Preparation and biodistribution studies of a radiogallium-acetylacetonate bis (thiosemicarbazone) complex in tumor-bearing rodents.

Abstract

Various radiometal complexes have been developed for tumor imaging, especially Ga-68 tracer. In the present study, the development of a radiogallium bis-thiosemicarbazone complex has been reported. [(67)Ga] acetylacetonate bis(thiosemicarbazone) complex ([(67)Ga] AATS) was prepared starting [(67)Ga]Gallium acetate and freshly prepared acetylacetonate bis (thiosemicarbazone) (AATS) in 30 min at 90°C. The partition co-efficient and the stability of the tracer were determined in final solution (25°C) and the presence of human serum (37°C) up to 24 h. The biodistribution of the labeled compound in wild-type and fibrosarcoma-bearing rodents were determined up to 72 h. The radiolabled Ga complex was prepared in high radiochemical purity (> 97%, HPLC) followed by initial biodistribution data with the significant tumor accumulation of the tracer in 2 h which is far higher than free Ga-67 cation while the compound wash-out is significantly faster. Above-mentioned pharmacokinetic properties suggest an interesting radiogallium complex while prepared by the PET Ga radioisotope, (68)Ga, in accordance with the physical half life, for use in fibrosarcoma tumors, and possibly other malignancies.

• Authors: Amir Reza Jalilian, Hassan Yousefnia, Kamaleddin Shafaii, Aytak Novinrouz, Amir Abbas Rajamand
• Journal: Iranian journal of pharmaceutical research : IJPR (Iran J Pharm Res) Vol. 11 Issue 2 Pg. 523-31 ( 2012) ISSN: 1735-0328 [Print] Netherlands
• PMID: 24250475 (Publication Type: Journal Article)