pH-Responsive Polymersome Microparticles as Smart Cyclodextrin-Releasing Agents

Biomacromolecules. 2019 Oct 14;20(10):4001-4007. doi: 10.1021/acs.biomac.9b01083. Epub 2019 Oct 3.


Cyclodextrins (CDs) are increasingly drawing attention as potential therapeutic tools in the treatment of cholesterol-associated diseases. However, bioavailability and delivery of CDs in the monomeric form still remain challenging. CD-based macromolecular systems seem to display a promising capacity in overcoming some of these limitations. Therefore, smart, stimuli-responsive nanosystems are currently being investigated in order to provide improved CD-releasing agents. Herein, we present a novel class of CD-based polymersome microparticles (CD-PMs) designed for potential therapeutic use. A new synthetic route to obtain a CD-appended, pH-sensitive polymer that self-assembles into a stable polymersome microparticle is reported. Through an easy-to-use approach, a benzoic imine bond is incorporated into a poly(ε-caprolactone) backbone and employed as a building block in the construction of the nanoarchitecture. The CD-PMs show cellular uptake representing a promising potential therapeutic tool in the treatment of cholesterol-associated conditions such as neurodegenerative diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line
  • Cell-Derived Microparticles / chemistry*
  • Cholesterol / metabolism
  • Cyclodextrins / chemistry*
  • Human Umbilical Vein Endothelial Cells
  • Humans
  • Hydrogen-Ion Concentration
  • Macromolecular Substances / chemistry
  • Neurodegenerative Diseases / drug therapy
  • Neurodegenerative Diseases / metabolism
  • Polymers / chemistry*
  • Polymers / pharmacology


  • Cyclodextrins
  • Macromolecular Substances
  • Polymers
  • Cholesterol