Synthesis, quality control, and bio‐evaluation of ^99mTc‐cyclophosphamide

Abstract

Cancer is found to be the leading cause of death worldwide characterized by uncontrolled cell division. Nuclear medicines imaging using radiopharmaceuticals have pronounced potential for the diagnosis and treatment of cancers. Cyclophosphamide (CPH) is an antineoplastic drug which targets selectively cancer cells. In the present work, labeling of CPH with Tc-99m is performed for diagnostic purpose, which gave labeling yield as high as 99% using 20 μg SnCl ·2H O, 200 μg of ligand at pH 7 for 10 min reaction time at room temperature. The characterization of the prepared complex was performed using ITLC, electrophoresis, and HPLC. In vitro stability was analyzed in the presence of human serum at 37°C which has maximum value of 94 ± 0.5. The biodistribution studies of Tc-CPH were performed in normal and tumor bearing Swiss Webster mice. The high accumulation of Tc-CPH was observed in liver and tumours respectively at 4 hr after injection. Biodistribution results revealed that Tc-CPH may be a potential tumour diagnostic agent simultaneously with chemotherapy.

Applying Quality by Design Principles in the Development and Preparation of a New Radiopharmaceutical: Technetium-99m-Imatinib Mesylate

“…Several studies concerning the usage of reducing agents such as stannous derivatives were identified in the literature. ,− …”

The Chemical Scaffold of Theranostic Radiopharmaceuticals: Radionuclide, Bifunctional Chelator, and Pharmacokinetics Modifying Linker

“…It was initially reported that the chelator T 4 CPP (5,10,15,20-tetrakis[4-(carboxymethyleneoxy)phenyl]porphyrin) accumulates selectively in mammary tumor-bearing rats and sarcoma tumor-bearing mice. Then, a water-soluble porphyrin was developed, namely, T 3,4 BCPP (5,10,15,20-tetrakis[3,4-bis(carboxymethyleneoxy)phenyl]porphyrin), which was later patented by the Indian Patent Office [ 177 , 178 ]. T 3,4 BCPP was also reported to accumulate more in tumor cells compared to normal tissue or cells.…”

Radiosynthesis, radiochemical, and biological characterization of 177Lu‐labeled diethylenetriamine penta‐acetic acid

“…Another benefit of 177 Lu is that as a consequence of de‐excitation of the excited states, gamma‐(γ) radiation, having energies in the range 50‐350 keV, is also emitted that can penetrate out from the body; hence it is useful for clinical imaging purposes. A major responsibility of the nuclear medicine physician is to know and understand completely the biodistribution patterns of a radionuclide therapy . Because of to this reason, the physician is so‐called the “captain of the ship.” In the current scenario, pharmaceutical chemists are trying their best to find more effective and safer therapeutic agents for different chronic diseases …”

“…A major responsibility of the nuclear medicine physician is to know and understand completely the biodistribution patterns of a radionuclide therapy. [10][11][12][13][14] Because of to this reason, the physician is so-called the "captain of the ship." In the current scenario, pharmaceutical chemists are trying their best to find more effective and safer therapeutic agents for different chronic diseases.…”