Use of labelled cisplatin obtained by direct irradiation in a preliminary biodistribution study

The proposal of this work was to investigate the effect of the radioactive complex of platinum(II) with tetracycline, [PtCl 2 (C 22 H 24 N 2 O 8 )]*, or [Tc-Pt(II)]*, on K562 cells-blood human cells of leukemia-and verify if the internal radio-chemotherapy would be able to produce additional effects compared with the non-labelled complex, [PtCl 2 (C 22 H 24 N 2 O 8 )], or [Tc-Pt(II)]. The concentration required to inhibit 50 % of cellular growth, (IC 50 ), was 2.5 ± 0.2 lM for [Tc-Pt(II)]* and 14.5 ± 0.9 lM for the non-labelled molecule [Tc-Pt(II)]. This result suggest that the [Tc-Pt(II)]* could be a potent radiosensitizer evoking a supra additive effect. Treatment using the internal radiochemotherapy may be a useful alternative to reduce the drug concentration required for effective inhibition of the tumor growth.

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Internal computational dosimetry of natural cisplatin activated in neutron flux

Bussolotti¹,

Krstić²,

Nikezić³

et al. 2022

Braz. J. Rad. Sci.

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Cisplatin is currently used in the treatment of numerous types of tumors, such as head and neck, esophagus, bladder, testicle. However, the cisplatin use is limited due to its cytotoxic effects. Thus, considering its side effects, lines of research are looking for new technologies to reduce the dose of the chemotherapeutic agent needed to control the disease, which may reduce these side effects. The objective of this work was to perform the internal dosimetry of 191Pt radioisotope derived from the activation of natural cisplatin, thus contributing to the evaluation of the feasibility of a new radiopharmaceutical of natural cisplatin activated by neutrons for application in humans. The dosimetry was obtained with Monte Carlo simulations using two stylized phantoms developed by authors Dragana Krstic and Dragoslav Nikezic and the ICRP adult reference voxelized phantoms. As results, differences were observed between absorbed doses estimated using the two types of phantoms (analytical and voxelized). The highest doses noted in the analytical phantom were in the kidneys (1.58 mGy/MBq), liver (1.32 mGy/MBq), spleen (1.23 mGy/MBq), bladder wall (0.74 mGy/MBq), gallbladder wall (0.56 mGy/MBq), pancreas (0.41 mGy/MBq), and adrenals (0.39 mGy/MBq). For the voxelized phantoms, the highest doses obtained were: kidneys (1.46 mGy/MBq), spleen (1.13 mGy/MBq), liver (1.11 mGy/MBq), gallbladder wall (0.47 mGy/MBq), adrenals (0.41 mGy/MBq), bladder wall (0.36 mGy/MBq), and pancreas (0.29 mGy/MBq). The effective dose was 0.22 mSv/MBq for the analytical phantom, a value similar to that obtained with voxelized phantoms (0.20 mSv/MBq).

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Use of labelled cisplatin obtained by direct irradiation in a preliminary biodistribution study

Abstract: This work presents the preparation of radiolabelled cis-dichlorodiammineplatinum (II), CDDP

Cited by 3 publications

References 11 publications

Evaluation of the synergetic radio-chemotherapy effects of the radio labelled cisplatin for the treatment of glioma

Evaluation of the synergetic radio-chemotherapy effects of the radio labelled cisplatin for the treatment of glioma

Investigation of the potential antitumor radioactive complex of platinum(II) with tetracycline

Internal computational dosimetry of natural cisplatin activated in neutron flux

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