Polyphenol-stabilized coacervates for enzyme-triggered drug delivery

Nat Commun. 2024 Aug 24;15(1):7295. doi: 10.1038/s41467-024-51218-8.

Abstract

Stability issues in membrane-free coacervates have been addressed with coating strategies, but these approaches often compromise the permeability of the coacervate. Here we report a facile approach to maintain both stability and permeability using tannic acid and then demonstrate the value of this approach in enzyme-triggered drug release. First, we develop size-tunable coacervates via self-assembly of heparin glycosaminoglycan with tyrosine and arginine-based peptides. A thrombin-recognition site within the peptide building block results in heparin release upon thrombin proteolysis. Notably, polyphenols are integrated within the nano-coacervates to improve stability in biofluids. Phenolic crosslinking at the liquid-liquid interface enables nano-coacervates to maintain exceptional structural integrity across various environments. We discover a pivotal polyphenol threshold for preserving enzymatic activity alongside enhanced stability. The disassembly rate of the nano-coacervates increases as a function of thrombin activity, thus preventing a coagulation cascade. This polyphenol-based approach not only improves stability but also opens the way for applications in biomedicine, protease sensing, and bio-responsive drug delivery.

MeSH terms

  • Drug Delivery Systems*
  • Drug Liberation
  • Heparin / chemistry
  • Humans
  • Peptides / chemistry
  • Peptides / metabolism
  • Polyphenols* / chemistry
  • Proteolysis
  • Tannins* / chemistry
  • Thrombin* / chemistry
  • Thrombin* / metabolism

Substances

  • Polyphenols
  • Thrombin
  • Tannins
  • Heparin
  • Peptides