Development of 111In labeled insulin for receptor imaging/therapy View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2009-03

AUTHORS

A. R. Jalilian, J. Garousi, M. Akhlaghi, P. Rowshanfarzad

ABSTRACT

In order to target insulin receptors in various diabetic and insulinoma conditions, human recombinant insulin was successively labeled with [111In]-indium chloride after conjugation with freshly prepared cyclic DTPA-dianhydride (ccDTPA). The best results of the conjugation were obtained by addition of 0.5 mL of an insulin pharmaceutical solution (5 mg/mL, in phosphate buffer, pH 8) to a glass tube pre-coated with DTPA-dianhydride (0.01 mg) at 25 °C with continuous mild stirring for 30 minutes. Radio-thin layer chromatography (RTLC), instant thin layer chromatography (ITLC) and high performance liquid chromatography (HPLC) have shown an overall radiochemical purity of higher than 93% at optimized conditions (specific activity = 550–750 MBq/mg, radiochemical yield =81%). The white blood cell labeling capacity of the tracer was determined up to 4 hours at 37 °C. Preliminary in vivo studies in normal rat model was performed to determine the biodistribution of the radiotracer up to 48 hours. It showed a high liver and spleen uptake of the tracer which is consistent with other reported radiolabeled insulins. SPECT images have also shown high liver accumulation of the tracer. More... »

PAGES

791

References to SciGraph publications

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s10967-008-7360-y

DOI

http://dx.doi.org/10.1007/s10967-008-7360-y

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1044274779


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