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Novel liver macromolecular MR contrast agent with a polypropylenimine diaminobutyl dendrimer core: Comparison to the vascular MR contrast agent with the polyamidoamine dendrimer core
Author(s) -
Kobayashi Hisataka,
Kawamoto Satomi,
Saga Tsuneo,
Sato Noriko,
Hiraga Akira,
Ishimori Takayoshi,
Akita Yukio,
Mamede Marcelo H.,
Konishi Junji,
Togashi Kaori,
Brechbiel Martin W.
Publication year - 2001
Publication title -
magnetic resonance in medicine
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.696
H-Index - 225
eISSN - 1522-2594
pISSN - 0740-3194
DOI - 10.1002/mrm.1259
Subject(s) - dendrimer , conjugate , contrast (vision) , mri contrast agent , chemistry , gadolinium , biochemistry , computer science , mathematical analysis , mathematics , organic chemistry , artificial intelligence
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.