Comparative biodistribution of thin-coated iron oxide nanoparticles TCION: Effect of different bisphosphonate coatings

• Published in: Drug development research 2001-12, Vol.54 (4), p.173-181
• Main Authors: Portet, David, Denizot, Benoît, Rump, Elmar, Hindre, François, Le Jeune, Jean-Jacques, Jallet, Pierre
• Format: Article
• Language: English
• Subjects: Biological and medical sciences; bone targeting; General pharmacology; Medical sciences; MPS; MRI; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; tissular diffusion; vascular remanence
• ISSN: 0272-4391; 1098-2299
• DOI: 10.1002/ddr.10027

Because the nature of their coatings influences the biodistribution of nanocolloids, five different bisphosphonates bearing OH, NH2, NMe2, and N+Me3 groups were evaluated in vivo. 59Fe‐labeled iron cores were coated by the different molecules and tested by intravenous injection to healthy adult male Wistar rats. The initial phase was estimated with 59Fe‐ and 99mTc‐labeled nanoparticles biodistribution. The different coatings do not change hydrodynamic radius (∼12 nm) and relaxivities. The negative surface charge is half for particles coated with bisphosphonates bearing quaternary ammonium compared to those bearing a hydroxyl function. Nanoparticle vascular initial half disappearance time range between 25 and 39 min, with hepatic capture between 50 and 80% ID at 18 h. Bones and muscles fix globally around 35 % ID at 18 h, with high concentrations in the mineral bones. Hydroxy‐bisphosphonates and quaternary ammonium‐bisphosphonate‐coated nanoparticles are the most efficient for blood remanence, weak liver capture, and bone targeting. Drug Dev. Res. 54:173–181, 2001. © 2002 Wiley‐Liss, Inc.