Igor Jacobs1,
Siem Wouters1, Henk Keizer2, Henk Janssen2,
Eliana Gianolio3, Silvio Aime4, Gustav J. Strijkers1,
Klaas Nicolay1
1Biomedical
NMR, Department of Biomedical Engineering, Eindhoven University of
Technology, Eindhoven, Netherlands; 2SyMO-Chem BV, Eindhoven,
Netherlands; 3Dipartimento di Chimica & Centro di Imaging
Molecolare, Universit degli Studi di Torino, Torino, Italy; 4Dipartimento
di Chimica & Centro di Imaging Molecolare, Universit degli Studi di
Torino, Torino, N\A, Italy
DCE-MRI is widely used for evaluation of tumor treatment. Macromolecular contrast agents may be preferred for determination of specific pharmacokinetic parameters and treatment-induced vascular changes. In this study (albumin-binding) dendritic contrast agents of various molecular weights were extensively characterized. Albumin-binding (confirmed in vitro) led to increased circulation half-lives, while a size-dependent range of circulation half-lives was observed for the non-albumin-binding dendrimers. Tumor/muscle uptake ratios of the dendrimers were higher than of Gd-DOTA. These findings imply that these agents likely possess a range of tumor wash-in and wash-out rates, making them suitable for investigation of the size-dependency of pharmacokinetic parameters.