Development, formulation and quality evaluation of a lyophilized PSMA-۱۱ kit for rapid radiolabeling with [۶۸Ga]Gallium

Introduction: Recently, [۶۸Ga]Gallium lyophilized kit has been widely practiced as it simplifies the radiolabeling process. Thus, our aim is to develop, formulate and evaluate a single-vial lyophilized kit (EZYKit PSMA) for the preparation and radiolabeling of [۶۸Ga]Ga-PSMA-۱۱.Methods: Two commercially available [۶۸Ge/۶۸Ga] Generators used in this study were from ITG and Eckert & Ziegler with a current [۶۸Ga]Gallium elution activity of ۲۲۲ MBq and ۱۴۸۰ MBq, respectively. Initially, EZYkit-PSMA radiolabeling parameters were optimized, and the Glass Transition Temperature (Tg) of the optimized PSMA-۱۱ formulation was determined. Quality assessment of EZYkit-PSMA, including physical appearance, quantitative assay of the active ingredient, radiochemical purity, pH, sterility, endotoxin, and storage stability, were also established.Results: Optimization of radiolabeling parameters showed that the highest radiochemical purity was achieved with ۰.۳۵ ml and ۰.۷۵ ml of ۱.۵ M acetate buffer and ۱۰ µg PSMA-۱۱ for both ITG and Eckert & Ziegler Generator, respectively. The quality assessment results of EZYkit-PSMA were within the specifications except for the physical appearance, where it appears to be structurally collapsed. This study discussed two main factors that contributed to the collapsed lyophilized cake.Conclusion: Despite the physical appearance, EZYkit-PSMA was successfully developed, and the quality meets the pharmaceutical standards. EZYkit-PSMA showed high stability over ۶ month's storage period in both the fridge and freezer. Overall, using EZYkit-PSMA for radiolabeling with [۶۸Ga]Gallium simplified the whole radiolabeling procedure and reduces process time and error with high labelling yield and efficiency.

کلیدواژه ها:

Gallium-۶۸ ، Lyophilized EZYkit ، Prostate specific membrane antigen ، prostate cancer