Abstract: AimTo investigate the biodistribution and the hepatoctyes targeting of cationic liposome containing 3β-［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 hepatoctyes and non-hepatoctyes 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.