Radiosynthesis and quality control of [[67]GA]-3,4-dimethoxylated porphyrin complex as a possible imaging agent

Radiolabeled porphyrins are potential tumor avid radiopharmaceuticals because of their impersonation in the human body, ability to complex various radionuclides, water solubility, low toxicity etc. In this work a radiogallium porphyrin complex has been developed. [67Ga] labeled 5,10,15,20-tetrakis [3,4-dimethoxyphenyl] porphyrin [[67Ga]-TDMPP] was prepared using freshly prepared [67Ga]GaCl[3] and 5,10,15,20-tetrakis [3,4-dimethoxyphenyl] porphyrin [H[2]TDMPP] for 60 min at 100°C. Stability of the complex was checked in final formulation and human serum for 24 h, followed by biodistribution and imaging studies in wild type rats up to 24 h. The radiocomplex was obtained with radiochemical purity >99% [ITLC] and >98% [HPLC]], specific activity: 12-15 GBq/mmol. The partition coefficient was determined [log P=1.63]. A detailed comparative pharmacokinetic study performed for 67Ga cation and [67Ga]-TDMPP. The complex was mostly washed out from the circulation through kidneys. Myocardial uptake was significantly observed by SPECT and biodistribution studies. Knee and shoulder joints demonstrated significant activity uptake in 2h post injection. Higher water solubility of the complex due to ionic nature of the complex is an advantage for rapid wash-out of the complex from the system, the complex has significant joint uptake compared to other radiolabeled porphyrins which the mechanisms are explained

Indium-111 maltolate complex as a cell labeling agent for SPECT imaging

Due to the cell labeling potentials of various metal-maltol complexes, the idea of developing a possible cell labeling imaging agent using single photon emission computed chromatography [SPECT] with [[m]ln]-maltolate complex has been investigated. [[IH]In] labeled 3-hydroxy-2-methyl-4H-pyran-4-onate [[m]In]-maltolate] was prepared using freshly prepared [[IH]In]InCl[3] and 3-hydroxy-2-methyl-4H-pyran-4-onate in a sodium salt form in 25 min at 45°C. Stability of the complex was checked in final formulation and human serum for 48 h. The partition coefficient was calculated for the compound followed by biodistribution and imaging studies. [[IU]In]-maltolate was successively used in the radiolabeling of red blood cells for diagnostic studies. The complex was prepared successfully [radiochemical purity: >98% ITLC, >98% HPLC specific activity: 15-17 GBq/mmol, log P=0.278]. The complex is mostly washed out from the circulation through kidneys in 24h. the cell labeling efficacy was significant at the time of experiment. [[In]ln]-maltolate can be an interesting cell imaging agent, due to stability and cell avidity of metal maltol complexes, however, further biodistribution studies in various cells as well as diagnostic protocols is necessary

Development of Ga-67 maltolate complex as an imaging agent

Due to the antitumor activity of Gallium MAL complex, as well as recent findings on new targeted biomolecules in malignant cells through this complex, the development of radiolabeled gallium complex for future imaging studies was targeted. Ga-67 labeled 3-hydroxy-2-methyl-4H-pyran-4-onate [Ga-67 MAL] was prepared using freshly prepared Ga-67 chloride and 3-hydroxy-2-methyl-4H-pyran-4-onate in a sodium salt form in 25 min at 40°C. The stability of the complex was checked in final formulation and human serum for 24 h followed by the administration in Swiss mice for biodistribution studies. The complex was prepared in high radiochemical purity [> 97% ITLC, > 98% HPLC] and specific activity of 13-14 GBq/mmol and was stable in the presence of serum for 48 h. The partition coefficient was calculated for the compound [log;? = 0.40]. A detailed comparative pharmacokinetic study was performed for Ga-67 cation and Ga-67-MAL. The complex is more rapidly washed out from the circulation through kidneys and liver compared to Ga-67 cation and can be an interesting tumor imaging agent due to the fact that the cold compound is undergoing clinical trials as a safe and potential therapeutic agent for cancer

Radiosynthesis and biological evaluation of [111]in-tris [8-hydroxy-2-methylquinoline] complex as a possible imaging agent

Due to the interesting pharmacological properties of radiolabeled metal oxine derivatives such as cell internalization, tumor avidity and antiproteosome activity, [111]In-tris[8-Hydroxy-2-methylquinoline] [[111]In-HMQ] was developed in this study. [111]In-HMQ was prepared using [111]InCl[3] and 8-Hydroxy-2-methylquinoline [HMQ] for 60 min at 100[degree sign] C [radiochemical purity: >99% ITLC, >99% HPLC, specific activity: 13-14 GBq/mmol]. Stability of the complex was checked in final formulation and in the presence of human serum for 48 h. The partition coefficient was calculated for the compound [log P=0.68]. The biodistribution of the labeled compound in vital organs of wild-type rats was studied using scarification studies and SPECT up to 24 h. A detailed comparative pharmacokinetic study for [111] In cation and [111]In-HMQ are performed up to 24h. The complex is mostly cleaned from the circulation by kidneys and is a compound rapidly washing from the circulation. The biodistribution of the complex in tumor models is on-going

Production, quality control and imaging of [64]Cu-ATSM in healthy rabbits for clinical applications

[[64]Cu]diacetyl-bis[N[4]-methylthiosemicarbazone] [[[64]Cu]ATSM] is a well-established hypoxia imaging tracer with reproducible production and significant specifity. In this work the high yield production and quality control as well as imaging studies in healthy rabbits is reported. Copper-64 produced via the [68]Zn[p, alpha n] [64]Cu nuclear reaction [30 MeV protons at 180 micro A] was used for the preparation of [[64]Cu]diacetyl-bis[N4-methylthiosemicarbazone][[ [64]Cu]ATSM]. Followed by quality control and administration to healthy rats as well as healthy rabbits for biodistribution and imaging studies respectively. [64]Cu[2+] [500 mCi, separation yield> 95%, radionuclide purity>96%] was used for [[64]Cu]ATSM production [radiochemical purity>99%, specific activity of 300 Ci/mmol] followed by administration to healthy rabbits and coincidence imaging demonstrating uptake in liver, kidney and bowel as shown by other reports in various rodents and human. [[64]Cu]ATSM radiopharmaceutical is produced and now available in large quantities for research and/or clinical trials in the country