Browsing by Author "Ari, K"

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    One-step conjugation of glycylglycine with [18F]FDG and a pilot PET imaging study
    Senisik, AM; Içhedef, Ç; Kilçar, AY; Uçar, E; Ari, K; Göksoy, D; Parlak, Y; Bilgin, BES; Teksöz, S
    This study describes a single step conjugation of Glycylglycine (GlyGly) which is a small peptide, with [F-18]FDG via oxime formation. Amiooxy-functionalization of GlyGly (AO-GlyGly) was accomplished through the reaction of Boc-aminooxy succinimide ester. Conjugation reaction was performed at 100 A degrees C for 30 min in a vial containing AO-GlyGly and [F-18]FDG solution. The radiolabeled product ([F-18]FDG-GlyGly) was obtained with 98.65 +/- 0.35% yield without any purification step which makes this method more attractive for F-18 radiolabeling. The present study is concluded with an in vivo pilot animal PET study to assess biodistribution and kinetics of chemoselectively [F-18]FDG tagged GlyGly in vivo.
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    99mTc(I) carbonyl-radiolabeled lipid based drug carriers for temozolomide delivery and bioevaluation by in vitro and in vivo
    Ari, K; Uçar, E; Içhedef, Ç; Kilçar, AY; Medine, EI; Parlak, Y; Bilgin, BES; Aydin, B; Gümüser, FG; Teksöz, S
    In preclinical research radiolabeled nanoparticles have been attracting interest as a new class of imaging probes. Assuming good stability of solid lipid nanoparticles (SLNs) under physiological conditions, radiolabeled SLNs can be used for imaging and measuring uptake in target tissue. Present study was performed to evaluate biological behavior of temozolomide (TMZ) loaded solid lipid nanoparticles (SLN-TMZ) in vivo and in vitro. Lipid nanoparticles were prepared by emulsification and low-temperature solidification method. zeta potential, morphology and particle size of nanoparticles were determined. Biological behavior of( 99m)Tc(CO)(3)(+) radiolabeled SLN-TMZ were investigated in vitro on U87/Daoy cell lines and in vivo on female Wistar Albino rats. Obtained results of in vitro incorporation, in vivo biodistribution and gamma imaging studies on radiolabeled SLN-TMZ show that the radiolabeled solid lipid nanoparticles could have potential as a drug delivery system for TMZ.
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    Evaluation of New 99mTc(CO)3+ Radiolabeled Glycylglycine In Vivo
    Senisik, AM; Içhedef, C; Kilçar, AY; Uçar, E; Ari, K; Parlak, Y; Bilgin, ES; Teksöz, S
    Background: Peptide-based agents are used in molecular imaging due to their unique properties, such as rapid clearance from the circulation, high affinity and target selectivity. Many of the radiolabeled peptides have been clinically experienced with diagnostic accuracy. The aim of this study was to investigate in vivo biological behavior of [Tc-99m(CO)(3)(H2O)(3)](+) radiolabeled glycylglycine (GlyGly). Methods: Glycylglycine was radiolabeled with a high radiolabeling yield of 94.69 +/- 2%, and quality control of the radiolabeling process was performed by thin layer radiochromatography (TLRC) and High-Performance Liquid Radiochromatography (iIPLRC). Lipophilicity study for radiolabeled complex (Tc-99m(CO)(3)-Gly-Gly) was carried out using solvent extraction. The in vivo evaluation was performed by both biodistribution and SPECT imaging. Results: The high mdiolabelling yield of Tc-99m(CO)(3)-GlyGly was obtained and verified by TLRC and HPLRC as well. According to the in vivo results, SPECT images and biodistribution data are in good accordance. The excretion route from the body was both hepatobiliary and renal. Conclusion: This study shows that Tc-99m(CO)(3)-GlyGly has the potential to be used as a peptide-based imaging agent. Further studies, Tc-99m(CO)(3)-GlyGly can be performed on tumor-bearing animals.
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    Synthesis, characterization and radiolabeling of folic acid modified nanostructured lipid carriers as a contrast agent and drug delivery system
    Ucar, E; Teksoz, S; Ichedef, C; Kilcar, AY; Medine, EI; Ari, K; Parlak, Y; Bilgin, BES; Unak, P
    Nanostructured lipid carriers (NLCs) are the new generation of solid lipid drug delivery systems. Their suitability as contrast agents for gamma scintigraphy is an attracting major attention. The aim of current study was to prepare surface modified nanostructured lipid carrier system for paclitaxel (PTX) with active targeting and imaging functions. In accordance with the purpose of study, PTX loaded nanostructured lipid carriers (NLCs) prepared, modified with a folate derivative and radiolabeled with technetium-99 m tricarbonyl complex (Tc-99 m(CO)(3)(+)). Cellular incorporation ratios of radiolabeled nanoparticles (Tc-99 m(CO)(3)-PTX-NLC) were investigated in vitro on three cancer cell lines. Additionally in vivo animal studies conducted to evaluate biological behavior of Tc-99 m(CO)(3)-PTX-NLC on female Wistar Albino rats. Biodistribution results showed that the folate derivative modified Tc-99 m(CO)(3)-PTX-NLC had considerably higher uptake in folate receptor positive organs. The data obtained from present study could be useful in the design of biodegradable drug carriers of PTX and folate receptor based tumor imaging agents.