Evaluation of a Bispidine-Based Chelator for Gallium-68 and of the Porphyrin Conjugate as PET/PDT Theranostic Agent |
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| Authors: | Dr. Thomas W. Price Dr. Steven Y. Yap Dr. Raphaël Gillet Huguette Savoie Dr. Loïc J. Charbonnière Prof. Ross W. Boyle Dr. Aline M. Nonat Dr. Graeme J. Stasiuk |
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| Affiliation: | 1. School of Life Sciences, Faculty of Health Sciences, University of Hull, Cottingham Road, Hull, HU6 7RX UK;2. Chemistry, School of Mathematical and Physical Sciences, University of Hull, Cottingham Road, Hull, HU6 7RX UK;3. Equipe de Synthèse pour l'Analyse (SynPA), CNRS, IPHC UMR 7178, Université de Strasbourg, 67000 Strasbourg, France |
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| Abstract: | In this study a bispidine ligand has been applied to the complexation of gallium(III) and radiolabelled with gallium-68 for the first time. Despite its 5-coordinate nature, the resulting complex is stable in serum for over two hours, demonstrating a ligand system well matched to the imaging window of gallium-68 positron emission tomography (PET). To show the versatility of the bispidine ligand and its potential use in PET, the bifunctional chelator was conjugated to a porphyrin, producing a PET/PDT-theranostic, which showed the same level of stability to serum as the non-conjugated gallium-68 complex. The PET/PDT complex killed >90 % of HT-29 cells upon light irradiation at 50 μm . This study shows bispidines have the versatility to be used as a ligand system for gallium-68 in PET. |
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| Keywords: | bispidine gallium-68 porphyrin radiochemistry theranostic |
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