High-performance dendritic contrast agents for X-ray computed tomography imaging using potent tetraiodobenzene derivatives

J Control Release. 2016 Mar 28:226:258-67. doi: 10.1016/j.jconrel.2016.01.036. Epub 2016 Jan 23.

Abstract

The use of computed tomography (CT) for vascular imaging is critical in medical emergencies requiring urgent diagnostic decisions, such as cerebral ischemia and many cardiovascular diseases. Small-molecule iodinated contrast media are often injected intravenously as radiopaque agents during CT imaging to achieve high contrast enhancement of vascular systems. The rapid excretion rate of these agents is overcome by injecting a significantly high dose of iodine, which can have serious side effects. Here we report a simple method to prepare blood-pool contrast agents for CT based on dendrimers for the first time using tetraiodobenzene derivatives as potent radiopaque moieties. Excellent in vivo safety has been demonstrated for these small (13-22nm) unimolecular water-soluble dendritic contrast agents, which exhibit high contrast enhancement in the blood-pool and effectively extend their blood half-lives. Our method is applicable to virtually any scaffold with suitable surface groups and may fulfill the current need for safer, next-generation iodinated CT contrast agents.

Keywords: Computed tomography; Dendrimers; In vivo imaging; Iodinated contrast agents; Nanomedicine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Contrast Media / adverse effects
  • Contrast Media / chemistry*
  • Contrast Media / pharmacokinetics
  • Dendrimers / adverse effects
  • Dendrimers / chemistry*
  • Dendrimers / pharmacokinetics
  • HeLa Cells
  • Humans
  • Iodobenzenes / adverse effects
  • Iodobenzenes / chemistry*
  • Iodobenzenes / pharmacokinetics
  • Male
  • Mice, Inbred C57BL
  • Nylons / adverse effects
  • Nylons / chemistry*
  • Nylons / pharmacokinetics
  • Tomography, X-Ray Computed*

Substances

  • Contrast Media
  • Dendrimers
  • Iodobenzenes
  • Nylons
  • PAMAM-G4