A novel galactose-PEG-conjugated biodegradable copolymer is an efficient gene delivery vector for immunotherapy of hepatocellular carcinoma

Biomaterials. 2018 Nov:184:20-30. doi: 10.1016/j.biomaterials.2018.08.064. Epub 2018 Sep 1.

Abstract

Successful immunogene therapy depends not only on the therapeutic gene but also on the gene delivery vector. In this study, we synthesized a novel copolymer consisting of low-molecular-weight polyethylenimine (PEI) cross-linked by myo-inositol (INO) and conjugated with a galactose-grafted PEG chain, named LA-PegPI. We characterized the chemical structure and molecular weight of the copolymer and particle properties of LA-PegPI/pDNA. Furthermore, we showed that LA-PegPI/pDNA polyplexes possessed excellent stability in physiological salt solution, low cytotoxicity, and high transfection efficiency in the asialoglycoprotein receptor (ASGPR)-positive liver cells in vitro. Importantly, we also showed that through intraperitoneal injection of LA-PegPI/pDNA nanoparticles, the reporter gene was forcefully expressed in the liver hepatocytes of mice. Finally, we documented that intraperitoneal injection of LA-PegPI/pIL15 nanoparticles effectively suppressed tumor growth and prolonged survival time of tumor-bearing mice via activation of CD8+ T cells and NK cells and upregulation of the cytokines IFN-γ, TNF, and IL12 in an orthotopic hepatocellular carcinoma mouse model. Interestingly, LA-PegPI/pluc nanoparticles could effectively stimulate the proliferation of NK cells and inhibit tumor growth in this model. In summary, LA-PegPI is a useful gene vector for immunogene therapy of hepatocellular carcinoma, and its potential for clinical application warrants further study.

Keywords: Galactose; IL15; Immunogene therapy; Liver target; Polyethylenimine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Asialoglycoprotein Receptor / genetics*
  • Carcinoma, Hepatocellular / immunology
  • Carcinoma, Hepatocellular / metabolism
  • Carcinoma, Hepatocellular / therapy*
  • Cell Line, Tumor
  • Cross-Linking Reagents / chemistry
  • DNA / administration & dosage
  • Drug Carriers
  • Female
  • Galactose / chemistry*
  • Genes, Reporter
  • Hepatocytes / pathology
  • Humans
  • Immunotherapy
  • Inositol / chemistry
  • Interleukin-15 / genetics
  • Interleukin-15 / metabolism*
  • Liver Neoplasms / immunology
  • Liver Neoplasms / metabolism
  • Liver Neoplasms / therapy*
  • Mice, Inbred BALB C
  • Molecular Weight
  • Nanoparticles / chemistry
  • Plasmids
  • Polyethylene Glycols / chemistry*
  • Polyethyleneimine / chemistry

Substances

  • Asialoglycoprotein Receptor
  • Cross-Linking Reagents
  • Drug Carriers
  • Interleukin-15
  • Polyethylene Glycols
  • Inositol
  • Polyethyleneimine
  • DNA
  • Galactose