A functionalized superparamagnetic iron oxide colloid as a receptor directed MR contrast agent.
We have synthesized a surface functionalized superparamagnetic iron oxide colloid whose clearance from the vascular compartment was inhibited by asialofetuin but not fetuin. Unlike other particulate or colloidal magnetic resonance (MR) contrast agents, the agent of the current communication is not withdrawn from the vascular compartment by cells of the macrophage-monocyte phagocytic system, as indicated by its selective increase in hepatic relaxation rates. Because of this we refer to this colloid as a hepatic selective (HS) MR contrast agent. At 20 mumol Fe/kg the HS MR agent darkened MR images of liver. The HS MR agent exhibited no acute toxicity when injected into rats at 1800 mumol Fe/kg. Based on these observations, surface functionalized superparamagnetic iron oxide colloids may be the basis of MR contrast agents internalized by receptor mediated endocytosis generally, and by the asialoglycoprotein receptor in particular.
Josephson
L
L
Advanced Magnetics Inc., Cambridge, Massachusetts 01238.
Groman
E V
EV
Menz
E
E
Lewis
J M
JM
Bengele
H
H
D000818:Animals; D001212:Asialoglycoproteins; D003102:Colloids / Q000737:chemistry; D003287:Contrast Media; D003911:Dextrans; D052203:Ferrosoferric Oxide; D060748:Fetuins; D005685:Galactans / Q000494:pharmacology; D007457:Iodine Radioisotopes; D007501:Iron / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D008099:Liver / Q000033:anatomy & histology / Q000166:cytology / Q000378:metabolism; D008279:Magnetic Resonance Imaging; D058185:Magnetite Nanoparticles; D010087:Oxides / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D011919:Rats, Inbred Strains; D011955:Receptors, Drug / Q000378:metabolism; D013154:Spleen / Q000033:anatomy & histology; D000509:alpha-Fetoproteins / Q000032:analysis / Q000493:pharmacokinetics / Q000494:pharmacology
D001212:Asialoglycoproteins; D003102:Colloids; D003287:Contrast Media; D003911:Dextrans; D060748:Fetuins; D005685:Galactans; D007457:Iodine Radioisotopes; D058185:Magnetite Nanoparticles; D010087:Oxides; D011955:Receptors, Drug; D000509:alpha-Fetoproteins; C017029:asialofetuin; D007501:Iron; C065507:ferumoxides; C005653:arabinogalactan; D052203:Ferrosoferric Oxide