Vol 12, No 2 (2009)
Research paper
Published online: 2010-03-12
The development of radiogallium-acetylacetonate bis(thiosemicarbazone) complex for tumour imaging
Nucl. Med. Rev 2009;12(2):65-71.
Abstract
BACKGROUND: Various radiometal complexes have been developed
for tumour imaging, especially Ga-68 tracer. In this work,
the development of a radiogallium bis(thiosemicarbazone) complex
has been reported.
MATERIAL AND METHODS: [67Ga]acetylacetonate bis(thio-semicarbazone) complex ([67Ga]AATS) was prepared starting with [67Ga]Gallium acetate and freshly prepared acetylacetonate bis(thiosemicarbazone) (AATS) for 30 min at 90ºC. The partition co-efficient and stability of the tracer was determined in final solution (25ºC) and the presence of human serum (37ºC) for up to 24 hours. The biodistribution of the labelled compound in wild-type and fibrosarcoma-bearing rodents were determined for up to 72 hours.
RESULTS: The radiolabelled Ga complex was prepared to a high radiochemical purity (> 97%, HPLC) followed by initial biodistribution data with the significant tumour accumulation of the tracer at two hours, which is far higher than free Ga-67 cation, while the compound wash-out is significantly faster.
CONCLUSION: The above-mentioned pharmacokinetic properties suggest an interesting radiogallium complex prepared by the PET Ga radioisotope, 68Ga, in accordance with the physical half life, for use in fibrosarcoma tumours and possibly in other malignancies.
MATERIAL AND METHODS: [67Ga]acetylacetonate bis(thio-semicarbazone) complex ([67Ga]AATS) was prepared starting with [67Ga]Gallium acetate and freshly prepared acetylacetonate bis(thiosemicarbazone) (AATS) for 30 min at 90ºC. The partition co-efficient and stability of the tracer was determined in final solution (25ºC) and the presence of human serum (37ºC) for up to 24 hours. The biodistribution of the labelled compound in wild-type and fibrosarcoma-bearing rodents were determined for up to 72 hours.
RESULTS: The radiolabelled Ga complex was prepared to a high radiochemical purity (> 97%, HPLC) followed by initial biodistribution data with the significant tumour accumulation of the tracer at two hours, which is far higher than free Ga-67 cation, while the compound wash-out is significantly faster.
CONCLUSION: The above-mentioned pharmacokinetic properties suggest an interesting radiogallium complex prepared by the PET Ga radioisotope, 68Ga, in accordance with the physical half life, for use in fibrosarcoma tumours and possibly in other malignancies.
Keywords: Gallium-67acetyl acetone bis(thiosemicarbazonate)biodistributionfibrosarcoma
