Glucose-Responsive Polymeric Micelles via Boronic Acid-Diol Complexation for Insulin Delivery at Neutral pH

Biomacromolecules. 2019 Feb 11;20(2):871-881. doi: 10.1021/acs.biomac.8b01508. Epub 2019 Jan 22.

Abstract

In the present study, glucose-responsive polymeric complex micelles based on the complexation of phenylboronic-acid-based (PBA-based) block copolymer and diol-functionalized polymers are reported. The phenylboronic-acid- and diol-based block copolymers were successfully synthesized in only two reaction steps using reversible addition-fragmentation chain-transfer (RAFT) polymerization and postpolymerization modification of the obtained poly[( N-acryloylmorpholine- block-( N-acryloylmorpholine- co-pentafluorophenyl acrylate)], poly[(AMP- b-(AMP- co-PFPA)], reactive block copolymer. The self-assembly of the complex micelles was investigated under neutral conditions using dynamic light scattering (DLS) and transmission electron microscopy (TEM). The interaction of the PBA block copolymer and diol-containing polymer via boronate ester bond was investigated by 1H NMR and UV-vis spectroscopy. The complex micelles enhanced the glucose responsiveness under physiological conditions compared to simple PBA micelles. Furthermore, the successful glucose-triggered release of FITC-insulin from the polymeric micelles was investigated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylic Resins / chemistry
  • Boronic Acids / chemistry*
  • Drug Carriers / chemical synthesis*
  • Drug Liberation
  • Fluorocarbons / chemistry
  • Glucose / chemistry*
  • Hydrogen-Ion Concentration
  • Insulin / administration & dosage*
  • Micelles*
  • Stimuli Responsive Polymers / chemical synthesis*

Substances

  • Acrylic Resins
  • Boronic Acids
  • Drug Carriers
  • Fluorocarbons
  • Insulin
  • Micelles
  • Stimuli Responsive Polymers
  • poly(acryloylmorpholine)
  • Glucose