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《Acta Pharmaceutica Sinica》 2006-01
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Liver targeting of cationic liposomes modified with soybean-derived sterylglucoside in vitro

SHI Jing~1, QI Xian-rong~1*, YANG Li~1, FEI Ran~2 , WEI Lai~2(1. Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing 100083, China; 2. Institute of Hepatology, People’s Hospital, Peking University, Beijing 100044, China)  
Aim To construct a liposomal liver targeting delivery system by adding soybean-derived sterylglucoside (SG) to the cationic liposomes. Methods 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 HepG_2 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. Results All 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 HepG_2 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 (P0.05). Conclusion It showed that SG/Brij-35 modified cationic liposomes are potentially useful drug carrier to liver but may be affected by different modification.
【Fund】: 国家自然科学基金资助项目(30371265)
【CateGory Index】: R94
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