Stealth polymeric vesicles via metal-free click coupling

Biomacromolecules. 2013 Sep 9;14(9):2996-3000. doi: 10.1021/bm400940h. Epub 2013 Aug 21.

Abstract

The strain-promoted azide-alkyne cycloaddition represents an optimal metal-free method for the modular coupling of amphiphilic polymer blocks. Hydrophilic poly(oxazoline) (PMOXA) or poly(ethylene glycol) (PEG) A-blocks were coupled with a hydrophobic poly(siloxane) B-block to provide triblock copolymers capable of self-assembling into vesicular nanostructures. Stealth properties investigated via a complement activation assay revealed the superior in vitro stealth attributes of polymeric vesicles synthesized via a metal-free approach to those coupled via the widely used copper-catalyzed click method. Furthermore, the ability to change a single parameter, such as the hydrophilic block, allowed the direct comparison of the biocompatibility properties of triblock copolymers containing PMOXA or PEG. Our studies convincingly demonstrate the need for a metal-free approach, both in preventing cytotoxicity while imparting optimal stealth properties for potential biomedical applications.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Biocompatible Materials / chemical synthesis*
  • Biocompatible Materials / chemistry
  • Biocompatible Materials / toxicity
  • Bridged Bicyclo Compounds / chemistry
  • Click Chemistry
  • Complement Activation / drug effects
  • Cycloaddition Reaction
  • Hemolysis / drug effects
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Nanoparticles / chemistry*
  • Oxazoles / chemistry
  • Particle Size
  • Polyethylene Glycols / chemical synthesis*
  • Polyethylene Glycols / chemistry
  • Polyethylene Glycols / toxicity
  • Sheep, Domestic
  • Siloxanes / chemical synthesis*
  • Siloxanes / chemistry
  • Siloxanes / toxicity

Substances

  • Biocompatible Materials
  • Bridged Bicyclo Compounds
  • Oxazoles
  • Siloxanes
  • bicyclo(6.1.0)nonyne
  • poly(2-oxazoline)
  • Polyethylene Glycols