Novel liver macromolecular MR contrast agent with a polypropylenimine diaminobutyl dendrimer core: Comparison to the vascular MR contrast agent with the polyamidoamine dendrimer core

As MRI contrast agents, more hydrophobic molecules reportedly accumulate in the liver and thus are potentially useful as liver MRI contrast agents. In this study, a generation‐4 polypropylenimine diaminobutane dendrimer (DAB‐Am64), which is expected to be more hydrophobic than the generation‐4 polyamidoamine dendrimer (PAMAM‐G4D), was used to synthesize a conjugate with 2‐( p ‐isothiocyanatobenzyl)‐6‐methyl‐diethylenetriaminepentaacetic acid (1B4M) [DAB‐Am64‐(1B4M‐Gd) 64 ] for complexing Gd(III) ions. This DAB conjugate quickly accumulated in the liver and its characteristics were studied and compared with those of a PAMAM conjugate [PAMAM‐G4D‐(1B4M‐Gd) 64 ], which is known to be a useful vascular MRI contrast agent, in regard to its availability as a liver MRI contrast agent. DAB‐Am64‐(1B4M‐Gd) 64 accumulated significantly more in the liver and less in blood than PAMAM‐G4D‐(1B4M‐Gd) 64 ( P < 0.001). Contrast‐enhanced MRI with DAB‐Am64‐(1B4M‐Gd) 64 was able to homogeneously enhance liver parenchyma and visualize both portal and hepatic veins of 0.5 mm diameter in mice. In conclusion, DAB‐Am64‐(1B4M‐Gd) 64 is a good candidate for a liver MRI contrast agent. Magn Reson Med 46:795–802, 2001. © 2001 Wiley‐Liss, Inc.