Biodistribution and hepatocytes targeting of cationic liposomes surface-modified with sterylglucoside and golyethylene glycol.
- Author:
Jing SHI
1
;
Wen-Wei YAN
;
Xian-Rong QI
;
Li YANG
;
Li ZHANG
Author Information
- Publication Type:Journal Article
- MeSH: 1,2-Dipalmitoylphosphatidylcholine; administration & dosage; pharmacokinetics; Animals; Area Under Curve; Cholestenes; administration & dosage; pharmacokinetics; Cholesterol; administration & dosage; analogs & derivatives; pharmacokinetics; Drug Carriers; Drug Delivery Systems; Hepatocytes; metabolism; Liposomes; administration & dosage; pharmacokinetics; Male; Mice; Oligodeoxyribonucleotides, Antisense; administration & dosage; pharmacokinetics; Phosphatidylethanolamines; administration & dosage; pharmacokinetics; Polyethylene Glycols; administration & dosage; pharmacokinetics; Tissue Distribution
- From: Acta Pharmaceutica Sinica 2004;39(7):551-555
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo investigate the biodistribution and the hepatocytes targeting of cationic liposome containing 3beta[N-( N',N'-dimethylaminoethane) carbamoyl] cholesterol (DC-Chol) and surface-modified liposomes with sterylglucoside (SG) and polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE).
METHODSCationic liposomes (CL) composed of DC-Chol and dipalmitoylphosphatidylcholine (DPPC), SG/PEG modified cationic liposome (SG/PEG-CL), both contained trace 3H-cholesterol (3H-Chol) as radiolabel, were prepared. The liposomes encapsulating 125I-labled antisense oligodeoxynucleotide (125I-asODN) (SG/PEG-CL-asODN) were also prepared. The biodistribution of CL, SG/PEG-CL, SG/PEG-C2-asODN as well as 125I-asODN solution, were studied. The radioactivities in hepatocytes and non-hepatocytes after administration of CL and SG/PEG-CL were determined by infuseing method.
RESULTSCL and SG/PEG CL significantly aggregated in liver. The distribution of SG/PEG CL was significantly higher in hepatocytes (P < 0.01) and lower in non-hepatocytes (P < 0.01) than that of CL. The concentrations of SG/PEG-CL-asODN in liver and spleen were significantly higher than that of asODN solution (P < 0.01).
CONCLUSIONCationic liposome modified with SG/PEG changed the distribution of asODN. Cationic liposome can target hepatocytes more effective after being modified with SG.