Hyaluronic Acid Conjugates of TLR7/8 Agonists for Targeted Delivery to Secondary Lymphoid Tissue

Bioconjug Chem. 2018 Aug 15;29(8):2741-2754. doi: 10.1021/acs.bioconjchem.8b00386. Epub 2018 Jul 17.

Abstract

Immunogens carried in lymphatic fluid drain via afferent vessels into regional lymph nodes and facilitate the efficient induction of appropriate immune responses. The lymphatic system possesses receptors recognizing hyaluronic acid (HA). Covalent conjugates of small-molecule TLR7/8 agonists with HA are entirely devoid of immunostimulatory activity in vitro. In murine models of immunization, however, such conjugates traffic to lymph nodes, where they are "unmasked", releasing the small molecule TLR7/8 agonist from the carrier polysaccharide. The resulting focal immunostimulation is manifested in potent adjuvantic effects with negligible systemic exposure. The efficient delivery of immunogens has been a major challenge in the development of subunit vaccines, and enhancing targeted delivery of immunogens to secondary lymphoid organs might be a promising approach for improving vaccine efficacy, as well as safety.

Publication types

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

MeSH terms

  • Adjuvants, Immunologic / administration & dosage
  • Adjuvants, Immunologic / pharmacology*
  • Animals
  • Cytokines / biosynthesis
  • Dose-Response Relationship, Drug
  • Enzyme-Linked Immunosorbent Assay
  • Humans
  • Hyaluronic Acid / chemistry*
  • Immunoconjugates / metabolism
  • Immunoconjugates / pharmacology*
  • Inflammation Mediators / metabolism
  • Lymph Nodes / drug effects*
  • Membrane Glycoproteins / agonists*
  • Mice
  • Proof of Concept Study
  • Toll-Like Receptor 7 / agonists*
  • Toll-Like Receptor 8 / agonists*
  • Vaccines / administration & dosage

Substances

  • Adjuvants, Immunologic
  • Cytokines
  • Immunoconjugates
  • Inflammation Mediators
  • Membrane Glycoproteins
  • TLR8 protein, mouse
  • Tlr7 protein, mouse
  • Toll-Like Receptor 7
  • Toll-Like Receptor 8
  • Vaccines
  • Hyaluronic Acid