Liver targeting liposomes containing beta-sitosterol glucoside with regard to penetration-enhancing effect on HepG2 cells.
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| Abstract |
The aim of this study was to examine the interaction of soybean-derived sterylglucoside (SG) with the human hepatoblastoma cell line HepG2 with regard to the penetration-enhancing effect of beta-sitosterol glucoside (Sit-G) to clarify the accumulation of SG-containing liposomes (SG-liposomes) to the liver in vivo. The approach was based on measurement of the association of SG-liposomes labeled with 1,1'-dioctadecyl-3,3,3',3'-tetramethylindocarbocyanine perchlorate (Dil) in terms of asialoglycoprotein receptor (ASGP-R)-mediated endocytosis, affinity of Sit-G using lAsys and the association of FITC-dextran 4400 (FD-4) increased by Sit-G with the cells. The association of SG-liposomes was decreased by addition of asialofetuin, suggesting that SG-liposomes might be taken up via ASGP-R. Sit-G showed higher affinity with HepG2 cells than HeLa cells, and enhanced the association of FD-4 depending on the incubation time and Sit-G concentrations. Significant positive correlations were found between Sit-G and FD-4 association with the cells, indicating that Sit-G enhanced the drug penetration by distribution in cell membranes. The high degree of liver association of SG-liposomes in vivo might be related to recognition of glucose residues of SG by ASGP-R and to the high affinity and penetration-enhancing effect of Sit-G with hepatocytes.
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| Authors | Kumi Kawano, Kouji Nakamura, Kyoko Hayashi, Tsuneji Nagai, Kozo Takayama, Yoshie Maitani |
| Journal | Biological & pharmaceutical bulletin (Biol Pharm Bull) Vol. 25 Issue 6 Pg. 766-70 (Jun 2002) ISSN: 0918-6158 [Print] Japan |
| PMID | 12081144 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't) |
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