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Öğe 89Zr-Labeled DFO@Durvalumab-HSA nanoparticles: In vitro potential for triple-negative breast cancer(Wiley, 2024) Yurt, Fatma; Ozel, Derya; Karagul, Seyma; Tuncel, Ayca; Durkan, Kubra; Medine, Emin IlkerThis study presents the development and evaluation of a DFO@mAb-NP (DFO@Durvalumab-HSA-DTX nanoparticle) nanoplatform for imaging in triple-negative breast cancer (TNBC). The nanoplatform demonstrated significant changes postconjugation with DFO, evidenced by increased particle size from 178.1 +/- 5 nm to 311 +/- 26 nm and zeta potential alteration from -31.9 +/- 3 mV to -40.5 +/- 0.8 mV. Fourier-transform infrared spectroscopy and ultraviolet spectral analyses confirmed successful DFO conjugation, with notable shifts in peak wavelengths. High labeling efficiency was achieved with Zr-89, as indicated by thin layer radio chromatography and high-performance liquid radio chromatography results, with labeling efficiencies of 98 +/- 2% for Zr-89-DFO@mAb and 96 +/- 3% for Zr-89-DFO@mAb-NP. The nanoplatforms maintained stability over 24 h, showing less than 5% degradation. Lipophilicity assays revealed logP values of 0.5 +/- 0.03 for Zr-89-DFO@mAb-NP and 0.98 +/- 0.2 for Zr-89-DFO@mAb, indicating a higher lipophilic tendency in the radiolabeled Durvalumab. Cell uptake experiments showed an initial high uptake in MDA-MB-468 cells (45.1 +/- 3.2%), which decreased over time, highlighting receptor-specific interactions. These comprehensive findings suggest the promising potential of the DFO@mAb-NP nanoplatform for targeted imaging in TNBC, with implications for improved diagnostic accuracy and treatment strategies.Öğe Antitumor properties of bromelain loaded trastuzumab conjugated niosomes in HER2+breast cancer cells(Elsevier, 2024) Tut, Ezgi; Guldu, Ozge Kozgus; Medine, Emin IlkerThere are multiple forms of treatment for cancer treatment, but since the treatment process also damages healthy cells. Accordingly, in recent years, in the light of nanotechnological studies, cancer cell targeted drugs known as smart drugs have attracted attention. Niosome is one of the preferred nanoparticle systems in these studies. Bromelain is a protease mixture obtained from the pineapple stem or fruit. In recent years, it has been shown in many cell types that it has anticancer properties due to its proteolytic activity. In this study, bromelain was encapsulated into niosomes with 32 +/- 2.9 % efficiency for the treatment of breast cancer, which is the most common type of cancer in women. Specific targeting of niosome-encapsulated bromelain to HER2+ SKBR-3 cell line was performed by trastuzumab (herceptin) conjugation. DLS, FTIR, XPS, TEM were used for particle characterization. Niosomes (Nio) showed particle size of 134.3 +/- 8.1 nm, Bromelain loaded niosomes (Nio-Br) showed particle size of 165.6 +/- 11.5 nm. As a result of TEM analysis, it was shown that morphologically spherical and targeted sizes of niosomes of approximately 100 nm were synthesized. FTIR and XPS analyzes were performed to confirm pegylation and trastuzumab conjugation. Cytotoxicity and apoptosis studies of Nio-Br, Nio-Br-PEG-Tra, Tra samples carried out in SKBR-3 and MDA-MB-231 cell lines. Determined IC50 values of final product on SKBR-3 and MDA-MB-231 cell lines respectively 77.51 +/- 5.39 mu g/mL and 238.1 +/- 16.62 mu g/mL. As a result of in vitro studies, final product is more toxic on HER2+ SKBR-3 cell line thanks to trastuzumab in structure. At the same time final product has more apoptotic effect connected to toxic characteristic. Formed molecule in this study was designed for HER2+ breast cancer cells. According to obtained in vitro experiment results, this designed molecule has potential to be drug delivery system for HER2+ breast cancer.Öğe Complexation of gallic acid involving La3+, Sm3+, Th4+ and UO22+ ions in aqueous solution by potentiometry at various temperatures(Springer, 2024) Sismanoglu, Tuba; Ichedef, Cigdem; Akdut, Gizem; Soylu, Guelin Selda Pozan; Medine, Emin Ilker; Teksoz, SerapIn this study, the complexation of gallic acid with various lanthanide and actinide ions (La3+, Sm3+, Th4+, and UO22+) was investigated under aqueous conditions at elevated temperatures by potentiometric titration, with ionic strength of I = 0.10 mol dm-3 KCl. Stability constants for complexation of related metal-ions were determined using HYPERQUAD2013 software. The formation of complexes was considered at temperatures of 25 degrees C, 37 degrees C, and 45 degrees C. By examining the dependence of complex formation on temperature, the thermodynamic parameters of each complex were calculated. It was observed that the stability constant values varied with temperature. Additionally, cytotoxicity studies were conducted on MCF-7 and A-549 cell lines as part of the conclusion.Öğe Diethylstilbestrol glucuronide (DESG): synthesis, labeling with radioiodine and in vivo/in vitro evaluations(Springer, 2013) Yilmaz, Tayfun; Unak, Perihan; Muftuler, Fazilet Zumrut Biber; Medine, Emin Ilker; Sakarya, Serhan; Ichedef, Cigdem Acar; Unak, TuranDiethylstilbestrol (DES) is a synthetic non-steroidal estrogen, pharmacologic effects of which resemble natural estrons; today it is being used to treat some types of postmenopausal breast cancer and advanced prostate cancer. The aim of current study is conjugation of glucuronic acid (G) to DES and to evaluate radiopharmaceutical potential of this estrogen glucuronide derivative (DESG) which is specific to beta glucuronidase enzyme consisting tumor cells. Taking into consideration the compatibility to the chemical structures of the synthesized product, I-131 and I-125 were chosen as the appropriate radionuclides and DESG was labeled with these radionuclides utilizing iodogen method. The radiochemical yields of I-125/131-DESG were over 90 % according to thin layer radio chromatography method. The biodistribution of I-131-DESG in healthy female Wistar Albino rats has been investigated and the range of the breast/blood and breast/muscle ratios were approximately 2 and 13 in 240 min for ER unsaturated studies. Effects of the radioiodinated DES and DESG on the cells were examined using MCF-7, A-549, Caco-2 cell lines. I-125-DESG has higher incorporation percentages than I-125-DES on MCF-7 cells. The radioiodinated DESG has the desired radiopharmaceutical properties which could be candidate radiopharmaceuticals for diagnosis and especially radionuclide therapy of breast tumors.Öğe Diethylstilbestrol glucuronide (DESG): synthesis, labeling with radioiodine and in vivo/in vitro evaluations(Springer, 2013) Yilmaz, Tayfun; Unak, Perihan; Muftuler, Fazilet Zumrut Biber; Medine, Emin Ilker; Sakarya, Serhan; Ichedef, Cigdem Acar; Unak, TuranDiethylstilbestrol (DES) is a synthetic non-steroidal estrogen, pharmacologic effects of which resemble natural estrons; today it is being used to treat some types of postmenopausal breast cancer and advanced prostate cancer. The aim of current study is conjugation of glucuronic acid (G) to DES and to evaluate radiopharmaceutical potential of this estrogen glucuronide derivative (DESG) which is specific to beta glucuronidase enzyme consisting tumor cells. Taking into consideration the compatibility to the chemical structures of the synthesized product, I-131 and I-125 were chosen as the appropriate radionuclides and DESG was labeled with these radionuclides utilizing iodogen method. The radiochemical yields of I-125/131-DESG were over 90 % according to thin layer radio chromatography method. The biodistribution of I-131-DESG in healthy female Wistar Albino rats has been investigated and the range of the breast/blood and breast/muscle ratios were approximately 2 and 13 in 240 min for ER unsaturated studies. Effects of the radioiodinated DES and DESG on the cells were examined using MCF-7, A-549, Caco-2 cell lines. I-125-DESG has higher incorporation percentages than I-125-DES on MCF-7 cells. The radioiodinated DESG has the desired radiopharmaceutical properties which could be candidate radiopharmaceuticals for diagnosis and especially radionuclide therapy of breast tumors.Öğe Examination of the Association Between 3,4-Divanillyltetrahydrofuran Lignan (Urtica dioica Origin) and Prostate Cancer Cells by I-131 Radiolabeling(Mary Ann Liebert, Inc, 2020) Tekin, Volkan; Guldu, Ozge Kozgus; Medine, Emin Ilker; Muftuler, Fazilet Zumrut BiberBackground: Prostate cancer is the most common type of cancer for men in many countries. One of the various prostate cancer therapy methods is hormone therapy, and explaining the association between androgen hormones and prostate cancer is a critical role for successful prostate cancer treatment. Materials and Methods: in the current study, the behavior of 3,4- divanillyltetrahydrofuran (DTH) was examined against prostate cancer cells, which have androgen sensitivity differences [LNCaP (+), PC3 (-)]. For this aim, DTH was obtained by extraction of Urtica dioica roots. the molecular structure of isolated compound was confirmed as DTH by liquid chromatography-mass spectrometry and nuclear magnetic resonance spectroscopy analyses. To evaluate the association of androgen sensitivity, DTH was radiolabeled with I-131, and cell uptake assay was performed by using I-131-radiolabeled DTH. Also, cytotoxicity (WST-1) assay of DTH was performed against LNCaP and PC3 cells to determinate the toxic effects of DTH on different androgen mechanisms. Results: the results of assays on cells have shown that DTH lignan behaves different like being more toxic to LNCaP cells than PC3 cells, depending on androgen sensitivity. Conclusion: the results may contribute both the research topics of phytolignan prostate cancer and androgen-sensitive prostate cancer.Öğe In Vitro Determination of Wound. Healing Potential of Axonge(H M P Communications, 2017) Bilgi, Ahmet; Muftuler, Fazilet Zumrut Biber; Akman, Levent; Medine, Emin Ilker; Bilgi, Pinar Tonbaklar; Guldu, Ozge Kozgus; Gokulu, Sevki Goksun; Tekin, Volkan; Terek, Mustafa CosanBackground. Research on treatment alternatives that improve wound healing is an ever-evolving area in medicine, and a wound healing agent that carries minimal pain, discomfort, and scarring for patients with burn wounds, venous and decubitis ulcers, traumatic wounds, and many others is needed. The phases of wound healing include homeostasis, inflammation, migration, proliferation, and maturation. Adeps suillus (axonge) is known as a therapeutic agent for skin diseases and mainly consists of triglycerides. Objective. In the current study, the proliferation effect of axonge was determined on human normal epidermal keratinocyte (HaCaT) cells and human normal foreskin fibroblast cell line (BJ) cells. Materials and Methods. Experimental steps included preparation of HaCaT and BJ cell lines, axonge's stable tetrazolium salt-based proliferation assay, and evaluation of the wound healing effect of axonge on HaCaT and BJ cells. Results. Axonge concentrations of 3.12 mu g/mL, 6.25 mu g/mL, 12.5 mu g/mL, 25 mu g/mL, and 50 mu g/mL showed no cytotoxic effect on both HaCaT and BJ cells for 24, 48, and 72 hours. Considering the wound area of HaCaT cells, after 6 hours the wound healing effect of the axonge group reached almost 70% and then stopped. According to the results of the study on. BJ cells, after 6 hours axonge wound closure was found to be 50% while the control group was only 10%. Conclusion. On the basis of this study, the authors determined that axonge might have potential for use in wound healing.Öğe In vitro evaluation of radiolabeled (I-125) methanol extracts of yarrow in cell lines of MCF-7, PC-3, A-549 and Caco-2(Springer, 2013) Kilcar, Ayfer Yurt; Cekic, Betul; Muftuler, Fazilet Zumrut Biber; Unak, Perihan; Medine, Emin IlkerNowadays, cancer is still the second leading cause of death all over the world. Therefore, natural products which have anticancer and antitumor properties are come into prominence. Achillea family is known with anticancer and antitumor activity. Yarrow which has over a hundred bioactive compounds is a member of Achillea family. In current study; components of yarrow which was obtained after methanol extraction and purification were radiolabeled with I-125 and effects of these radiolabeled components on the cells were examined with using Caco-2, MCF-7, A-549, PC-3 cell lines. As a result of these studies, seven peaks were obtained and the highest radiolabeling yield was calculated for I-125 radiolabeled Peak 7 (95.00 +/- A 7.07, n = 4). To screen the biological properties of these radiolabeled peaks at determined cell lines, our ongoing effort was to evaluate incorporation percentage with time dependent. Furthermore, I-125-Peak 7 had highest incorporation ratio for whole cell lines and its incorporation percentage was increased with time dependent. Results of these in vitro studies were compatible with previous in vivo studies and traditional use of yarrow plants.Öğe In Vitro Incorporation of Radioiodinated Eugenol on Adenocarcinoma Cell Lines (Caco2, MCF7, and PC3)(Mary Ann Liebert, Inc, 2017) Dervis, Emine; Kilcar, Ayfer Yurt; Medine, Emin Ilker; Tekin, Volkan; Cetkin, Buse; Uygur, Emre; Muftuler, Fazilet Zumrut BiberRecently, the synthesis of radiolabeled plant origin compounds has been increased due to their high uptake on some cancer cell lines. Eugenol (EUG), a phenolic natural compound in the essential oils of different spices such as Syzygium aromaticum (clove), Pimenta racemosa (bay leaves), and Cinnamomum verum (cinnamon leaf), has been exploited for various medicinal applications. EUG has antiviral, antioxidant, and anti-inflammatory functions and several anticancer properties. The objective of this article is to synthesize radioiodinated (I-131) EUG and investigate its effect on Caco2, MCF7, and PC3 adenocarcinoma cell lines. It is observed that radioiodinated EUG would have potential on therapy and imaging due to its notable uptakes in studied cells.Öğe In Vitro/In Vivo Evaluation of Radiolabeled [Tc-99m(CO)(3)](+)-Hydroxyurea and Fluorescein Isothiocyanate-Hydroxyurea(Mary Ann Liebert, Inc, 2016) Yilmaz, Baris; Teksoz, Serap; Kilcar, Ayfer Yurt; Ucar, Eser; Ichedef, Cigdem; Medine, Emin Ilker; Ari, KadirThe aim of current study is to examine hydroxyurea (HU), which is an antineoplastic drug used for the treatment of leukemia, sickle-cell disease, HIV, psoriasis, thrombocythemia, and various neoplastic diseases in two aspects. The active ingredient hydroxyurea was obtained by purification of the capsule form drug, commercially named as HYDREA. Then, [Tc-99m(CO)(3)](+)core radiolabeling with HU was performed as first aspect. Quality control studies of Tc-99m(CO)(3)-HU complex were performed by thin-layer radiochromatography and high-performance liquid radiochromatography methods. The results demonstrated that the radiolabeling yield was quite high (98.43%+/- 2.29%). Also, Tc-99m(CO)(3)-HU complex has good stability during the 24-hour period. Biological behavior of Tc-99m(CO)(3)-HU complex is evaluated by biodistribution studies on Wistar Albino rats. Fluorescein isothiocyanate (FITC) labeling of HU was performed as second aspect. Fluorometric evaluation of binding efficacy and fluorescence imaging studies on MCF7 and Hela cell lines were carried out. It was thought that the knowledge achieved in this study would contribute to using Tc-99m(CO)(3)-HU complex as an imaging agent, which inhibits the DNA synthesis selectively, by inhibiting ribonucleotide reductase enzyme. It was observed that FITC-HU has noteworthy incorporation on both cell lines.Öğe An in-vivo pilot study into the effects of FDG-mNP in cancer in mice(Public Library Science, 2018) Aras, Omer; Pearce, Gillian; Watkins, Adam J.; Nurili, Fuad; Medine, Emin Ilker; Guldu, Ozge Kozgus; Tekin, Volkan; Wong, Julian; Ma, Xianghong; Ting, Richard; Unak, Perihan; Akin, OguzPurpose Previously, fluorodeoxy glucose conjugated magnetite nanoparticles (FDG-mNPs) injected into cancer cells in conjunction with the application of magnetic hyperthermia have shown promise in new FDG-mNPs applications. The aim of this study was to determine potential toxic or unwanted effects involving both tumour cells and normal tissue in other organs when FDG-mNPs are administered intravenously or intratumourally in mice. Materials and methods FDG-mNPs were synthesized. A group of six prostate-tumour bearing mice were injected with 23.42 mg/ml FDG-mNPs (intravenous injection, n = 3; intratumoural injection into the prostate tumour, n = 3). Mice were euthanized and histological sampling of tissue was conducted for the prostate tumour, as well as for lungs, lymph nodes, liver, kidneys, spleen, and brain, at 1 hour (n = 2) and 7 days (n = 4) post-injection. A second group of two normal (non-cancerous) mice received the same injection intravenously into the tail vein and were euthanised at 3 and 6 months post-injection, respectively, to investigate if FDG-mNPs remained in organs at those time points. Results In prostate-tumour bearing mice, FDG-mNPs concentrated in the prostate tumour, while relatively small amounts were found in the organs of other tissues, particularly the spleen and the liver; FDG-mNP concentrations decreased over time in all tissues. In normal mice, no detrimental effects were found in either mouse at 3 or 6 months. Conclusion Intravenous or intratumoural FDG-mNPs can be safely administered for effective cancer cell destruction. Further research on the clinical utility of FDG-mNPs will be conducted by applying hyperthermia in conjunction with FDG-mNPs in mice.Öğe Investigation of Therapeutic Efficiency of Bleomycin and Bleomycin-Glucuronide Labeled with I-131 on the Cancer Cell Lines(Mary Ann Liebert, Inc, 2013) Ediz, Melis; Avcibasi, Ugur; Unak, Perihan; Muftuler, Fazilet Zumrut Biber; Medine, Emin Ilker; Kilcar, Ayfer Yurt; Demiroglu, Hasan; Gumuser, Fikriye Gul; Sakarya, SerhanThe 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.Öğe Investigation of therapeutic efficiency of phenytoin (PHT) labeled with radioactive I-131 in the cancer cell lines(Springer, 2016) Uzaras, Cansu; Avcibasi, Ugur; Demiroglu, Hasan; Medine, Emin Ilker; Kilcar, Ayfer Yurt; Muftuler, Fazilet Zumrut Biber; Unak, PerihanThe 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.Öğe Isolation of resveratrol from peanut sprouts, radioiodination and investigation of its bioactivity on neuroblastoma cell lines(Springer, 2020) Karatay, Kadriye Busra; Kilcar, AyferYurt; Guldu, Ozge Kozgus; Medine, Emin Ilker; Muftuler, Fazilet Zumrut BiberRecently, natural antioxidant substances have been purified in a significant increasing incline from different plants for diagnosis and treatment options. in the current study, Resveratrol (RES) was isolated and radioiodinated with iodine-131 ([I-131]iodo-RES). Cell culture studies were conducted on neuroblastoma cells (SY-SH5Y and SK-N-AS) to investigate the bioavailability of [I-131]iodo-RES. the radioiodination yield of RES was 98.81 +/- 0.37% (n = 6). Uptake values up to 25% were observed notably on SK-N-AS cells until 24 h. Briefly; the current study will contribute to the development of novel radiolabeled plant origin agents for the imaging of neuroblastoma cells.Öğe Nanoencapsulation of green tea catechin (-)-Epigallocatechin-3-Gallate (EGCG) in niosomes and assessment of its anticancer activity against lung cancer(Elsevier, 2024) Evren, Damla Karaman; Guldu, Ozge Kozgus; Tut, Ezgi; Medine, Emin IlkerLung cancer is one of the leading causes of cancer-related deaths worldwide. In chemotherapy, the use of strong cytotoxic drugs and the specificity problems of these drugs also affect healthy cells and tissues. For this reason, the purpose of cancer treatment is to ensure that a suitable drug directly affects cancer cells at the appropriate dose. With nanotechnology, steps have been taken for an effective treatment that develops nano-transporters to deliver the drug molecule to the target cell in a specific, controlled manner. Another development is the discovery of theranostic agents used for both diagnostic and therapeutic purposes. In this study, a smart molecule was developed using the anticancer and antioxidant Epigallocatechin-3-Gallate (EGCG) molecule found in green tea, which is commonly consumed in our society. This molecule was encapsulated with niosomes to increase its stability and specificity. In this study, niosomes with an average size of 150 nm were synthesized using the thin film hydration technique. The zeta potential value of niosomes varied between -25 mV and -30 mV. Niosomes have been functionalized with indocyanine green (ICG) fluorescent dye and made suitable for optical imaging. The encapsulation efficiencies of the EGCG molecule and the ICG fluorescent dye were 10.1 % and 34.4 %, respectively. The release of EGCG from niosomes was an initial fast and then a slower release. 32 % of EGCG was released from niosomes within the first 3 h. Also, Cetuximab molecule was conjugated to niosomes with 75.8 % efficiency in order to provide lung cancer specificity and increase the anticancer effect. DLS, FTIR, XPS and TEM were used in the characterization phase of nanoparticles. While DLS and TEM provide information about dimensional analysis, FTIR and XPS were performed to verify the conjugations. Cytotoxicity, apoptosis, fluorescence imaging and incorporation studies of the molecule design created for theranostic purposes in A549 lung carcinoma and BEAS-2B normal bronchial epithelial cells were examined in vitro. As a result of these studies, it was determined that the synthesized molecule design has more involvement, toxic and apoptotic effects on A549 lung carcinoma cells. In this study, the therapeutic efficacy of the synthesized niosomal molecule design on the target cell and its potential to be used in cancer treatment were revealed and it is thought that it will contribute to the field of biotechnology.Öğe Preparation and in vitro investigation of prostate-specific membrane antigen targeted lycopene loaded niosomes on prostate cancer cells(Elsevier, 2023) Kusdemir, Bekir Cem; Guldu, Ozge Kozgus; Kilcar, Ayfer Yurt; Medine, Emin IlkerIn this study, it's aimed to develop prostate-specific membrane antigen (PSMA) targeted niosomes with a multifunctional theranostic approach.With this aim, PSMA-targeted niosomes were synthesized by a thin-film hydration method followed by bath sonication. Drug-loaded niosomes (Lyc-ICG-Nio) were coated with DSPE-PEG-COOH (Lyc-ICG-Nio-PEG) and subsequently anti-PSMA antibody conjugated to niosomes (Lyc-ICG-Nio-PSMA) with amide bond formation.Dynamic light scattering (DLS) analysis showed that the hydrodynamic diameter of Lyc-ICG-Nio-PSMA was approximately 285 nm and it was found with transmission electron microscopy (TEM) that the niosome formulation was spherical. Encapsulation efficiency was 45% and %65 upon dual encapsulation of ICG and lycopene. The results of fourier-transform infrared spectroscopy (FTIR) and X-ray photoelectron spectroscopy (XPS) demonstrated that PEG coating and antibody coupling were successfully done.In vitro studies showed that cell viability decreased when lycopene was entrapped into niosomes applied while the total apoptotic cell population rose slightly. When Lyc-ICG-Nio-PSMA was applied to cells, decreased cell viability and enhanced apoptotic effect were seen compared to those for Lyc-ICG-Nio.In conclusion, it was demonstrated that targeted niosomes displayed improved cellular association and decreased cell viability on PSMA + cells.Öğe A promising radiolabeled drug delivery system for methotrexate: synthesis and in vitro evaluation of Tc-99m labeled drug loaded uniform mesoporous silica nanoparticles(Springer, 2021) Ichedef, Cigdem; Aydin, Burcu; Hamurisci, Selin Irdel; Teksoz, Serap; Medine, Emin IlkerIn present study, we describe a promising radiolabeled drug delivery system for Methotrexate (MTX), an anticancer drug used in the treatment of breast cancer. Uniform and re-dispersible MSN were synthesized with a particle size of as 42.55 +/- 1.45 nm. Then, MTX was loaded into the surface modified MSN with DTPA over 95% loading capacity. Subsequently, MTX loaded MSN carrier system was radiolabeled with Tc-99 m (Tc-99m-MTX-MSN) with 92.20 +/- 0.8% radiolabeling yield. Furthermore, in vitro evaluation on estrogen positive (ER +) MCF7 and estrogen negative (ER-) A549 cells lines were performed for determining apoptotic and cytotoxic effects of MTX-MSN, and incorporation behavior of Tc-99m-MTX-MSN. Drug loaded MSN particles were exhibit higher uptake in MCF7 cells than A549 cells.Öğe Radioiodination of cyclin dependent kinase inhibitor Olomoucine loaded Fe@ Au nanoparticle and evaluation of the therapeutic efficacy on cancerous cells(Walter De Gruyter Gmbh, 2017) Takan, Gokhan; Guldu, Ozge Kozgus; Medine, Emin IlkerMagnetic nanoparticles have promising biomedical applications such as drug delivery, novel therapeutics and diagnostic imaging. Magnetic drug delivery combination works on the delivery of magnetic nanoparticles loaded with drug to the target tissue by means of an external magnetic field. Gold coated iron oxide (Fe@ Au) nanoparticles can provide useful surface chemistry and biological reactivity. Covalent conjugation to the Fe@ Au nanoparticles through cleavable linkages can be used to deliver drugs to tumor cells, then the drug can be released by an external. In this paper, purine based cyclin dependent kinases (CDKs) inhibitor Olomoucine (Olo) [2-(Hydroxyethylamino)-6-benzylamino-9-methylpurine] was loaded on gold coated iron oxide (Fe@ Au) nanoparticles and radiolabeled with I-131 to combine magnetic targeted drug delivery and radiotherapy. Fe@ Au nanoparticles were synthesized by microemulsion method. The characterization of nanoparticles was examined by TEM, VSM and XRD. Amine activation was utilized by cysteamine hydrochloride and then CDI was used for conjugation of Olomoucine. Antiproliferative effect and cytotoxicity of Olomoucine loaded Fe@ Au nanoparticles (Fe@ Au-Olo) were investigated on MCF7 and A549 cell lines. Proliferation rate was decreased while uptake of Fe@ Au-Olo on both cell lines was high in comparison with Olomoucine. Also, enhanced incorporation ratio was observed under external magnetic field.Öğe Radioiodination of Pimonidazole as a Novel Theranostic Hypoxia Probe(Bentham Science Publ Ltd, 2021) Inci, Ilknur Demir; Tekin, Volkan; Kilcar, Ayfer Yurt; Guldu, Ozge Kozgus; Medine, Emin Ilker; Karatay, Kadriye Busra; Dervis, EmineBackground: Tumors are defined as abnormal tissue masses, and one of the most important factors leading to the growth of these abnormal tissue masses is Vascular Endothelial Growth Factor, which stimulates angiogenesis by releasing cells under hypoxic conditions. Hypoxia has a vital role in cancer therapy, thus it is important to monitor hypoxia. The hypoxia marker Pimonidazole (PIM) is a candidate biomarker of cancer aggressiveness. Objective: The study aimed to perform radioiodination of PIM with Iodine-131 (I-131) to join a theranostic approach. For this purpose, PIM was derived as PIM-TOS to be able to be radioiodinated. Methods: PIM was derived via a tosylation reaction. Derivatization product (PIM-TOS) was radioiodinated by using iodogen method and was analyzed by High-Performance Liquid Chromatography and Liquid chromatography-mass spectrometry. Thin layer radiochromatography was utilized for its quality control studies. Results: PIM was derived successfully after the tosylation reaction. The radioiodination yield of PIM-TOS was over 85%. Conclusion: In the current study, radioiodination potential of PIM with I-13(1), as a potential theranostic hypoxia agent was investigated. Further experimental studies should be performed for developing a novel hypoxia probe including theranostics approaches.Öğe Synthesis and characterization of folic acid-chitosan nanoparticles loaded with thymoquinone to target ovarian cancer cells(Springer, 2020) Ince, Iskender; Yildirim, Yeliz; Guler, Gunnur; Medine, Emin Ilker; Ballica, Gulsah; Kusdemir, Bekir Cem; Goker, ErdemThe aim of the present research was to formulate and characterize radioiodinated folic acid-chitosan conjugated thymoquinone nanoparticles (FATQCSNPs) and to increase targeting ability on ovarian cancer cell. the dose of drug-loading into the FATQCSNPs and the amount of folic acid on the FATQCSNPs surface were determined as a 20.0 +/- 1% and 46.0 +/- 0.5%, respectively. Cell viabilities (%) determined on SKOV-3 and Caco-2 cells for 48 h. TQ, TQCS and FATQCS were very cytotoxic with lower IC50 values on both cell lines. At specific-activity-dependent incorporation study, the incorporation efficiencies of I-131-FATQCSNPs was higher than that of I-131-TQ on SKOV3 cell lines.
