Activable Nano-Immunomodulator Assembled from π-Extended Naphthalenediimide for Precision Photothermal Immunotherapy

Angew Chem Int Ed Engl. 2024 Jun 3;63(23):e202401250. doi: 10.1002/anie.202401250. Epub 2024 Apr 30.

Abstract

A nano-immunomodulator (R-NPT NP) comprising a tumor microenvironment (TME) activable resiquimod (R848) and a π-extended NIR-absorbing naphthophenanthrolinetetraone (NPT) has been engineered for spatiotemporal controlled photothermal immunotherapy. R-NPT NP demonstrated excellent photostability, while R848 promoted synergistic immunity as a toll-like receptor 7/8 (TLR7/8) agonist. Upon accumulation at the tumor site, R-NPT NP released R848 in response to redox metabolite glutathione (GSH), triggering dendritic cell (DC) activation. The photothermal effect endowed by R-NPT NP can ablate tumors directly and trigger immunogenic cell death to augment immunity after photoirradiation. The synergistic effect of GSH-liable TLR7/8 agonist and released immunogenic factors leads to a robust evocation of systematic immunity through promoted DC maturation and T cell infiltration. Thus, R-NPT NP with photoirradiation achieved 99.3 % and 98.2 % growth inhibition against primary and distal tumors, respectively.

Keywords: J-aggregation; glutathione activable effect; organic assembly; photothermal immunotherapy; π-extended naphthalenediimide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Dendritic Cells / drug effects
  • Dendritic Cells / immunology
  • Humans
  • Imidazoles / chemistry
  • Imidazoles / pharmacology
  • Imides* / chemistry
  • Imides* / pharmacology
  • Immunologic Factors* / chemistry
  • Immunologic Factors* / pharmacology
  • Immunotherapy*
  • Mice
  • Nanoparticles / chemistry
  • Naphthalenes* / chemistry
  • Naphthalenes* / pharmacology
  • Photothermal Therapy
  • Tumor Microenvironment / drug effects

Substances

  • Immunologic Factors
  • naphthalenediimide
  • Naphthalenes
  • Imides
  • Imidazoles