Radiosynthesis, molecular modeling studies and biological evaluation of 99mTc-Ifosfamide complex as a novel probe for solid tumor imaging.

Abstract:

PURPOSE:Ifosfamide as a chemotherapeutic drug is used for the treatment of different cancer types. The purpose of this study is the preparation of 99mTc-ifosfamide complex to be evaluated as a potential candidate for tumor imaging. MATERIALS AND METHODS:The radiolabeling of ifosfamide with technetium-99m was carried out by mixing 4mg ifosfamide and 5 μg of SnCl2.2H2O with 400 MBq Na99mTcO4 at pH 9 for 30 min at room temperature. Computer simulation studies were performed using Accelrys Discovery Studio 2.5 operating system to illustrate the interaction of ifosfamide and 99mTc-ifosfamide complexes with DNA. The in-vivo biodistribution of 99mTc-ifosfamide was studied in tumor-bearing Albino mice. RESULTS:A new 99mTc-ifosfamide complex was synthesized with a good radiochemical yield of 90.3 ± 2.1% under the optimized conditions and exhibited in-vitro stability up to 2 h. Biodistribution studies showed good uptake in tumor site and high uptake in tumor site with T/NT ∼3 after 60 min post-injection. Besides, the molecular docking study confirmed that the complexation of ifosfamide with technetium-99m does not abolish its binding to the target receptor. CONCLUSION:These promising results afford a new radiopharmaceutical that could be used as a potential tumor imaging.

journal_name

Int J Radiat Biol

authors

Motaleb MA,El-Safoury DM,Abd-Alla WH,Awad GAS,Sakr TM

doi

10.1080/09553002.2019.1524945

subject

Has Abstract

pub_date

2018-12-01 00:00:00

pages

1134-1141

issue

12

eissn

0955-3002

issn

1362-3095

journal_volume

94

pub_type

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