A novel ^99mTc‐diester complex as tumor targeting agent: Synthesis, radiolabeling, and biological distribution study

Abstract

The target of this study is the synthesis of a new diester derivative and radiolabeling with one of the most effective diagnostic radioisotopes to be investigated as a novel targeting radiotracer for tumor imaging. 10‐[2‐(9‐Carboxynonanoyloxy)propoxy]‐10‐oxodecanoic acid was synthesized in excellent yield and characterized by Fourier‐transform infrared spectroscopy, mass, 1H‐NMR, and 13C‐NMR spectra. The diester was technetium‐99m (99mTc) radiolabeled by direct technique using sodium dithionite as a reducing agent. The labeling parameters such as diester amount, reducing agent amount, pH of the medium, and reaction time were optimized. High radiochemical yield of 95.10 ± 0.41% and in vitro stability in serum up to 12 h have been obtained on complexation of the synthesized diester with Tc‐99m. Evaluation of the diester anticancer activity against breast cancer cell line (MCF‐7) showed high percent of inhibition about 61.5% at 100 μg/ml. The rhenium complex of the diester was synthesized and characterized by liquid chromatography–mass spectrometry (ESI) and elemental analysis depending on the strong chemical resemblance between Tc and Re. Biodistribution studies of 99mTc‐diester complex showed high target to nontarget ratio (T/NT) equals 6.24 ± 0.09 in tumor‐bearing mice at 30‐min postinjection, suggesting this complex could be used as hopeful solid tumor‐imaging agent.

Fabrication of Nanocrystals for Enhanced Distribution of a Fatty Acid Synthase Inhibitor (Orlistat) as a Promising Method to Relieve Solid Ehrlich Carcinoma-Induced Hepatic Damage in Mice

“…To assess the in vitro stability, 1.8 mL of freshly collected human blood and 0.2 mL of 99m Tc-ORL-NC were combined. After the combination was incubated at 25 °C for 24 h, 50 µL of the mixture was removed at various intervals and examined on chromatography paper [ 68 ].…”