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Targeted and synergistic therapy for hepatocellular carcinoma: monosaccharide modified lipid nanoparticles for the co-delivery of doxorubicin and sorafenib

Authors Duan W, Liu Y

Received 23 February 2018

Accepted for publication 31 May 2018

Published 11 July 2018 Volume 2018:12 Pages 2149—2161

DOI https://doi.org/10.2147/DDDT.S166402

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Editor who approved publication: Professor Jianbo Sun


Wendu Duan, Yan Liu

Department of Hepatobiliary Surgery, Affiliated Hospital of Hebei University, Baoding, Hebei Province 071000, People’s Republic of China

Purpose: Targeted hepatocellular carcinoma therapy was carried out to improve the efficacy of liver cancer treatment. The purpose of this study was to design an N-acetylgalactosamine (NAcGal) modified and pH sensitive doxorubicin (DOX) prodrug (NAcGal-DOX) for the construction of lipid nanoparticles (LNPs).
Methods: NAcGal-DOX and sorafenib (SOR) co-loaded LNPs were designed and the synergistic effects were evaluated on human hepatic carcinoma (HepG2) cells in vitro and anti-hepatic carcinoma mice model in vivo.
Results: Cellular uptake efficiency of NAcGal modified LNPs was significantly higher than unmodified LNPs. NAcGal modified LNPs showed the most significant inhibition effect among all the samples tested. The results revealed that the LNPs system achieved significant synergistic effects, best tumor inhibition ability and the lowest systemic toxicity.
Conclusion: These results proved that the NAcGal conjugated and pH sensitive co-delivery nano-system could be a promising strategy for treatment of hepatocellular carcinoma.

Keywords: hepatocellular carcinoma, asialoglycoprotein receptor, N-acetylgalactosamine, pH sensitive, prodrug

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