Targeted Codelivery of an Antigen and Dual Agonists by Hybrid Nanoparticles for Enhanced Cancer Immunotherapy

Nano Lett. 2019 Jul 10;19(7):4237-4249. doi: 10.1021/acs.nanolett.9b00030. Epub 2019 Mar 21.

Abstract

Among approaches of current cancer immunotherapy, a dendritic cell (DC)-targeted vaccine based on nanotechnology could be a promising way to efficiently induce potent immune responses. To enhance DC targeting and vaccine efficiency, we included imiquimod (IMQ), a toll-like receptor 7/8 (TLR 7/8) agonist, and monophosphoryl lipid A (MPLA), a TLR4 agonist, to synthesize lipid-polymer hybrid nanoparticles using PCL-PEG-PCL and DOTAP (IMNPs) as well as DSPE-PEG-mannose (MAN-IMNPS). The spatiotemporal delivery of MPLA (within the outer lipid layer) to extracellular TLR4 and IMQ (in the hydrophobic core of NPs) to intracellular TLR7/8 can activate DCs synergistically to improve vaccine efficacy. Ovalbumin (OVA) as a model antigen was readily absorbed by positively charged DOTAP and showed a quick release in vitro. Our results demonstrated that this novel nanovaccine enhanced cellular uptake, cytokine production, and maturation of DCs. Compared with the quick metabolism of free OVA-agonists, the depot effect of OVA-IMNPs was observed, whereas MAN-OVA-IMNPs promoted trafficking to secondary lymphoid organs. After immunization with a subcutaneous injection, the nanovaccine, especially MAN-OVA-IMNPs, induced more antigen-specific CD8+ T cells, greater lymphocyte activation, stronger cross-presentation, and more generation of memory T cells, antibody, IFN-γ, and granzyme B. Prophylactic vaccination of MAN-OVA-IMNPs significantly delayed tumor development and prolonged the survival in mice. The therapeutic tumor challenge indicated that MAN-OVA-IMNPs prohibited tumor progression more efficiently than other formulations, and the combination with an immune checkpoint blockade further enhanced antitumor effects. Hence, the DC-targeted vaccine codelivery with IMQ and MPLA adjuvants by hybrid cationic nanoparticles in a spatiotemporal manner is a promising multifunctional antigen delivery system in cancer immunotherapy.

Keywords: Hybrid nanoparticles; TLR agonists; antigen; cancer immunotherapy; vaccine delivery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antigens, Neoplasm* / immunology
  • Antigens, Neoplasm* / pharmacology
  • CD8-Positive T-Lymphocytes / immunology
  • CD8-Positive T-Lymphocytes / pathology
  • Cancer Vaccines* / immunology
  • Cancer Vaccines* / pharmacokinetics
  • Cancer Vaccines* / pharmacology
  • Dendritic Cells / immunology*
  • Dendritic Cells / pathology
  • Drug Delivery Systems*
  • Imiquimod* / immunology
  • Imiquimod* / pharmacokinetics
  • Imiquimod* / pharmacology
  • Immunotherapy*
  • Lipid A / analogs & derivatives*
  • Lipid A / immunology
  • Lipid A / pharmacokinetics
  • Lipid A / pharmacology
  • Mice
  • Nanoparticles*
  • Neoplasms, Experimental* / immunology
  • Neoplasms, Experimental* / pathology
  • Neoplasms, Experimental* / therapy
  • Toll-Like Receptors / agonists*
  • Toll-Like Receptors / immunology

Substances

  • Antigens, Neoplasm
  • Cancer Vaccines
  • Lipid A
  • Toll-Like Receptors
  • monophosphoryl lipid A
  • Imiquimod