Hepatocytes targeting of cationic liposomes modified with soybean sterylglucoside and polyethylene glycol.
OBJECTIVE
In this study, a hepatocyte-specific targeting technology was developed by modifying cationic liposomes with soybean sterylglucoside (SG) and polyethylene glycol (PEG) (C/SG/PEG-liposomes).


METHODS
The liposomal transfection efficiencies in HepG(2) 2.2.15 cells were estimated with the use of fluorescein sodium (FS) as a model drug, by flow cytometry. The antisense activity of C/SG/PEG-liposomes entrapped antisense oligonucleotides (ODN) was determined as HBsAg and HBeAg in HepG(2) 2.2.15 cells by ELISA. The liposome uptake by liver and liver cells in mice was carried out after intravenous injection of (3)H-labeled liposomes.


RESULTS
C/SG-liposomes entrapped FS were effectively transfected into HepG(2) 2.2.15 cells in vitro. C/SG/PEG-liposomes entrapped ODN, reduced the secretion of both HBsAg and HBeAg in HepG(2) 2.2.15 cells when compared to free ODN. After in vivo injection of (3)H-labeled C/SG/PEG-liposomes, higher radiation accumulation was observed in the hepatocytes than non-parenchymal cells of the liver.


CONCLUSIONS
C/SG/PEG-liposomes mediated gene transfer to the liver is an effective gene-delivery method for hepatocytes-specific targeting, which appears to have a potential for gene therapy of HBV infections.
Qi
Xian-Rong
XR
Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China. qixr2001@yahoo.com.cn
Yan
Wen-Wei
WW
Shi
Jing
J
D000818:Animals; D006528:Carcinoma, Hepatocellular; D002412:Cations / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D002782:Cholestenes; D022781:Hepatocytes / Q000502:physiology*; D008081:Liposomes / Q000493:pharmacokinetics*; D008113:Liver Neoplasms; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D011092:Polyethylene Glycols; D013025:Glycine max; D014162:Transfection / Q000379:methods*; D014316:Tritium
D002412:Cations; D002782:Cholestenes; D008081:Liposomes; C096056:soy derived sterylglucoside mixture; D014316:Tritium; D011092:Polyethylene Glycols