open access

Vol 11, No 2 (2008)
Published online: 2008-11-05
Submitted: 2012-01-23
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Biodistribution of two 131I-IMBA preparations, differently labelled, in mice with experimental B16 melanoma tumours

Michał Janczak, Janusz Kapuściński, Elżbieta Mikiciuk-Olasik, Marek Różalski, Anna Płachcińska, Jacek Kuśmierek
Nucl. Med. Rev 2008;11(2):48-52.

open access

Vol 11, No 2 (2008)
Published online: 2008-11-05
Submitted: 2012-01-23

Abstract

BACKGROUND:Numerous reports indicate that some iodinated compounds of benzamide derivatives display a strong affinity to the cells of melanoma. In the present report, a compound [N-(2-diethylaminoethyl)-3-iodo-4metyoxybenzamide (131I-IMBA)] has been prepared by two different labelling methods. Biodistribution of the injected compound was followed in mice with experimentally induced B16 melanoma tumours, and tumour/ tissue ratios were studied as a function of time post administration.
MATERIAL AND METHODS: The iodinated 131I-IMBA was obtained by means of 131I exchange for nonradioactive iodine atoms (method I) and by means of 131I substitution for a metalorganic group (method II). The last preparation was purified by chloroform extraction. The chemical purity was assessed by means of ascending thin layer chromatography (TLC). The biodistribution of 131I-IMBA in C57 Black mice was studied in animals with experimentally induced B16 mice melanoma tumours.
RESULTS: The mean labelling efficiency exceeded 95 and 80 % for methods I and II, respectively, at radiochemical purity > 95% in both cases. 131I-IMBA was vividly cumulated by melanoma tumours in mice. At 24-hours post 131I-IMBA administration the values of tumour /non-tumour ratios for the compound labelled by method II reached the following values: tumour/liver 10 ± 3, tumour/lung 15 ± 12, tumour/blood 153 ± 39, tumour/intestines 176 ± 26, tumour/kidneys 270 ± 107, and tumour/muscle 448 ± 82. These values exceeded, by an order of magnitude, the corresponding ratios for the same compound labelled by method I.
CONCLUSIONS: High values of tumour/non-tumour ratios indicate that 131I-IMBA could be a promising radiopharmaceutical for clinical diagnosis (staging) of melanomas in humans.

Abstract

BACKGROUND:Numerous reports indicate that some iodinated compounds of benzamide derivatives display a strong affinity to the cells of melanoma. In the present report, a compound [N-(2-diethylaminoethyl)-3-iodo-4metyoxybenzamide (131I-IMBA)] has been prepared by two different labelling methods. Biodistribution of the injected compound was followed in mice with experimentally induced B16 melanoma tumours, and tumour/ tissue ratios were studied as a function of time post administration.
MATERIAL AND METHODS: The iodinated 131I-IMBA was obtained by means of 131I exchange for nonradioactive iodine atoms (method I) and by means of 131I substitution for a metalorganic group (method II). The last preparation was purified by chloroform extraction. The chemical purity was assessed by means of ascending thin layer chromatography (TLC). The biodistribution of 131I-IMBA in C57 Black mice was studied in animals with experimentally induced B16 mice melanoma tumours.
RESULTS: The mean labelling efficiency exceeded 95 and 80 % for methods I and II, respectively, at radiochemical purity > 95% in both cases. 131I-IMBA was vividly cumulated by melanoma tumours in mice. At 24-hours post 131I-IMBA administration the values of tumour /non-tumour ratios for the compound labelled by method II reached the following values: tumour/liver 10 ± 3, tumour/lung 15 ± 12, tumour/blood 153 ± 39, tumour/intestines 176 ± 26, tumour/kidneys 270 ± 107, and tumour/muscle 448 ± 82. These values exceeded, by an order of magnitude, the corresponding ratios for the same compound labelled by method I.
CONCLUSIONS: High values of tumour/non-tumour ratios indicate that 131I-IMBA could be a promising radiopharmaceutical for clinical diagnosis (staging) of melanomas in humans.
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Keywords

melanoma; aminoalkyl-iodobenzamides; radioiodinated IMBA

About this article
Title

Biodistribution of two 131I-IMBA preparations, differently labelled, in mice with experimental B16 melanoma tumours

Journal

Nuclear Medicine Review

Issue

Vol 11, No 2 (2008)

Pages

48-52

Published online

2008-11-05

Bibliographic record

Nucl. Med. Rev 2008;11(2):48-52.

Keywords

melanoma
aminoalkyl-iodobenzamides
radioiodinated IMBA

Authors

Michał Janczak
Janusz Kapuściński
Elżbieta Mikiciuk-Olasik
Marek Różalski
Anna Płachcińska
Jacek Kuśmierek

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