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Öğe 99m Tc(I) carbonyl-radiolabeled lipid based drug carriers for temozolomide delivery and bioevaluation by in vitro and in vivo(De Gruyter, 2019) Arl K.; Uçar E.; Içhedef Ç.; Yurt Kllçar A.; Medine E.I.; Parlak Y.; Saylt Bilgin B.E.; Aydln B.; Gümüşer F.G.; 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. ? 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. © 2019 Walter de Gruyter GmbH, Berlin/Boston 2019.Öğe Bioevaluation of 99mTc(I) carbonyl-radiolabeled amino acid coated magnetic nanoparticles in vivo(Elsevier Ltd, 2019) Büyükok O.; Uçar E.; İçhedef Ç.; Çetin O.; Teksöz S.In this paper, amino acid coated and radiolabeled magnetic nanoparticles (MNPs) were prepared as a potential diagnostic agent. Magnetic nanoparticles were synthesized and functionalized by L-alanine and L-cysteine amino acids in one step. Besides surface functionalization, amino acid coating also provided favourable particle size. Structural characterization was performed by scanning electron microscopy. We obtained 30–38 nm and 22–30 nm diameter ranges with spherical shape for L-alanine and L-cysteine coated nanoparticles, separately. Then L-alanine and L-cysteine coated MNPs were radiolabeled with 99mTc(I)-tricarbonyl core (99mTc(CO)3-Alanine-MNP, 99mTc(CO)3-Cysteine-MNP) with a labeling yield of 63 ± 3% and 74 ± 2%. Pure radiolabeled magnetic particles were obtained by washing them with saline solution, and the radiochemical purity of 99mTc(CO)3-Alanine-MNP and 99mTc(CO)3-Cysteine-MNP were found as 94.3 ± 0.47% and 97.6 ± 1.06% in each of the final solution, respectively. In addition, both radiolabeled nanoparticles were stabile up to 4 h at 37 °C temperature in vitro conditions. After radiolabeling with 99m-Technetium tricarbonyl core, biological behaviour of nanoparticles was evaluated for each in vivo on male Wistar Albino rats. © 2019 Elsevier B.V.Öğe Effect of rosemary (Rosmarinus officinalis) extract on the biodistribution of 99mTc sulphur colloid and on the radiolabeled blood constituents(Sociedade Brasileira de Farmacognosia, 2013) Uçar E.; Teksöz S.; Içhedef C.; Kilçar A.Y.; Ünak P.With this study we evaluated the effects of the herb rosemary (Rosmarinus officinalis L. Lamiaceae) extract on the labeling of blood constituents with technetium-99m (99mTc) labeled sulphur colloid and on the biodistribution of 99mTc-Sulphur Colloid in Wistar albino rats. For this purpose, two groups of animals (male wistar rats, 130-140 g) were treated (1 mL) with a rosemary extract (750 mg/kg body wt.,n=9) and water (control, n=9) separately by gavage for five days. 99mTc-Sulphur Colloid was administrated by intravenous injection; organs/tissues were withdrawn and weighted. Blood was centrifuged, plasma and blood cells were isolated. The radioactivity was counted to calculate the percentage of activity per gram for each organ/tissue and percentage of activity in blood cells and plasma. A signifi cant increase (p<0.05) in the uptake of 99mTc-Sulphur Colloid in the liver after the treatment with rosemary extract was observed. These results indicate that the substances or metabolites of the rosemary extract would change the biodistribution of 99mTc-Sulphur Colloid.Öğe Evaluation of new 99mTc(CO)3 + radiolabeled glycylglycine In Vivo(Bentham Science Publishers, 2019) Şenışık A.M.; İçhedef Ç.; Kılçar A.Y.; Uçar E.; Arı K.; Parlak Y.; 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 [99mTc(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 (HPLRC). Lipophilicity study for radiolabeled complex (99mTc(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 radiolabelling yield of 99mTc(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 99mTc(CO)3-GlyGly has the potential to be used as a peptide-based imaging agent. Further studies, 99mTc(CO)3-GlyGly can be performed on tumor-bearing animals. © 2019 Bentham Science Publishers.Öğe One-step conjugation of glycylglycine with [18F]FDG and a pilot PET imaging study(Springer Netherlands, 2018) Şenk A.M.; İçhedef Ç.; Kılçar A.Y.; Uçar E.; Arı K.; Göksoy D.; Parlak Y.; Sayıt Bilgin B.E.; Teksöz S.This study describes a single step conjugation of Glycylglycine (GlyGly) which is a small peptide, with [18F]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 °C for 30 min in a vial containing AO-GlyGly and [18F]FDG solution. The radiolabeled product ([18F]FDG-GlyGly) was obtained with 98.65 ± 0.35% yield without any purification step which makes this method more attractive for 18F radiolabeling. The present study is concluded with an in vivo pilot animal PET study to assess biodistribution and kinetics of chemoselectively [18F]FDG tagged GlyGly in vivo. © 2018, Akadémiai Kiadó, Budapest, Hungary.Öğe Preparation and bioevaluation of 99mTc-carbonyl complex of guanine(2011) Içhedef C.; Teksöz S.; Şenocak K.; Uçar E.; KIlçar A.Y.The aim of this study is to prepare radiolabeled guanine with 99mTc(CO) 3 + core. For this purpose, guanine has been radiolabeled with 99mTc(CO) 3 + core. Quality control study of radiolabeled guanine molecule with 99mTc(CO) 3 + core was performed by thin layer radio chromatography (TLRC) and high performance liquid radio chromatography (HPLRC). The results showed that the radiolabeling yield was quite high (94 ± 3%). Beside that 99mTc(CO) 3-Gua complex has showed good in vitro stability during the 24 h period. Radiopharmaceutical potential of this complex was evaluated in Wistar Albino Rats. It was concluded that 99mTc(CO) 3-Gua could be used as a nucleotide radiopharmaceutical for in vivo applications. © 2011 Akadémiai Kiadó, Budapest, Hungary.Öğe Thymidine kinase enzyme selective imaging radiopharmaceutical: 99mTc(CO)3-Ganciclovir(2013) Gedik B.; Teksöz S.; Içhedef Ç.; Kilçar A.Y.; Medine E.I.; Uçar E.The aim of this study is to radiolabel ganciclovir, known as having selective antiviral properties against thymidine kinase, with technetium tricarbonylcore (99mTc(CO)3 + and to investigate the biological behavior of this complex in vitro and in vivo. Commercially provided Ganciclovir (GCV) was radiolabeled with 99mTc(CO)3-. Initially, optimum radiolabeling conditions were determined by analyzing factors such as temperature, pH and time. Quality control of the radiolabeled compound was performed. The radiolabeling yield was found to be 97%. The 99mTc(CO)3 -GCV complex also displayed good in vitro stability during the 24 h period. In vitro cell uptake studies showed that the 99mTc(CO)3-GCV complex is highly uptaken in A-549, PC-3, HeLa cell lines according to the control group 99mTc(I)-tricarbonyl core. The knowledge gained from in vivo and in vitro studies of 99mTc(CO)3-GCV could contribute to the development of a new HSV1-tk gene imaging agent. © by Oldenbourg Wissenschaftsverlag, München.
