Synthesis and biodistribution of 99m Tc-PyDA as a potential marker for tumor hypoxia imaging

The ^99m Tc-pyrimidine-4,5-diamine (^99m Tc-PyDA) complex was prepared. The yield under the optimum conditions (5 mg of PyDA, pH 8, 25 μg of SnCl₂·2H₂O) was 96 ± 3%. The complex is stable in vitro for 24 h. The complex was tested on mice as potential marker for tumor hypoxia imaging. The complex showed high tumor hypoxia uptake with the target/nontarget (T/NT) ratio as high as ～3.     

Radiolabeling,quality control,and biodistribution of <Superscript>99m</Superscript>Tc-sulfadiazine as an infection imaging agent

Abstract—Sulfadiazine (antibiotic used for treating bacterial infections) was labeled with ^99mTc with the aim of the development of a new radiopharmaceutical for infection imaging. The influence of the reaction parameters such as the substrate and SnCl₂·2H₂O concentrations, pH of the reaction mixture, and reaction time on the labeling yield was examined, and the labeling conditions were optimized. The maximum radiochemical yield of ^99mTc-sulfadiazine (94.7%) was obtained by using 50 µg of SnCl₂·2H₂O and 1 mg of sulfadiazine at pH 5. The radiochemical purity of the labeled compound was evaluated by ITLC and HPLC. The biological distribution of ^99mTc-sulfadiazine in mice with experimentally induced Staphylococcus aureus infection in the right thigh was studied, and the bacterial infected thigh/normal thigh (target-to-nontarget, T/NT) ratio was evaluated. The T/NT ratio for ^99mTc-sulfadiazine was found to be 3.6, which is comparable to the commercially available ^99mTc-ciprofloxacin (3.8), indicating that ^99mTc-sulfadiazine can be used for infection imaging.     

In vivo study of anti‐epidermal growth factor receptor antibody‐based iron oxide nanoparticles (anti‐EGFR‐SPIONs) as a novel MR imaging contrast agent for lung cancer (LLC1) cells detection

Superparamagnetic iron oxide nanoparticles (SPIONs) conjugated with anti‐epidermal growth factor receptor monoclonal antibody (anti‐EGFR‐SPIONs) were characterised, and its cytotoxicity effects, ex vivo and in vivo studies on Lewis lung carcinoma (LLC1) cells in C57BL/6 mice were investigated. The broadband at 679.96 cm⁻¹ relates to Fe–O, which verified the formation of the anti‐EGFR‐Mab with SPIONs was obtained by the FTIR. The TEM images showed spherical shape 20 and 80 nm‐sized for nanoparticles and the anti‐EGFR‐SPIONs, respectively. Results of cell viability at 24 h after incubation with different concentrations of nanoprobe showed it has only a 20% reduction in cell viabilities. The synthesised nanoprobe administered by systemic injection into C57BL/6 mice showed good Fe tumour uptake and satisfied image signal intensity under ex vivo and in vivo conditions. A higher concentration of nanoprobe was achieved compared to non‐specific and control, indicating selective delivery of nanoprobe to the tumour. It is concluded that the anti‐EGFR‐SPIONs was found to be as an MR imaging contrast nanoagent for lung cancer (LLC1) cells detection.Inspec keywords: toxicology, biomedical MRI, lung, magnetic particles, biomedical materials, nanofabrication, nanomagnetics, transmission electron microscopy, nanomedicine, superparamagnetism, nanoparticles, iron compounds, proteins, cellular biophysics, molecular biophysics, cancer, tumours, Fourier transform infrared spectraOther keywords: MR imaging contrast agent, LLC1, superparamagnetic iron oxide nanoparticles, Lewis lung carcinoma cells, ex vivo conditions, cell viability, antiepidermal growth factor receptor antibody‐based iron oxide nanoparticles, antiEGFR‐SPION, lung cancer cell detection, antiepidermal growth factor receptor monoclonal antibody, cytotoxicity effects, C57BL‐6 mice, antiEGFR‐Mab, FTIR spectra, TEM, spherical shape, incubation, nanoprobe concentrations, systemic injection, Fe tumour uptake, image signal intensity, in vivo conditions, time 24.0 hour, Fe₃ O₄      

MiRNA‐145‐5p expression and prospective molecular mechanisms in the metastasis of prostate cancer

The clinicopathological implication and prospective molecular mechanisms of miRNA‐145‐5p in the metastasis of prostate cancer (PCa) stand unclear. Herein, it is found that miRNA‐145‐5p expression was remarkably reduced in 131 cases of metastatic PCa than 1371 cases of localised ones, as the standardised mean differences (SMD) was −1.26 and the area under the curve (AUC) was 0.86, based on miRNA‐chip and miRNA‐sequencing datasets. The potential targets of miRNA‐145‐5p in metastatic PCa (n = 414) was achieved from the intersection of miRNA‐145‐5p transfected metastatic PCa cell line data, differential expression of metastatic PCa upregulated genes and online prediction databases. TOP2A was screened as one of the target hub genes by PPI network analysis, which was adversely related to miRNA‐145‐5p expression in both metastatic PCa (r = −0.504) and primary PCa (r = −0.281). Gene‐chip and RNA‐sequencing datasets, as well as IHC performed on clinical PCa samples, showed consistent upregulated expression of TOP2A mRNA and protein in PCa compared with non‐PCa. The expression of TOP2A mRNA was also significantly higher in metastatic than localised PCa with the SMD being 1.72 and the AUC of sROC being 0.91. In summary, miRNA‐145‐5p may participate in PCa metastasis by binding TOP2A and be useful as a biomarker for the detection of metastatic PCa.     

Radioiodination of 3-amino-2-quinoxalinecarbonitrile 1,4-dioxide and its biological distribution in Erhlich ascites cancer bearing mice as a preclinical tumor imaging agent

3-Amino-2-quinoxalinecarbonitrile 1,4-dioxide (QN) was labeled with ¹²⁵I, and the biological distribution of the product was studied. ¹²⁵I-QN was prepared by direct electrophilic substitution reaction using N-bromosuccinimide (NBS) as an oxidizing agent. The radiochemical yield of 92% was reached under the following optimum conditions: pH 7, 15 min, 100 μg of QN, and 75 μg of NBS. The labeled QN was stable for up to 12 h post labeling. Biodistribution study of ¹²⁵I-QN in tumor-bearing mice reflected that it accumulated in tissues with high proliferation rate with preferential accumulation in tumor sites. ¹²⁵I-QN was incorporated rapidly in the tumor site (T/NT = 4 at 2 h post injection), and then its content slowly decreased, whereas in the other tissues it decreased rapidly. The results obtained encourage the use of ¹²³I-QN as a tumor imaging agent.     

Functionalisation of Fe3 O4 nanoparticles by 2‐((pyrazol‐4‐yl) methylene) hydrazinecarbothioamide enhances the apoptosis of human breast cancer MCF‐7 cells

Cancer is a major cause of death. Thus, the incidence and mortality rate of cancer is globally important. Regarding vast problems caused by chemotherapy drugs, efforts have progressed to find new anti‐cancer drugs. Pyrazole derivatives are known as components with anti‐cancer properties. In here, Fe₃ O₄ nanoparticles were first functionalized with (3‐chloropropyl) trimethoxysilane, then 2‐((pyrazol‐4‐yl) methylene) hydrazinecarbothioamide (P) was anchored on the surface of magnetic nanoparticles (PL). The synthesized nano‐compounds were characterized using Fourier transform infrared spectroscopy, X‐ray diffraction, scanning electron microscopy, Zeta potential, dynamic light scattering, and energy‐dispersive x‐ray spectrometry analyses. The cytotoxicity effect was evaluated using MTT assay, apoptosis test by Flow cytometry, cell cycle analysis, Caspase‐3 activity assay and Hoechst staining on MCF‐7 cell line. The high toxicity for tumor cells and low toxicity on normal cells (MCF10A) was considered as an important feature (selectivity index, 10.9). Based on results, the IC50 for P and PL compounds were 157.80 and 131.84 μM/ml respectively. Moreover, apoptosis inducing, nuclear fragmentation, Caspase 3 activity and induction of cell rest in sub‐G1 and S phases, were also observed. The inhibitory effect of PL was significantly higher than P, which could be due to the high penetrability of Fe₃ O₄ nanoparticles.Inspec keywords: magnetic particles, drugs, nanomedicine, biochemistry, cancer, light scattering, scanning electron microscopy, molecular biophysics, iron compounds, electrokinetic effects, nanofabrication, tumours, X‐ray diffraction, cellular biophysics, nanoparticles, biomedical materials, toxicology, nanomagnetics, Fourier transform infrared spectra, enzymes, X‐ray chemical analysisOther keywords: anticancer properties, Fe₃ O₄ magnetic nanoparticles, (3‐chloropropyl) trimethoxysilane, energy‐dispersive X‐ray spectrometry, cell cycle analysis, MCF‐7 cell line, tumour cells, human breast cancer MCF‐7 cells, mortality rate, pyrazole derivatives, 2‐((pyrazol‐4‐yl) methylene) hydrazinecarbothioamide, chemotherapy drugs, heterocyclic components, nanocompounds, X‐ray diffraction, scanning electron microscopy, Zeta potential, dynamic light scattering, cytotoxicity effect, MTT assay, apoptosis test, caspase‐3 activity assay, Hoechst staining, MCF10A nontumourigenic cells, cell rest induction, nuclear fragmentation, Fe₃ O₄      

Synthesis,characterisation and potential biomedical applications of magnetic core–shell structures: carbon‐, dextran‐, SiO2 ‐ and ZnO‐coated Fe3 O4 nanoparticles

Due to the strong effect of nanoparticles'' size and surface properties on cellular uptake and bio‐distribution, the selection of coating material for magnetic core–shell nanoparticles (CSNPs) is very important. In this study, the effects of four different biocompatible coating materials on the physical properties of Fe₃ O₄ (magnetite) nanoparticles (NPs) for different biomedical applications are investigated and compared. In this regard, magnetite NPs are prepared by a simple co‐precipitation method. Then, CSNPs including Fe₃ O₄ as a core and carbon, dextran, ZnO (zincite) and SiO₂ (silica) as different shells are synthesised using simple one‐ or two‐step methods. A comprehensive study is carried out on the prepared samples using X‐ray diffraction, vibrating sample magnetometry, transmission electron microscopy and Fourier transform infrared spectroscopy analyses. According to the authors'' findings, it is suggested that carbon‐ and dextran‐coated magnetite NPs with high M _s have great potential in the application of magnetic resonance imaging contrast agents. Moreover, silica‐coated magnetite NPs with high coercivity are potentially suitable candidates for hyperthermia and ZnO‐coated Fe₃ O₄ is potentially suitable for photothermal therapy.Inspec keywords: iron compounds, carbon, silicon compounds, zinc compounds, nanomedicine, biomedical materials, nanofabrication, nanoparticles, magnetic particles, coatings, X‐ray diffraction, magnetometry, transmission electron microscopy, Fourier transform spectra, infrared spectra, biomedical MRI, hyperthermia, radiation therapyOther keywords: biomedical applications, magnetic core‐shell nanoparticles, CSNP, cellular uptake, biodistribution, coating material, biocompatible coating materials, co‐precipitation, dextran, zincite, silica, X‐ray diffraction, vibrating sample magnetometry, transmission electron microscopy, Fourier transform infrared spectroscopy, magnetic resonance imaging contrast agents, hyperthermia, photothermal therapy, SiO₂ ‐Fe₃ O₄ , ZnO‐Fe₃ O₄      

CdO nanoparticles,c‐MWCNT nanoparticles and CdO nanoparticles/c‐MWCNT nanocomposite fibres: in vitro assessment of anti‐proliferative and apoptotic studies in HeLa cancer cell line

A simple ultrasonic assisted chemical technique was used to synthesise cadmium oxide (CdO) nanoparticles (NPs) and CdO NPs/c‐Multiwalled carbon nanotube (c‐MWCNT) nanocomposite fibres.To confirm the physio‐chemico properties and to analyse surface morphology of the obtained nanomaterials X‐Ray Diffraction (XRD), Fourier Transform Infrared Spectroscopy (FTIR) and field emission scanning electron microscopy (FESEM) were performed. To evaluate the anti‐cancer property of CdO NPs, c‐MWCNT NPs and CdO NPs/c‐MWCNT nanocomposite fibres, an anti‐proliferative assay test (Methylthiazolyl diphenyl‐ tetrazolium bromide ‐ MTT assay) were performed on HeLa cells which further estimated IC50 value (Least concentration of sample in which nearly 50% of cells remain alive) under in‐vitro conditions. On comparison, CdONPs/c‐MWCNT based system was found to be superior by achieving 52.3% cell viability with its minimal IC50 value of 31.2 μg/ml. Lastly, the CdO NPs based system was taken up for an apoptotic study using DNA fragmentation assay for estimating its ability to cleave the DNA of the HeLa cells into internucleosomal fragments using the agarose gel electrophoresis method. In conclusion, based on our observations, CdO NPs/c‐MWCNT hybrid based system can be further used for the development of efficient drug delivery and therapeutic systems.Inspec keywords: drug delivery systems, electrophoresis, oxidation, toxicology, DNA, nanoparticles, drugs, field emission electron microscopy, scanning electron microscopy, nanofabrication, surface morphology, cancer, X‐ray diffraction, nanomedicine, cellular biophysics, filled polymers, biomedical materials, molecular biophysics, biochemistry, Fourier transform infrared spectra, multi‐wall carbon nanotubesOther keywords: c‐MWCNT nanoparticles, apoptotic study, HeLa cancer cell line, cadmium oxide nanoparticles, c‐MWCNT NPs, anti‐proliferative assay test [methyl thiazolyl diphenyl‐tetrazolium bromide assay], human epithelioid cervix carcinoma cells, live cells, CdO NP‐based system, IC50 concentration, HeLa cell line, cell deaths, CdO‐C     

Synthesis,physicochemical characterisation and biological activity of anandamide/ɛ‐polycaprolactone nanoparticles obtained by electrospraying

Drug encapsulation in nanocarriers such as polymeric nanoparticles (Nps) may help to overcome the limitations associated with cannabinoids. In this study, the authors’ work aimed to highlight the use of electrospraying techniques for the development of carrier Nps of anandamide (AEA), an endocannabinoid with attractive pharmacological effects but underestimated due to its unfavourable physicochemical and pharmacokinetic properties added to its undesirable effects at the level of the central nervous system. The authors characterised physicochemically and evaluated in vitro biological activity of anandamide/ɛ‐polycaprolactone nanoparticles (Nps‐AEA/PCL) obtained by electrospraying in epithelial cells of the human proximal tubule (HK2), to prove the utility of this method and to validate the biological effect of Nps‐AEA/PCL. They obtained particles from 100 to 900 nm of diameter with a predominance of 200–400 nm. Their zeta potential was −20 ± 1.86 mV. They demonstrated the stable encapsulation of AEA in Nps‐AEA/PCL, as well as its dose‐dependent capacity to induce the expression of iNOS and NO levels and to decrease the Na⁺ /K⁺ ATPase activity in HK2 cells. Obtaining Nps‐AEA/PCL by electrospraying would represent a promising methodology for a novel AEA pharmaceutical formulation development with optimal physicochemical properties, physical stability and biological activity on HK2 cells.Inspec keywords: cellular biophysics, molecular biophysics, nanoparticles, nanofabrication, biochemistry, encapsulation, drugs, neurophysiology, electrokinetic effects, enzymes, biomedical materials, nanomedicine, polymers, sprayingOther keywords: electrospraying techniques, pharmacological effects, pharmacokinetic properties, in vitro biological activity, biological effect, HK2 cells, optimal physicochemical properties, polymeric nanoparticles, AEA pharmaceutical formulation development, anandamide‐ε‐polycaprolactone nanoparticles, drug encapsulation, nanocarriers, endocannabinoid, central nervous system, epithelial cells, human proximal tubule, zeta potential, stable encapsulation, dose‐dependent capacity, Na⁺ ‐K⁺ ATPase activity, physical stability, size 100.0 nm to 900.0 nm, NO, Na⁺ ‐K⁺      

Synthesis and characterisation of iron oxide nanoparticles conjugated with epidermal growth factor receptor (EGFR) monoclonal antibody as MRI contrast agent for cancer detection

The aim of this study is to synthesise superparamagnetic iron oxide nanoparticles conjugated with anti‐epidermal growth factor receptor monoclonal antibody (ANTI‐EGFR‐SPION) and investigate its physicochemical characterisation and biocompatibility as a targeted magnetic resonance imaging (MRI) contrast agent for the EGFR‐specific detection in EGFR expressing tumour cells. These particles employed biocompatible polymers, poly(D,L‐lactide‐co‐glycolide) (PLGA) and polyethylene glycol aldehyde (PEG‐aldehyde), to increase the half‐life of particles in circulation and reduce their side effects. The Fe₃ O₄ ‐loaded PLGA‐PEG‐aldehyde nanoparticles were prepared by a modified water‐in‐oil‐in‐water double emulsion method. The EGFR antibody was conjugated to the surface of SPIONs using the aldehyde‐amine reaction. Synthesised conjugates (nanoprobes) were characterised using Fourier transform infrared spectrophotometry, dynamic light scattering, transmission electron microscopy images, and vibrating‐sample magnetometery, and the results showed that the conjugation was successful. The mean diameter of nanoprobes was about 25 nm. These nanoprobes exhibited excellent water‐solubility, stability, and biocompatibility. Meanwhile, MR susceptibility test proved that synthesised nanoprobes can be managed for negative contrast enhancement. The results of this study suggested the potential use of these nanoprobes for non‐invasive molecular MRI in EGFR detection in the future.Inspec keywords: solubility, nanomedicine, cancer, spectrophotometry, emulsions, biomedical MRI, nanomagnetics, nanofabrication, tumours, nanoparticles, magnetic particles, molecular biophysics, light scattering, proteins, cellular biophysics, Fourier transform spectra, superparamagnetism, polymers, transmission electron microscopy, iron compoundsOther keywords: physicochemical characterisation, superparamagnetic iron oxide nanoparticles, novel targeting cancer detection, anti‐epidermal growth factor receptor monoclonal antibody, ANTI‐EGFR‐SPION, biocompatibility, targeted magnetic resonance imaging contrast agent, EGFR‐specific detection, EGFR expressing tumour cells, biocompatible polymers, PLGA‐PEG‐aldehyde nanoparticles, modified water‐in‐oil‐in‐water double emulsion method, EGFR antibody, aldehyde‐amine reaction, synthesised conjugates were characterised using Fourier, transmission electron microscopy images, synthesised nanoprobes, EGFR detection, size 25.0 nm, Fe₃ O₄      

Design,synthesis, <Superscript>99<Emphasis Type="Italic">m</Emphasis></Superscript>Tc labeling,and biological evaluation of a novel pyrrolizine derivative as potential anti-inflammatory agent

The design and synthesis of ethyl 4-(6-amino-7-cyano-2,3-dihydro-1H-pyrrolizine-5-carboxamido)-benzoate (KH16) were discussed, and its structure was determined. The anti-inflammatory activity of a new compound was evaluated using in vitro cyclooxygenase (COX) inhibitory assay. KH16 exhibits higher selectivity to COX-2 than to COX-1 with the selectivity index of 3.46. KH16 was labeled with ^99mTc with the maximum radiochemical yield of ^99mTc-KH16 of 90.5 ± 1.5%. Biodistribution of ^99mTc-KH16 in normal, infected, and inflamed mice was studied. The uptake in inflamed muscle was higher than that in normal muscle throughout the examined time interval. This work is a step ahead in the direction of using pyrrolizine derivatives for site-specific delivery to the inflamed tissue.     

Synthesis and comparative assessment of antiradical activity,toxicity, and biodistribution of κ‐carrageenan‐capped selenium nanoparticles of different size: in vivo and in vitro study

In the present study, water‐soluble hybrid selenium‐containing nanocomposites have been synthesised via soft oxidation of selenide‐anions, preliminarily generated from elemental bulk‐selenium in the base‐reduction system ‘N₂ H₄ –NaOH’. The nanocomposites obtained consist of Se⁰ NPs (4.6–24.5 nm) stabilised by κ‐carrageenan biocompatible polysaccharide. The structure of these composite nanomaterials has been proven using complementary physical–chemical methods: X‐ray diffraction analysis, transmission electron microscopy, optical spectroscopy, and dynamic light scattering. Optical ranges of ‘emission/excitation’ of aqueous solutions of nanocomposites with Se⁰ NPs of different sizes are established and the most important parameters of their luminescence are determined. For the obtained nanocomposites, the expressed antiradical activity against free radicals 2,2‐diphenyl‐1‐picrylhydrazyl and 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulphonic acid has been found, the value of which depends on the size of selenium nanoparticles. It is experimentally revealed that all obtained nanocomposites are low toxic (LD₅₀ >2000 mg/kg). It is also found that small selenium nanoparticles (6.8 nm), in contrast to larger nanoparticles (24.5 nm), are accumulated in organisms to significantly increase the level of selenium in the liver, kidneys, and brain (in lesser amounts) of rats.Inspec keywords: nanobiotechnology, free radical reactions, oxidation, enzymes, selenium, solubility, nanofabrication, transmission electron microscopy, X‐ray diffraction, free radicals, reduction (chemical), biomedical materials, nanoparticles, nanomedicine, light scattering, organic‐inorganic hybrid materials, biochemistry, nanocompositesOther keywords: κ‐carrageenan biocompatible polysaccharide, composite nanomaterials, complementary physical–chemical methods, X‐ray diffraction analysis, transmission electron microscopy, optical spectroscopy, dynamic light scattering, optical ranges, expressed antiradical activity, 2,2‐diphenyl‐1‐picrylhydrazyl, 3‐ethylbenzothiazoline‐6‐sulphonic acid, comparative assessment, toxicity, κ‐carrageenan‐capped selenium nanoparticles, water‐soluble hybrid selenium‐containing nanocomposites, soft oxidation, selenide‐anions, elemental bulk‐selenium, base‐reduction system, free radicals, 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulphonic acid, selenium nanoparticles, nanocomposites, liver, kidneys, brain, luminescence, size 4.6 nm to 24.5 nm     

Radiochemical and biological characterization of <Superscript>99<Emphasis Type="Italic">m</Emphasis></Superscript>Tc-oxiracetam as a model for brain imaging

^99mTc-oxiracetam was prepared. It can be used as a radiotracer for brain imaging. Under the optimum conditions (0.5 mg of oxiracetam, 50 μg of SnCl₂·2H₂O, pH 7, room temperature, 30 min), the radio-chemical yield determined by chromatographic methods reached 96%. Biodistribution studies with mice showed that the brain uptake of the complex was 5.1% injected dose per gram (% ID/g) at 5 min post injection. In this parameter, the complex surpasses the commercially available ^99mTc-ECD (4.7% ID/g) and ^99mTc-HMPAO (2.25% ID/g).     

Green synthesis of Cordia myxa incubated ZnO,Fe2O3, and Co3O4 nanoparticle: Characterization,and their response as biological and photocatalytic agent

The imperative necessity for new therapy and catalysts has risen significantly due to infectious agents that are multi-resistant and organic toxins draining into our ecosystem. To address these problems, highly biocompatible Cordia myxa incubated I-ZnO, I-Co₃O₄, and I-Fe₂O₃ NPs were prepared and characterized by using a variety of techniques, including ultraviolet–visible spectroscopy (UV–vis), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR). The XRD diffraction pattern confirmed that I-ZnO hexagonal, while I-Co₃O₄ and I-Fe₂O₃ cubic structure. UV–vis spectra show the energy bandgap for I-ZnO, I-Fe₂O₃, and I-Co₃O₄ 3.35 eV, 2.32 eV, and 2.44 eV, respectively. TEM analyses show the patterns of the morphology of I-ZnO as flower-shaped, I-Fe₂O₃ as rectangular, I-Co₃O₄ looks like prism crystals. EDX mapping confirmed the elemental presence of Zn, Fe, Co in the samples. The antibacterial study show that the I-NPs have bigger zone of inhibition (ZOI) than pristine NPs. The highest percentage for E-coli strain obtained in this trend (I- Fe₂O₃)_81%>(I-ZnO)_76%>(I-Co₃O₄)_63%. Photocatalytic activity results revealed that the MB dye degraded after 80 min and efficiencies of I-(Fe₂O₃)_{98.38 %}>I-ZnO_98.12%>(I-Co₃O₄)_93.93%. Furthermore, the green synthesis strategy certifies a new pathway for minimizing infections, oxidative stress, and degradation of key pollutants from the environment.     

Preparation and biological evaluation of <Superscript>99<Emphasis Type="Italic">m</Emphasis></Superscript>Tc-timonacic acid as a new complex for hepatobiliary imaging

Timonacic acid (TCA) was successfully labeled with ^99m Tc. The influence exerted on the reaction by the substrate and reducing agent concentrations, pH of the reaction mixture, and reaction time was examined, and in vitro stability of ^99m Tc-TCA was evaluated. The maximum labeling yield was 98.5 ± 0.6%. The complex was stable throughout the working period (6 h). A study of in-vivo biodistribution in mice showed that the maximum uptake of ^99m Tc-TCA in the liver was 22.3 ± 0.3% of the injected activity per gram of the tissue or organ (% ID/g) at 30 min post injection. The clearance from the mice appeared to proceed via the circulation mainly through the kidneys and urine (approximately 56% of the injected dose at 1 h after injection). The liver uptake of ^99m Tc-TCA is higher than that of ^99m Tc-UDCA (ursodeoxycholic acid); therefore, ^99m Tc-TCA shows more promise for liver SPECT.     

Synthesis and characterisation of neem leaf extract, 2, 3‐dehydrosalanol and quercetin dihydrate mediated silver nano particles for therapeutic applications

The utility of green silver nanoparticles (AgNPs) in veterinary medicine is steadily increasing as they have many therapeutic applications against pathogens and arthropods of livestock. In this study, green AgNPs using neem (N‐AgNPs), 2,3‐dehydrosalanol (2,3‐DHS‐AgNPs) and quercetin dihydrate (QDH‐AgNPs) were synthesised and characterised. Synthesised compounds were characterised by UV‐Vis spectroscopy and the peak absorbance was recorded at 370 nm for neem extract. For N‐AgNPs, 2,3‐DHS‐AgNPs and QDH‐AgNPs, the maximum absorbance peaks were at 430, 230 and 220 nm, respectively. The FTIR analysis confirmed the synthesis of green AgNPs. The XRD pattern of N‐AgNPs showed the peaks corresponding to whole spectra of 2 θ values ranging from 10–80. The relatively higher intensity of (111, 222) planes in face centred cubic crystalline structure supports the formation of synthesised AgNPs. In DLS analysis, the hydrodynamic diameter of neem leaf extract was found to be 259.8 nm, followed by 5.3, 6.7 and 261.8 nm for 2,3‐DHS‐AgNPs, N‐AgNPs and QDH‐AgNPs, respectively. Based on the transmission electron microscopy and scanning electron microscopy image analyses, confirmed the formation of N‐AgNPs, 2,3‐DHS‐AgNPs and QDH‐AgNPs. These eco‐friendly phyto‐AgNPs may be of use as an effective alternative to chemical control methods against the arthropods of livestock.Inspec keywords: nanoparticles, silver, nanomedicine, biomedical materials, nanofabrication, Fourier transform infrared spectra, ultraviolet spectra, visible spectra, X‐ray diffraction, light scattering, transmission electron microscopy, scanning electron microscopy, aggregation, veterinary medicineOther keywords: 2,3‐dehydrosalanol mediated silver nanoparticles, quercetin dihydrate mediated silver nanoparticles, therapeutic applications, green silver nanoparticles, veterinary medicine, Azadirachta indica, UV‐visible spectroscopy, Fourier transformed infrared analysis, X‐ray diffraction, (111) planes, (222) planes, face centred cubic crystalline structure, dynamic light scattering, hydrodynamic diameter, aqueous neem leaf extract, transmission electron microscopy, hexagonal shape, pencil head shape, cuboid shape, scanning electron microscopy, aggregation, arthropod infesting livestock, Ag, in‐vivo antiectoparasitic activity, in‐vitro antiectoparasitic activity     

Effect of chitosan with different molecular weight on the stability,antioxidant and anticancer activities of well‐dispersed selenium nanoparticles

This study was designed to evaluate and compare the stability, antioxidant and anticancer activities of selenium nanoparticles (SeNPs) decorated with different molecular weight (MW) of chitosan (CS) (1500 Da, 48 kDa, 510 kDa). The size range of well‐dispersed SeNPs was effectively controlled by I⁻ first and then coated with CS. The morphology, size and surface charge of generated SeNPs were characterised by several technologies. Fourier transform infrared spectroscopy was used to investigate the relationship between SeNPs and CS. SeNPs decorated with CS (510 kDa) can keep stable for more than 45 days. As observed from the results of a simple photometric system, the antioxidant activities of decorated SeNPs were enhanced compared to undecorated SeNPs. SeNPs coated with higher MW of CS (510 kDa) showed the strongest antioxidant activities. Moreover, the treatments of SeNPs decorated with CS inhibited the growth of HepG2 cells in a time‐ and dose‐dependent manner. The proposed results demonstrated the critical roles of the MW of CS on the stability, antioxidant and anticancer properties of CS‐coated SeNPs, which provided an important design cue for future applications of functional foods and additives.Inspec keywords: selenium, drug delivery systems, cellular biophysics, nanoparticles, molecular biophysics, cancer, biomedical materials, biochemistry, polymers, nanomedicine, Fourier transform infrared spectra, surface charging, surface morphologyOther keywords: chitosan, surface charge, anticancer properties, anticancer activities, antioxidant activities, molecular weight, selenium nanoparticles, CS‐coated SeNP, Fourier transform infrared spectroscopy, photometric system, HepG2 cells, time 45.0 d, Se     

Polyacrylamide–punicic acid conjugate‐based micelles for flutamide delivery in PC3 cells of prostate cancer: synthesis,characterisation and cytotoxicity studies

The aim of the present study was to synthesize a novel biopolymeric micelle based on punicic acid (PA) and polyacrylamide (PAM) for carrying chemotherapeutic drugs used in prostate cancer treatment. A polymer composite micelle was prepared by chemical conjugation between PAM and PA. The micelles were prepared by self‐assembly via film casting followed by ultrasonication method. The successful production of PAMPA copolymeric micelles was confirmed using FTIR, 1H‐NMR, and TEM. Then, flutamide was loaded in the designed nanomicelles and they were characterized. The cell cytotoxicity of the micelles was studied on PC3 cells of prostate cancer. The prepared nanomicelles showed the particle size of 88 nm, PDI of 0.246, zeta potential of −9 mV, drug loading efficiency of 94.5%, drug release of 85.6% until 10 hours in pH 7.4 and CMC of 74.13 μg/ml. The cell viability in blank nanocarriers was about 70% in PC3 cells at concentration of 25 μM. More significant cytotoxic effects were seen for flutamide loaded micelles at this concentration compared to the free drug. The results suggest that the PAMPA co‐polymeric nanomicelles can be utilized as an effective carrier to enhance the cytotoxic effects of flutamide in prostate cancer.Inspec keywords: nanoparticles, cellular biophysics, drugs, biomedical materials, drug delivery systems, colloids, hydrophilicity, pH, transmission electron microscopy, particle size, cancer, casting, toxicology, electrokinetic effects, polymer blends, proton magnetic resonance, nanomedicine, self‐assembly, nanofabrication, Fourier transform infrared spectraOther keywords: PC3 cells, chemotherapeutic drugs, prostate cancer treatment, polymer composite micelle, chemical conjugation, proton nuclear magnetic resonance, cell cytotoxicity, prepared nanomicelles, drug loading efficiency, drug release, critical micelle concentration, cell viability, cytotoxic effects, flutamideloaded micelles, flutamide delivery, polyacrylamide‐punicic acid conjugate‐based micelles, PAMPA copolymeric nanomicelles, biopolymeric micelle, PAM‐punicic acid copolymer copolymeric micelles, hydrophilic shell, self‐assembly, film casting, ultrasonication method, Fourier transform infrared spectra, transmission electron microscopy, particle size, polydisperity index, zeta potential, pH, blank nanocarriers, time 10.0 hour     

Characterization of the biocompatible magnetic colloid on the basis of Fe3O4 nanoparticles coated with dextran, used as contrast agent in magnetic resonance imaging

The magnetic resonance imaging contrast agent, the so-called Endorem colloidal suspension on the basis of superparamagnetic iron oxide nanoparticles (mean diameter of 5.5 nm) coated with dextran, were characterized on the basis of several measurement techniques to determine the parameters of their most important physical and chemical properties. It is assumed that each nanoparticle is consisted of Fe3O4 monodomain and it was observed that its oxidation to gamma-Fe2O3 occurs at 253.1 degrees C. The M?ssbauer spectroscopy have shown a superparamagnetic behavior of the magnetic nanoparticles. The Magnetic Resonance results show an increase of the relaxation times T1, T2, and T2* with decreasing concentration of iron oxide nanoparticles. The relaxation effects of SPIONs contrast agents are influenced by their local concentration as well as the applied field strength and the environment in which these agents interact with surrounding protons. The proton relaxation rates presented a linear behavior with concentration. The measured values of thermo-optic coefficient dn/dT, thermal conductivity kappa, optical birefringence delta n0, nonlinear refractive index n2, nonlinear absorption beta' and third-order nonlinear susceptibility |chi(3)| are also reported.     

Characterisation of sol–gel method synthesised MgZnFe2 O4 nanoparticles and its cytotoxic effects on breast cancer cell line,MDA MB‐231 in vitro

In this study, nanocrystalline magnesium zinc ferrite nanoparticles were successfully prepared by a simple sol–gel method using copper nitrate and ferric nitrate as raw materials. The calcined samples were characterised by differential thermal analysis/thermogravimetric analysis, Fourier transform infrared spectroscopy and X‐ray diffraction. Transmission electron microscopy revealed that the average particle size of the calcined sample was in a range of 17–41 nm with an average of 29 nm and has spherical size. A cytotoxicity test was performed on human breast cancer cells (MDA MB‐231) and (MCF‐7) at various concentrations starting from (0 µg/ml) to (800 µg/ml). The sample possessed a mild toxic effect toward MDA MB‐231 and MCF‐7 after being examined with MTT (3‐[4, 5‐dimethylthiazol‐2‐yl]‐2, 5 diphenyltetrazolium bromide) assay for up to 72 h of incubation. Higher reduction of cells viability was observed as the concentration of sample was increased in MDA MB‐231 cell line than in MCF‐7. Therefore, further cytotoxicity tests were performed on MDA MB‐231 cell line.Inspec keywords: sol‐gel processing, nanoparticles, nanofabrication, magnesium compounds, zinc compounds, toxicology, biological organs, cancer, cellular biophysics, nanomedicine, calcination, differential thermal analysis, Fourier transform infrared spectra, X‐ray diffraction, transmission electron microscopy, particle size, organic compoundsOther keywords: sol‐gel method, cytotoxic effects, breast cancer cell line, MDA MB‐231 in vitro, nanocrystalline magnesium zinc ferrite nanoparticles, copper nitrate, ferric nitrate, raw materials, calcined samples, differential thermal analysis, thermogravimetric analysis, Fourier transform infrared spectroscopy, X‐ray diffraction, transmission electron microscopy, average particle size, cytotoxicity testing, human breast cancer cells, mild toxic effect, 3‐[4,5‐dimethylthiazol‐2‐yl]‐2,5 diphenyltetrazolium bromide) assay, cell viability, MCF‐7, MDA MB‐231 cell line, size 17 nm to 41 nm