In vitro and in vivo studies with no-carrier added radioiodinated MIBG.

R. Franceschini, A. Pecorale, M. Chinol, M. L. Calcagni, T. Servidei, R. Riccardi, L. Troncone

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Abstract

An important drawback of radioiodinated MIBG prepared by isotopic exchange (maximum specific activity: 100 Ci/mmol) is that a considerable amount of carrier is present in the "ready to use" radiopharmaceutical, thus affecting MIBG uptake in the target cells. To improve the therapeutic utility of MIBG an interesting method was developed for the no-carrier-added (n.c.a.) radioiodination of MIBG via a halodesilylation reaction using 3-trimethylsilybenzylguanidine (TMSBG) as precursor. In order to investigate its possible clinical usefulness, n.c.a. [125I]- and [131I]MIBG was prepared according this procedure. HPLC analysis of the labeling mixture showed that the labeling yield reached values greater than 98% within 20 minutes at 70 degrees C. HPLC fraction containing [131I]MIBG was then recovered and tetrahydrofurane was removed under nitrogen stream. Biodistribution studies were performed in BALB/c normal mice and compared with those obtained using [131I]MIBG prepared by isotopic exchange. Preliminary results showed that at 4 hours myocardial uptake was significantly higher than that of c.a. MIBG (20.3 +/- 0.4 %ID/g). Adrenal uptake gradually increased over time; at 24 hours adrenal uptake was almost twofold that a 1 hour. MIBG uptake was also studied in the human neuroblastoma cell line SH-SY5Y which has a specific uptake system for MIBG. The kinetic parameters for MIBG in this line are: km = 0.27 +/- 0.03 microM, Vmax = 39.5 + 1.8 pmol/10(6) cell/10 min. Preliminary data from in vitro binding studies showed that significantly higher levels of specifically incorporated radioactivity can be achieved using n.c.a. [125I]MIBG instead of c.a. [125I]MIBG.

Original languageEnglish
Pages (from-to)72-77
Number of pages6
JournalQuarterly Journal of Nuclear Medicine
Volume39
Issue number4 Suppl 1
Publication statusPublished - Dec 1995

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3-Iodobenzylguanidine
In Vitro Techniques
High Pressure Liquid Chromatography
Radiopharmaceuticals
Neuroblastoma
Radioactivity

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

Cite this

Franceschini, R., Pecorale, A., Chinol, M., Calcagni, M. L., Servidei, T., Riccardi, R., & Troncone, L. (1995). In vitro and in vivo studies with no-carrier added radioiodinated MIBG. Quarterly Journal of Nuclear Medicine, 39(4 Suppl 1), 72-77.

In vitro and in vivo studies with no-carrier added radioiodinated MIBG. / Franceschini, R.; Pecorale, A.; Chinol, M.; Calcagni, M. L.; Servidei, T.; Riccardi, R.; Troncone, L.

In: Quarterly Journal of Nuclear Medicine, Vol. 39, No. 4 Suppl 1, 12.1995, p. 72-77.

Research output: Contribution to journalArticle

Franceschini, R, Pecorale, A, Chinol, M, Calcagni, ML, Servidei, T, Riccardi, R & Troncone, L 1995, 'In vitro and in vivo studies with no-carrier added radioiodinated MIBG.', Quarterly Journal of Nuclear Medicine, vol. 39, no. 4 Suppl 1, pp. 72-77.
Franceschini R, Pecorale A, Chinol M, Calcagni ML, Servidei T, Riccardi R et al. In vitro and in vivo studies with no-carrier added radioiodinated MIBG. Quarterly Journal of Nuclear Medicine. 1995 Dec;39(4 Suppl 1):72-77.
Franceschini, R. ; Pecorale, A. ; Chinol, M. ; Calcagni, M. L. ; Servidei, T. ; Riccardi, R. ; Troncone, L. / In vitro and in vivo studies with no-carrier added radioiodinated MIBG. In: Quarterly Journal of Nuclear Medicine. 1995 ; Vol. 39, No. 4 Suppl 1. pp. 72-77.
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