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In vivo preclinical evaluation of the new 68Ga-labeled beta-cyclodextrin in prostaglandin E2 (PGE2) positive tumor model using positron emission tomography.
Trencsényi, György; Kis, Adrienn; Szabó, Judit P; Ráti, Ágnes; Csige, Katalin; Fenyvesi, Éva; Szente, Lajos; Malanga, Milo; Méhes, Gábor; Emri, Miklós; Kertész, István; Vecsernyés, Miklós; Fenyvesi, Ferenc; Hajdu, István.
Afiliación
  • Trencsényi G; Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary. Electronic address: trencsenyi.gyorgy@med.unideb.hu.
  • Kis A; Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
  • Szabó JP; Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
  • Ráti Á; Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
  • Csige K; Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
  • Fenyvesi É; Cyclolab Cyclodextrin R&D Laboratory Ltd., H-1097, Illatos St. 7, Budapest, Hungary.
  • Szente L; Cyclolab Cyclodextrin R&D Laboratory Ltd., H-1097, Illatos St. 7, Budapest, Hungary.
  • Malanga M; Cyclolab Cyclodextrin R&D Laboratory Ltd., H-1097, Illatos St. 7, Budapest, Hungary.
  • Méhes G; Department of Pathology, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
  • Emri M; Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
  • Kertész I; Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
  • Vecsernyés M; Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
  • Fenyvesi F; Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
  • Hajdu I; Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
Int J Pharm ; 576: 118954, 2020 Feb 25.
Article en En | MEDLINE | ID: mdl-31935470
The cyclooxygenase-2 (COX-2)/prostaglandin E2 (PGE2) pathway plays an important role in tumor development and formation of metastases. It was earlier reported that cyclodextrin derivatives have a high affinity to form complexes with PGE2. Based on these results radiolabeled cyclodextrins - as new radiopharmaceuticals - may open a new pathway in the in vivo imaging and diagnosis of PGE2 positive tumors. The aims of this study were to synthetize the PGE2 specific 68Ga-labeled NODAGA-randomly methylated beta-cyclodextrin (68Ga-NODAGA-RAMEB) and investigate its tumor-targeting properties. NODAGA-RAMEB was labeled with Gallium-68 (68Ga), and the radiochemical purity (RCP%), partition coefficient (logP values), and in vitro-in vivo stability of 68Ga-NODAGA-RAMEB were determined. After intravenous injection of 68Ga-NODAGA-RAMEB the accumulation in organs and tissues was monitored in vivo by positron emission tomography (PET) and ex vivo by gamma counter in BxPC-3 and PancTu-1 tumor-bearing CB17 SCID mice. The RCP% of the newly synthesized 68Ga-NODAGA-RAMEB was higher than 98%. The molar activity was 15.34 ± 1.93 GBq/µmol. The logP of 68Ga labeled NODAGA-RAMEB was - 3.63 ± 0.04. Biodistribution studies showed high accumulation of 68Ga-NODAGA-RAMEB in PGE2 positive BxPC-3 tumors; approximately 15-20-fold higher radiotracer uptake was observed, than that of the background. 68Ga-labeled RAMEB is a promising radiotracer in PET diagnostics of PGE2 positive tumors.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dinoprostona / Radiofármacos / Beta-Ciclodextrinas / Evaluación Preclínica de Medicamentos / Radioisótopos de Galio / Neoplasias Tipo de estudio: Prognostic_studies Límite: Animals / Humans / Male Idioma: En Revista: Int J Pharm Año: 2020 Tipo del documento: Article Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dinoprostona / Radiofármacos / Beta-Ciclodextrinas / Evaluación Preclínica de Medicamentos / Radioisótopos de Galio / Neoplasias Tipo de estudio: Prognostic_studies Límite: Animals / Humans / Male Idioma: En Revista: Int J Pharm Año: 2020 Tipo del documento: Article Pais de publicación: Países Bajos