Combinations of Piperine with Hydroxypropyl-β-Cyclodextrin as a Multifunctional System

Piperine is an alkaloid that has extensive pharmacological activity and impacts other active substances bioavailability due to inhibition of CYP450 enzymes, stimulation of amino acid transporters and P-glycoprotein inhibition. Low solubility and the associated low bioavailability of piperine limit its potential. The combination of piperine with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) causes a significant increase in its solubility and, consequently, an increase in permeability through gastrointestinal tract membranes and the blood–brain barrier. X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR) were used to characterize interactions between piperine and HP-β-CD. The observed physicochemical changes should be combined with the process of piperine and CD system formation. Importantly, with an increase in solubility and permeability of piperine as a result of interaction with CD, it was proven to maintain its biological activity concerning the antioxidant potential (2,2-diphenyl-1-picryl-hydrazyl-hydrate assay), inhibition of enzymes essential for the inflammatory process and for neurodegenerative changes (hyaluronidase, acetylcholinesterase, butyrylcholinesterase).     

Electrospun fiber membranes from blends of poly(vinylidene fluoride) with fouling‐resistant zwitterionic copolymers

Nonwoven super‐hydrophobic fiber membranes have potential applications in oil–water separation and membrane distillation, but fouling negatively impacts both applications. Membranes were prepared from blends comprising poly(vinylidene fluoride) (PVDF) and random zwitterionic copolymers of poly(methyl methacrylate) (PMMA) with sulfobetaine methacrylate (SBMA) or with sulfobetaine‐2‐vinylpyridine (SB2VP). PVDF imparts mechanical strength to the membrane, while the copolymers enhance fouling resistance. Blend composition was varied by controlling the PVDF‐to‐copolymer ratio. Nonwoven fiber membranes were obtained by electrospinning solutions of PVDF and the copolymers in a mixed solvent of N,N‐dimethylacetamide and acetone. The PVDF crystal phases and crystallinities of the blends were studied using wide‐angle X‐ray diffraction and differential scanning calorimetry (DSC). PVDF crystallized preferentially into its polar β‐phase, though its degree of crystallinity was reduced with increased addition of the random copolymers. Thermogravimetry (TG) showed that the degradation temperatures varied systematically with blend composition. PVDF blends with either copolymer showed significant increase of fouling resistance. Membranes prepared from blends containing 10% P(MMA‐ran‐SB2VP) had the highest fouling resistance, with a fivefold decrease in protein adsorption on the surface, compared to homopolymer PVDF. They also exhibited higher pure water flux, and better oil removal in oil–water separation experiments. © 2018 Society of Chemical Industry     

Improved method for roadside barrier length of need modeling using real-world trajectories

The 2011 AASHTO Roadside Design Guide (RDG) contains perhaps the most widely used procedure for choosing an appropriate length of need (LON) for roadside barriers. However, this procedure has several limitations. The procedure uses a highly simplified model of vehicle departure, and the procedure does not allow designers to specify an explicit level of protection. A new procedure for choosing LON that addresses these limitations is presented in this paper. This new procedure is based on recent, real-world road departure trajectories and uses this departure data in a more realistic way. The new procedure also allows LON to be specified for a precisely known level of protection – a level which can be based on number of crashes, injury outcomes or even estimated crash cost – while still remaining straightforward and quick to use like the 2011 RDG procedure.     

In situ measurements of human cough aerosol hygroscopicity

The airborne dynamics of respiratory droplets, and the transmission routes of pathogens embedded within them, are governed primarily by the diameter of the particles. These particles are composed of the fluid which lines the respiratory tract, and is primarily mucins and salts, which will interact with the atmosphere and evaporate to reach an equilibrium diameter. Measuring organic volume fraction (OVF) of cough aerosol has proved challenging due to large variability and low material volume produced after coughing. Here, the diametric hygroscopic growth factors (GF) of the cough aerosol produced by healthy participants were measured in situ using a rotating aerosol suspension chamber and a humidification tandem differential mobility analyser. Using hygroscopicity models, it was estimated that the average OVF in the evaporated cough aerosol was 0.88 ± 0.07 and the average GF at 90% relative humidity (RH) was 1.31 ± 0.03. To reach equilibrium in dry air the droplets will reduce in diameter by a factor of approximately 2.8 with an evaporation factor of 0.36 ± 0.05. Hysteresis was observed in cough aerosol at RH = ∼35% and RH = ∼65% for efflorescence and deliquescence, respectively, and may depend on the OVF. The same behaviour and GF were observed in nebulized bovine bronchoalveolar lavage fluid.     

Discovery of Affinity-Based Probes for Btk Occupancy Assays

Bruton's tyrosine kinase (Btk) is an attractive target for the treatment of a wide array of B-cell malignancies and autoimmune diseases. Small-molecule covalent irreversible Btk inhibitors targeting Cys481 have been developed for the treatment of such diseases. In clinical trials, probe molecules are required in occupancy studies to measure the level of engagement of the protein by these covalent irreversible inhibitors. The result of this pharmacodynamic (PD) activity provides guidance for appropriate dosage selection to optimize inhibition of the drug target and correlation of target inhibition with disease treatment efficacy. This information is crucial for successful evaluation of drug candidates in clinical trials. Based on the pyridine carboxamide scaffold of a novel solvent-accessible pocket (SAP) series of covalent irreversible Btk inhibitors, we successfully developed a potent and selective affinity-based biotinylated probe 12 (2-[(4-{4-[5-(1-{5-[(3aS,4S,6aR)-2-oxo-hexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanamido}-3,6,9,12-tetraoxapentadecan-15-amido)pentanoyl]piperazine-1-carbonyl}phenyl)amino]-6-[1-(prop-2-enoyl)piperidin-4-yl]pyridine-3-carboxamide). Compound 12 has been used in Btk occupancy assays for preclinical studies to determine the therapeutic efficacy of Btk inhibition in two mouse lupus models driven by TLR7 activation and type I interferon.     

Lateral ion implant straggle and mask proximity effect

Lateral scattering of retrograde well implants is shown to have an effect on the threshold voltage of nearby devices. The threshold voltage of both NMOSFETs and PMOSFETs increases in magnitude for conventional retrograde wells, but for triple-well isolated NMOSFETs the threshold voltage decreases for narrow devices near the edge of the well. Electrical data, SIMS, and SUPREM4 simulations are shown that elucidate the phenomenon.     

Measuring College Students' Motives for Playing Drinking Games.

Students may choose to play drinking games not only for reasons related to alcohol consumption but also because of incentives related to other aspects of play (competition, fun, interpersonal dominance, etc.). College students (120 men and 167 women) completed measures of motives for playing (based on T. J. Johnson, S. Hamilton, & V. L. Sheets, 1999) and consequences of playing drinking games. Exploratory principal-components analysis identified 8 reasons for playing. Men and women differed in their endorsement of the factors. Motives for play directly predicted consequences of play independently of alcohol consumption. Specific motives predicted specific types of consequences. In multiple regression analyses, Conformity motives were negatively related to consequences and may represent a form of protective motive. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Mechanics of plain-woven fabrics for inflated structures

Pressurized fabric tubes, pressure-stabilized beams (known as air beams) and air-inflated structures are considered to be valuable technologies for lightweight, rapidly deployable structures. Design optimization of an inflated structure depends on a thorough understanding of woven fabric mechanics. In this paper the bending response of woven pressure-stabilized beams have been experimentally tested and analytically investigated. Additionally, the micromechanical effects of interacting tows have been studied through finite element models containing contact surfaces and nonlinear slip/stick conditions. Local unit cell models consisting of pairs of woven tows were created to characterize the effective constitutive relations. The material properties from the unit cell models were then used for the global continuum model subjected to 4-point flexure. An experimental set-up was designed and manufactured for testing of Vectran and PEN air beams. The air beam mid-span deflections were measured as functions of inflation pressure and bending load. Plots of the elastic and shear moduli with respect to the pressure and coefficient of friction have been generated. It was determined that the effective elastic and shear moduli were functions of inflation pressure, the material used and the geometry of the weave. It was shown that pneumatic or pressurized tube structures differ fundamentally from conventional metal structures.     

Social Support and Social Strain Among Husbands and Wives: A Multilevel Analysis.

In response to recent calls in the literature for within-person examinations of social support processes over time, this study explores the relationships of spousal support, spousal strain, and well-being among husbands and wives, both within the same day and across days. Eighty-three couples were interviewed and completed a structured diary twice daily for 1 week. The results of multilevel hierarchical modeling suggest that both spousal support and spousal strain made significant, independent contributions to concurrent negative affect, although only spousal support was a significant predictor of next-day negative affect. Spousal strain interacted with spousal support to predict next-day negative affect. Direct and moderating effects of perceived marital adjustment on negative affect were discussed. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Intergranular corrosion of a light aircraft aluminum alloy propeller

Examination of the wreckage of a light aircraft revealed that approximately 20 cm was missing from one tip of the aluminum alloy propeller. Fractographic and metallographic examination of the remaining portion of the propeller revealed extensive grain-boundary separation in the vicinity of the fracture, and grain edges and corners rounded by corrosion on the fracture surface. Energy dispersive X-ray analysis (EDXA) revealed fluorine on, and in the vicinity of, the fracture surface. In the ensuing litigation, it was asserted that the crash occurred because the propeller fractured in flight as the result of intergranular attack caused by the use of a fluorine-bearing cleaner.