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2-hydroxypropyl-ß-cyclodextrin (HPßCD) nanofiber films have high surface-to-volume ratio and show high dissolution rate of hydrophobic drugs. However, the solubility-enhancement effect of HPßCD films may not be enough to include an effective dose in a sublingually administrable film. Moreover, unmodified HPßCD films are very brittle and difficultly transported and/or handled. So, the addition of polyethylene glycol (PEG) as a plasticizer was suggested to improve their ultimate tensile strength (UTS) and solubilization of hydrophobic drugs. Accordingly, six nanofiber films were developed and characterized, using three molecular weights of PEG (400, 1500 and 6000 Da) with two concentrations each (1:100 and 2:100 PEG:HPßCD), in addition to the unmodified HPßCD nanofibrous film. The results revealed that adding 1:100 of PEG 400 increases the UTS (â¼2-fold) and the average fiber diameter (AFD) (â¼3-fold). Moreover, the addition of PEG 400 significantly increased the solubility of two hydrophobic model drugs; coumarin (up to 7.7-fold of the original solubility) and 2-nitroimidazole (up to 1.6-fold of the original solubility). However, with higher PEG concentration/molecular weight, both AFD and UTS of the films decreased. On the other hand, it was noted that the solubility of the two model drugs decreased upon using 1500-Da PEG, and then increased with 6000-Da PEG.
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Nanofibras , 2-Hidroxipropil-beta-Ciclodextrina , Interacciones Hidrofóbicas e Hidrofílicas , Nanofibras/química , SolubilidadRESUMEN
Pyridazine and thiazole derivatives have various biological activities such as antimicrobial, analgesic, anticancer, anticonvulsant, antitubercular and other anticipated biological properties. Chitosan can be used as heterogeneous phase transfer basic biocatalyst in heterocyclic syntheses. Novel 1-thiazolyl-pyridazinedione derivatives were prepared via multicomponent synthesis under microwave irradiation as ecofriendly energy source and using the eco-friendly naturally occurring chitosan basic catalyst with high/efficient yields and short reaction time. All the prepared compounds were fully characterized by spectroscopic methods, and their in vitro biological activities were investigated. The obtained results were compared with those of standard antibacterial/antifungal agents. DFT calculations and molecular docking studies were used to investigate the electronic properties and molecular interactions with specific microbial receptors.
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Antibacterianos/síntesis química , Antifúngicos/síntesis química , Piridazinas/síntesis química , Tiazoles/síntesis química , Antibacterianos/química , Antibacterianos/farmacología , Antifúngicos/química , Antifúngicos/farmacología , Bacterias/efectos de los fármacos , Infecciones Bacterianas/tratamiento farmacológico , Técnicas Químicas Combinatorias , Farmacorresistencia Bacteriana , Hongos/efectos de los fármacos , Humanos , Microondas , Simulación del Acoplamiento Molecular , Micosis/tratamiento farmacológico , Piridazinas/química , Piridazinas/farmacología , Tiazoles/química , Tiazoles/farmacologíaRESUMEN
Dry powder inhalers (DPIs) are considered a main drug delivery system through pulmonary route. The main objective of this work is to study the flow of differently shaped microparticles in order to find the optimum shape of drug particles that will demonstrate the best flow to the deep lung. The flowability of particles in air or any fluid depends particularly on the drag force which is defined as the resistance of the fluid molecules to the particle flow. One of the most important parameters that affect the drag force is the particles' shape. Computational simulations using COMSOL Multi Physics 5.2 software were performed for investigating the particles flow in the air pathways of lung, and the drag force was calculated for different particles shapes. This was accomplished by screening a set of 17 possible shapes that are expected to be synthesized easily in the micro-scale. In addition, the macro-scale behavior of the investigated shapes was also simulated so as to compare the behavior of the flowing particles in both cases. A very big difference was found between the behavior of particles' flow in the micro and macro scales, but a similar behavior can be obtained if the flow velocity of the microparticles is very high. It was also found that the micro-triangle with aspect ratio 2:1 has the least drag force in both deep and upper lung; so, it should be the shape of choice during the process of particle synthesis for pulmonary drug delivery.
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Aerosoles/química , Preparaciones Farmacéuticas/química , Sistema Respiratorio/efectos de los fármacos , Administración por Inhalación , Simulación por Computador , Sistemas de Liberación de Medicamentos/métodos , Inhaladores de Polvo Seco/métodos , Humanos , Hidrodinámica , Tamaño de la PartículaRESUMEN
We report the fabrication, characterisation (SEM/EDX, TEM, XRD, XPS and Raman spectroscopy) and electrochemical properties of graphite and graphene paste electrodes with varying lateral flake sizes. The fabricated paste electrodes are electrochemically analysed using both outer-sphere and inner-sphere redox probes, namely; hexaammineruthenium(iii) chloride, N,N,N',N'-tetramethyl-p-phenylenediamine (TMPD), potassium ferrocyanide(ii) and ammonium ferrous(ii) sulphate. Upon comparison of different graphite paste electrodes, a clear correlation between the lateral flake sizes (La), ranging from 1.5 mm-0.5 µm, and electrochemical activity (heterogeneous electron transfer (HET) kinetics) is evident, where an improvement in the HET is observed at smaller lateral flake sizes. We infer that the beneficial response evident when employing laterally smaller flakes is due to an increased number of edge plane like-sites/defects available upon the electrode surface, facilitating electron transfer. Interestingly, given that the overall lateral flake sizes of the graphenes utilised (10.0-1.3 µm) were significantly smaller than those studied previously, an improvement in HET kinetics was also evident with the reduction of lateral flake size; the extent to which is redox-probe dependent. Improvements are observed up to a distinct point, termed the 'lateral size threshold' (ca. ≤2 µm) where the electrochemical reversible limit is approached. Further support is provided from density functional theory (DFT), exploring the electronic structure (i.e. HOMO-LUMO) as a function of flake size, which demonstrates that the coverage of edge plane like-sites/defects comprising the geometric structure of the relatively small graphene flakes is such that effectively the entire flake has become electrochemically active. In this study, the importance of lateral flake size with respect to electrochemical reactivity at carbon-based electrodes has been demonstrated alongside a structural relationship upon HET performance, a phenomenon that has not previously been described in the literature. Such work is both highly important and informative for the field of electrochemistry and electrode performance, with potential implications in a plethora of areas, ranging from novel renewable energy sources to electroanalytical sensing platforms.
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A comprehensive study of the interaction between nitrophenols (π-acceptors) and amiodarone (AM) was performed using electronic absorption spectra. The key point is to clarify the erroneous interpretation of the interaction between nitrophenols and one of the basic organic drugs. Matching of the experimental UV-vis spectra and the theoretical ones obtained by DFT calculations revealed that the tertiary amino group of AM reacts with the phenol compounds under investigation via proton-transfer but not charge-transfer (C.T.) mechanisms, unlike what is commonly known about this type of interaction. The interaction was carried out in solutions of different basic pH values to study the effect of hydrogen ion concentration on the reaction. The results show that the reaction is a simple acid-base reaction. As a result, this reaction cannot be used by analytical chemists for determination of one of the studied compounds due to its very low selectivity. TD-DFT as well as geometry optimization of the nitrophenols were calculated with the B3LYP functional, using aug-cc-pvDZ and LanL2DZ as basis sets for ionic and neutral compounds, respectively. The theoretical spectra of possible interactions between AM and nitrophenols result in the same spectra of ionized nitrophenols alone, indicating no possibility for the formation of charge-transfer complexes.
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Amiodarona/química , Fenol/química , Transporte de Electrón , Electrones , Modelos Moleculares , Conformación Molecular , Teoría Cuántica , Análisis EspectralRESUMEN
Food safety became one of the most critical issues owing to the large expansion of international trading and emission of various pollutants in air, water and soil. Fungal contamination of food and feed has attracted most of the attention in the last decade because of the emerging analytical tools that facilitate the detection and discrimination of fungal species in imported foodstuff, seeds, grains, plants, meats etc. In this work, we give an insight on the application of integrated attenuated total reflection-Fourier transform infrared (ATR-FTIR) spectroscopy and artificial-intelligence algorithms to the determination and discrimination of fungal species/strains which potentially infect plants, seeds and grains. The proposed method is based on a microcontroller which allows the PC to analyze a large number of samples via serial connection with an UART module. Penicillium chrysogenum, Aspergillus niger, Aspergillus fumigatus, Aspergillus solani, Aspergillus flavus and two different strains of Fusarium oxysporum were used as model microorganisms. The use of artificial-intelligence algorithms herein provides the advantage of automation enabling high throughput screening of large numbers of food samples in less than 5 s. In addition, the classification accuracy is enhanced by applying these machine-learning classification techniques. Principle component analysis (PCA) was used in order to extract the spectral discriminative features from the recorded fungal FTIR spectra. Three intelligent methods of classification; namely, artificial neural network (ANN), support-vector machine (SVM) and k-nearest neighbor (KNN), were used in this study in order to prove that integration of spectroscopic measurements with varying machine-learning methods give a simple analytical tool for detection and classification of foodborne pathogens. All the utilized classifiers gave an accuracy of 100 % and were able to discriminate different species and/or strains of the investigated fungi in few milliseconds.
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Rheumatoid arthritis (RA), an autoimmune disease impacting the joints, significantly diminishes the quality of life for patients. Conventional treatments predominantly rely on oral or injectable formulations, underscoring the crucial need for an effective topical remedy. The present study reports a novel triple-layered transdermal platform for efficient RA treatment. The patches are based on an electrospun/electrosprayed diclofenac (DIC)-conjugated polyvinyl alcohol (PVA) nanofibers/nanoparticles (NFs/NPs) composite layer sandwiched between an electrospun supporting layer of polycaprolactone (PCL) NFs, and a 3D-printed sodium alginate-based hydrogel (HG) layer incorporating sodium hyaluronate (HA) and rosuvastatin (ROS)-loaded core-shell lipid nanocapsules (LNCs). The ingeniously designed transdermal patches release the chemically conjugated DIC via skin-secreted esterases at the inflamed sites. The LNCs and patches were characterized using DLS, FTIR, DSC, and electron microscopy. ROS-loaded LNCs (<50 nm as per the TEM micrographs) were able to release about 97 % of ROS during 5 days. In-vitro and in-vivo evaluations definitively established the efficacy of the developed platform, showcasing a substantial reduction in IL-6 and TNF-α through sandwich ELISA measurements in cell culture and Rattus norvegicus plasma samples. Besides, the stained photomicrographs of the rats' ankle joints confirmed the alleviation of the RA symptoms via reducing cell infiltration with a preserved joint tissue structure.
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Artritis Reumatoide , Nanocápsulas , Nanofibras , Humanos , Ratas , Animales , Hidrogeles/química , Nanofibras/química , Alginatos/química , Calidad de Vida , Especies Reactivas de Oxígeno , Artritis Reumatoide/tratamiento farmacológico , Impresión TridimensionalRESUMEN
Water pollution from organic dyes poses a serious danger to the environment. In the present work, we report a novel adsorbent (ADFS) based on azo-dye-functionalized superparamagnetic iron oxide nanoparticles (SPIONs) for the removal of the anionic dye bromophenol blue (BPB) from contaminated water. The fabricated SPIONs, azo dye, and ADFS adsorbent were characterized with FTIR and UV-vis absorption spectroscopy, 1HNMR spectroscopy, mass spectrometry, SEM imaging, dynamic light scattering (DLS), zeta potential measurements, vibrating sample magnetometry, thermogravimetric analysis, differential thermal analysis, and X-ray diffraction analysis. DLS measurements showed a particle size of 46.1 and 176.5 nm for the SPIONs and the ADFS, respectively. The adsorbent exhibited an adsorption capacity of 7.43 mg g-1 and followed the pseudo-second-order kinetics model (r2 = 0.9981). The ADFS could efficiently remove BPB from water after stirring for 120 minutes at room temperature and pH 2. The adsorption process was proved to occur via physisorption, as revealed by the Freundlich isotherm (n = 1.82 and KF = 11.5). Thermodynamic studies implied that the adsorption is spontaneous (-8.03 ≤ ΔG ≤ -0.58 kJ mol-1) and enthalpy-driven might take place via van der Waals interactions and/or hydrogen bonding (ΔH = -82.19 kJ mol-1 and ΔS = -0.24 kJ mol-1 K-1).
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Numerous pollutants endanger the safety and purity of water, making water pollution a major worldwide concern. The health of people and aquatic ecosystems are at risk from these contaminants, which include hazardous microbes, industrial waste, and agricultural runoff. Fortunately, there appears to be a viable option to address this problem with adsorptive water treatment techniques. The present study presents a magnetic adsorbent (MMIP) based on molecularly imprinted polyaniline and magnetite nanoparticles for the solid-phase extraction of diclofenac, an anti-inflammatory medication, from industrial wastewater. The adsorbent nanomaterial was characterized using dynamic light scattering, zeta potential measurement, vibrating sample magnetometry, X-ray diffraction, and scanning electron microscopy. The MMIP demonstrated a particle size of 86.3 nm and an adsorption capacity of 139.7 mg g-1 at 600 mg L-1 of diclofenac and after a 200 min incubation period. The highest %removal was attained at pH range of 3-7. The adsorption process follows the pseudo-second order kinetic model. In addition, it was found that the adsorption process is enthalpy-driven and may occur via hydrogen bonding and/or van der Waals interactions.
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We report herein a fluorescent molecularly imprinted polymer (FMIP) for the solid-phase extraction (SPE) and fluorimetric determination of hydrochlorothiazide (HCTZ) in water. The FMIP is based on fluorescent polystyrene nanoparticles embedded within a molecularly imprinted polyaniline (PANI) matrix. The operational adsorption parameters such as the initial HCTZ concentration, incubation time and the solution pH were found to influence the removal efficiency. At optimum conditions, a high adsorption capacity of the FMIP was found (2.08 mg g-1). Evidence of the adsorption process was confirmed by the change in the FMIP physicochemical properties measured by FTIR absorption spectroscopy and electron microscopy. Based on the regression R2 values and the consistently low values of the adsorption statistical error functions, equilibrium data were best fitted to both Freundlich and Temkin isotherms. Moreover, the pseudo-second-order kinetic model described the adsorption kinetics, and the mechanism of the adsorption process was explained by the intraparticle diffusion model. Upon studying adsorption thermodynamics, negative ΔG values (-26.18 kJ mol-1 at room temperature) were obtained revealing that the adsorption process is spontaneous. Interestingly, the maximum adsorption capacity was obtained at 298 K, pH 7.0, and using a high HCTZ concentration, thus revealing the suitability of the proposed FMIP for easy and fast SPE of HCTZ. The FMIP showed an imprinting factor of 1.19 implying the selectivity over the corresponding FNIP. Eventually, the proposed FMIP was successfully applied to the spectrofluorimetric determination of HCTZ in aqueous samples with %recovery values close to 100%.
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BACKGROUND: Overcoming the failure percentage of orthodontic mini-screws (OMSs), which is about 30% of overall orthodontic cases, especially in malocclusion treatment that requires orthopaedic heavy forces, is a great challenge. Bacterial infections, soft tissue and bone inflammation, and weak connections between bones and the OMS surface are among the main causalities of this failure. OBJECTIVE: The aim of the study is to evaluate in vitro the microbiological activities of the deposited nanomaterials (Silver/hydroxyapatite nanoparticles (Ag/HA NPs) and zinc oxide nanoparticles (ZnO NPs)) in terms of microbial inhibition. In addition, the in-vitro cytotoxicity and cytocompatibility of the synthesized nano-coatings prior to their in-vivo application in animal models were tested on four types of cells, namely, fibroblasts, osteocytes, osteoblasts, and oral epithelial cells. MATERIALS AND METHODS: Ag/HA NPs and ZnO NPs were built up onto the surface of titanium OMSs by electrochemical deposition. This electrochemical deposition was performed on 50 orthodontic mini screws and the deposited materials were characterized with the aid of scanning electron microscopy with energy dispersive X-ray spectroscopy (SEM/EDX) analysis, X-ray Diffraction (XRD) and nano-scratch test. In addition, the microbiological activities of the deposited nanomaterials were explored in vitro in terms of microbial inhibition. Furthermore, the cytotoxicity and cytocompatibility were tested on four types of cells, namely, fibroblasts, osteocytes, osteoblasts and oral epithelial cells. RESULTS: SEM images revealed spherical Ag NPs in the range of 40-70nm in diameter, rod-shaped HA NPs and porous scaly ZnO NPs on the surface of the OMSs. XRD analysis confirmed the crystal structures of AgNPs, HA NPs, and ZnO NPs. ZnO NPs coated OMS had the highest antimicrobial activity than Ag/HA coated OMS against Gram-positive, Gram-negative and fungal strains. Moreover, after incubation, the decrease in the number of bacterial colonies was significant with ZnO and Ag/HA nanoparticles (with the greatest decrease for the former), due to the potent antibacterial effect of nanoparticles against Escherichia coli and Enterococcus faecalis. Moreover, ZnO NPs-coated OMSs showed a better cytocompatibility with oral epithelium, bone cells, and fibroblasts compared to Ag/HA NPs. CONCLUSION: The suggested nanocoating is a promising strategy to overcome the development of an inflammatory zone around the fixed OMSs.
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Óxido de Zinc , Animales , Óxido de Zinc/farmacología , Óxido de Zinc/química , Plata/farmacología , Plata/química , Titanio , Durapatita/farmacología , InflamaciónRESUMEN
Ticagrelor is one of the most recent antiplatelet agents used to inhibit platelet aggregation via blocking the ADP receptors of the subtype P2Y12. It belongs to the non-thienopyridine class. The drug was first discovered by Astra Zeneca and approved for use in 2011 by the FDA. Ticagrelor is usually used for the prevention and treatment of thromboembolism in adult patients with acute coronary syndrome. This chapter include an overview on the physical properties, chemical properties, mode of action, pharmacokinetics and common uses of ticagrelor. In addition, the reported methods of ticagrelor assay will be discussed briefly in order to help analysts to find the most convenient method for its estimation in routine analysis. The methods of synthesis used for the preparation of ticagrelor will also be covered in this chapter. Moreover, the analytical and characterization techniques used to characterize ticagrelor row material are summarized herein.
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Síndrome Coronario Agudo , Adenosina , Síndrome Coronario Agudo/tratamiento farmacológico , Adenosina/farmacocinética , Adenosina/uso terapéutico , Adulto , Humanos , Agregación Plaquetaria , Inhibidores de Agregación Plaquetaria/farmacocinética , Inhibidores de Agregación Plaquetaria/uso terapéutico , Antagonistas del Receptor Purinérgico P2Y/farmacocinética , Antagonistas del Receptor Purinérgico P2Y/uso terapéutico , Ticagrelor/farmacología , Ticagrelor/uso terapéuticoRESUMEN
Water contamination is regarded as one of the world's worst tragedies owing to the continual depletion of water resources suitable for drinking and agriculture. Researchers have recently been interested in developing novel and more effective adsorbents for wastewater purification. We report herein a magnetic adsorbent nanomaterial for the removal of the anionic dye bromocresol green (BCG) from wastewater. The adsorbent is based on superparamagnetic iron oxide (cubic Fe3O4) nanoparticles (SPIONs) coated with a high-molecular-weight azo dye synthesized via diazo coupling of vitamin B1 with a trisubstituted benzene derivative. The proposed adsorbent was characterized using scanning electron microscopy, FTIR and 1H-NMR spectroscopy, mass spectrometry, dynamic light scattering, vibrating sample magnetometry, thermal analysis, and X-ray diffraction crystallography. At room temperature and pH 2.0, the synthesized adsorbent showed an average particle size of 65.9 ± 8.0 nm, a high magnetization saturation (65.58 emu g-1), a high equilibrium adsorption capacity (36.91 mg g-1). Adsorption of BCG was found to take place via a physisorption mechanism and followed a pseudo-second-order rate kinetics. Thermodynamic studies revealed that the adsorption process is enthalpy driven by hydrogen bonding and/or van der Waals interactions. After treating water samples with the suggested adsorbent, it can be easily removed from water using a strong external magnetic field.
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Smoking is a life-threatening habit; that is why many nicotine-replacement therapies (NRTs), which include chewing gums, nicotine patches, lozenges, mouth sprays, inhalers and nasal sprays that are usually administered for 8-12 weeks, have been reported for smoking cessation. We report the fabrication of patches comprising nanomicelles-in-coaxial nanofibers (NFs) for the transdermal delivery of varenicline (VAR) tartrate, a partial agonist of the α4ß2 receptor subtype, for smoking cessation. The cores of the fabricated coaxial NF structures are composed of polyethylene oxide, VAR-loaded Pluronic F127 nanomicelles (NPs) and free VAR, while the shell consists of a blend of cellulose acetate (CA) and polycaprolactone (PCL) in a ratio of 1 : 9 (w/w) that incorporates 50% (wt%) free VAR. The morphology and the coaxial structure of the NFs were investigated using TEM, SEM and fluorescent microscopy. The physicochemical and mechanical properties of the scaffolds were analyzed using FTIR, DSC, DLS, TGA and a universal testing machine. SEM micrographs depict NFs with a size ranging from 793.7 ± 518.9 to 324.5 ± 144.1 nm. In vitro release of VAR reaches almost 100% after 3, 9 and 28 days for free VAR, VAR-loaded NPs and the NPs-in-NFs patches, respectively, while the ex vivo release tested using albino rat skin, over a period of 60 days, showed up to 94% sustained release of VAR. Besides, skin permeation, in vivo release and plasma concentrations of VAR from the NF transdermal patches were monitored via cyclic voltammetric measurements during the course of treatment. DFT calculations as well as mathematical release kinetic models were performed in order to study the release mechanism. The cell viability of human skin fibroblast (HSF) cells in the case of plain and VAR-loaded NFs was 75.09 and 32.11%, respectively. The in vivo results showed that VAR was being continuously released from the transdermal patch over a period of 14 days. Besides, the treatment with VAR-loaded patches did not cause any severe conditions in the studied animal model. The new fabricated NPs-in-NFs transdermal patch for VAR tartrate delivery is considered as an effective, economic, safe and long-acting NRT for smoking cessation.
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Nanofibras , Cese del Hábito de Fumar , Animales , Nanofibras/química , Nicotina , Cese del Hábito de Fumar/métodos , Prevención del Hábito de Fumar , Tartratos , Dispositivos para Dejar de Fumar Tabaco , RatasRESUMEN
We report the development and evaluation of a series of well-designed single-dose extracellular matrix (ECM)-mimicking nanofibers (NFs)-reinforced hydrogel (HG)-based skin substitute for wound healing. The HG matrix of the proposed skin substitute is composed of gelatin (GE) and sodium alginate (SA), and incorporates hyaluronic acid (HA) as a key component of the natural ECM, as well as the antimicrobial Punica granatum extract (PE). This HG nanocomposite was cross-linked by the biocompatible N-(3-(dimethylamino)propyl)-N'-ethylcarbodiimide hydrochloride (EDC) cross-linker, and was reinforced with fragmented trans-ferulic acid (FA)-loaded cellulose acetate/polycaprolactone (PCL/CA) NFs. The NFs were obtained via wet electrospinning into a poly(vinyl alcohol) (PVA) coagulating solution to closely resemble the porous structure of the ECM fibers, which facilitates cell migration, attachment, and proliferation. The proposed design of the skin substitute allows adjustable mechanical characteristics and outstanding physical properties (swelling and biodegradability), as well as an excellent porous microstructure. The developed skin substitutes were characterized using Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and electron microscopy. In addition, the biodegradability, biocompatibility, bioactivity, mechanical, and in vitro drug release characteristics were investigated. Moreover, an in vivo excisional full-thickness defect model was conducted to assess skin regeneration and healing effectiveness. The average diameters of the plain and FA-loaded NFs are 210 ± 12 nm and 452 ± 25 nm, respectively. The developed ECM-mimicking skin substitutes demonstrated good antibacterial activity, free-radical scavenging activity, cytocompatibility, porosity, water absorption ability, and good biodegradability. In vivo application of the ECM-mimicking skin substitutes revealed their excellent wound-healing activity and their suitability for single-dose treatment of deep wounds with reducing the wound diameter to 0.95 mm after 15 days of treatment. Moreover, the histological investigation of the wound area demonstrated that the applied skin substitutes have not only enhanced the wound healing progress, but also can participate in improving the quality of the regenerated skin in the treated area via facilitating collagen fibers regeneration and deposition.
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Nanocompuestos , Nanofibras , Piel Artificial , Alginatos/química , Antibacterianos , Gelatina , Nanocompuestos/uso terapéutico , Nanofibras/uso terapéuticoRESUMEN
Aims: Development of antimicrobial agents having the ability to prevent bacterial biofilm formation which causes serious health problems, especially with antibiotic-resistant bacterial strains. Materials and methods: The use of 1,3-diaryl enones as structural motifs to access the pyridine core. Antimicrobial activities of the synthesized compounds against methicillin-susceptible Staphylococcus aureus, methicillin-resistant S. aureus and vancomycin-resistant S. aureus bacterial strains were investigated. Results: The newly synthesized bis-enones were used as building blocks to access some novel highly substituted bis-pyridine derivatives. Several novel bis-compounds showed great bacterial biofilm eradication activity. Conclusion: A new series of bis-chalcones was synthesized and their structural diversity was exploited to access the corresponding, more biologically active, pyridine core. These bis-pyridines showed respectable antibacterial activities against various drug-resistant bacterial strains: namely, methicillin-susceptible, methicillin-resistant and vancomycin-resistant S. aureus.
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Staphylococcus aureus Resistente a Meticilina , Simulación del Acoplamiento Molecular , Meticilina , Pruebas de Sensibilidad Microbiana , Antibacterianos/farmacología , Antibacterianos/químicaRESUMEN
PURPOSE: Intending to obtain Punica granatum L. extract (PE)-loaded drug delivery system of better impact and biomedical applicability, the current study reports the use of crosslinked PVA nanofibers (NFs) as platforms incorporating different amounts of biosynthesized PE-CS-gold nanoparticles (PE-CS-Au NPs). METHODS: PE-conjugated CS-Au nanoparticles (PE-CS-Au NPs) were synthesized via green chemistry approach. The formation of PE-CS-Au NPs was confirmed by UV spectroscopy, DLS, SEM and STEM. PE-CS-Au NPs were then dispersed into polyvinyl alcohol (PVA) solution at different ratios, where the optimized ratios were selected for electrospinning and further studies. Crosslinking of PE-CS-Au NPs loaded PVA nanofibers (NFs) was performed via glutaraldehyde vapor. The morphology, chemical compositions, thermal stability and mechanical properties of PE-CS-Au NPs loaded NFs were evaluated by SEM, FTIR and DSC. Swelling capacity, biodegradability, PE release profiles, release kinetics, antibacterial and cell biocompatibility were also demonstrated. RESULTS: By incorporating PE-CS-Au NPs at 0.6% and 0.9%, the diameters of the nanofibers decreased from 295.7±83.1 nm in neat PVA to 165.6±43.4 and 147.8±42.7 nm, respectively. It is worth noting that crosslinking and incorporation of PE-CS-Au NPs improved thermal stability and mechanical properties of the obtained NFs. The release of PE from NFs was controlled by a Fickian diffusion mechanism (n value Ë0.5), whereas Higuchi was the mathematical model which could describe this release. The antibacterial activity was found to be directly proportional to the amount of the incorporated PE-CS-Au NPs. The human fibroblasts (HFF-1) showed the highest viability (123%) by seeding over the PVA NFs mats containing 0.9% PE-CS-Au NPs. CONCLUSION: The obtained results suggest that the electrospun PVA NFs composites containing 0.9% PE-CS-Au NPs can be used as antibacterial agents against antibiotic-resistant bacteria, and as suitable scaffolds for cell adhesion, growth and proliferation of fibroblast populations.
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Nanopartículas del Metal , Nanofibras , Granada (Fruta) , Antibacterianos/farmacología , Quitosano , Fibroblastos/efectos de los fármacos , Oro , Humanos , Extractos Vegetales/farmacología , Alcohol PolivinílicoRESUMEN
A lab-on-paper colorimetric sensor for detection and quantification of bacterial meat spoilage is reported. Bromocresol purple (BCP) and bromothymol blue (BTB) were used for the construction of the proposed sensor. An Android application allowing fast detection and accurate quantification of bacteria in the spoiled chicken meat samples was developed. The sensor was applied to the determination of spoilage in real chicken-meat samples, at chiller and room temperatures, and can be used for producing smart meat-packaging films. Linearity ranges were found to be 11.2 × 103 to 1.12 × 106 and 38.0 × 103 to 1.12 × 106 CFU g-1 for BTB and BCP, respectively. The calibration plots showed correlation coefficients (r) of 0.9998 (slope: 2.48 g CFU-1) and 0.9999 (slope: 1.95 g CFU-1) in case of bromothymol blue and bromocresol purple, respectively. The Android application uses standard images to plot a calibration curve for calculating the microbial count in the samples and relates it to the standard limits. Thereafter, the application shows a message with the product's freshness degree ranging from excellent to poor.
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We report a new adsorbent nanocomposite material based on matrix-dispersed superparamagnetic iron oxide nanoparticles (SPIONs) in molecularly-imprinted polyaniline for the removal of chlorpyrifos (CPF), a hazardous organophosphate pesticide, from water. The synthesized magnetic molecularly-imprinted polymer (MMIP) was characterized by FTIR spectroscopy, XRD, magnetic susceptibility, DLS, zeta potential measurement, SEM and high-resolution TEM imaging. The average size of the naked SPIONs ranges from 15 to 30 nm according to the high-resolution TEM analysis. Moreover, the adsorption kinetics, thermodynamic parameters (ΔG, ΔH and ΔS), adsorption isotherms and rebinding conditions were investigated in detail. The proposed MMIP has an imprinting factor of 1.64. In addition, it showed a high experimental adsorption capacity of 1.77 mg g-1 and a removal efficiency of nearly 80%. The fabricated MMIP material demonstrated excellent magnetic susceptibility allowing for easy separation using an external magnetic field. The adsorption mechanism of CPF onto the MMIP adsorbent followed the second-order kinetics model and fitted to the Temkin adsorption isotherm. By studying the adsorption thermodynamics, negative ΔG values (-1.955 kJ mol-1 at room temperature) were obtained revealing that the adsorption process is spontaneous. Furthermore, the maximum adsorption capacity was obtained at room temperature (ca. 303 K), neutral pH and using a high CPF concentration.
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Every year, about 1 out of 9 get burnt in Egypt, with a mortality rate of 37%, and they suffer from physical disfigurement and trauma. For the treatment of second-degree burns, we aim at making a smart bandage provided with control of drug release (using chitosan nanoparticles) to enhance the healing process. This bandage is composed of natural materials; namely, cellulose acetate (CA), chitosan, and propolis (bee resin) as the loaded drug. Cellulose acetate nanofibers were deacetylated by NaOH after optimizing the reaction time and the concentration of NaOH solution, and the product was confirmed with FTIR analysis. Chitosan/propolis nanoparticles were prepared by ion gelation method with size ranging from 100 to 200 nm and a polydispersity index of 0.3. Chitosan/propolis nanoparticles were preloaded in the CA solution to ensure homogeneity. Loaded deacetylated cellulose nanofibers have shown the highest hydrophobicity measured by contact angle. Cytotoxicity of propolis and chitosan/propolis nanoparticles were tested and the experimental IC50 value was about 137.5 and 116.0 µg/mL, respectively, with p-value ≤0.001. In addition, chitosan/propolis nanoparticles loaded into cellulose nanofibers showed a cell viability of 89.46% in the cell viability test. In-vivo experiments showed that after 21 days of treatment with the loaded nanofibers repairing of epithelial cells, hair follicles and sebaceous glands in the skin of the burn wound were found in albino-mice model.