ABSTRACT
Bleomycins are DNA-binding biomolecules, which can be used as targeted therapy carriers when labeled with particle-emitters such as Yb-175. In this work the development of Yb-175 bleomycin [[175]Yb-BLM] has been reported. Yb-175 chloride was obtained by thermal neutron irradiation [3 × 10[13] n.cm[-2].s[-1]] of natural Yb2O3 samples at various neutron fluxes and irradiation times. The radionuclide dissolved in acidic media [120mCi/mg] was used in the bleomycin [5 mg] labeling in buffer solution and warming at 60[degree sign]C for 48 h. Radiochemical purity was determined by ITLC as well as specific activity calculation followed by stability studies. Biodistribution studies of free Yb-175 and [175]Yb-BLM were performed in wild-type mice up to 8 days. At optimized conditions radiochemical purity of 97 +/- 0.88% and specific activity of 1360 MBq/mM was obtained. Biodistribution studies of free Yb-175 demonstrated liver and bone uptake while in case of [175]Yb-BLM the target tissues were lung, liver and spleen.[175]Yb-BLM complex was prepared at the optimized conditions and suitable characteristics. The accumulation of the radiolabeled compound in lungs, liver and spleen demonstrates a similar pattern to the other radiolabeled bleomycins. Further studies are to be performed for application of this labeled compound in tumor-bearing models
ABSTRACT
Developing new bone pain palliation agents is a mandate in handling end-stage cancer patients around the world. Possibly, Lu-177 ethylenediaminetetramethylene phosphonic acid [[177]Lu-EDTMP] is a therapeutic agent which can be widely used in bone palliation therapy. In this study, [177]Lu-EDTMP complex was prepared successfully using synthesized EDTMP ligand and [177]LuCl[3]. Lu-177 chloride was obtained by thermal neutron irradiation [4 _ 10[13] n.cm[-2]s[-1]] of natural Lu[2]O[3] samples. Radiochemical purity of [177]Lu-EDTMP was determined by ITLC [more than 99%]. Stability studies of the final preparations in the presence of human serum were performed. The biodistribution of [177]Lu-EDTMP and [177]LuCl[3] in wild-type rats was studied by SPECT imaging. A comparative accumulation study for [177]Lu-EDTMP and [177]LuCl[3] was performed for vital organs up to 7 days. The complex was obtained in high radiochemical purity [more than 99%]. The complex was stable in vitro in presence of human serum as well as final formulation. Significant bone uptake [> 70%] was observed for the radiopharmaceutical. Due to better physical properties of Lu-177 compared to Sm-153 and acceptable biodistribution results of the compound, [177]Lu-EDTMP seemed to be an interesting new candidate for clinical trials for bone pain palliation therapy
ABSTRACT
In this research, [[166]Ho]Holmium chitosan complex production is described in details, followed by determination of complex radiochemical purity, stability and biodistribution [after intra-articular injection] in wild-type male rats. Finally a Ho-166 based chitosan kit for ultimate radiosynovectomy as well as radiotherapy applications was developed. [166]Ho-chitosan complex was prepared using chitosan concentrations and [166]HoCl[3] followed by intra-articular injection and biodistribution studies in wild-type rats including and excluding injected knee. The [[166]Ho]Holmium chitosan complex was prepared with high radiochemical yield [>95%] in the optimized condition [35mg/3ml of chitosan in%1 AcOH, pH. 3, >98%, ITLC] was injected to wild-type rats followed by the biodistribution studies of the compound among the tissues excluding the injected knee data. Intra-articular injection of [[166]Ho]holmium chitosan complex to male wild-type rats and investigation of leakage of activity in the body showed that most of injected dose has remained in injection site 144 h after injection. Successful development and formulation of [166]Ho-chitosan kit is described. This kit has the potential for use in clinical setting namely for radiosynovectomy and cancer radiochemotherapy
ABSTRACT
Nowadays various bone pain palliative therapeutic agents have been developed for bone metastases. Among those, [153]Sm-ethylenediamine tetramethylene phosphonic acid [[153]Sm-EDTMP] is the major therapeutic agent which is widely used in the world. In this study, production, quality control and biodistribution studies of this therapeutic radiopharmaceutical have been presented and followed by imaging studies in a wild-type rabbit for the first time in order to make preparations for this agent to be officially approved in the country. [153]Sm-EDTMP was produced using [153]Sm-SmCl[3], prepared by neutron activation of an enriched [152]Sm sample [purity >98%], and in-house synthesized EDTMP in 4h at 100°C. The analytical data for the structure determination and purity of the ligand was obtained and shown to be identical to an authentic sample from a European vendor. The Radiochemical purity of [153]Sm-EDTMP was checked by RTLC and ITLC. The biodistribution of [153]Sm-EDTMP in wild-type rodents was checked and SPECT imaging as well as following sacrificing the animal. The radiolabeled Sm complex was prepared in high radiochemical purity [>99%, RTLC] followed by initial biodistribution data with the significant bone accumulation [>70%] of the tracer in 48h which is comparable with the reported methods. The produced [153]Sm-EDTMP properties suggest good potential for efficient use of this radiopharmaceutical for bone pain palliation and as substitute for other agents, such as [89]SrCl[2] and [32]P, currently used in the country