Functionalized low-density lipoprotein nanoparticles for in vivo enhancement of atherosclerosis on magnetic resonance images

Bioconjug Chem. 2012 Nov 21;23(11):2313-9. doi: 10.1021/bc300561e. Epub 2012 Nov 1.

Abstract

To allow visualization of macrophage-rich and miniature-sized atheromas by magnetic resonance (MR) imaging, we have converted low-density lipoprotein (LDL) into MR-active nanoparticles via the intercalation of a 1,4,7,10-tetraazacyclodecane-1,4,7-triacetic acid (DO3A) derivative and the subsequent coordination reaction with Gd(3+). After careful removal of nonchelated Gd(3+), an MR-active LDL (Gd(3+)-LDL) with a remarkably high payload of Gd(3+) (in excess of 200 Gd(3+) atoms per particle) and a high relaxivity (r(1) = 20.1 s(-1) mM(-1) per Gd(3+) or 4040 s(-1) mM(-1) per LDL) was obtained. Dynamic light-scattering photon correlation spectroscopy (DLS) and cryo transmission electron microscope (cryoTEM) images showed that Gd(3+)-LDL particles did not aggregate and remained of a similar size (25-30 nm) to native LDL. Intravenous injection of Gd(3+)-LDL into an atherosclerotic mouse model (ApoE(-/-)) resulted in an extremely high enhancement of the atheroma-bearing aortic walls at 48 h after injection. Free Gd(3+) dissociation from Gd(3+)-LDL was not detected over the imaging time window (96 h). Because autologous LDL can be isolated, modified, and returned to the same patient, our results suggest that MR-active LDL can potentially be used as a noninfectious and nonimmunogenic imaging probe for the enhancement of atheroplaques presumably via the uptake into macrophages inside the plaque.

Publication types

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

MeSH terms

  • Animals
  • Apolipoproteins E / deficiency
  • Apolipoproteins E / genetics
  • Atherosclerosis / diagnosis*
  • Atherosclerosis / genetics
  • Disease Models, Animal
  • Gadolinium / chemistry
  • Gadolinium / pharmacokinetics
  • Heterocyclic Compounds, 1-Ring / chemistry
  • Heterocyclic Compounds, 1-Ring / pharmacokinetics
  • Humans
  • Lipoproteins, LDL* / chemistry
  • Lipoproteins, LDL* / pharmacokinetics
  • Magnetic Resonance Imaging*
  • Mice
  • Mice, Inbred C57BL
  • Molecular Structure
  • Nanoparticles* / chemistry
  • Organometallic Compounds* / chemistry
  • Organometallic Compounds* / pharmacokinetics
  • Radiopharmaceuticals* / chemistry
  • Radiopharmaceuticals* / pharmacokinetics
  • Tissue Distribution

Substances

  • 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid
  • Apolipoproteins E
  • Heterocyclic Compounds, 1-Ring
  • Lipoproteins, LDL
  • Organometallic Compounds
  • Radiopharmaceuticals
  • Gadolinium