ArticlePharmaceutical research2002
Targeting efficiency of galactosylated liposomes to hepatocytes in vivo: effect of lipid composition.
Article in Pharmaceutical research, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 60 citations in OpenAlex.
- Targeted Hepatic Delivery of Bioactive Molecules via Nanovesicles: Recent Developments and Emerging Directions.Journal of personalized medicine · 2025Review
- Effect of Cholesterol Content of Lipid Composition in mRNA-LNPs on the Protein Expression in the Injected Site and Liver After Local Administration in Mice.Journal of pharmaceutical sciences · 2023Article
- Role of Liposomes-Based Stem Cell for Multimodal Cancer Therapy.Stem cell reviews and reports · 2020Review
- Anticancer activities of phytoconstituents and their liposomal targeting strategies against tumor cells and the microenvironment.Advanced drug delivery reviews · 2020Review
- Liver-targeted antiviral peptide nanocomplexes as potential anti-HCV therapeutics.Biomaterials · 2015Article
- Liposomes in tissue engineering and regenerative medicine.Journal of the Royal Society, Interface · 2014Review
- Receptor-mediated hepatocyte-targeted delivery of primaquine phosphate nanocarboplex using a carbohydrate ligand.Drug delivery and translational research · 2014Article
- Synthesis of novel tetravalent galactosylated DTPA-DSPE and study on hepatocyte-targeting efficiency in vitro and in vivo.International journal of nanomedicine · 2013Article
- Preliminary Study on Hepatocyte-Targeted Phosphorus-31 MRS Using ATP-Loaded Galactosylated Chitosan Oligosaccharide Nanoparticles.Gastroenterology research and practice · 2013Article
- Sustained liver targeting and improved antiproliferative effect of doxorubicin liposomes modified with galactosylated lipid and PEG-lipid.AAPS PharmSciTech · 2010Article
- Liposomal delivery of doxorubicin to hepatocytes in vivo by targeting heparan sulfate.International journal of pharmaceutics · 2009Article
- Nano-vectors for efficient liver specific gene transfer.International journal of nanomedicine · 2008Review
- Effective targeting of liposomes to liver and hepatocytes in vivo by incorporation of a Plasmodium amino acid sequence.Pharmaceutical research · 2006Article
- Biodistribution characteristics of galactosylated emulsions and incorporated probucol for hepatocyte-selective targeting of lipophilic drugs in mice.Pharmaceutical research · 2004Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo investigate the effects of the lipid composition of galactosylated liposomes on their targeted delivery to hepatocytes.
methodsSeveral types of liposomes with a particle size of about 90 nm were prepared using distearoyl-L-phosphatidylcholine (DSPC), cholesterol (Chol) and cholesten-5-yloxy-N-(4-((1-imino-2-D- thiogalactosylethyl)amino)butyl)formamide (Gal-C4-Chol), and labeled with [3H]cholesterol hexadecyl ether. Their tissue disposition was investigated in mice following intravenous injection. The binding and internalization characteristics were also studied in HepG2 cells.
resultsCompared with [H]DSPC/Chol (60:40) liposomes, [3H]DSPC/Chol/Gal-C4-Chol (60:35:5) liposomes exhibit extensive hepatic uptake. Separation of the liver cells showed that galactosylated liposomes are preferentially taken up by hepatocytes, whereas those lacking Gal-C4-Chol distribute equally to hepatocytes and nonparenchymal cells (NPC). Increasing the molar ratio of DSPC to 90% resulted in enhanced NPC uptake of both liposomes, suggesting their uptake via a mechanism other than asialoglycoprotein receptors. DSPC Chol/Gal-C4-Chol (60:35:5) and DSPC/Chol/Gal-C4-Chol (90:5:5) liposomes exhibited similar binding to the surface of HepG2 cells, but the former were taken up faster by the cells.
conclusionsThe recognition of galactosylated liposomes by the asialoglycoprotein receptors is dependent on the lipid composition. Cholesterol-rich galactosylated liposomes, exhibiting less non-specific interaction and greater receptor-mediated uptake, are better for targeting drugs to hepatocytes in vivo.
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