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Thermosensitive nanoparticles with pH-triggered degradation and release of anti-inflammatory cell-penetrating peptides

Biomacromolecules. 2012 Aug 13;13(8):2578-84. doi: 10.1021/bm300826v. Epub 2012 Aug 1.

Abstract

Poly(N-isopropylacrylamide-2-acrylamido-2-methyl-1-propanesulfonate) [poly(NIPAm-AMPS)] nanoparticles can be cross-linked with hydrolytically degradable N,O-dimethacryloyl hydroxylamine (DMHA) in order to yield a pH-sensitive drug delivery system that slowly erodes above pH 5.0. Varying the composition of degradable DMHA and nondegradable MBA cross-linking allows for engineered variation of particle size and degradation kinetics. Utilizing sulfated comonomer AMPS provides for increased passive loading of anti-inflammatory mitogen-activated protein kinase-activated protein kinase 2 (MK2)-inhibiting cell-penetrating peptide KAFAKLAARLYRKALARQLGVAA (KAFAK) between 24.3% and 29.2% (w/w) for nanoparticles with 5 mol % cross-linker. Nanoparticles were shown to be nontoxic in vitro and were effective at delivering a therapeutically active dose of KAFAK to THP1 human monocytes to suppress tumor necrosis factor α (TNF-α) expression during lipopolysaccharide (LPS)-induced inflammation. This thermosensitive nanoparticle system is an excellent platform for passive diffusive loading in deionized water and release in physiologically relevant ionic strength media of environmentally sensitive peptide therapeutics.

MeSH terms

  • Acrylamides / chemistry*
  • Anti-Inflammatory Agents / chemistry*
  • Anti-Inflammatory Agents / pharmacology
  • Cell Line
  • Cell Survival / drug effects
  • Cell-Penetrating Peptides / chemistry*
  • Cell-Penetrating Peptides / pharmacology
  • Cross-Linking Reagents / chemistry
  • Humans
  • Hydrogen-Ion Concentration
  • Hydrolysis
  • Hydroxylamines / chemistry
  • Intracellular Signaling Peptides and Proteins / antagonists & inhibitors
  • Lipopolysaccharides / pharmacology
  • Nanocapsules / chemistry*
  • Nanocapsules / toxicity
  • Nanocapsules / ultrastructure
  • Particle Size
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology
  • Protein Serine-Threonine Kinases / antagonists & inhibitors
  • Temperature
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Acrylamides
  • Anti-Inflammatory Agents
  • Cell-Penetrating Peptides
  • Cross-Linking Reagents
  • Hydroxylamines
  • Intracellular Signaling Peptides and Proteins
  • Lipopolysaccharides
  • Nanocapsules
  • Protein Kinase Inhibitors
  • Tumor Necrosis Factor-alpha
  • MAP-kinase-activated kinase 2
  • Protein Serine-Threonine Kinases