Liver targeting of cationic liposomes modified with soybean-derived sterylglucoside in vitro

AimTo construct a liposomal liver targeting delivery system by adding soybean-derived sterylglucoside (SG) to the cationic liposomes. MethodsThe physico-chemical properties of SG modified cationic lipsomes were investigated using fluorescein sodium (FS) as a model drug, as well as the interaction of SG modified liposomes with HepG₂ 2.2.15 cells in the point of involvement of asialoglycoprotein receptor (ASGP-R) mediated transfection. Liver targeting of modified cationic liposomes were also investigated using liver perfusing technique, and hepatoctyes and non-hepatoctyes were separated and examined after perfusing. ResultsAll the formula yielded high incorporation efficiency (83.12%-91.74%), small particle size (93.0-124.4 nm). The ζ potential of blank liposomes all showed positive values. The transfection efficiency of FS entrapped in SG-liposomes with HepG₂ 2.2.15 was significantly higher than that of liposomes without modification. The transfection of SG-liposomes were reduced significantly by the 20/30 mmol galactose as a competitor of ASGP-R. All the cationic liposomes showed high level of liver uptake of FS. Compared with the uptake of non-hepatoctyes of each respectively, only SG/Brij-35 liposomes showed difference in FS uptake by hepatoctyes (P<0.05). ConclusionIt showed that SG/Brij-35 modified cationic liposomes are potentially useful drug carrier to liver but may be affected by different modification.