Liver targeting of cationic liposomes modified with soybean-derived sterylglucoside in vitro / 药学学报

ABSTRACT

<p><b>AIM</b>To construct a liposomal liver targeting delivery system by adding soybean-derived sterylglucoside (SG) to the cationic liposomes.</p><p><b>METHODS</b>The 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 hepatocytes and non-hepatocytes were separated and examined after perfusing.</p><p><b>RESULTS</b>All the formula yielded high incorporation efficiency (83.12% - 91.74%), small particle size (93.0 - 124.4 nm). The zeta 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-hepatocytes of each respectively, only SG/Brij-35 liposomes showed difference in FS uptake by hepatocytes (P < 0.05).</p><p><b>CONCLUSION</b>It showed that SG/Brij-35 modified cationic liposomes are potentially useful drug carrier to liver but may be affected by different modification.</p>