Browsing by Author "Medine, EI"

Now showing 1 - 7 of 7
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    Synthesis, radiolabeling and in vivo biodistribution of diethylstilbestrol phosphate derivative (DES-P)
    Ünak, P; Müftüler, FZB; Içhedef, Ç; Medine, EI; Özmen, K; Ünak, T; Kilçar, AY; Gümüser, FG; Parlak, Y; Bilgin, ES
    Diethylstilbestrol (DES) is a well known, nonsteroidal estrogen with high affinity for the estrogen receptor (ER). Today DES is used to treat breast and prostate cancers. A phosphate derivative of DES [Diethylstilbestrol diphosphate (DES-P)] which is specific to tumor cells consisting alkaline phosphatase enzyme was synthesized and labeled with Tc-99m using tin chloride as reducing agent. In vivo biological activity of Tc-99m labeled diethylstilbestrol phosphate compound (Tc-99m-DES-P) was examined by biodistribution studies on Wistar Albino rats. Statistical evaluation was performed using SPSS 13 program. The percentage (%) radiolabeling yield of Tc-99m-DES-P and quality control studies were done by Thin Layer Radio Chromatography (TLRC). Results showed that, Tc-99m-DES-P may be proposed as an imaging agent for ER enriched tumors such as uterus and prostate and their metastases in bones.
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    Multifunctional molecular imaging probes for estrogen receptors: 99mTc labeled diethylstilbestrol (DES) conjugated, cuinp quantum dot nanoparticles (DESCIP)
    Moharrami, P; Unak, P; Guldu, OK; Medine, EI; Gumuser, G; Bilgin, ES; Aras, O
    A theranostic nanoparticle was synthesized based on diethylstilbestrol conjugated with phosphate, copper, and indium (DESCIP) and labelled with Tc-99m which can be used for SPECT imaging of ER-enriched cancers. In vitro biological activity of Tc-99m-DESCIP was examined in breast adenocarcinoma cells (MCF-7), prostatic carcinoma cells (PC-3), and pulmonary epithelial cells (A-549). In vivo lymph node imaging was performed in normal and receptor blocked female New Zealand rabbits. Results demonstrated that Tc-99m-DESCIP and DESCIP has potential for imaging ER-enriched tumors such as breast and prostate tumors, and their metastases in the lung, as well as improving management for their therapies.
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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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    Investigation of therapeutic efficiency of phenytoin (PHT) labeled with radioactive 131I in the cancer cell lines
    Uzaras, C; Avcibasi, U; Demiroglu, H; Medine, EI; Kilçar, AY; Müftüler, FZB; Ünak, P
    The aim of this study is to determine the incorporations of PHT radiolabeled with I-131 (I-131-PHT) on U-87 MG, Daoy and A549 cancerous cell lines. For this, cold and radio-labeling studies were carried out. The radio-labeling yield of I-131-PHT was obtained about 95 %. Subsequently, cell culture studies were carried out and radio-labeling yields of I-131, I-131-PHT on U-87 MG, Daoy and A549 cancerous cells were investigated. Cell culture studies demonstrated that the incorporation values of (IPHT)-I-131 on the three cell lines decreased with increasing radioactivity. Consequently, I-131-PHT may be a good radiopharmaceutical for targeting radionuclide therapy of Central Nervous System Tumors.
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    Investigation of Therapeutic Efficiency of Bleomycin and Bleomycin-Glucuronide Labeled with 131I on the Cancer Cell Lines
    Ediz, M; Avcibasi, U; Ünak, P; Müftüler, FZB; Medine, EI; Kilçar, AY; Demiroglu, H; Gümüser, FG; Sakarya, S
    The aim of this study is to determine the incorporations of radiolabeled bleomycin (I-131-BLM) and bleomycin-glucuronide (I-131-BLMGLU) on PC-3 (human prostate carcinoma cell line), Caco-2 (human colon adenocarcinoma cell line), Hutu-80 (Human Duodenum adenocarcinoma cell line), and A549 (Human lung adenocarcinoma epithelial cell line) cancerous cell lines. For this purpose, BLM and BLMGLU enyzmatically synthesized were labeled with I-131, quality control studies were done and the incorporation yields of I-131-BLM and I-131-BLMGLU on these cell lines were measured. Quality-control studies showed that the radiolabeling yields were obtained as 95% and 90% for I-131-BLM and I-131-BLMGLU, respectively. Also, as a result of the cell culture studies, it was found that I-131-BLM and I-131-BLMGLU had higher incorporation on PC-3 cells than that of other cell lines. In addition to this, it was reported that the incorporation yield of I-131-BLMGLU was higher than that I-131-BLM. At the end of the study, cytotoxicities of BLM and BLMGLU on PC-3 cancerous cell line were inspected and fluorescent images of BLM and BLMGLU were taken on PC-3 cells by using fluorescein isothiocyanate. In conclusion, cell culture studies demonstrated that the incorporation values of I-131-BLMGLU on the four cell lines were about five to six times higher than I-131-BLM. Radiolabeled glucuronide derivatives can be used in cancer therapy and tumor imaging, depending on the properties of radioiodine for the beta-glucuronidase-rich tissues because glucuronidation leads to rapid and higher incorporation on adenocarcinoma cells.
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    Thymoquinone Glucuronide Conjugated Magnetic Nanoparticle for Bimodal Imaging and Treatment of Cancer as a Novel Theranostic Platform
    Ince, I; Müftüler, ZB; Medine, EI; Güldü, ÖK; Takan, G; Ergönül, A; Parlak, Y; Yildirim, Y; Çakar, B; Bilgin, ES; Aras, Ö; Göker, E; Ünak, P
    Background: Theranostic oncology combines therapy and diagnosis and is a new field of medicine that specifically targets the disease by using targeted molecules to destroy the cancerous cells without damaging the surrounding healthy tissues. Objective: We aimed to develop a tool that exploits enzymatic TQ release from glucuronide (G) for the imaging and treatment of lung cancer. We added magnetic nanoparticles (MNP) to enable magnetic hyperthermia and MRI, as well as 131I to enable SPECT imaging and radionuclide therapy. Methods: A glucuronide derivative of thymoquinone (TQG) was enzymatically synthesized and conjugated with the synthesized MNP and then radioiodinated with 131I. New Zealand white rabbits were used in SPECT and MRI studies, while tumor modeling studies were performed on 6-7-week-old nude mice utilized with bioluminescence imaging. Results: Fourier-transform infrared spectroscopy (FTIR) and nuclear magnetic resonance (NMR) spectra confirmed the expected structures of TQG. The dimensions of nanoparticles were below 10 nm and they had rather polyhedral shapes. Nanoparticles were radioiodinated with 131I with over 95% yield. In imaging studies, in xenograft models, tumor volume was significantly reduced in TQGMNP-treated mice but not in non-treated mice. Among mice treated intravenously with TQGMNP, xenograft tumor models disappeared after 10 and 15 days, respectively. Conclusion: Our findings suggest that TQGMNP in solid, semi-solid and liquid formulations can be developed using different radiolabeling nuclides for applications in multimodality imaging (SPECT and MRI). By altering the characteristics of radionuclides, TQGMNP may ultimately be used not only for diagnosis but also for the treatment of various cancers as an in vitro diagnostic kit for the diagnosis of beta glucuronidase-rich cancers.
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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.