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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.
This article was published in the following journal.
Name: International journal of pharmaceutics
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Derivative of beta-cyclodextrin that is used as an excipient for steroid drugs and as a lipid chelator.
Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.
Studies determining the effectiveness or value of processes, personnel, and equipment, or the material on conducting such studies. For drugs and devices, CLINICAL TRIALS AS TOPIC; DRUG EVALUATION; and DRUG EVALUATION, PRECLINICAL are available.
Aldo-keto reductase that functions as a bi-directional 17 BETA, 20 ALPHA-HYDROXYSTEROID DEHYDROGENASE. It catalyzes the reduction of PROSTAGLANDIN D2 and PROSTAGLANDIN H2, as well as the oxidation of 9alpha,11beta-PGF2 to prostaglandin D2. It can also interconvert estrogens, ANDROGENS; and PROGESTINS between their active forms and inactive metabolites.
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