Development of a ready-to-use PSMA-11 kit formulation and biological evaluation of binding affinity
Carregando...
Data
Data de publicação
Orientador
Título da Revista
ISSN da Revista
Título do Volume
É parte de
É parte de
É parte de
Advances in Molecular Imaging
Exportar
Resumo
Introduction: 68Ga-PSMA-11 is considered the gold standard in detection of micro and oligometastases in advanced prostate cancer, being used for therapeutic planning, as well as, potentially, for evaluating response to treatment. The development of ready-to-use lyophilized kit of PSMA-11 adds quality and safety to the routine use of this radiopharmaceutical and represents a pharmacotechnical challenge as it must preserve the integrity and specificity of the ligand. Methods: PSMA-11 kit formulation was proposed, considering radiolabeling parameters and the preservation of the peptide during the lyophilization process, using mannitol as an excipient. Critical temperature characterization studies were carried out using DSC equipment and the freeze-drying process was developed. The direct radiolabeling conditions were evaluated and standardized using 68Ge/68Ga generator eluate from two different manufacturers (ITG and Eckert & Ziegler). The radiochemical purity was evaluated by TLC and HPLC. Biological evaluation was carried out with lyophilized PSMA-11 to demonstrate the integrity of the peptide and preservation of biological activity after the lyophilization process. Results: Based on critical temperature characterization studies, the freeze-drying cycle was designed to reach a freezing temperature of around −40˚C and primary drying at 2˚C. Using 20 mg of mannitol, an intact and elegant lyophilized cake was obtained. PSMA-11 lyophilized kit was directly labeled with 68Ga eluate from 68Ge/68Ga GMP generators (ITG and Eckert & Ziegler) resulting in % RP > 95% at pH 4.0 to 4.5. The results obtained from in vitro and in vivo biological competition studies confirmed the preservation of PSMA-11 affinity for the receptor after lyophilization. Conclusion: A lyophilized formulation (Kit) of PSMA-11 was successfully obtained, which preserved the integrity and biological activity of the peptide and guaranteed radiolabeling efficiency.
Como referenciar
FREIRE, MARIA R.V.B.; BEXIGA, NATALIA M.; STEPHANO, MARCO A.; OLIVEIRA, JOAO E.; SOARES, CARLOS R.J.; MIRANDA, ANA C.C.; BARBOSA, ANNA C. de A.; BARBOZA, MARYCEL F. de; GARCIA, LAURA F.; TEIXEIRA, LUIZ F.S.; BELLINI, MARIA H.M.; SILVA, NATANAEL G. da; BALIEIRO, LUIZA M.; MENDES, JOEL; ARAUJO, ELAINE B. de. Development of a ready-to-use PSMA-11 kit formulation and biological evaluation of binding affinity. Advances in Molecular Imaging, v. 13, n. 2, p. 7-22, 2024. DOI: 10.4236/ami.2024.132002. Disponível em: https://repositorio.ipen.br/handle/123456789/48761. Acesso em: 20 Mar 2026.
Esta referência é gerada automaticamente de acordo com as normas do estilo IPEN/SP (ABNT NBR 6023) e recomenda-se uma verificação final e ajustes caso necessário.