Document Detail


Liver targeting liposomes containing beta-sitosterol glucoside with regard to penetration-enhancing effect on HepG2 cells.
MedLine Citation:
PMID:  12081144     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Kumi Kawano; Kouji Nakamura; Kyoko Hayashi; Tsuneji Nagai; Kozo Takayama; Yoshie Maitani
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Biological & pharmaceutical bulletin     Volume:  25     ISSN:  0918-6158     ISO Abbreviation:  Biol. Pharm. Bull.     Publication Date:  2002 Jun 
Date Detail:
Created Date:  2002-06-25     Completed Date:  2002-12-31     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9311984     Medline TA:  Biol Pharm Bull     Country:  Japan    
Other Details:
Languages:  eng     Pagination:  766-70     Citation Subset:  IM    
Affiliation:
Institute of Medicinal Chemistry, Hoshi University, Tokyo, Japan.
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MeSH Terms
Descriptor/Qualifier:
Asialoglycoprotein Receptor / metabolism
Asialoglycoproteins / metabolism
Binding, Competitive / drug effects
Carcinoma, Hepatocellular / metabolism
Cell Membrane / drug effects,  metabolism
Cell Membrane Permeability / drug effects
Excipients / metabolism
Fluorescein-5-isothiocyanate
Humans
Liposomes / metabolism*
Liver / metabolism*
Liver Neoplasms / metabolism
Sitosterols / metabolism*
Tumor Cells, Cultured
alpha-Fetoproteins / metabolism
Chemical
Reg. No./Substance:
0/Asialoglycoprotein Receptor; 0/Asialoglycoproteins; 0/Excipients; 0/Liposomes; 0/Sitosterols; 0/alpha-Fetoproteins; 0/asialofetuin; 3326-32-7/Fluorescein-5-isothiocyanate; 474-58-8/lyoniside

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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