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.
Similar content being viewed by others
References
V. S. Awasthi, A. B. Gambhir, B. Sewatkar, Nucl. Med. Biol., 21 (1994) 251.
N. Dozio, M. Scavini, A. Beretta, E. Sarugeri, S. Sartori, C. Belloni, F. Dosio, A. Savi, F. Fazio, J. C. Sodoyez, G. Pozza, J. Clin. Endocrinol. Metab., 83 (1998) 643.
N. Dozio, E. Sarugeri, M. Scavini, A. Beretta, C. Belloni, F. Dosio, A. Savi, F. Fazio, F. Sodoyez-Goffaux, G. Pozza, J. Invest. Med., 49 (2001) 85.
Y. Shai, K. L. Kirk, M. A. Channing, B. B. Dunn, M. A. Lesniak, R. C. Eastman, R. D. Finn, J. Roth, K. A. Jacobson, Biochemistry, 28 (1989) 4801.
K. J. Guenther, S. Yoganathan, R. Garofalo, T. Kawabata, T. Strack, R. Labiris, M. Dolovich, R. Chirakal, J. F. Valliant, J. Med. Chem., 49 (2006) 1466.
H. L. Hachiya, S. T. Treves, C. R. Kahn, J. C. Sodoyez, F. Sodoyez-Goffaux, J. Clin. Endocrinol. Metab., 64 (1987) 801.
R. C. Eastman, R. E. Carson, K. A. Jacobson et al., Diabetes, 41 (1992) 855.
A. R. Jalilian, J. Garousi, E. Gholami, M. Akhlaghi, F. Bolourinovin, S. Rajabifar, Nukleonika, 54 (2007) 32.
H. Sadeghpour, A. R. Jalilian, M. Akhlaghi, M. Kamali-Dehghan, M. Mirzaii, J. Radioanal. Nucl. Chem., 278 (2008) 117.
A. R. Jalilian, P. Rowshanfarzad, K. Shafaii, M. Kamali-dehghan, J. Moafian, M. Akhlaghi, M. Babaii, S. Rajabifar, M. Mirzaii, Nukleonika, 50(3) (2005) 91.
M. Mirzaii, H. Afarideh, S. M. Haji-Saied, K. Ardaneh, Proc. 15 th Intern. Conf. on Cyclotrons and Their Applications, Caen, France, 1998, p. 65.
Z. Marczenko, in: Spectrophotometric Determination of Elements, John Wiley & Sons, New York, 1976, p. 238.
Z. Marczenko, in: Spectrophotometric Determination of Elements, John Wiley & Sons, New York, 1976, p. 176.
D. J. Hnatowich, W. W. Layne, R. L. Child, D. Lanteigne, M. A. Davis, T. W. Griffin, P. W. Doherty, Science, 220 (1983) 613.
W. C. Eckelman, S. M. Karesh, R. C. Reba, J. Pharm. Sci., 64 (1975) 704.
M. A. Green, M. J. Welch, Nucl. Med. Biol., 16 (1989) 435.
A. R. Jalilian, Y. Yari-Kamrani, M. Kamali-dehghan, S. Rajabifar, J. Radioanal. Nucl. Chem., 275 (2008) 109.
A. Camagna, R. L. De Pirro, L. Tardella, L. Rossetti, R. Lauro, P. Caprari, P. Samoggia, G. Salvo, Diabetes, 32 (1983) 1017.
J. Sodoyez, F. Sodoyez-Goffaux, R. Von Frenckell, C. J. De Vos, S. Treves, C. R. Kahn, J. Clin. Invest., 75 (1985) 1455.
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Jalilian, A.R., Garousi, J., Akhlaghi, M. et al. Development of 111In labeled insulin for receptor imaging/therapy. J Radioanal Nucl Chem 279, 791–796 (2009). https://doi.org/10.1007/s10967-008-7360-y
Received:
Published:
Issue Date:
DOI: https://doi.org/10.1007/s10967-008-7360-y