Co-encapsulation of synthetic lipidated TLR4 and TLR7/8 agonists in the liposomal bilayer results in a rapid, synergistic enhancement of vaccine-mediated humoral immunity

J Control Release. 2019 Dec 10:315:186-196. doi: 10.1016/j.jconrel.2019.10.025. Epub 2019 Oct 22.

Abstract

To increase vaccine immunogenicity, modern vaccines incorporate adjuvants, which serve to enhance immune cross-protection, improve humoral and cell-mediated immunity, and promote antigen dose sparing. Pattern recognition receptors (PRRs), including the Toll-like receptor (TLR) family are promising targets for development of agonist formulations for use as vaccine adjuvants. Combinations of co-delivered TLR4 and TLR7/8 ligands have been demonstrated to have synergistic effects on innate and adaptive immune response. Here, we create liposomes that stably co-encapsulate CRX-601, a synthetic TLR4 agonist, and UM-3004, a lipidated TLR7/8 agonist, within the liposomal bilayer in order to achieve co-delivery, allow tunable physical properties, and induce in vitro and in vivo immune synergy. Co-encapsulation demonstrates a synergistic increase in IL-12p70 cytokine output in vitro from treated human peripheral blood mononuclear cells (hPBMCs). Further, co-encapsulated formulations give significant improvement of early IgG2a antibody titers in BALB/c mice following primary vaccination when compared to single agonist or dual agonists delivered in separate liposomes. This work demonstrates that co-encapsulation of TLR4 and lipidated TLR7/8 agonists within the liposomal bilayer leads to innate and adaptive immune synergy which biases a Th1 immune response. Thus, liposomal co-encapsulation may be a useful and flexible tool for vaccine adjuvant formulation containing multiple TLR agonists.

Keywords: Co-delivery; Influenza vaccine; Influenza virus; Liposome; Toll-like receptor (TLR); Vaccine adjuvant.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adjuvants, Immunologic / administration & dosage*
  • Animals
  • Drug Delivery Systems
  • Drug Synergism
  • Female
  • Heterocyclic Compounds, 3-Ring / administration & dosage*
  • Heterocyclic Compounds, 3-Ring / immunology
  • Heterocyclic Compounds, 3-Ring / pharmacology
  • Humans
  • Immunity, Humoral / immunology*
  • Leukocytes, Mononuclear / immunology
  • Liposomes
  • Mice
  • Mice, Inbred BALB C
  • Monosaccharides / administration & dosage*
  • Monosaccharides / immunology
  • Monosaccharides / pharmacology
  • Th1 Cells / immunology
  • Toll-Like Receptor 4 / agonists
  • Toll-Like Receptor 7 / agonists
  • Toll-Like Receptor 8 / agonists
  • Vaccines / administration & dosage*
  • Vaccines / immunology

Substances

  • Adjuvants, Immunologic
  • Heterocyclic Compounds, 3-Ring
  • Liposomes
  • Monosaccharides
  • Toll-Like Receptor 4
  • Toll-Like Receptor 7
  • Toll-Like Receptor 8
  • Vaccines