Pharmacokinetics of Gd(DO3A‐Lys) and MR imaging studies in an orthotopic U87MG glioma tumor model

Abstract

Pharmacokinetics of Gd(DO3A-Lys), a macrocyclic gadolinium-based magnetic resonance imaging (MRI) contrast agent functionalized with a lysine derivative, was studied in Wistar rats. Kinetic data were fitted using a two-compartment model and revealed Gd(DO3A-Lys) to have a distribution half-life, t1/2 (α), of 1.3 min, an elimination half-life, t1/2 (β), of 24.9 min and a large volume of distribution, VD , of 0.49 L/kg indicative of the agent being able to rapidly distribute into tissues and organs. Contrast-enhanced magnetic resonance angiography (CE-MRA) in an orthotopic U87MG glioma mouse model demonstrated considerable enhancement of both the tumor and surrounding vasculature after intravenous administration of Gd(DO3A-Lys). Applying dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) in the glioma of different sizes further showed distinct uptake characteristics and patterns of enhancement, which suggests the potential for differentiating changes at different stages of tumor growth. Our results indicate that Gd(DO3A-Lys) could be a promising candidate for glioma MR imaging.

Smart Magnetic and Fluorogenic Photosensitizer Nanoassemblies Enable Redox‐Driven Disassembly for Photodynamic Therapy

“…We next investigated the capacity of NP‐RGD for fluorescence/MR bimodality imaging‐guided PDT of U87MG tumor in living mice. The blood half‐life ( t 1/2 ) of NP‐RGD in nude mice was examined, which was approximate ≈1.8 h, significantly longer than that of Dotarem ( t 1/2 ≈20 min) [23] (Figure S29). Such an increased t 1/2 may help NP‐RGD prolong circulation in the blood for enhanced delivery into tumor tissues.…”

Smart Magnetic and Fluorogenic Photosensitizer Nanoassemblies Enable Redox‐Driven Disassembly for Photodynamic Therapy

“…In all, these results prove that NP-RGD could act promising activatable PSs conferring on demand PDT activity to kill tumor cells. We next investigated the capacity of NP-RGD for fluorescence/MR bimodality imaging-guided PDT of U87MG tumor in living mice.T he blood half-life (t 1/2 )o f NP-RGD in nude mice was examined, which was approximate % 1.8 h, significantly longer than that of Dotarem (t 1/2 % 20 min) [23] (Figure S29). Such an increased t 1/2 may help NP-RGD prolong circulation in the blood for enhanced delivery into tumor tissues.…”

Synthesis and in vivo magnetic resonance imaging evaluation of biocompatible branched copolymer nanocontrast agents

“…These contrast agents possess r 1 relaxivity values of 3-6 mM -1 s -1 at higher magnetic field. 46,47 Small molecular contrast agents which were protein bounded showed intravascular characteristics and have a r 1 relaxivity of 6 mM -1 s -1 at higher a magnetic field. 48 In our study of N2(Gd), r 1 relaxivity (14.16 mM…”