PEG-g-poly(GdDTPA-co-L-cystine): a biodegradable macromolecular blood pool contrast agent for MR imaging

Bioconjug Chem. 2004 Nov-Dec;15(6):1424-30. doi: 10.1021/bc049828r.

Abstract

Biodegradable PEGylated Gd-DTPA l-cystine copolymers, PEG-g-poly(GdDTPA-co-l-cystine), were prepared and tested as a blood pool contrast agent in mice. The biodegradable macromolecular agent was designed to be broken down into smaller Gd complexes by endogenous thiols via the disulfide-thiol exchange reaction to facilitate the clearance of Gd complexes after the contrast-enhanced MRI examination. Gd-DTPA l-cystine copolymers were synthesized by condensation polymerization of l-cystine and DTPA-dianhydride in water followed by chelating with Gd(OAc)(3). MPEG-NH(2) (MW = 2000) was then conjugated to the polymeric backbone in different ratios. The macromolecular contrast agent was readily degraded with the incubation of l-cysteine. It also demonstrated superior contrast enhancement in the heart and blood vessels as compared to a low molecular weight control agent, Gd-(DTPA-BMA). At 1 h postcontrast, the PEGylated macromolecular agent still showed prominent enhancement, while little contrast enhancement was detectable in the blood pool by the control agent. PEG-g-poly(GdDTPA-co-l-cystine) shows promise as an MR blood pool imaging agent.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Contrast Media / chemistry
  • Contrast Media / metabolism*
  • Cystine / blood*
  • Cystine / chemistry
  • Gadolinium DTPA / blood*
  • Gadolinium DTPA / chemistry
  • Macromolecular Substances / blood
  • Macromolecular Substances / chemistry
  • Magnetic Resonance Imaging / methods*
  • Mice
  • Polyethylene Glycols / chemistry
  • Polyethylene Glycols / metabolism*

Substances

  • Contrast Media
  • Macromolecular Substances
  • Polyethylene Glycols
  • Cystine
  • Gadolinium DTPA