Search results for: 68Ga

Authors: Archana Mukherjee, Aruna Korde, Sudipta Chakraborty, H. D. Sarma, Grace Samuel, M. R. A. Pillai

Abstract:

Radiolabeled cyclic RGD peptides targeting integrin αvβ3 are reported as promising agents for the early diagnosis of metastatic tumors. With an aim to improve tumor uptake and retention of the peptide, cyclic RGD peptide dimer E[c (RGDfK)] 2 (E = Glutamic acid, f = phenyl alanine, K = lysine) coupled to the bifunctional chelator DOTA was custom synthesized and radiolabelled with 68Ga. Radiolabelling of cyclic RGD peptide dimer with 68Ga was carried out using HEPES buffer and biological evaluation of the complex was done in nude mice bearing HT29 tumors.

Keywords: 68Ga peptides, Angiogenesis imaging, Cyclic RGD peptides, PET Imaging.

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Authors: Anton A. Larenkov, Alesya Ya Maruk

Abstract:

In the present study, highly effective iTLC single strip method for the determination of radiochemical purity (RCP) of ⁶⁸Ga-BCA-peptides was developed (with no double-developing, changing of eluents or other additional manipulation). In this method iTLC-SG strips and commonly used eluent TFA_aq. (3-5 % (v/v)) are used. The method allows determining each of the key radiochemical forms of ⁶⁸Ga (colloidal, bound, ionic) separately with the peaks separation being no less than 4 σ. Rf = 0.0-0.1 for ⁶⁸Ga-colloid; Rf = 0.5-0.6 for ⁶⁸Ga-BCA-peptides; Rf = 0.9-1.0 for ionic ⁶⁸Ga. The method is simple and fast: For developing length of 75 mm only 4-6 min is required (versus 18-20 min for pharmacopoeial method). The method has been tested on various compounds (including ⁶⁸Ga-DOTA-TOC, ⁶⁸Ga-DOTA-TATE, ⁶⁸Ga-NODAGA-RGD₂ etc.). The cross-validation work for every specific form of ⁶⁸Ga showed good correlation between method developed and control (pharmacopoeial) methods. The method can become convenient and much more informative replacement for pharmacopoeial methods, including HPLC.

Keywords: DOTA-TATE, 68Ga, quality control, radiochemical purity, radiopharmaceuticals, iTLC.

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Authors: S. Zolghadri, H. Yousefnia, A. R. Jalilian

Abstract:

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.

Keywords: Absorbed dose, EDTMP, 68Ga, rats.

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