Targeting of lanthanide(III) chelates of DOTA-type glycoconjugates to the hepatic asyaloglycoprotein receptor: cell internalization and animal imaging studies (pages 246–258)
M. I. M. Prata, A. C. Santos, S. Torres, J. P. André, J. A. Martins, M. Neves, M. L. García-Martín, T. B. Rodrigues, P. López-Larrubia, S. Cerdán and C. F. G. C. Geraldes
Article first published online: 19 OCT 2006 | DOI: 10.1002/cmmi.111
Radiolabeled [153Sm]3+-DOTA-amide dendrimeric thioglycoconjugates with terminal galactosyl groups (eg. 153SmDOTAGal2) efficiently enter hepatoma cells in vitro (gamma activity cell studies) and Wistar rat liver in vivo (biodistribution, gamma-imaging and pharmacokinetics) via the asialoglycoprotein receptor mediated endocytosis, a process blocked by asialofetuin. However, the DCE-MRI assessment of the corresponding Gd3+ chelates shows liver-to-kidney contrast effects not significantly better than those shown by GdDTPA. The quick wash-out of these hydrophilic complexes from the liver may prevent their sufficient concentration within the hepatocytes.