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In vivo preclinical evaluation of the new Ga-labeled beta-cyclodextrin in prostaglandin E2 (PGE2) positive tumor model using positron emission tomography.

07:00 EST 11th January 2020 | BioPortfolio

Summary of "In vivo preclinical evaluation of the new Ga-labeled beta-cyclodextrin in prostaglandin E2 (PGE2) positive tumor model using positron emission tomography."

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 Ga-labeled NODAGA-randomly methylated beta-cyclodextrin (Ga-NODAGA-RAMEB) and investigate its tumor-targeting properties. NODAGA-RAMEB was labeled with Gallium-68 (Ga), and the radiochemical purity (RCP%), partition coefficient (logP values), and in vitro-in vivo stability of Ga-NODAGA-RAMEB were determined. After intravenous injection of Ga-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 Ga-NODAGA-RAMEB was higher than 98%. The molar activity was 15.34±1.93 GBq/μmol. The logP of Ga labeled NODAGA-RAMEB was -3.63±0.04. Biodistribution studies showed high accumulation of Ga-NODAGA-RAMEB in PGE2 positive BxPC-3 tumors; approximately 15-20-fold higher radiotracer uptake was observed, than that of the background. Ga-labeled RAMEB is a promising radiotracer in PET diagnostics of PGE2 positive tumors.

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This article was published in the following journal.

Name: International journal of pharmaceutics
ISSN: 1873-3476
Pages: 118954

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