Jump to main content
Jump to site search

Issue 1, 2020
Previous Article Next Article

Collaborative assembly of doxorubicin and galactosyl diblock glycopolymers for targeted drug delivery of hepatocellular carcinoma

Author affiliations

Abstract

Hepatocellular carcinoma (HCC) patients suffer from severe pain due to the serious systemic side effects and low efficiency of chemotherapeutic drugs, and it is important to develop novel drug delivery systems to circumvent these issues. In this study, a series of galactose-based glycopolymers, poly(N-(prop-2-enoyl)-β-D-galactopyranosylamine)-b-poly(N-isopropyl acrylamide) (pGal(OH)-b-pNIPAA), were prepared through a sequential reversible addition-fragmentation chain transfer (RAFT) polymerization and tetrabutylammonium hydroxide (TBAOH)-mediated removal of acetyl groups. Hydrophilic doxorubicin hydrochloride was introduced to undergo collaborative assembly with poly(N-(prop-2-enoyl)-β-D-peracetylated galactosamine)-b-poly(N-isopropyl acrylamide) (pGal(Ac)-b-pNIPAA) via TBAOH treatment. pGal-b-pNIPAA/doxorubicin (DOX) delivery nanoparticles (GND NPs) formed by collaborative assembly were fully characterized by NMR, TEM and FT-IR, indicating the well-controlled formation of particles with uniform size and high efficiency in terms of drug loading and encapsulation compared with conventional adsorption methods. Meanwhile, the GND NPs were observed to be rapidly disintegrated under acidic conditions and resulted in an increased release of DOX. Cellular experiments showed that pGal-b-pNIPAA/DOX is apparently an asialoglycoprotein receptor (ASGPR)-mediated target of HCC, resulting in enhanced cellular uptake to HepG2 cells and anti-tumor efficacy in vitro. Furthermore, GND NPs III exerted more sustainable and effective anti-tumor effects compared to free DOX on a transgenic zebrafish TO(KrasG12V) model in vivo. These results indicated that the biocompatible nanomaterials developed by collaborative assembly with galactosyl diblock glycopolymers and DOX may serve as a promising candidates for targeting therapy of HCC.

Graphical abstract: Collaborative assembly of doxorubicin and galactosyl diblock glycopolymers for targeted drug delivery of hepatocellular carcinoma

Back to tab navigation

Supplementary files

Article information


Submitted
04 Oct 2019
Accepted
09 Nov 2019
First published
18 Nov 2019

Biomater. Sci., 2020,8, 189-200
Article type
Paper

Collaborative assembly of doxorubicin and galactosyl diblock glycopolymers for targeted drug delivery of hepatocellular carcinoma

J. Li, Y. Zhang, C. Cai, X. Rong, M. Shao, J. Li, C. Yang and G. Yu, Biomater. Sci., 2020, 8, 189
DOI: 10.1039/C9BM01604J

Social activity

Search articles by author

Spotlight

Advertisements