Development of In-111 labeled insulin for receptor imaging/therapy

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

Research output: Contribution to journalArticle

11 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)791-796
Number of pages6
JournalJournal of Radioanalytical and Nuclear Chemistry
Volume279
Issue number3
DOIs
Publication statusPublished - 1 Mar 2009

Cite this