AIM： 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 ...AIM： 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 HepG2 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 HepG2 2.2.15 cells by ELISA. The liposome uptake by liver and liver cells in mice was carried out after intravenous injection of 3H-labeled liposomes. RESULTS： C/SG-liposomes entrapped FS were effectively transfected into HepG2 2.2.15 cells in vitro. C/SG/PEG-Iiposomes entrapped ODN, reduced the secretion of both HBsAg and HBeAg in HepG2 2.2.15 cells when compared to free ODN. After in vivo injection of ^3H-labeled C/SG/PEG-liposomes, higher radiation accumulation was observed in the hepatocytes than non-parenchymal cells of the liver. CONCLUSION： 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.展开更多
基金Supported by the National Natural Science Foundation of China,No. 30371265
文摘AIM： 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 HepG2 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 HepG2 2.2.15 cells by ELISA. The liposome uptake by liver and liver cells in mice was carried out after intravenous injection of 3H-labeled liposomes. RESULTS： C/SG-liposomes entrapped FS were effectively transfected into HepG2 2.2.15 cells in vitro. C/SG/PEG-Iiposomes entrapped ODN, reduced the secretion of both HBsAg and HBeAg in HepG2 2.2.15 cells when compared to free ODN. After in vivo injection of ^3H-labeled C/SG/PEG-liposomes, higher radiation accumulation was observed in the hepatocytes than non-parenchymal cells of the liver. CONCLUSION： 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.
