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Öğe 99mTc-labeled, tofacitinib citrate encapsulated chitosan microspheres loaded in situ gel formulations for intra-articular treatment of rheumatoid arthritis(Wiley, 2024) Karpuz, Merve; Aydin, Husniye Hande; Ozgenc, Emre; Erel-Akbaba, Gulsah; Atlihan-Gundogdu, Evren; Senyigit, ZeynepInflammatory diseases including rheumatoid arthritis are major health problems. Although different techniques and drugs are clinically available for the diagnosis and therapy of the disease, novel approaches regarding radiolabeled drug delivery systems are researched. Hence, in the present study, it was aimed to design, prepare, and characterize (99)mTc-radiolabeled and tofacitinib citrate-encapsulated microsphere loaded poloxamer in situ gel formulations for the intra-articular treatment. Among nine different microsphere formulations, MS/TOFA-9 was chosen as the most proper one due to particle size, high encapsulation efficiency, and in vitro drug release behavior. Poloxamer 338 at a concentration of 15% was used to prepare in situ gel formulations. For intra-articular administration, microspheres were dispersed in an in situ gel containing 15% Poloxamer 338 and characterized in terms of gelation temperature, viscosity, rheological, mechanical, and spreadability properties. After the determination of the safe dose for MS/TOFA-9 and PLX-MS/TOFA-9 as 40 mu L/mL in the cell culture study performed on healthy cells, the high anti-inflammatory effects were due to significant cellular inhibition of fibroblasts. In the radiolabeling studies with (99)mTc, the optimum radiolabeling condition was determined as 200 ppm SnCl2 and 0.5 mg ascorbic acid, and both (99)mTc-MS/TOFA-9 and (99)mTc-PLX-MS/TOFA-9 exhibited high cellular binding capacity. In conclusion, although further in vivo experiments are required, PLX-MS/TOFA-9 was found to be a promising agent for intra-articular injection in rheumatoid arthritis.Öğe Applying Quality by Design Principles in the Development and Preparation of a New Radiopharmaceutical: Technetium-99m-Imatinib Mesylate(Amer Chemical Soc, 2020) Gundogdu, Evren; Demir, Emine Selin; Ozgenc, Emre; Yegen, Gizem; Aksu, BuketThe clinical impact and accessibility of Tc-99m tracers for cancer diagnosis would be greatly enhanced by the availability of a new, simple, and easy labeling process and radiopharmaceuticals. in this study, Technetium-99m-imatinib mesylate ([Tc-99m]TcIMT) was developed and prepared as a new radiopharmaceutical for breast cancer diagnosis. the effect of critical process parameters on the product quality and stability of [Tc-99m]TcIMT was investigated using the quality by design concept of the ICH Q8 (Pharmaceutical Development) guideline. [Tc-99m]TcIMT was subjected to in vitro cell binding studies to determine healthy and cancer cell affinity using HaCaT and MCF-7 cells, respectively. the optimal radiolabeling procedure with 1 mg of IMT, 500 mu g of stannous chloride, 0.1 mg of ascorbic acid, and (1m)Ci Tc-99m radioactivity was obtained for [Tc-99m]TcIMT. the pH of the reaction mixture was adjusted to 10 and allowed to react for 15 min at room temperature. the radiochemical purity of [Tc-99m]TcIMT was found to be higher than 90% at room temperature up to 6 h. Chromatography analysis revealed >85% [Tc-99m]Tc1MT complex formation with promising stability in saline, cell medium, and serum up to 6 h. the radiolabeled complex showed a higher cell-binding ratio to MCF-7 cells (88.90% +/- 3.12) than HaCaT cells (45.64 +/- 4.72) when compared to Tc-99m. Our findings show that the developed preparation method for [Tc-99m]TcIMT falls well within the proven acceptable ranges. Applying quality by design (QbD) principles is feasible and worthwhile for the preparation of [Tc-99m]TcIMT. in conclusion, radiochemical purity, stability, and in vitro cell binding evaluation of the [Tc-99m]TCIMT complex indicate that the agent can be utilized for imaging of breast cancer cells.Öğe Development and Evaluation of Liquid and Solid Lipid Based Drug Delivery Systems Containing Technetium-99m-Radiolabeled Alendronate Sodium(Bentham Science Publ Ltd, 2018) Gundogdu, Evren; Ekinci, Meliha; Ozgenc, Emre; Ozdemir, Derya, I; Asikoglu, MakbuleObjective: The purpose of this study was to develop lipid-water based drug delivery system of Alendronate Sodium (ALD) in liquid and solid form obtained by using spray drying method and compare these two forms with radioactive cell culture studies. Methods: This study included the development of liquid and solid form obtained by spray drying method, radiolabelling of ALD with Tc-99m, preparation of formulations containing Tc-99m-ALD and evaluation of their permeability with Caco-2 cell. The liquid formulations have been developed by using various surfactants, co-surfactants, oil and water phases. Physicochemical characterizations like droplet size, polydispersity index (PDI) and zeta potential measurements and short term stability studies were investigated. Results: According to the measurement results, two oil in water formulations (F1-L and F2-L) were selected and spray dried with Buchi mini spray dryer apparatus to provide solid formulations (F -S and F2-S). ALD was labeled with Tc-99m and added to formulations. The effect of experimental conditions on radiolabeling efficiency of ALD and stability of all formulations containing Tc-99m-ALD were investigated through Radio Thin Layer Chromatography (RTLC). It was observed that the labeling efficiency of ALD was greater than 90% and all formulations were found to be stable up to 6 h at room temperature. Permeability of radiolabeled ALD from all formulations was performed by using Caco-2 cells. According to the cell culture studies, permeability from spray dried formulations of ALD was found higher than liquid formulations. Conclusion: As a conclusion, spray dried formulations could be a promising drug delivery system for enhancing the permeability of ALD. Furthermore, this study is a good example of the use of radio-labeled compounds in drug development.Öğe Development and radiolabeling of lipid nanoparticles with [Tc-99m]Tc-HMPAO: Characterization, stability, cytotoxicity and cell binding studies(Marmara Univ, 2022) Atlihan-Gundogdu, Evren; Ekinci, Meliha; Ozgenc, Emre; Demir, Emine Selin; Ilem-Ozdemir, DeryaIn this study, we aimed to develop new lipid based nanoparticles (LPNs) and radiolabeled LPNs with [Tc-99m]Tc-HMPAO to investigate its cell binding capacity comparatively with [Tc-99m]Tc-HMPAO on different cancer cells. According to obtained results, LPNs with zeta potential of -27.4 +/- 0.95 mV, particle size of 93.5 +/- 1.17 nm, and polydispersity index of 0.35 +/- 0.04 were successfully developed. The optimum radiolabeling efficiency was found to be above 90% at 15-min of incubation time. The cell binding capacity of [Tc-99m]Tc-HMPAO-LPNs was found to be higher than [Tc-99m]Tc-HIYIPAO in cancer cell lines. The results demonstrated that [Tc-99m]Tc-HMPAO-LPNs may be a promising agent for cancer diagnosis alternatively to [Tc-99m]Tc-HMPAO.Öğe Development of freeze-dry kits containing imatinib and different chelating agents: characterization, stability and cytotoxicity studies(Marmara Univ, 2022) Ozgenc, Emre; Gundogdu, EvrenThe current study aims to develop new freeze-dry kits containing Imatinib and different chelating agents for breast cancer treatment and diagnosis as theranostics. Four formulations (Kit-1, Kit-2, Kit-3, and Kit-4) were prepared, and the characterization of formulations was assessed utilizing particle size, polydispersity index, zeta potential, fourier transform infra-red analysis, ultraviolet spectrum analysis, differential calorimetry, and thermogravimetric analysis. They were also evaluated for stability at different storage conditions and cytotoxicity effect on fibroblast NIH-3T3 cells. The particle size, polydispersity index, and zeta potential of developed formulations were found to be between 6953.6 +/- 131.6 and 5888.3 +/- 131.6 nm, 0.481 +/- 0.24 and 0.319 +/- 0.18, -594.5 +/- 59.6 and -477.3 +/- 25.32 mV, respectively. Fourier transform infra-red analysis, ultraviolet spectrum, differential calorimetry, and thermogravimetric analysis have proven that IMT and chelating agents formed complexes in kit formulations. Also, they exhibited stable facility and above 90% of cell viability on fibroblast NIH-3T3 cells. By the result of our study, kit formulations can be a favorable drug delivery system in the treatment and diagnosis of breast cancer with a non-toxic effect on healthy cells.Öğe The effect of radiolabeled nanostructured lipid carrier systems containing imatinib mesylate on NIH-3T3 and CRL-1739 cells(Taylor & Francis Ltd, 2020) Gundogdu, Evren Atlihan; Demir, Emine Selin; Ekinci, Meliha; Ozgenc, Emre; Ilem Ozdemir, Derya; Senyigit, Zeynep; Asikoglu, MakbuleThe aim of current study is to develop new nanostructured lipid carrier systems (NLCSs) containing imatinib mesylate (IMT) and evaluate their targeting efficiency on NIH-3T3 as fibroblast cells and CRL-1739 as gastric adenocarcinoma cells with radiolabeled formulations. Three formulations (F1-IMT, F2-IMT and F3-IMT) were prepared and radiolabeled with 1 mCi/0.1 mL of [Tc-99m]Tc. The effect of reducing and antioxidant agents on radiolabeling process was evaluated and radiochemical purity of formulations was performed by radio thin-layer radiochromatography (RTLC). The results demonstrated that the radiochemical purity was found to be above 90% for [Tc-99m]Tc-F1-IMT and [Tc-99m]Tc-F2-IMT, while radiochemical purity of [Tc-99m]Tc-F3-IMT was found to be 85.61 +/- 2.24%. Also, [Tc-99m]Tc-F1-IMT and [Tc-99m]Tc-F2-IMT have better stability in cell medium and saline than [Tc-99m]Tc-F3-IMT. Targeting efficiency of [Tc-99m]Tc-F1-IMT and [Tc-99m]Tc-F2-IMT comparatively evaluated by cell binding studies with [Tc-99m]NaTcO4 on NIH-3T3 and CRL-1739 cells. The cell binding capacity and targeting/non-targeting cell uptake ratio of these two formulations was found to be higher than [Tc-99m]NaTcO4 in CRL-1739. It is thought that the knowledge achieved in this study would contribute to using [Tc-99m]Tc-F1-IMT and [Tc-99m]Tc F2-IMT as an diagnosis and treatment agents.Öğe Evaluation of F-18 FDG radiopharmaceuticals through Molecular Docking and radiation effects(Pergamon-Elsevier Science Ltd, 2023) Kilicoglu, Ozge; Sepay, Nayim; Ozgenc, Emre; Gundogdu, Evren; Kara, Umit; Alomairy, Sultan; Al-Buriahi, M. S.Fluorodeoxyglucose (FDG), marked with the most used Positron Emission Tomography (PET) radiopharmaceutical Fluorine-18 (F-18), is a glucose analog and is taken to living cells through membrane glucose carriers. F18 FDG involvement in tissue is proportional to glucose use. In many cancers, there is increased glucose use due to increased gluten expression and hexokinase activity. F-18 FDG PET is a proven method for diagnosis, staging, re-staging, and evaluation of treatment response in oncology. The purpose of this study is to find the effect of ionizing radiation on proteins in the mechanism of action of FDG and determine to Molecular mechanisms of F18 FDG accumulation in metabolism. In the study, two different models were used together, the first method, the study was Molecular Docking method for modeling molecules deconstructed and the structure of FDG was energy minimized by utilizing the density functional theory, and the B3LYP functional was used with 6-311G basis set. The second method was the Monte Carlo method for modeling ionizing radiation interactive with the potential routes of FDG metabolism within the cell. It was determined that the Gibbs free energy (Delta G) change was compatible with the ionizing radiation factors for binding of FDG to the aphthous regions of Glucose-6-phosphate isomerase (G1), hexokinase (G2), and glucose transporter-1 (G3) were selected. In this study, the strong binding of FDG to protein influences the effect of radiation on the active site of enzymes. The G1 and G3 shown in the study interacted with only one charged amino acid FDG, and the absence of an aromatic residue around it can be considered among the results of this study as the cause of the low protective effect against ionizing radiation.Öğe An Innovative Formulation Based on Nanostructured Lipid Carriers for Imatinib Delivery: Pre-Formulation, Cellular Uptake and Cytotoxicity Studies(Mdpi, 2022) Gundogdu, Evren; Demir, Emine-Selin; Ekinci, Meliha; Ozgenc, Emre; Ilem-Ozdemir, Derya; Senyigit, Zeynep; Gonzalez-Alvarez, IsabelImatinib (IMT) is a tyrosine kinase enzyme inhibitor and extensively used for the treatment of gastrointestinal stromal tumors (GISTs). A nanostructured lipid carrier system (NLCS) containing IMT was developed by using emulsification-sonication methods. The characterization of the developed formulation was performed in terms of its particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, loading capacity, sterility, syringeability, stability, in vitro release kinetics with mathematical models, cellular uptake studies with flow cytometry, fluorescence microscopy and cytotoxicity for CRL-1739 cells. The particle size, PDI, loading capacity and zeta potential of selected NLCS (F16-IMT) were found to be 96.63 +/- 1.87 nm, 0.27 +/- 0.15, 96.49 +/- 1.46% and -32.7 +/- 2.48 mV, respectively. F16-IMT was found to be stable, thermodynamic, sterile and syringeable through an 18 gauze needle. The formulation revealed a Korsmeyer-Peppas drug release model of 53% at 8 h, above 90% of cell viability, 23.61 mu M of IC50 and induction of apoptosis in CRL-1739 cell lines. In the future, F16-IMT can be employed to treat GISTs. A small amount of IMT loaded into the NLCSs will be better than IMT alone for therapy for GISTs. Consequently, F16-IMT could prove to be useful for effective GIST treatment.Öğe Microemulsion Drug Delivery Systems for Radiopharmacy Studies(Suamthi Publications, 2016) Ozgenc, Emre; Ekinci, Meliha; Ozdemir, DeryaIlem; Gundogdu, Evren; Asikoglu, MakbuleMicroemulsions have been used increasingly for last year's because of ideal properties like favorable drug delivery, ease of preparation and physical stability. They have been improved the solubility and efficacy of the drug and reduce the side effects. Use of radiolabeled microemulsions plays an alternative role in drug delivery systems by investigating the formation, stability and application of microemulsions in radiopharmacy. Gama scintigraphic method is well recognized for developing and detecting the biodistribution of newly developed drugs or formulation. This review will focus on how radionuclides are able to play role with characterization studies of microemulsion drug delivery systems.Öğe Pre-clinic study of radiopharmaceutical for Covid-19 inactivation: Dose distribution with Monte Carlo Simulation(Pergamon-Elsevier Science Ltd, 2022) Kilicoglu, Ozge; Kara, Umit; Ozgenc, Emre; Gundogdu, EvrenMonte Carlo simulation method and Nuclear Medicine MIRD method were used to evaluate the effect of ra-diopharmaceuticals on Covid-19 disease. The mean absorbed organ dose in the target organ and gamma radi-ation emitter attenuation properties such as linear attenuation coefficients, energy absorption build-up factors (EABF), exposure build-up factors (EBF), and relative dose distributions (RDD) were examined. The results showed that radiopharmaceuticals containing gamma radiation emitters which are densely ionizing charged particles induced membrane damage and produced protein damage.Öğe Protein and Gene Delivery Systems for Neurodegenerative Disorders: Where Do We Stand Today?(Mdpi, 2022) Siafaka, Panoraia, I; Okur, Mehmet Evren; Erim, Pelin Dilsiz; Caglar, Emre Sefik; Ozgenc, Emre; Gundogdu, Evren; Koprulu, Rabia Edibe ParlarIt has been estimated that every year, millions of people are affected by neurodegenerative disorders, which complicate their lives and their caregivers' lives. To date, there has not been an approved pharmacological approach to provide the complete treatment of neurodegenerative disorders. The only available drugs may only relieve the symptoms or slow down the progression of the disease. The absence of any treatment is quite rational given that neurodegeneration occurs by the progressive loss of the function or structure of the nerve cells of the brain or the peripheral nervous system, which eventually leads to their death either by apoptosis or necrotic cell death. According to a recent study, even though adult brain cells are injured, they can revert to an embryonic state, which may help to restore their function. These interesting findings might open a new path for the development of more efficient therapeutic strategies to combat devastating neurodegenerative disorders. Gene and protein therapies have emerged as a rapidly growing field for various disorders, especially neurodegenerative diseases. Despite these promising therapies, the complete treatment of neurodegenerative disorders has not yet been achieved. Therefore, the aim of this review is to address the most up-to-date data for neurodegenerative diseases, but most importantly, to summarize the available delivery systems incorporating proteins, peptides, and genes that can potentially target such diseases and pass into the blood-brain barrier. The authors highlight the advancements, at present, on delivery based on the carrier, i.e., lipid, polymeric, and inorganic, as well as the recent studies on radiopharmaceutical theranostics.Öğe Radiolabeled Trastuzumab Solid Lipid Nanoparticles for Breast Cancer Cell: in Vitro and in Vivo Studies(Amer Chemical Soc, 2022) Ozgenc, Emre; Karpuz, Merve; Arzuk, Ege; Gonzalez-Alvarez, Marta; Sanz, Marival Bermejo; Gundogdu, Evren; Gonzalez-Alvarez, IsabelRadiolabeled trastuzumab (TRZ) loaded solid lipid nano-particles (SLNs) were prepared by high shear homogenization and sonication techniques. The apoptosis mechanism of TRZ-SLNs was studied only with the MCF-7 cell line, while the cytotoxicity and cell binding capacity were investigated using breast cancer cells (MCF-7 and MDA-MB-231) and the human keratinocyte cell line (HaCaT). The particle sizes of TRZ-SLNs were found to be below 100 nm, and they possessed a negative charge. The high radiolabeling efficiency and good radiolabeling stability in saline and a cell culture medium were obtained in the results of radiolabeling studies. According to the in vitro studies, TRZ-SLNs were found to be biocompatible, and they effectively induced apoptosis in MCF-7 cells. After the parenteral injection of TRZ-SLNs into rats, a sustained release profile in blood circulation was achieved compared with free drug solution by the evaluation of pharmacokinetic parameters. As a conclusion, the study reveals that Technetium-99m (Tc-99m radiolabeled) TRZ loaded SLN formulations could be promising theranostic agents based on their characterization profiles, in vitro cellular uptake and apoptosis induction capacity, and in vivo pharmacokinetic profiles.Öğe Radiolabeling, Quality Control, and Cell Binding Studies of New 99mTc-Labeled Bisphosphonates: 99mTc-Ibandronate Sodium(Galenos Publ House, 2023) Ekinci, Meliha; Ozdemir, Derya Ilem; Ozgenc, Emre; Gundogdu, Evren; Asikoglu, MakbuleObjectives: Early detection of bone cancer is critical for treating symptoms, minimizing pain, and increasing overall quality of life. It is critical to develop novel radiopharmaceuticals with high labeling efficiency and stability for the diagnosis of bone cancer. This research aims to design a novel radiopharmaceutical that may be used to diagnose bone cancer.Materials and Methods: In this study, ibandronate sodium (IBD), a bisphosphonate analog, was radiolabeled with technetium-99m [99mTc] and quality control tests on the newly developed radiopharmaceutical ([99mTc]Tc-IBD) were performed using radioactive thin layer chromatography. After that, the incorporation of [99mTc]Tc-IBD into hydroxyapatite (HA) crystals and a human bone osteosarcoma cell line (U2OS) was tested.Results: According to the results obtained, optimal radiolabeling procedure was obtained for [99mTc]Tc-IBD with 200 mu g.mL-1 IBD, 20 mu g stannous chloride, and 99mTc with 37 MBq radioactivity. The reaction mixture was adjusted to pH 5.5 and incubated at room temperature for 15 min. The radiochemical purity of [99mTc]Tc-IBD was found to be greater than 95% at room temperature for up to 6 h. Additionally, chromatography analysis showed >95% [99mTc]Tc-IBD complex formation with promising stability for up to 24 h in saline and up to 2 h in cell medium. The percentage binding of IBD to HA was 83.70 +/- 3.67 and the logP of [99mTc]Tc-IBD was-1.1014. The radiolabeled complex exhibited a higher rate of cell incorporation to U2OS cells compared to Reduced/Hydrolyzed 99mTcO4-.Conclusion: The newly produced radiopharmaceutical is very promising according to the results of in vitro cell culture, HA binding, and quality studies, and will be a step forward for further studies in nuclear medicine for bone cancer diagnostics.Öğe Recent developments in cancer therapy and diagnosis(Springernature, 2020) Atlihan-Gundogdu, Evren; Ilem-Ozdemir, Derya; Ekinci, Meliha; Ozgenc, Emre; Demir, Emine Selin; Sanchez-Dengra, Barbara; Gonzalez-Alvarez, IsabelBackground The cancer is serious health problem and leading cause of death in the world. Area covered There have intensively studied for diagnosis and therapy of this disease and these studies provided important insights into their mechanism of action and therapeutic/diagnostic effects. The accurence rates of cancer has dramatic increase, particularly in the developed countries. Although there are many different strategies about diagnosis and treatment for cancer, more effective new approaches are needed. Expert opinion In this review, we summarize recent developments on cancer diagnosis, radiopharmaceuticals in cancer diagnosis, nanoparticulate systems in cancer diagnosis, T cells in cancer diagnosis, cancer therapy and pharmacokinetic of anticancer drugs. We thought that while there are some current limitations such as clinical studies, ranging from diagnosis to theraphy, future improvements in cancer diagnosis and treatment will meet the most relevant issues required for the eventual approval of nano-drugs, radiopharmaceuticals, T cells in clinical practice.Öğe Tc-99m-Labeled, Colistin Encapsulated, Theranostic Liposomes for Pseudomonas aeruginosa Infection(Springer, 2023) Karpuz, Merve; Temel, Aybala; Ozgenc, Emre; Tekintas, Yamac; Erel-Akbaba, Gulsah; Senyigit, Zeynep; Atlihan-Gundogdu, EvrenInfectious diseases are still the major issue not only due to antibiotic resistance but also causing deaths if not diagnosed at early-stages. Different approaches including nanosized drug delivery systems and theranostics are researched to overcome antibiotic resistance, decrease the side effects of antibiotics, improve the treatment response, and early diagnose. Therefore, in the present study, nanosized, radiolabeled with Tc-99m, colistin encapsulated, neutral and cationic liposome formulations were prepared as the theranostic agent for Pseudomonas aeruginosa infections. Liposomes exhibited appropriate physicochemical properties thanks to their nano-particle size (between 173 and 217 nm), neutral zeta potential value (about - 6.5 and 2.8 mV), as well as encapsulation efficiency of about 75%. All liposome formulations were radiolabeled with over 90% efficiency, and the concentration of stannous chloride was found as 1 mg.mL(-1) to obtain maximum radiolabeling efficiency. In alamar blue analysis, neutral liposome formulations were found more biocompatible compared with the cationic formulations. Neutral colistin encapsulated liposomes were found to be more effective against P. aeruginosa strain according to their time-dependent antibacterial effect, in addition to their highest bacterial binding capacity. As conclusion, theranostic, nanosized, colistin encapsulated, neutral liposome formulations were found as promising agents for the imaging and treating of P. aeruginosa infections.
