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Preparation, quality control, and biodistribution assessment of [ 111 In]In‐DOTA‐PR81 in BALB/c mice bearing breast tumors
Author(s) -
Abbas Abadi Sareh,
Alirezapour Behrouz,
Kertész István,
Rasaee Mohammad Javad,
Mohammadnejad Javad,
Paknejad Malihe,
Yousefnia Hassan,
Zolghadri Samaneh
Publication year - 2021
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3897
Subject(s) - dota , biodistribution , chemistry , in vivo , in vitro , nuclear medicine , imaging agent , chelation , radiochemistry , microbiology and biotechnology , biochemistry , medicine , organic chemistry , biology
In this study, [ 111 In]In‐DOTA‐PR81 was developed, and its preliminary preclinical qualifications were assessed for single photon emission computed tomography (SPECT) imaging of breast cancer. DOTA‐NHS‐ester was practiced and successively purified by molecular filtration. The chelate:mAb ratio was determined by spectrophotometry. DOTA‐PR81 was radiolabeled with In‐111 and its radiochemical yield, in vitro stability, in vitro internalization, and immunoreactivity tests were performed. SPECT imaging and tissue counting were applied to evaluate the tissue distribution of [ 111 In]In‐DOTA‐hIgG and [ 111 In]In‐DOTA‐PR81 in BALB/c mice bearing breast tumors. The radiochemical yield of [ 111 In]In‐DOTA‐PR81 complex was >95.0 ± 0.5% (ITLC), and the specific activity was 170 ± 44 MBq/mg. Conjugation reaction resulted in the average number of chelators attached to a mAb (c/a) of 3.4 ± 0.3:1. The radioimmunoconjugate showed immunoreactivity towards MCF7 cell line and MUC1 antigen while its significant in vitro and in vivo stability were investigated over 48 h, respectively (93.0 ± 1.2% in phosphate‐buffered saline (PBS) and 84.0 ± 1.3% in human serum). The peak concentration of internalized activity of [ 111 In]In‐DOTA‐PR81 was between 4 to 6 h. In comparison with control probes, the complex was accumulated with high specificity and sensitivity at the tumor site. Achieved results indicated that [ 111 In]In‐DOTA‐PR81 could be contemplated as an appropriate radiotracer for prognostic imaging of antigens in oncology.