Dual targeting improves microbubble contrast agent adhesion to VCAM-1 and P-selectin under flow

J Control Release. 2009 Dec 3;140(2):100-7. doi: 10.1016/j.jconrel.2009.08.001. Epub 2009 Aug 8.

Abstract

To improve ultrasound contrast agents targeted to the adhesion molecules P-selectin and VCAM-1 for the purpose of molecular imaging of atherosclerotic plaques, perfluorocarbon-filled phospholipid microbubble contrast agents were coupled by a polyethylene glycol-biotin-streptavidin bridge with mAb MVCAM.A(429), a sialyl Lewis(x) polymer (PAA-sLe(x)), or both (dual). Approximately three hundred thousand antibody molecules were coupled to the surface of each microbubble. Recombinant mouse P-selectin and/or VCAM-1 coated on flow chambers showed saturation of binding at approximately 15 ng/microl, resulting in 800 and 1200 molecules/microm(2) for P-selectin and VCAM-1, respectively. Dual substrates coated with equal concentrations of P-selectin and VCAM-1 had site densities between 50 and 60% of single substrates. When microbubbles were perfused through flow chambers at 5 x 10(6) microbubbles/ml (wall shear stress from 1.5 to 6 dyn/cm(2)) dual-targeted microbubbles adhered almost twice as efficiently as single-targeted microbubbles at 6 dyn/cm(2). The present study suggests that dual-targeted contrast agents may be useful for atherosclerotic plaque detection at physiologically relevant shear stresses.

MeSH terms

  • Animals
  • Antibodies, Monoclonal / chemistry
  • Antibodies, Monoclonal / metabolism*
  • Atherosclerosis / diagnostic imaging*
  • Atherosclerosis / metabolism
  • Biotin / chemistry
  • Contrast Media / chemistry
  • Contrast Media / metabolism*
  • Fluorocarbons / chemistry
  • Fluorocarbons / metabolism*
  • Iodine Radioisotopes
  • Mice
  • Microbubbles*
  • Oligosaccharides / chemistry
  • Oligosaccharides / metabolism*
  • P-Selectin / metabolism*
  • Perfusion
  • Phospholipids / chemistry
  • Polyethylene Glycols / chemistry
  • Protein Binding
  • Recombinant Proteins / metabolism
  • Sialyl Lewis X Antigen
  • Streptavidin / chemistry
  • Stress, Mechanical
  • Ultrasonography
  • Vascular Cell Adhesion Molecule-1 / metabolism*

Substances

  • Antibodies, Monoclonal
  • Contrast Media
  • Fluorocarbons
  • Iodine Radioisotopes
  • Oligosaccharides
  • P-Selectin
  • Phospholipids
  • Recombinant Proteins
  • Sialyl Lewis X Antigen
  • Vascular Cell Adhesion Molecule-1
  • Polyethylene Glycols
  • Biotin
  • Streptavidin