RESUMEN
Developing new radiosynovectomy agents is of great importance due to the aging of human populations around the world and increasing the incidence of inflammatory diseases. In this work, Sm-153 chitosan agent was developed for the first time in our country and preparation and quality control of the compound is described. Sm-153 chloride was obtained by thermal neutron flux [4-5 x 10[13] n.cm [-2]. S[-1] of natural Sm[2]O[3] sample, dissolved in acidic media. [153] Sm-samarium chloride [370 MBq] was used in preparation of [153] Sm-chitosan complex followed by quality control using MeOH: H[2]O: acetic acid [4: 4: 2] as mobile phase. The complex stability and viscosity were checked in the final solution up to 2 days. The complex solution and [153]Sm[3+] [80 micro Ci/100 micro l] were injected intra-articularly into male rat knee joint followed by scarification studies 6d post injection. Sm-153 chitosan was prepared successfully with high radiochemical purity [>99%, ITLC] at room temperature after 10-30 min followed by autoclave sterilization. The complex was stable at room temperature and 37 [degree sign] C up to 2 days. No significant leackage of dose from injection site and its distribution in organs were observed up to 6 days for [153] Sm-chitosan. Approximately, more than 90% of injected dose remained in injection site after 6d. The complex is a dedicated agent for radiosynovectomy. The experience from this study would lead to the development of more sophisticated radiosynovectomy radiopharmaceuticals for human use in the country
RESUMEN
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
RESUMEN
Hypoxia is an important determinant for biological behavior of malignant solid tumors. In vitro and in vivo studies have shown that tumor hypoxia is associated with an increased likelihood of local recurrence and distant metastasis, as well as resistance to radiation therapy and certain types of chemotherapy. Studies have shown that some copper-bis thiosemicarbazones especially, Cu-ATSM accumulates avidly in hypoxic cells, but washes out rapidly from normoxic cell. [[61]Cu]-diacetyl-bis [N4-methylthiosemicarbazone] [[61]Cu]-ATSM] was prepared using house-made ATSM ligand and [[61]Cu]CuCl[2] produced via the [nat]Zn[p,x] [61]Cu [180[1/4]A proton irradiation, 22MeV, 3.2h] and purified by ion chromatography method. [[61]Cu]-ATSM was administered into normal and tumor bearing rodents up to 180 minutes followed by biodistribution and co-incidence imaging studies. Radionuclidic control showed the presence of 67.41[4.23%], 282.96[12.2%], 373[2.15%], 511[122.9%], 656[10.77%], 1186[3.75%] keV-rays from [61]Cu and showed a radionuclidic purity higher than 99%. The rest of activity was attributed to [61]Cu [0.23%]. [[61]Cu]-ATSM radiochemical purity was >99% shown by HPLC and RTLC methods. A significant difference was observed between tumor and non tumor accumulation. The method used in this research for the production and chemical separation of 61Cu was simple and cost effective. [[61]Cu]-ATSM is PET radiopharmaceutical for hypoxia imaging with an intermediate half life, and our experiments on this radiopharmaceutical have shown satisfactory results, suitable for future PET studies in human