Polyvinylpolypyrrolidone-Supported Chlorosulfonic Acid: An Efficient Catalyst for One-Pot Synthesis of Dihydropyrimidinones and Octahydroquinazolin-2,5-diones

Polyvinylpolypyrrolidone-supported chlorosulfonic acid has been successfully applied to perform one-pot reaction of arylaldehydes, urea, ethylacetoacetate, or cyclic 1,3-diketo compounds under solvent-free condition at 70°C to provide a series of dihydropyrimidinones and octahydroquinazolin-2,5-diones in good to excellent yields. The method offers several advantages such as high yield, short reaction time, simple workup, easy preparation, and reusability of the catalyst. The [PVPP-SO₃H]⁺Cl^? catalyst was characterized via Fourier transform infrared spectroscopy (FT-IR) and thermal gravimetric analysis (TGA). Moreover, the catalyst could be recycled several times without significant loss of its catalytic activity. Clean methodologies, easy work-up procedure, high yield, and simple preparation of the catalyst are some advantages of this article.     

Synthesis and evaluation of 99m Tc-NIDA and 99m Tc-DMIDA complexes for hepatobiliary imaging

1-Naphthylcarbamoylmethyliminodiacetic acid (NIDA) and diphenylmethylcarbamoylmethyliminodiacetic acid (DMIDA) were synthesized, characterized, and labeled with ^99m Tc using SnCl₂ as reducing agent. The parameters affecting the yield of ^99m Tc-NIDA and ^99m Tc-DMIDA were studied in detail. The optimum conditions ensuring high yield of ^99m Tc-NIDA (94.2 ± 2%) and ^99m Tc-DMIDA (93.1 ± 2%) are as follows: 30 mg of NIDA or DMIDA, 0.3 mg of SnCl₂·H₂O, pH 6, 15 min. The biodistribution in mice injected with ^99m Tc-NIDA and ^99m Tc-DMIDA showed high liver uptake at 10 min post injection, with fast biliary excretion. Accumulation of the activity in kidneys was negligible, especially after a long time post injection. Both ^99m Tc-NIDA and ^99m Tc-DMIDA can be applied as hepatobiliary imaging agents for the evaluation of the functional status of the hepatocytes and the patency of the biliary duct.     

Poly(glycerol sebacate) nanoparticles for ocular delivery of sunitinib: physicochemical,cytotoxic and allergic studies

Poly(glycerol sebacate) (PGS) is a new biodegradable polymer with good biocompatibility used in many fields of biomedicine and drug delivery. Sunitinib‐loaded PGS/gelatine nanoparticles were prepared by the de‐solvation method for retinal delivery and treatment of diabetic retinopathy. The nanoparticles were characterised by Fourier‐transform infrared and differential scanning calorimetry. The effects of different formulation variables including drug‐to‐carrier ratio, gelatine‐to‐PGS ratio, and glycerine‐to‐sebacate ratio were assessed on the encapsulation efficiency (EE%), particle size, release efficiency (RE), and zeta potential of the nanoparticles. The in vitro cytotoxicity of PGS/gelatine nanoparticles was studied on L929 cells. Draize test on rabbit eyes was also done to investigate the possible allergic reactions caused by the polymer. Glycerine/sebacic acid was the most effective parameter on the EE and RE. Gelatine‐to‐PGS ratio had the most considerable effect on the particle size while the RE was more affected by the glycerine/sebacic acid ratio. The optimised formulation (S₁ G_0.7 D_21.2) exhibited a particle size of 282 nm, 34.6% EE, zeta potential of −8.9 mV, and RE% of about 27.3% for drug over 228 h. The 3‐(4,5‐dimethylthuazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide assay indicated PGS/gelatine nanoparticles were not cytotoxic and sunitinib‐loaded nanoparticles were not toxic at concentrations <36 nM.Inspec keywords: polymers, differential scanning calorimetry, toxicology, drug delivery systems, solvation, eye, encapsulation, particle size, drugs, biodegradable materials, nanofabrication, nanomedicine, nanoparticles, gelatin, Fourier transform infrared spectraOther keywords: gelatine‐to‐PGS ratio, glycerine‐to‐sebacate ratio, particle size, zeta potential, sunitinib‐loaded nanoparticles, biodegradable polymer, retinal delivery, differential scanning calorimetry, drug‐to‐carrier ratio, allergic reactions, physicochemistry, cytotoxicity, poly(glycerol sebacate) nanoparticles, sunitinib ocular delivery, drug delivery, sunitinib‐loaded PGS‐gelatine nanoparticles, Fourier‐transform, in vitro cytotoxicity, biocompatibility, Draize test, rabbit eyes, 3‐(4,5‐dimethylthuazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide assay     

Empirical model for plasticity‐induced crack closure based on Kmax and ΔK

The mean stress has a significant effect on crack propagation life and must be included in prediction models. However, there is no consensus in the fatigue community regarding the dominant mechanism explaining the mean stress effect. The concept of crack closure has been widely used and several empirical models can be found in literature. The stress ratio, R, is usually the main parameter of these models, but present numerical results showed a significant influence of K_max. A new empirical model is therefore proposed here, dependent on K_max and ΔK, with four empirical constants. The model also includes the effect of material's yield stress, and two additional parameters were defined to account for stress state and crack closure parameter. A comparison was made with Kujawski's and Glinka's parameters, for a wide range of loading conditions. ΔK_eff lies between Kujawski's and Glinka's parameters, and some agreement is evident, although the concepts are quite different. The crack opening model was applied to literature results and was able to collapse da/dN–ΔK curves for different stress ratios to a single master curve.     

Novel Self‐Reinforced Films Based on Poly (3‐Hydroxybutyrate‐Co‐3‐Hydroxyvalerate) (PHBV) and PHBV Microparticles

Biodegradable self‐reinforced films of poly (3‐hydroxybutyrate‐co‐3‐hydroxyvalerate) (PHBV) and PHBV microparticles were prepared through the solvent casting method (srPHBV). Differential scanning calorimetry (DSC), wide angle X‐ray scattering (WAXS) and polarized optical microscopy results confirmed the nucleating effect of PHBV microparticles. WAXS proved that diffractograms of PHBV and srPHBV‐6 films at room temperature contain the main characteristic diffraction peaks of an orthorhombic α‐type crystalline structure. Small angle X‐ray scattering (SAXS) showed a similar decrement rate of long spacing in PHBV and srPHBV films. SAXS/WAXS data revealed that when the amount of filler was increased, lamellae thickness grew. Transmission electron microscopy images illustrated well filler dispersion in the srPHBV films. Scanning electron microscopy results exhibited a significant reduction in porosity for srPHBV films once the PHBV microparticles were added. Atomic force microscopy analysis showed higher surface roughness after filler incorporation. Samples of srPHBV films showed higher barrier properties against water vapor, oxygen, and carbon dioxide. Combined properties of srPHBV films revealed the possibility of being suitable candidates for food packaging applications. POLYM. ENG. SCI., 59:E120–E128, 2019. © 2018 Society of Plastics Engineers     

Development of a 2-D 2-group neutron noise simulator for hexagonal geometries

In this paper, the development of a neutron noise simulator for hexagonal-structured reactor cores using both the forward and the adjoint methods is reported. The spatial discretisation of both 2-D 2-group static and dynamic equations is based on a developed box-scheme finite difference method for hexagonal mesh boxes. Using the power iteration method for the static calculations, the 2-group neutron flux and its adjoint with the corresponding eigenvalues are obtained by the developed static simulator. The results are then benchmarked against the well-known CITATION computer code. The dynamic calculations are performed in the frequency domain which leads to discarding of the time discretisation. Then, the developed 2-D 2-group neutron noise simulator calculates both the discretised forward and the adjoint reactor transfer function between a point source and its induced neutron noise, by assuming the neutron noise source as an “absorber of variable strength” type. The neutron noise induced by a “vibrating absorber” type of noise source may also be modeled using the calculated transfer function. The viability of the simulator is verified for different benchmark cases.     

A Novel Alternative Method for Modeling the Effects of Air Temperature and Slice Thickness on Quality and Drying Kinetics of Tomato Slices: Superposition Technique

The effect of air temperature (AT) and slice thickness (ST) on the quality and drying kinetics of tomato slices were studied. The drying period of tomato slices to reach the moisture content of 15% (wb) ranged from 2.6 to 18.7 h. The water diffusivity, activation energy, and resistance to diffusion ranged from 1.4 × 10^?10 to 2.8 × 10^?9 m²/s, 21.25 to 23.4 kJ/mol, and from 939 to 4590 m² s/kg, respectively. Drying had a significant effect on ascorbic acid, soluble solid, acidity, and pH (P = 0.01). The ascorbic acid degradation was greatly influenced by ST. The results show that time-temperature superposition technique (TTST) was very efficient in the modeling of the drying process. The proposed TTST provides a novel alternative in curve-fitting exercise of drying data. Neural networks also showed favorable performance in estimating the drying functions.     

Current Concepts on Genetic Aspects of Mitochondrial Dysfunction in Amyotrophic Lateral Sclerosis

Amyotrophic Lateral Sclerosis (ALS), neurodegenerative motor neuron disorder is characterized as multisystem disease with important contribution of genetic factors. The etiopahogenesis of ALS is not fully elucidate, but the dominant theory at present relates to RNA processing, as well as protein aggregation and miss-folding, oxidative stress, glutamate excitotoxicity, inflammation and epigenetic dysregulation. Additionally, as mitochondria plays a leading role in cellular homeostasis maintenance, a rising amount of evidence indicates mitochondrial dysfunction as a substantial contributor to disease onset and progression. The aim of this review is to summarize most relevant findings that link genetic factors in ALS pathogenesis with different mechanisms with mitochondrial involvement (respiratory chain, OXPHOS control, calcium buffering, axonal transport, inflammation, mitophagy, etc.). We highlight the importance of a widening perspective for better understanding overlapping pathophysiological pathways in ALS and neurodegeneration in general. Finally, current and potentially novel therapies, especially gene specific therapies, targeting mitochondrial dysfunction are discussed briefly.