Micelles for delivery of nitric oxide

J Am Chem Soc. 2009 Oct 14;131(40):14413-8. doi: 10.1021/ja905123t.

Abstract

We designed block copolymer pro-amphiphiles and amphiphiles for providing very long-term release of nitric oxide (NO). A block copolymer of N-acryloylmorpholine (AM, as a hydrophile) and N-acryloyl-2,5-dimethylpiperazine (AZd, as a hydrophilic precursor) was synthesized. The poly(N-acryloyl-2,5-dimethylpiperazine) (PAZd) is water-soluble, but chemical reaction of the secondary amines with NO to form a N-diazeniumdiolate (NONOate) converts the hydrophilic PAZd into a hydrophobic poly(sodium-1-(N-acryloyl-2,5-dimethylpiperazin-1-yl)diazen-1-ium-1,2-diolate) (PAZd.NONOate), driving aggregation. The PAM block guides this process toward micellization, rather than precipitation, yielding ca. 50 nm spherical micelles. The hydrophobic core of the micelle shielded the NONOate from the presence of water, and thus protons, which are required for NO liberation, delaying release to a remarkable 7 d half-life. Release of the NO returned the original soluble polymer. The very small NO-loaded micelles were able to penetrate complex tissue structures, such as the arterial media, opening up a number of tissue targets to NO-based therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylic Resins / chemical synthesis
  • Acrylic Resins / chemistry*
  • Azo Compounds / chemistry
  • Micelles*
  • Nitric Oxide / chemistry*
  • Nitric Oxide Donors / chemical synthesis
  • Nitric Oxide Donors / chemistry*
  • Piperazines / chemical synthesis
  • Piperazines / chemistry*

Substances

  • Acrylic Resins
  • Azo Compounds
  • Micelles
  • Nitric Oxide Donors
  • Piperazines
  • diazeniumdiolate
  • poly(acryloylmorpholine)
  • Nitric Oxide