals; D002784:Cholesterol; D004305:Dose-Response Relationship, Drug; D006801:Humans; D006845:Hydrocarbons, Fluorinated / Q000097:blood*; D008081:Liposomes; D008297:Male; D008657:Metabolic Clearance Rate; D051379:Mice; D010713:Phosphatidylcholines / Q000097:blood*; D011092:Polyethylene Glycols; D051381:Rats; D011919:Rats, Inbred Strains; D013997:Time Factors
D006845:Hydrocarbons, Fluorinated; D008081:Liposomes; D010713:Phosphatidylcholines; D011092:Polyethylene Glycols; D002784:Cholesterol; C010942:1,2-distearoyllecithin