A New Buffer for Gallium-68 Labeling Suitable for use in Nuclear Medicine; Triethanolamine (TEA)

Abstract

Background: Radiopharmaceuticals labeled with [68Ga] from positron emission tomog-raphy (PET) radionuclides are utilized in nuclear medicine for non-invasive in vivo molecular im-aging. Buffer solutions for radiolabeling play an important role as choosing the right buffer for the reaction helps to obtain high yield radiopharmaceuticals. Zwitterionic organic buffer 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES), sodium acetate (CH3COONa), sodium bicarbonate (NaHCO3) buffers are widely used for labeling of peptides with [68Ga]Cl3. They can be used for peptide labelings with the acidic [68Ga]Cl3 precursor of triethanolammonium (TEA) buffer. The cost and toxicity of TAE buffer are relatively low. Method: For [68Ga]GaPSMA-HBED-CC and [68Ga]GaDOTA-TATE labeling, the effectiveness of TEA buffer without chemical impurities in radiolabeling reactions and QC parameters in successful labeling was investigated. Results: The method used to label [68Ga]Cl3 with PSMA-HBED-CC peptide in the presence of TEA buffer was successful when applied at room temperature. High purity radiosynthesis suitable for clinical use was performed to obtain DOTA-TATE peptide with the addition of 363K temperature and radical scavenger. Quality control tests with R-HPLC have shown that this method is suitable for clinical use. Conclusion: We present an alternative procedure for labeling PSMA-HBED-CC and DOTA-TATE peptides with [68GaCl3] to obtain high radioactive doses of final radiopharmaceutical products used in nuclear medicine clinical applications. We have provided a quality-controlled final product that can be used in clinical diagnostic procedures. With the use of an alternative buffer, these methods could be adapted to semi-automatic or automated modules routinely used in nuclear medicine laboratories to label [68Ga]-based radiopharmaceuticals. © 2023 Bentham Science Publishers.