Browsing by Author "Sakr T.M."

Now showing 1 - 15 of 15

Adaptation of hard gelatin capsules for oral delivery of aqueous radiopharmaceuticals
(Springer, 2019) Omar S.M.; Abdel-Rashid R.S.; AlAssaly M.K.; Sakr T.M.; Faculty of Pharmacy; Ahram Canadian University; Giza; Egypt; Department of Pharmaceutics and Industrial Pharmacy Faculty of Pharmacy; Helwan University; Ain Helwan; Cairo; 11795; Egypt; Ministry of Interior; Medical Services; Cairo; Egypt; Faculty of Pharmacy; October University of Modern Sciences and Arts; Cairo; Egypt; Radioactive Isotopes and Generators; Atomic Energy Authority; Cairo; Egypt
Purpose: Oral administration of Iodine?131 (I?131) solutions causes high risk of contamination for patients and dispensers. The objective of the study was to adapt hard gelatin capsules (HGCs) for filling with radiopharmaceutical solutions without deformation. Methods: Polystyrene (PS) internally lining films with different thicknesses were used to protect HGCs. The insulated HGCs were evaluated for their physicochemical characteristics and rupturing time in different dissolution media. HGCs internally lined with PS were examined for withstand loading with different volumes and radioactivities of I?131 solutions. Radioactivity release was studied in deionized water and acidic media. Quality control of released I?131 was inspected for radiochemical purities. Results: There was a directly proportion between PS lining thickness and stability of HGCs after filling with 500�?l aqueous methylene blue solution. HGCs internally lined with PS 100�?m thickness withstand deformation for ? two months; however showed fast in-vitro rupturing time in different dissolution media. Internally lined HGCs loaded with different volumes and radioactivities of I?131 solutions resisted for one week without radioactive leakage. Yet, revealed complete release of I?131 after 20�min in dissolution media with great radiochemical purity. Conclusion: The study promises safely I?131 aqueous solution delivery via adapted HGCs. [Figure not available: see fulltext.]. � 2019, Springer Nature Switzerland AG.
Brain targeted rivastigmine mucoadhesive thermosensitive In situ gel: Optimization, in vitro evaluation, radiolabeling, in vivo pharmacokinetics and biodistribution
(Editions de Sante, 2018) Abouhussein D.M.N.; Khattab A.; Bayoumi N.A.; Mahmoud A.F.; Sakr T.M.; Pharmaceutics Department; National Organization for Drug Control and Research (NODCAR); Giza; Egypt; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Pharmaceutics Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt
The purpose of our investigation was to promote the bioavailability and the brain delivery of rivastigmine tartarate (RV) through optimization of mucoadhesive thermosensitive in situ gel via intranasal (IN) route. The mucoadhesive in situ gels were developed using pluronic F127 (PF127) as thermogelling agent and different mucoadhesive polymers. A full factorial design was implemented to study the influence of three factors; pluronic type at two levels (PF127, PF127/PF68), mucoadhesive polymer type at four levels (HPMC, Chitosan, Carbopol 934 and NaCMC) and mucoadhesive polymer concentration at two levels (0.5 and 1%w/v). The studied responses were sol-gel temperature, consistency, gel strength, adhesion work and T50% of drug release. In vivo pharmacokinetic and biodistribution studies of the selected formula were investigated using radiolabeling approach using normal albino mice. The optimal RV in situ gel (PF127 and 1% Carbopol 934) showed significant transnasal permeation (84%) which was reflected in better distribution to the brain (0.54 %ID/g), when compared to RV IN solution (0.16 %ID/g) and RV IV intravenous solution (0.15 %ID/g). In conclusion, the investigated results showed the potential use of mucoadhesive in situ gel as a promising system for brain targeting of RV via the transnasal delivery system. � 2017 Elsevier B.V.
Design, synthesis and biological evaluation of some novel sulfonamide derivatives as apoptosis inducers
(Elsevier Masson SAS, 2017) Mohamed K.O.; Nissan Y.M.; El-Malah A.A.; Ahmed W.A.; Ibrahim D.M.; Sakr T.M.; Motaleb M.A.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St.; Cairo; 11562; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt; National Cancer Institute; Cancer Biology Department; Cairo University; Egypt; Faculty of Science; Cairo University; Cairo; Egypt; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt
Several novel thiazolidinone and fused thiazolidinone derivatives bearing benzenesulfonamide moiety were synthesized and confirmed via spectral and elemental analyses. The newly synthesized compounds were evaluated for their cytotoxic activity on colorectal cancer cell line (Caco-2). All the synthesized compounds showed better activity than the reference standards (Doxorubicin and 5-FU). Investigation of the apoptotic activity of the most active compounds revealed that compounds 3a, 5a, 5c and 6c activate both caspase-3 and Fas-ligand in Caco-2�cell line. Compound 3a was the most active compound with caspase-3 concentration of 0.43�nmol/mL and Fas-ligand concentration of 775.2�pg/mL in treated Caco-2�cells. Compound 3a was radiolabeled with 99mTc and its biodistribution pattern was evaluated in�vivo using normal Swiss Albino mice. 99mTc-compound 3a complex didn't exhibit any accumulation in any body organs except for its accumulation in the colon; target organ; where it showed 8.97��1.35 %ID/g at 15min p. i. that elevated till 16.02��2.43 %ID/g at 120min p. i. � 2017 Elsevier Masson SAS
I-131 doping of silver nanoparticles platform for tumor theranosis guided drug delivery
(Elsevier B.V., 2018) Sakr T.M.; Khowessah O.M.; Motaleb M.A.; Abd El-Bary A.; El-Kolaly M.T.; Swidan M.M.; Radioactive Isotopes and Generator Department; Hot Labs Center; Egyptian Atomic Energy Authority; PO13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Modern Sciences and Arts University; 6th October City; Egypt; Pharmaceutics and Industrial Pharmacy Department; Faculty of Pharmacy; Cairo University; PO11562; Cairo; Egypt; Labeled Compounds Department; Hot Labs Center; Egyptian Atomic Energy Authority; PO13759; Cairo; Egypt
Nanotechnology may be applied in medicine where the utilization of nanoparticles (?100 nm) for the delivery and targeting of theranostic agents is at the forefront of projects in cancer nano-science. This study points a novel one step synthesis approach to build up polyethylene glycol capped silver nanoparticles doped with I-131 radionuclide (131I-doped Ag-PEG NPs). The formula was prepared with average hydrodynamic size 21 nm, zeta potential � 25 mV, radiolabeling yield 98 � 0.76%, and showed good in-vitro stability in saline and mice serum. The in-vitro cytotoxicity study of cold Ag-PEG NPs formula as a drug carrier vehicle showed no cytotoxic effect on normal cells (WI-38 cells) at a concentration below 3 ?L/104 cells. The in-vivo biodistribution pattern of 131I-doped Ag-PEG NPs in solid tumor bearing mice showed high radioactivity accumulation in tumor tissues with maximum uptake of 35.43 � 1.12 and 63.8 � 1.3% ID/g at 60 and 15 min post intravenous (I.V.) and intratumoral injection (I.T.), respectively. Great potential of T/NT ratios were obtained throughout the experimental time points with maximum ratios 45.23 � 0.65 and 92.46 � 1.02 at 60 and 15 min post I.V. and I.T. injection, respectively. Thus, 131I-doped Ag-PEG NPs formulation could be displayed as a great potential tumor nano-sized theranostic probe. � 2018 Elsevier B.V.
In silico-based repositioning of phosphinothricin as a novel technetium-99m imaging probe with potential anti-cancer activity
(MDPI AG, 2018) Sakr T.M.; Khedr M.A.; Rashed H.M.; Mohamed M.E.; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; Cairo; 13759; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; 12111; Egypt; Department of Pharmaceutical Chemistry; Faculty of Pharmacy; Helwan University; Ein Helwan; Cairo; 11795; Egypt; College of Clinical Pharmacy; King Faisal University; Al-Hasaa; 31982; Saudi Arabia; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; Cairo; 13759; Egypt; Department of Pharmacognosy; Faculty of Pharmacy; University of Zagazig; Zagazig; 44519; Egypt
L-Phosphinothricin (glufosinate or 2-amino-4-((hydroxy(methyl) phosphinyl) butyric acid ammonium salt (AHPB)), which is a structural analog of glutamate, is a recognized herbicide that acts on weeds through inhibition of glutamine synthetase. Due to the structural similarity between phosphinothricin and some bisphosphonates (BPs), this study focuses on investigating the possibility of repurposing phosphinothricin as a bisphosphonate analogue, particularly in two medicine-related activities: image probing and as an anti-cancer drug. As BP is a competitive inhibitor of human farnesyl pyrophosphate synthase (HFPPS), in silico molecular docking and dynamic simulations studies were established to evaluate the binding and stability of phosphinothricin with HFPPS, while the results showed good binding and stability in the active site of the enzyme in relation to alendronate. For the purpose of inspecting bone-tissue accumulation of phosphinothricin, a technetium (99mTc)�phosphinothricin complex was developed and its stability and tissue distribution were scrutinized. The radioactive complex showed rapid, high and sustained uptake into bone tissues. Finally, the cytotoxic activity of phosphinothricin was tested against breast and lung cancer cells, with the results indicating cytotoxic activity in relation to alendronate. All the above results provide support for the use of phosphinothricin as a potential anti-cancer drug and of its technetium complex as an imaging probe. � 2018 by the authors.
Iron oxide nanoparticulate system as a cornerstone in the effective delivery of Tc-99m radionuclide: a potential molecular imaging probe for tumor diagnosis
(Springer, 2019) Swidan M.M.; Khowessah O.M.; El-Motaleb M.A.; El-Bary A.A.; El-Kolaly M.T.; Sakr T.M.; Labeled Compounds Department; Hot Labs Center; Egyptian Atomic Energy Authority; PO13759; Cairo; Egypt; Pharmaceutics and Industrial Pharmacy Department; Faculty of Pharmacy; Cairo University; PO11562; Cairo; Egypt; Radioactive Isotopes and Generator Department; Hot Labs Center; Egyptian Atomic Energy Authority; PO13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Modern Sciences and Arts University; 6th October City; Egypt
Background: The evolution of nanoparticles has gained prominence as platforms for developing diagnostic and/or therapeutic radiotracers. This study aims to develop a novel technique for fabricating a tumor diagnostic probe based on iron oxide nanoparticles excluding the utilization of chelating ligands. Methods: Tc-99m radionuclide was loaded into magnetic iron oxide nanoparticles platform (MIONPs) by sonication. 99mTc-encapsulated MIONPs were fully characterized concerning particles size, charge, radiochemical purity, encapsulation efficiency, in-vitro stability and cytotoxicity. These merits were biologically evaluated in normal and solid tumor bearing mice via different delivery approaches. Results: 99mTc-encapsulated MIONPs probe was synthesized with average particle size 24.08 7.9nm, hydrodynamic size 52nm, zeta potential -28mV, radiolabeling yield 96 0.83%, high in-vitro physiological stability, and appropriate cytotoxicity behavior. The in-vivo evaluation in solid tumor bearing mice revealed that the maximum tumor radioactivity accumulation (25.39 0.57, 36.40 0.59 and 72.61 0.82%ID/g) was accomplished at 60, 60 and 30min p.i. for intravenous, intravenous with physical magnet targeting and intratumoral delivery, respectively. The optimum T/NT ratios of 57.70, 65.00 and 87.48 were demonstrated at 60min post I.V., I.V. with physical magnet targeting and I.T. delivery, respectively. These chemical and biological characteristics of our prepared nano-probe demonstrate highly advanced merits over the previously reported chelator mediated radiolabeled nano-formulations which reported maximum tumor uptakes in the scope of 3.65 0.19 to 16.21 2.56%ID/g. Conclusion: Stabilized encapsulation of 99mTc radionuclide into MIONPs elucidates a novel strategy for developing an advanced nano-sized radiopharmaceutical for tumor diagnosis. [Figure not available: see fulltext.]. 2019, Springer Nature Switzerland AG.
Molecular modeling and preclinical evaluation of radioiodinated tenoxicam for inflammatory disease diagnosis
(Springer Netherlands, 2018) Sakr T.M.; Ibrahim I.T.; Abd-Alla W.H.; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; P.O. 13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; Labelled Compound Department; Hot Labs Center; Atomic Energy Authority; P.O. 13759; Cairo; Egypt; Department of Pharmaceutical Chemistry; Faculty of Pharmacy; Misr University for Science & Technology; P.O. 77; 6th of October; Egypt
Abstract: The aim of the presented study is to investigate a new promising radiopharmaceutical tracer able to visualize and differentiate inflammation versus infection in early stages. Radioiodinated tenoxicam (125I-tenoxicam) was prepared and its radiochemical yield and in vitro stability were assayed. The biodistribution studies were conducted on two different mice models: sterile inflammation and bacterial infection mice models. 125I-tenoxicam showed high T/NT accumulation in the inflammatory tissues revealing high selectivity to the inflammatory tissues in contrast to infection bearing mice. The docking study using CDOCKER protocol for tenoxicam and radioiodinated tenoxicam with COX enzymes was performed to confirm that radioiodinated tenoxicam still retaining COX enzymes selectivity. � 2018, Akad�miai Kiad�, Budapest, Hungary.
Nano-technology contributions towards the development of high performance radioisotope generators: The future promise to meet the continuing clinical demand
(Elsevier Ltd, 2017) Sakr T.M.; Nawar M.F.; Fasih T.W.; El-Bayoumy S.; Abd El-Rehim H.A.; Radioactive Isotopes and Generators Dept.; Hot Labs. Center; Atomic Energy Authority; Cairo; 13759; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; National Center for Radiation Research and Technology; Atomic Energy Authority; Cairo; Egypt
Nanostructured materials attracted considerable attention because of its high surface area to volume ratio resulting from their nano-scale dimensions. This class of sorbents is expected to have a potential impact on enhancement the efficacy of radioisotope generators for diagnostic and therapeutic applications in nuclear medicine. This review provides a summary on the importance of nanostructured materials as effective sorbents for the development of clinical-scale radioisotope generators and outlining the assessment of recent developments, key challenges and promising access to the near future. � 2017 Elsevier Ltd
Nano-titania: a novel purification and concentration adsorbent for 125I production for medical uses
(Springer Netherlands, 2017) Sakr T.M.; Fasih T.W.; Amin M.; Radioactive Isotopes and Generators Department; Hot Laboratories Centre; Atomic Energy Authority; Cairo; 13759; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt
Abstract: The presented work describes the efficient use of nano-crystalline titania (TiO2) to remove trace levels of cesium radio-contaminants (134Cs and 137Cs) in iodine-125 (125I) solution produced via neutron activation of natural 124Xe target. The adsorption parameters of TiO2 were investigated to attain the optimum purification and concentration conditions of 125I solution. The maximum sorption capacity of Cs and 125I were approximately 56 and 67�mg/g TiO2, respectively. The final 125I solution was of high radiochemical, radionuclidic and chemical purities, besides, it showed high radioactive concentration that confirming its suitability for nuclear medicine applications and 125I brachytherapy sources preparation. Graphical abstract: [Figure not available: see fulltext.]. � 2017, Akad�miai Kiad�, Budapest, Hungary.
Novel hydrazide-hydrazone and amide substituted coumarin derivatives: Synthesis, cytotoxicity screening, microarray, radiolabeling and in vivo pharmacokinetic studies
(Pharmacologyonline, 2018) Nasr T.; Bondock S.; Rashed H.M.; Fayad W.; Youns M.; Sakr T.M.; Department of Pharmaceutical Chemistry; Faculty of Pharmacy; Helwan University; Egypt; Department of Pharmaceutical Chemistry; Faculty of Pharmacy; Modern University for Technology and Information; Egypt; Department of Chemistry; Faculty of Science; Mansoura University; Mansoura; ET-35516; Egypt; Department of Chemistry; Faculty of Science; King Khalid University; Abha; 9004; Saudi Arabia; Labeled Compounds Department; Hot Labs Center; Egyptian Atomic Energy Authority; P.O. Code 13759; Cairo; Egypt; Drug Bioassay-Cell Culture Laboratory; Pharmacognosy Department; National Research Centre; Dokki; Giza 12622; Egypt; Department of Biochemistry and Molecularlar Biology; Faculty of Pharmacy; Helwan University; Egypt; Radioactive Isotopes and Generators Department; Hot Laboratories Centre; Atomic Energy Authority; P.O. Code 13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA)Giza; Egypt
The current work presents the synthesis and biological evaluation of new series of coumarin hydrazide-hydrazone derivatives that showed in vitro broad spectrum antitumor activities against resistant pancreatic carcinoma (Panc-1), hepatocellular carcinoma (HepG2) and leukemia (CCRF) cell lines using doxorubicin as reference standard. Bromocoumarin hydrazide-hydrazone derivative (BCHHD) 11b showed excellent anticancer activity against all tested cancer cell lines. Enzyme assays showed that BCHHD 11b induced apoptosis due to activation of caspases 3/7. Moreover, 11b inhibited GST and CYP3A4 in a dose dependent manner and the induced cell death could be attributed to metabolic inhibition. Moreover, 11b microarray analysis showed significant up- and down-regulation of many genes in the treated cells related to apoptosis, cell cycle, tumor growth and suppressor genes. All of the above presents BCHHD 11b as a potent anticancer agent able to overcome drug resistance. In addition, compound 11b was able to serve as a chemical carrier for 99mTc and the in vivo biodistribution study of 99mTc-11b complex revealed a remarkable targeting ability of 99mTc into solid tumor showing that 99mTc-11b might be used as a promising radiopharmaceutical imaging agent for cancer. � 2018 Elsevier Masson SAS
Preparation and biological profile of 99mTc-lidocaine as a cardioselective imaging agent using 99mTc eluted from 99Mo/99mTc generator based on AlMo gel
(Springer Netherlands, 2017) Sakr T.M.; Ibrahim A.B.; Fasih T.W.; Rashed H.M.; Radioactive Isotopes and Generators Department; Hot Laboratories Centre; Atomic Energy Authority; Cairo; 13759; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt
The current study is aimed to prepare 99mTc-lidocaine as a new myocardial perfusion-imaging agent. The used 99mTc was obtained from Al. 99Mo-molybdate(VI) gel matrix. 99mTc-lidocaine showed higher (15.4. 0.11% ID/g) and faster (15. min post injection) cardiac uptake than the recently studied 99mTc-valsartan and 99mTc-procainamide. Consequently, 99mTc-lidocaine will be a valuable myocardial SPECT agent for diagnosis of emergency patients. Besides, the receptor affinity study confirmed the selectivity of 99mTc-lidocaine for sodium channels in the heart. 2017, Akadmiai Kiad, Budapest, Hungary.
Radioiodinated doxorubicin as a new tumor imaging model: preparation, biological evaluation, docking and molecular dynamics
(Springer Netherlands, 2018) Ibrahim A.B.; Alaraby Salem M.; Fasih T.W.; Brown A.; Sakr T.M.; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; Cairo; 13759; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; Radioactive Isotopes and Generators Department; Hot Laboratories Centre; Atomic Energy Authority; Cairo; 13759; Egypt; Department of Chemistry; University of Alberta; Edmonton; Canada
Abstract: Non-invasive molecular imaging techniques are accruing more interest in the last decades. Several radiolabelling elements have been FDA-approved and are currently used to characterize tumors. In this study, the DNA intercalating agent doxorubicin was radiolabelled with 125I. Several parameters for the radiolabelling reaction were investigated and optimized. A maximum yield of 94 � 0.3% was reached after reacting 20�?g of doxorubicin with 200�?g Chloramine-T at pH 5 for 30�min. The in vivo stability of 125I-doxorubicin is validated by the low propensity for thyroid uptake in mice. The preclinical T/NT ratio was approximately 6.4 at 30 min. Docking and molecular dynamics confirmed that the radiolabelling of doxorubicin did not affect (or slightly improved its binding to DNA). Overall, 125I-doxorubicin was demonstrated to be a promising non-invasive probe for solid tumor imaging. Graphical Abstract: [Figure not available: see fulltext.]. � 2018, Akad�miai Kiad�, Budapest, Hungary.
Radioiodinated esmolol as a highly selective radiotracer for myocardial perfusion imaging: In silico study and preclinical evaluation
(Elsevier Ltd, 2018) Sakr T.M.; Sanad M.H.; Abd-Alla W.H.; Salama D.H.; Saleh G.M.; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Collage of Pharmaceutical Science and Drug Manufacturing; Misr University for Science & Technology; P.O. 77; 6th of October City; Giza; Egypt; Health Radiation Research department (Radiodiagnosis Unit); National Center for Radiation Research and Technology; Atomic Energy Authority; Cairo; Egypt
Challenges facing cardiovascular imaging necessitate innovation of better radiopharmaceuticals to augment or replace the existing ones. This research assesses the ability and competency of radioiodinated esmolol as a potential cardio selective imaging agent. Radioiodinated esmolol was synthesized with 97.3 � 0.3% radiochemical yield and with high stability up to 48 h at room temperature as well as in rat serum. Molecular modeling study was performed to confirm the binding of iodinated esmolol to ?1-adrenergic receptor. Its biodistribution studies in normal Swiss albino mice showed high heart uptake (38.5 � 0.11%ID/g at 5 min p.i.), heart/liver ratio nearly 3.85:1 and heart/lungs ratio was about 7:1 at 5 min p.i. The evidenced selectivity of the radioiodinated esmolol to ?1-adrenoceptor was confirmed by prior injection of cold esmolol. Gamma camera biodistribution pattern showed that radioiodinated esmolol accumulated selectively in heart. � 2018 Elsevier Ltd
Radiosynthesis, molecular modeling studies and biological evaluation of 99mTc-Ifosfamide complex as a novel probe for solid tumor imaging
(Taylor and Francis Ltd, 2018) Motaleb M.A.; El-Safoury D.M.; Abd-Alla W.H.; Awad G.A.S.; Sakr T.M.; Labelled Compounds Department; Hot Labs Center; Atomic Energy Authority; Cairo; Egypt; Pharmaceutical Chemistry Department; College of Pharmaceutical Sciences and Drug Manufacturing; Misr University for Science & Technology; Giza; Egypt; Pharmaceutics and Industrial Pharmacy Department; Faculty of Pharmacy; Ain Shams University; Cairo; Egypt; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt
Purpose: Ifosfamide as a chemotherapeutic drug is used for the treatment of different cancer types. The purpose of this study is the preparation of 99mTc-ifosfamide complex to be evaluated as a potential candidate for tumor imaging. Materials and methods: The radiolabeling of ifosfamide with technetium-99m was carried out by mixing 4mg ifosfamide and 5 ?g of SnCl2.2H2O with 400 MBq Na99mTcO4 at pH 9 for 30 min at room temperature. Computer simulation studies were performed using Accelrys Discovery Studio 2.5 operating system to illustrate the interaction of ifosfamide and 99mTc-ifosfamide complexes with DNA. The in-vivo biodistribution of 99mTc-ifosfamide was studied in tumor-bearing Albino mice. Results: A new 99mTc-ifosfamide complex was synthesized with a good radiochemical yield of 90.3. 2.1% under the optimized conditions and exhibited in-vitro stability up to 2 h. Biodistribution studies showed good uptake in tumor site and high uptake in tumor site with T/NT ?3 after 60 min post-injection. Besides, the molecular docking study confirmed that the complexation of ifosfamide with technetium-99m does not abolish its binding to the target receptor. Conclusion: These promising results afford a new radiopharmaceutical that could be used as a potential tumor imaging. 2018, Copyright 2018 Taylor & Francis Group, LLC.
Selenium nanomaterials in biomedicine An overview of new opportunities in nanomedicine of selenium
(Editions de Sante, 2018) Sakr T.M.; Korany M.; Katti K.V.; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Pharmaceutics Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Institute of Green Nanotechnology; Department of Radiology & Physics; University of Missouri; Columbia; MO 65212; United States; Missouri University Research Reactor; University of Missouri; Columbia; MO 65212; United States
Selenium is one of the most important dietary supplements in the human diet. It is incorporated into the synthesis of many antioxidant proteins, which serve as scavengers of reactive oxygen species such as glutathione peroxidase. Therefore, selenium has become antagonistic and resistant to many diseases resulting from oxidative stress such as arthritis, tumors, and heart and brain diseases. Selenium nanoparticles (SeNPs) have the potential to serve as new nutritional supplements with higher degradability, lower toxicity and ability to be cleared gradually from the body. Selenium nanoparticles have emerged as unusual selenium species with amazing prophylactic and therapeutic properties with dual synergistic effects of providing therapeutic cargo and improved anticancer activity. Recent investigations have also explored new applications of nano-scaled forms of selenium for a wide range of biological activities such as antibacterial and antifungal agents. Herein, we provide a focused account on the recent advances on various biomedical applications of selenium nanoparticles with a particular emphasis on their chemistry, nanotechnology and various applications in life sciences. � 2018 Elsevier B.V.