Next Article in Journal
A Flavonoid-Rich Extract from Bergamot Juice, Alone or in Association with Curcumin and Resveratrol, Shows Protective Effects in a Murine Model of Cadmium-Induced Testicular Injury
Next Article in Special Issue
Update on PET Tracer Development for Muscarinic Acetylcholine Receptors
Previous Article in Journal
Probiotics as a Treatment for “Metabolic Depression”? A Rationale for Future Studies
Previous Article in Special Issue
Feasibility of Developing Radiotracers for MDM2: Synthesis and Preliminary Evaluation of an 18F-Labeled Analogue of the MDM2 Inhibitor SP-141
Article

Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer

1
Hospital Israelita Albert Einstein, Sao Paulo 05652-900, Brazil
2
Department of Physiological Sciences, School of Medical Sciences, Santa Casa de Sao Paulo, Sao Paulo 01221-020, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: Gerald Reischl
Pharmaceuticals 2021, 14(5), 385; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050385
Received: 28 January 2021 / Revised: 6 March 2021 / Accepted: 9 March 2021 / Published: 21 April 2021
Prostate-specific membrane antigen (PSMA) is a glycoprotein present in the prostate, that is overexpressed in prostate cancer (PCa). Recently, PSMA-directed radiopharmaceuticals have been developed, allowing the pinpointing of tumors with the Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging techniques. The aim of the present work was to standardize and validate an automatic synthesis module-based radiolabeling protocol for [68Ga]Ga-PSMA-11, as well as to produce a radiopharmaceutical for PET imaging of PCa malignancies. [68Ga]Ga-PSMA-11 was evaluated to determine the radiochemical purity (RCP), stability in saline solution and serum, lipophilicity, affinity to serum proteins, binding and internalization to lymph node carcinoma of the prostate (LNCaP) cells, and ex vivo biodistribution in mice. The radiopharmaceutical was produced with an RCP of 99.06 ± 0.10%, which was assessed with reversed-phase high-performance liquid chromatography (RP-HPLC). The product was stable in saline solution for up to 4 h (RCP > 98%) and in serum for up to 1 h (RCP > 95%). The lipophilicity was determined as −3.80 ± 0.15, while the serum protein binding (SPB) was <17%. The percentages of binding to LNCaP cells were 4.07 ± 0.51% (30 min) and 4.56 ± 0.46% (60 min), while 19.22 ± 2.73% (30 min) and 16.85 ± 1.34% (60 min) of bound material was internalized. High accumulation of [68Ga]Ga-PSMA-11 was observed in the kidneys, spleen, and tumor, with a tumor-to-contralateral-muscle ratio of >8.5 and a tumor-to-blood ratio of >3.5. In conclusion, an automatic synthesis module-based radiolabeling protocol for [68Ga]Ga-PSMA-11 was standardized and the product was evaluated, thus verifying its characteristics for PET imaging of PCa tumors in a clinical environment. View Full-Text
Keywords: PSMA-11; gallium-68; automatic synthesis module; PET imaging; prostate cancer PSMA-11; gallium-68; automatic synthesis module; PET imaging; prostate cancer
Show Figures

Figure 1

MDPI and ACS Style

Fuscaldi, L.L.; Sobral, D.V.; Durante, A.C.R.; Mendonça, F.F.; Miranda, A.C.C.; da Cunha, M.L.; Malavolta, L.; Mejia, J.; de Barboza, M.F. Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer. Pharmaceuticals 2021, 14, 385. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050385

AMA Style

Fuscaldi LL, Sobral DV, Durante ACR, Mendonça FF, Miranda ACC, da Cunha ML, Malavolta L, Mejia J, de Barboza MF. Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer. Pharmaceuticals. 2021; 14(5):385. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050385

Chicago/Turabian Style

Fuscaldi, Leonardo L., Danielle V. Sobral, Ana C.R. Durante, Fernanda F. Mendonça, Ana C.C. Miranda, Marcelo L. da Cunha, Luciana Malavolta, Jorge Mejia, and Marycel F. de Barboza 2021. "Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer" Pharmaceuticals 14, no. 5: 385. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050385

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop