Polycarbonate-based ultra-pH sensitive nanoparticles improve therapeutic window

Nat Commun. 2020 Nov 17;11(1):5828. doi: 10.1038/s41467-020-19651-7.

Abstract

Stimuli-sensitive nanomaterials with cooperative response are capable of converting subtle and gradual biological variations into robust outputs to improve the precision of diagnostic or therapeutic outcomes. In this study, we report the design, synthesis and characterization of a series of degradable ultra-pH sensitive (dUPS) polymers that amplify small acidic pH changes to efficacious therapeutic outputs. A hydrolytically active polycarbonate backbone is used to construct the polymer with pH-dependent degradation kinetics. One dUPS polymer, PSC7A, can achieve activation of the stimulator of interferon genes and antigen delivery upon endosomal pH activation, leading to T cell-mediated antitumor immunity. While a non-degradable UPS polymer induces granulomatous inflammation that persists over months at the injection site, degradable PSC7A primes a transient acute inflammatory response followed by polymer degradation and complete tissue healing. The improved therapeutic window of the dUPS polymers opens up opportunities in pH-targeted drug and protein therapy.

Publication types

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

MeSH terms

  • Adjuvants, Immunologic / administration & dosage
  • Adjuvants, Immunologic / pharmacokinetics
  • Animals
  • Cancer Vaccines / administration & dosage
  • Cancer Vaccines / adverse effects
  • Cancer Vaccines / pharmacokinetics*
  • Cell Line, Tumor
  • Drug Delivery Systems
  • Hydrogen-Ion Concentration
  • Immunotherapy / methods
  • Magnetic Resonance Spectroscopy
  • Melanoma / therapy
  • Membrane Proteins / genetics
  • Membrane Proteins / metabolism
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Nanoparticles / administration & dosage
  • Nanoparticles / adverse effects
  • Nanoparticles / chemistry*
  • Nanoparticles / therapeutic use
  • Polycarboxylate Cement / chemistry*
  • Polycarboxylate Cement / metabolism
  • Polyethylene Glycols / chemistry
  • Polymers / chemical synthesis
  • Polymers / chemistry
  • Polymers / metabolism
  • T-Lymphocytes / immunology

Substances

  • Adjuvants, Immunologic
  • Cancer Vaccines
  • Membrane Proteins
  • Polycarboxylate Cement
  • Polymers
  • Sting1 protein, mouse
  • polycarbonate
  • Polyethylene Glycols