RESUMEN
Purpose: In this study, the human absorbed dose of 111In-DOTA-PR81 as a new radioimmunoconjugate for single-photon emission computed tomography (SPECT) imaging of MUC1 + breast cancer was determined. Materials and Methods: The complex was prepared at optimized conditions in about 1 h and 38°C. The radiochemical purity of the tracer was investigated using the instant thin-layer chromatography method method, showing purity of higher than 96%. After evaluating the stability of the product in human serum and room temperature, the biological distribution of the radiolabeled compound was studied in normal rats and tumor-bearing mice. Finally, the human absorbed dose of the complex was estimated based on animals' data using radiation dose assessment resource and Spark et al. methods. Results: High uptake of the complex in MUC1 + breast tumors compared to other nontarget organs shows that the radioimmunoconjugate is a beneficial agent for SPECT imaging of MUC1 + breast cancer. Human organs absorbed dose estimation of the complex demonstrated the highest amounts of the absorbed dose are in the liver and kidneys with 0.384 and 0.245 mGy/MBq, respectively. Conclusions: 111In-DOTA-PR81 radioimmunoconjugate is a high potential agent for MUC1 + breast cancer SPECT imaging and estimated absorbed dose values could helpfully use for the determination of the maximum injectable dose.
RESUMEN
Aims: Calculation of the absorbed dose in human organs is one of the first steps for developing new radiopharmaceuticals. The aim of this study is to estimate the human absorbed dose of a newly developed 68Ga-NODAGA-RGD-BBN radiolabeled compound. Materials and Methods: 68Ga-NODAGA-RGD-BBN was prepared by varying different parameters at optimized conditions. The stability of the radiolabeled peptide in phosphate-buffered saline (PBS) and in human serum was evaluated for 120 min. Afterward, the biodistribution of the complex was assessed in normal and tumor-bearing mice, at least for 120 min postinjection. Finally, the human absorbed dose of 68Ga-NODAGA-RGD-BBN was estimated based on mice data using Radiation Dose Assessment Resource and Spark method. Results: 68Ga-NODAGA-RGD-BBN was produced with radiochemical purity of more than 98% (high-performance liquid chromatography/ radio thin layer chromatography (RTLC)) with high stability in PBS buffer and in human serum at least for 2 h. The complex demonstrated high uptake in gastrin-releasing peptide receptor-expressing tumors compared to other nontarget organs. Furthermore, the dose assessment for the complex showed that the kidneys receive the highest absorbed dose in comparison with other organs. Conclusion: The result of this study showed that 68Ga-NODAGA-RGD-BBN is an effective and radiolabeled ligand for tumor detection, however more studies are still needed.