RRC ID 41596
著者 Kawano K, Nakamura K, Hayashi K, Nagai T, Takayama K, Maitani Y.
タイトル Liver targeting liposomes containing beta-sitosterol glucoside with regard to penetration-enhancing effect on HepG2 cells.
ジャーナル Biol Pharm Bull
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.
巻・号 25(6)
ページ 766-70
公開日 2002-6-1
DOI 10.1248/bpb.25.766
PMID 12081144
MeSH Asialoglycoprotein Receptor / metabolism Asialoglycoproteins / metabolism Binding, Competitive / drug effects Carcinoma, Hepatocellular / metabolism Cell Membrane / drug effects Cell Membrane / metabolism Cell Membrane Permeability / drug effects Excipients / metabolism Fetuins Fluorescein-5-isothiocyanate Humans Liposomes / metabolism* Liver / metabolism* Liver Neoplasms / metabolism Sitosterols / metabolism* Tumor Cells, Cultured alpha-Fetoproteins / metabolism
IF 1.863
引用数 12
WOS 分野 PHARMACOLOGY & PHARMACY
リソース情報
ヒト・動物細胞 Hep G2(RCB0468)