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.


Journal Details

This article was published in the following journal.

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


DeepDyve research library

PubMed Articles [13233 Associated PubMed Articles listed on BioPortfolio]

Enhancement of acid-sensing ion channel activity by prostaglandin E2 in rat dorsal root ganglion neurons.

Prostaglandin E2 (PGE2) and proton are typical inflammatory mediators. They play a major role in pain processing and hypersensitivity through activating their cognate receptors expressed in terminals ...

Radiosynthesis and preclinical evaluation of CCimbi-701 - Towards the imaging of cerebral 5-HT receptors.

The serotonin 7 (5-HT ) receptor is suggested to be involved in a broad variety of CNS disorders, but very few in vivo tools exist to study this important target. olecular imaging with positron emissi...

Serum PGE2, 15d-PGJ, PPARγ and CRP levels in patients with schizophrenia.

Many hypotheses have been proposed for the development of schizophrenia, including the one proposing that exogenous and endogenous factors are linked to inflammatory processes. There is strong evidenc...

A candidate pathogenic gene, zinc finger gene 217 (ZNF217) may contribute to polycystic ovary syndrome through prostaglandin E2.

Polycystic ovary syndrome is a complex endocrine condition with chronic inflammation. Prostaglandin E2 (PGE2) is a proinflammatory factor with an increased expression in the serum of women with polycy...


To evaluate the vitreous concentration of different nonsteroidal anti-inflammatory drugs (NSAIDs) after topical administration and the related prostaglandin E2 (PGE2) levels in patients undergoing par...

Clinical Trials [4577 Associated Clinical Trials listed on BioPortfolio]

Prostaglandin E2 Predicts the Outcome of Acute-on-chronic Liver Failure

Acute-on-chronic liver failure (ACLF) is an ailment with high incidence of multiorgan failure (MOF) and consequent mortality. Systemic inflammation and susceptibility to infection are char...

PGE2/IL-22 Pathway in Various Forms of Eczema

Objectives: Eczema is a chronic inflammatory skin condition characterised immunologically by T cellmediated inflammation. The pathogenic mechanisms involved in its development are incomple...

PGE2 Levels in Patient Treated With NSAIDs

The aim of this study is to determine vitreous levels of nonsteroidal antinflammatory drugs (NSAIDs) and prostaglandinE2 (PGE2) in eyes scheduled for vitrectomy. All patients received the...

Piroxicam-beta-Cyclodextrin on Tooth Sensitivity Caused by In-office Bleaching

Objectives: This study aims to evaluate the effectiveness of preemptive administration of non-steroidal anti-inflammatory Piroxicam-beta-Cyclodextrin on risk and level of tooth sensitivity...

Oxytocin vs. Prostaglandin for Induction of Labor in Primiparas With Prelabor Rupture of Membrane and Low Bishop

The purpose of the study is to compare between oxytocin to prostaglandin (PGE2), regarding time from induction of labor (IOL) to delivery among primiparas at term with prelabor rupture of ...

Medical and Biotech [MESH] Definitions

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.

Cell surface receptors that bind prostaglandins with high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin receptor subtypes have been tentatively named according to their relative affinities for the endogenous prostaglandins. They include those which prefer prostaglandin D2 (DP receptors), prostaglandin E2 (EP1, EP2, and EP3 receptors), prostaglandin F2-alpha (FP receptors), and prostacyclin (IP receptors).

Quick Search

DeepDyve research library

Searches Linking to this Article