Absorbed Dose Estimation of 68Ga-EDTMP in Human Organs

Bone metastases are observed in a wide range of cancers leading to intolerable pain. While early detection can help the physicians in the decision of the type of treatment, various radiopharmaceuticals using phosphonates like 68Ga-EDTMP have been developed. In this work, due to the importance of absorbed dose, human absorbed dose of this new agent was calculated for the first time based on biodistribution data in Wild-type rats. 68Ga was obtained from 68Ge/68Ga generator with radionuclidic purity and radiochemical purity of higher than 99%. The radiolabeled complex was prepared in the optimized conditions. Radiochemical purity of the radiolabeled complex was checked by instant thin layer chromatography (ITLC) method using Whatman No. 2 paper and saline. The results indicated the radiochemical purity of higher than 99%. The radiolabelled complex was injected into the Wild-type rats and its biodistribution was studied up to 120 min. As expected, major accumulation was observed in the bone. Absorbed dose of each human organ was calculated based on biodistribution in the rats using RADAR method. Bone surface and bone marrow with 0.112 and 0.053 mSv/MBq, respectively, received the highest absorbed dose. According to these results, the radiolabeled complex is a suitable and safe option for PET bone imaging.

Estimation of Human Absorbed Dose Using Compartmental Model

Dosimetry is an indispensable and precious factor in patient treatment planning to minimize the absorbed dose in vital tissues. In this study, compartmental model was used in order to estimate the human absorbed dose of 177Lu-DOTATOC from the biodistribution data in wild type rats. For this purpose, 177Lu-DOTATOC was prepared under optimized conditions and its biodistribution was studied in male Syrian rats up to 168 h. Compartmental model was applied to mathematical description of the drug behaviour in tissue at different times. Dosimetric estimation of the complex was performed using radiation absorbed dose assessment resource (RADAR). The biodistribution data showed high accumulation in the adrenal and pancreas as the major expression sites for somatostatin receptor (SSTR). While kidneys as the major route of excretion receive 0.037 mSv/MBq, pancreas and adrenal also obtain 0.039 and 0.028 mSv/MBq. Due to the usage of this method, the points of accumulated activity data were enhanced, and further information of tissues uptake was collected that it will be followed by high (or improved) precision in dosimetric calculations.

Estimated Human Absorbed Dose of 111In-BPAMD as a New Bone-Seeking SPECT-Imaging Agent

An early diagnosis of bone metastasis is very important for making a right decision on a subsequent therapy. One of the most important steps to be taken initially, for developing a new radiopharmaceutical is the measurement of organ radiation exposure dose. In this study, the dosimetric studies of a novel agent for SPECT-imaging of the bone metastasis, 111In-(4- {[(bis(phosphonomethyl))carbamoyl]methyl}7,10bis(carboxymethyl) -1,4,7,10-tetraazacyclododec-1-yl) acetic acid (111In-BPAMD) complex, have been carried out to estimate the dose in human organs based on the data derived from mice. The radiolabeled complex was prepared with high radiochemical purity in the optimal conditions. Biodistribution studies of the complex was investigated in the male Syrian mice at the selected times after injection (2, 4, 24 and 48 h). The human absorbed dose estimation of the complex was made based on data derived from the mice by the radiation absorbed dose assessment resource (RADAR) method. 111In-BPAMD complex was prepared with high radiochemical purity >95% (ITLC) and specific activities of 2.85 TBq/mmol. Total body effective absorbed dose for 111In-BPAMD was 0.205 mSv/MBq. This value is comparable to the other 111In clinically used complexes. The results show that the dose with respect to the critical organs is satisfactory within the acceptable range for diagnostic nuclear medicine procedures. Generally, 111In-BPAMD has interesting characteristics and it can be considered as a viable agent for SPECT-imaging of the bone metastasis in the near future.

Human Absorbed Dose Estimation of a New IN-111 Imaging Agent Based on Rat Data

The measurement of organ radiation exposure dose is one of the most important steps to be taken initially, for developing a new radiopharmaceutical. In this study, the dosimetric studies of a novel agent for SPECT-imaging of the bone metastasis, 111In- 1,4,7,10-tetraazacyclododecane-1,4,7,10 tetraethylene phosphonic acid (111In-DOTMP) complex, have been carried out to estimate the dose in human organs based on the data derived from rats. The radiolabeled complex was prepared with high radiochemical purity in the optimal conditions. Biodistribution studies of the complex was investigated in the male Syrian rats at selected times after injection (2, 4, 24 and 48 h). The human absorbed dose estimation of the complex was made based on data derived from the rats by the radiation absorbed dose assessment resource (RADAR) method. 111In-DOTMP complex was prepared with high radiochemical purity of >99% (ITLC). Total body effective absorbed dose for 111In- DOTMP was 0.061 mSv/MBq. This value is comparable to the other 111In clinically used complexes. The results show that the dose with respect to the critical organs is satisfactory within the acceptable range for diagnostic nuclear medicine procedures. Generally, 111In- DOTMP has interesting characteristics and can be considered as a viable agent for SPECT-imaging of the bone metastasis in the near future.