Pharmacokinetics of Chiral Dendrimer-Triamine-Coordinated Gd-MRI Contrast Agents Evaluated by in Vivo MRI and Estimated by in Vitro QCM

• Main Authors: Yuka Miyake, Syungo Ishikawa, Yu Kimura, Aoi Son, Hirohiko Imai, Tetsuya Matsuda, Hisatsugu Yamada, Akio Toshimitsu, Teruyuki Kondo
• Format: Article
• Language: English
• Published: MDPI AG 2015-12-01
• Series: Sensors
• Subjects: chiral dendrimer; gadolinium; contrast agent; magnetic resonance imaging (MRI); quartz crystal microbalance (QCM); association constant (Ka)
• Online Access: http://www.mdpi.com/1424-8220/15/12/29900

Recently, we developed novel chiral dendrimer-triamine-coordinated Gd-MRI contrast agents (Gd-MRI CAs), which showed longitudinal relaxivity (r1) values about four times higher than that of clinically used Gd-DTPA (Magnevist®, Bayer). In our continuing study of pharmacokinetic differences derived from both the chirality and generation of Gd-MRI CAs, we found that the ability of chiral dendrimer Gd-MRI CAs to circulate within the body can be directly evaluated by in vitro MRI (7 T). In this study, the association constants (Ka) of chiral dendrimer Gd-MRI CAs to bovine serum albumin (BSA), measured and calculated with a quartz crystal microbalance (QCM) in vitro, were found to be an extremely easy means for evaluating the body-circulation ability of chiral dendrimer Gd-MRI CAs. The Ka values of S-isomeric dendrimer Gd-MRI CAs were generally greater than those of R-isomeric dendrimer Gd-MRI CAs, which is consistent with the results of our previous MRI study in vivo.