ArticleAAPS PharmSciTech2010
Sustained liver targeting and improved antiproliferative effect of doxorubicin liposomes modified with galactosylated lipid and PEG-lipid.
Article in AAPS PharmSciTech, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 50 citations in OpenAlex.
- Advances in constructing biocompatible nanocarriers.Drug delivery and translational research · 2025Review
- Article
- Glycosylation shapes the efficacy and safety of diverse protein, gene and cell therapies.Biotechnology advances · 2023Review
- Identification of immune infiltration-related genes as prognostic indicators for hepatocellular carcinoma.BMC cancer · 2022Article
- Advances in Nanoliposomes for the Diagnosis and Treatment of Liver Cancer.International journal of nanomedicine · 2022Review
- Article
- Cleavable PEGylation: a strategy for overcoming the "PEG dilemma" in efficient drug delivery.Drug delivery · 2017Review
- Synthesis of novel tetravalent galactosylated DTPA-DSPE and study on hepatocyte-targeting efficiency in vitro and in vivo.International journal of nanomedicine · 2013Article
- Local targeted therapy of liver metastasis from colon cancer by galactosylated liposome encapsulated with doxorubicin.PloS one · 2013Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In this study, a cleavable PEG-lipid (methoxypolyethyleneglycol 2000-cholesteryl hemisuccinate, PEG(2000)-CHEMS) linked via ester bond and galactosylated lipid ((5-cholesten-3beta-yl) 4-oxo-4-[2-(lactobionyl amido) ethylamido] butanoate, CHS-ED-LA) were used to modify doxorubicin (DOX) liposome. DOX was encapsulated into conventional liposomes (CL), galactosylated liposomes (modified with CHS-ED-LA, GalL), pegylated liposomes (modified with PEG(2000)-CHEMS, PEG-CL), and pegylated galactosylated liposomes (modified with CHS-ED-LA and PEG(2000)-CHEMS, PEG-GalL) using an ammonium sulfate gradient loading method and then intravenously injected to normal mice. Both PEG-GalL DOX and GalL DOX gave relatively high overall drug targeting efficiencies to liver ((T(e))(liver)) and were mainly taken up by hepatocyte. However, PEG-GalL DOX showed unique "sustained targeting" characterized by slowed transfer of DOX to liver and reduced peak concentrations in the liver. The biodistribution and antitumor efficacy of various DOX preparations were studied in hepatocarcinoma 22 (H22) tumor-bearing mice. The inhibitory rate of PEG-GalL DOX to H22 tumors was up to 94%, significantly higher than that of PEG-CL DOX, GalL DOX, CL DOX, and free DOX, although the tumor distribution of DOX revealed no difference between PEG-GalL DOX and PEG-CL DOX. Meanwhile, the gradual increase in the liver DOX concentration due to the sustained uptake of PEG-GalL DOX formulations resulted in lower damage to liver. In conclusion, the present investigation indicated that double modification of liposomes with PEG(2000)-CHEMS, and CHS-ED-LA represents a potentially advantageous strategy in the therapy of liver cancers or other liver diseases.
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