A Glucose-Responsive Polymer Nanocarrier Based on Sulfonated Resorcinarene for Controlled Insulin Delivery

Chempluschem. 2019 Oct;84(10):1560-1566. doi: 10.1002/cplu.201900428.

Abstract

A nanocarrier (p(6SRA-5B)) for glucose-controlled insulin delivery consists of sulfonated resorcinarenes (SRA) that are assembled into a spherical shell and are attached to each other with phenylboronate linkers. p(6SRA-5B) is stable in water and blood plasma at normal glucose concentrations. At high glucose levels (>5 mM), p(6SRA-5B) dissociates into SRA and phenylboronates through competitive interaction with excess glucose. Insulin was successfully encapsulated into the cavity of p(6SRA-5B) and its release was investigated in water and blood plasma by NMR, UV, CD, and fluorescence spectroscopy. The results show that the dissociation of the nanocarrier and the insulin release occurs with an increase in glucose concentration. At 5 mM glucose, the nanocarrier is stable, and the insulin release does not exceed 10 %. Increasing the glucose concentration to 7.5-10 mM results in a 40-100 % insulin release. p(6SRA-5B) is thus a promising insulin nanocarrier for the treatment of type 1 diabetes.

Keywords: drug delivery; glucose; insulin; nanocarriers; resorcinarenes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Boronic Acids / chemistry
  • Calixarenes / chemistry*
  • Diabetes Mellitus, Type 1 / drug therapy
  • Drug Carriers / chemistry*
  • Drug Delivery Systems / methods*
  • Drug Liberation / drug effects
  • Glucose / pharmacology*
  • Humans
  • Insulin / administration & dosage*
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / chemistry
  • Polymers / chemistry
  • Sulfonic Acids / chemistry

Substances

  • Boronic Acids
  • Drug Carriers
  • Insulin
  • Polymers
  • Sulfonic Acids
  • resorcinarene
  • Calixarenes
  • Phenylalanine
  • Glucose
  • benzeneboronic acid