Diagnostic value of 99mTc-ubiquicidin scintigraphy in differentiation between osteomyelitis and bone tumors.

Aim: The differentiation of osteomyelitis from bone tumors is of great importance in clinical decision-making; however, the features of both osteomyelitis and bone tumors are noncontributory. Tc-ubiquicidin scintigraphy is a new promising method with the ability to specifically localize the infection site by bacterial cell membrane binding. This study aimed to evaluate the ability of this radiopeptide for the differentiation of these two entities.

Development of DOTA-Rituximab to be Labeled with Y for Radioimmunotherapy of B-cell Non-Hodgkin Lymphoma.

NHL is the most common hematologic cancer in adults. Rituximab is the FDA approved treatment of relapsed or refractory low grade B-cell Non-Hodgkin Lymphoma (NHL). But patients eventually become resistant to rituximab.

Technetium-99m Tricarbonyl Labeled a Broad-spectrum Quinolone as a Specific Imaging Agent in Infection Diseases.

Nuclear medicine imaging has been used to localize infection sites, and efforts have been continued to develop modified infection specific radiopharmaceuticals. In this study gemifloxacin as a broad-spectrum quinolone has been labeled with [Tc (CO) (HO)] core in order to evaluate its feasibility as an infection imaging agent for use. The stability of radioconjugate was checked in human serum at 37 °C and biodistribution was studied in mice.

Synthesis and evaluation of a Tc-labeled chemokine receptor antagonist peptide for imaging of chemokine receptor expressing tumors.

Objective: The chemokine receptor CXCR4 is highly expressed in tumor cells and plays an important role in tumor metastasis. In the present study, we report on the evaluation of a new radiopharmaceutical peptide for its potential to visualization for CXCR4-expressing tumors in vivo.

Methods: A CXCR4 antagonist analogue was synthesized using a standard Fmoc solid phase strategy and labeled with Tc via HYNIC and EDDA/tricine as coligands.

Functional Multi-Nanolayer Coatings of Amorphous Carbon/Tungsten Carbide with Exceptional Mechanical Durability and Corrosion Resistance.

A novel functional multilayer coating with periodically stacked nanolayers of amorphous carbon (a:C)/tungsten carbide (WC) and an adhesion layer of chromium (Cr) was deposited on 304 stainless steel using a dual magnetron sputtering technique. Through process optimization, highly densified coatings with high elasticity and shear modulus, excellent wear resistance, and minimal susceptibility to corrosive and caustic media could be acquired. The structural and mechanical properties of the optimized coatings were studied in detail using a variety of analytical techniques.

Modeling of lung cancer risk due to radon exhalation of granite stone in dwelling houses.

Aims: Due to increasing occurrences of lung cancer, radon exhalation rates, radon concentrations, and lung cancer risks in several types of commonly used granite stone, samples used for flooring in buildings, have been investigated.

Subjects And Methods: We measured the radon exhalation rates due to granite stones by means of an AlphaGUARD Model PQ2000 in a cube container with changeable floor by various granite stones. The lung cancer risk and percentage of lung cancer deaths (LCRn) due to those conditions were calculated using Darby's model.

Preparation and evaluation of rhenium-188-pamidronate as a palliative treatment in bone metastasis.

Objective: Rhenium-188-hydroxyethylidene diphosphonate (Re-HEDP) as a first generation bisphosphonate has been widely used for bone seeking radiopharmaceutical in cases of metastatic bone disease. No study has been yet reported on preparing a complex of Re with pamidronate (3-aminohydroxypropylidene-1,1-bisphosphonic acid) (PMA) as a second generation bisphosphonate. Based on this fact, it was hypothesized that a bone-seeking Re-PMA radiopharmaceutical could be developed as an agent for palliative radiotherapy of bone pain due to skeletal metastases.

Preparation and evaluation of APTES-PEG coated iron oxide nanoparticles conjugated to rhenium-188 labeled rituximab.

Radioimmuno-conjugated (Rhenium-188 labeled Rituximab), 3-aminopropyltriethoxysilane (APTES)-polyethylene glycol (PEG) coated iron oxide nanoparticles were synthesized and then characterized. Therapeutic effect and targeting efficacy of complex were evaluated in CD20 express B cell lines and tumor bearing Balb/c mice respectively. To reach these purposes, superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized using coprecipitation method and then their surface was treated with APTES for increasing retention time of SPIONs in blood circulation and amine group creation.

Development of a Radiolabeled Amlodipine Analog for L-type Calcium Channel Imaging.

Purpose: The non-invasive imaging and quantification of L-type calcium channels (also known as dihydropyridine channels) in living tissues is of great interest in diagnosis of congestive heart failure, myocardial hypertrophy, irritable bowel syndrome etc.

Methods: Technetium-99m labeled amlodipine conjugate ([99mTc]-DTPA-AMLO) was prepared starting freshly eluted (<1 h) 99mTechnetium pertechnetate (86.5 MBq) and conjugated DTPAAMLO at pH 5 in 30 min at room temperature in high radiochemical purity (>99%, RTLC; specific activity: 55-60 GBq/mmol).

A Tc-tricine-HYNIC-labeled Peptide Targeting the Melanocortin-1 Receptor for Melanoma Imaging.

Melanocortin-1 (MC1) receptor is an attractive melanoma-specific target for the development of α-MSH peptide based imaging and therapeutic agents. In this work a new lactam bridge α-MSH analogue was synthesized and radiolabeled with Tc via HYNIC chelator and tricine as co-ligand. Also, stability in human serum, receptor bound internalization and tissue biodistribution in tumor bearing nude mice were thoroughly investigated.

Preclinical Study of Ga-DOTATOC: Biodistribution Assessment in Syrian Rats and Evaluation of Absorbed Dose in Human Organs.

Objectives: Gallium-68 DOTA-DPhe-Tyr-Octreotide (Ga-DOTATOC) has been applied by several European centers for the treatment of a variety of human malignancies. Nevertheless, definitive dosimetric data are yet unavailable. According to the Society of Nuclear Medicine and Molecular Imaging, researchers are investigating the safety and efficacy of this radiotracer to meet Food and Drug Administration requirements.

Tc-tricarbonyl labeling of paclitaxel as an antimicrotubule agent and its evaluation in B16-F10 melanoma tumor-bearing mice.

In the present study paclitaxel (taxol) was labeled with [ Tc(CO) (H O) ] core. Labeling was optimized, and radiochemical analysis was determined by thin layer chromatography and high performance liquid chromatography. Radiocomplex was evaluated and verified further as a tumor characterization agent in B16-F10 melanoma tumor-bearing mice.

Development of an electrochemical W/Re generator as a technique for separation and purification of Re in radiopharmaceutical applications.

In this study, a simple electrochemical procedure adaptable for using low specific activity W for separation and purification of Re from W to obtain no carrier added (NCA) Re is developed. The electrochemical parameters were optimized to maximize the Re electrodeposition yield with minimal W contamination. Two cycle electrolysis procedure was developed.

A novel design of beam shaping assembly to use D-T neutron generator for BNCT.

In order to use 14.1MeV neutrons produced by d-T neutron generators, two special and novel Beam Shaping Assemblies (BSA), including multi-layer and hexagonal lattice have been suggested and the effect of them has been investigated by MCNP4C Monte Carlo code. The results show that the proposed BSA can provide the qualified epithermal neutron beam for BNCT.

Preparation, Biological Evaluation and Dosimetry Studies of 175Yb-Bis-Phosphonates for Palliative Treatment of Bone Pain.

Objective: Optimized production and quality control of ytterbium-175 (Yb-175) labeled pamidronate and alendronate complexes as efficient agents for bone pain palliation has been presented.

Methods: Yb-175 labeled pamidronate and alendronate (175Yb-PMD and 175Yb-ALN) complexes were prepared successfully at optimized conditions with acceptable radiochemical purity, stability and significant hydroxyapatite absorption. The biodistribution of complexes were evaluated up to 48 h, which demonstrated significant bone uptake ratios for 175Yb-PAM at all-time intervals.

Estimation of human absorbed dose for (166)Ho-PAM: comparison with (166)Ho-DOTMP and (166)Ho-TTHMP.

Objective: In this study, the human absorbed dose of holmium-166 ((166)Ho)-pamidronate (PAM) as a potential agent for the management of multiple myeloma was estimated.

Methods: (166)Ho-PAM complex was prepared at optimized conditions and injected into the rats. The equivalent and effective absorbed doses to human organs after injection of the complex were estimated by radiation-absorbed dose assessment resource and methods proposed by Sparks et al based on rat data.

Human absorbed dose estimation for a new (175)Yb-phosphonate based on rats data: Comparison with similar bone pain palliation agents.

In this work, the absorbed dose to human organs for (175)Yb-BPAMD was evaluated based on the biodistribution studies in rats. The results showed that the bone surface would receive the highest absorbed dose after injection of (175)Yb-BPAMD with 13.32mGy/MBq, while the other organs receive insignificant absorbed dose.

One-pot synthesis and sigma receptor binding studies of novel spirocyclic-2,6-diketopiperazine derivatives.

New spirocyclic-2,6-diketopiperazine derivatives containing benzylpiperidine and cycloalkane moieties were synthesized by a one-pot two-step sequential Ugi/intramolecular N-amidation process in moderate to good yields. The in vitro ligand-binding profile studies performed on the sigma-1 and sigma-2 receptors revealed that the σ1 affinities and subtype selectivities of three spirocyclic piperidine derivatives are generally comparable to those of spirocycloalkane analogues. Compared to the low σ1 affinities obtained for cycloalkyl-substituted spirocyclic-2,6-diketopiperazines with n=2, those with n=1 proved to have optimal fitting with σ2 subtype by exhibiting higher affinities.

Development of a (68)Ga-peptide tracer for PET GnRH1-imaging.

Objective: Total synthesis, quality control and preclinical evaluation of [(68)Ga]-DOTA-triptorelin ([(68)Ga]-DOTA-TRP) is reported as a possible PET radiotracer for GnRH receptor imaging.

Methods: DOTA-TRP was totally synthesized in two steps and after characterization went through radiolabelling optimization studies followed by tracer stability. The biodistribution of the tracer in normal male rats and 4T1 tumour-bearing mice was performed in 120 min after i.

Labeling and evaluation of (99m) Tc-tricarbonyl-meloxicam as a preferential COX-2 inhibitor for inflammation imaging.

Imaging of inflammation has an important role in dissolving problems in diagnosis and therapy of patients with inflammatory disorders. In this study meloxican as a nonsteroidal anti-inflammatory drug (NSAID) has been labeled with thechnetium-99m-tricarbonyl core ([(99m) Tc (CO)3 (H2 O)3 ](+) ) in order to evaluate its feasibility as an inflammation imaging agent for in vivo use. (99m) Tc-tricabonyl labeling of meloxicam was performed by its incubation with prepared precursor (99m) Tc-tricabonyl and heating in a boiling water bath for 30 min while various range of pH (1-9) was adjusted.

Assessment of the direct cyclotron production of (99m)Tc: An approach to crisis management of (99m)Tc shortage.

Nowadays, the cyclotron production of technetium-99m ((99m)Tc) has been increased, due to the worldwide (99m)Tc generator shortage. In the present work, an improved strategy for the production of (99m)Tc, using the proton irradiation of the enriched (100)Mo was developed. The performance of this method in terms of the production yield, chemical purity, radiochemical purity, as well as radionuclide purity was evaluated.

Grafting of [(64)Cu]-TPPF20 porphyrin complex on Functionalized nano-porous MCM-41 silica as a potential cancer imaging agent.

Mesoporous silica, MCM-41, functionalized with 3-aminopropyltriethoxysilane (APTES) was investigated as a potential drug delivery system, using [(64)Cu]-5, 10, 15, 20-tetrakis penta fluorophenyl porphyrin complex. [(64)Cu]-TPPF20 complex was grafted on functionalized MCM-41. The product was characterized by paper chromatography, FTIR spectroscopy, low angle X-ray diffraction, CHN and TGA/DTA analyses and atomic force microscopy.