Novel strategy for encapsulation and targeted delivery of poorly water-soluble active substances

Carriers for targeted delivery and controlled release of poorly water-soluble active substances (PWSAS) are facing three challenges: (a) the encapsulation issues, (b) limitations of PWSAS water solubility, and (c) burst drug release which can be pharmacologically dangerous and economically inefficient. The present study brings a novel strategy for encapsulation and controlled release of PWSAS—caffeine in concentrations which are higher than its maximal water solubility without the possibility of burst effect. The modification of hydrophilic carrier based on poly(methacylic acid) was done using casein and liposomes. To further increase the maximal caffeine loading inside the carrier nicotinamide was used. The release study of the encapsulated PWSAS was elaborated with respect to morphology of the carriers and interactions that could be established between its structural components. The carriers swelling and the release of caffeine and nicotinamide were also investigated depending on caffeine concentration, the presence of different liposomal formulations and the volume ratio of liposomal formulation, in three media with different pH simulating the path of the carrier through the human gastrointestinal tract. The synthesized carriers are promising candidates for encapsulation of PWSAS in concentrations which are higher than its maximal water solubility and for the targeted delivery of those dosages.     

Bioinformatic characterization of the extracellular lipases from Kluyveromyces marxianus

Lipases are hydrolytic enzymes that break the ester bonds of triglycerides, generating free fatty acids and glycerol. Extracellular lipase activity has been reported for the nonconventional yeast Kluyveromyces marxianus, grown in olive oil as a substrate, and the presence of at least eight putative lipases has been detected in its genome. However, to date, there is no experimental evidence on the physiological role of the putative lipases nor their structural and catalytic properties. In this study, a bioinformatic analysis of the genes of the putative lipases from K. marxianus L-2029 was performed, particularly identifying and characterizing the extracellular expected enzymes, due to their biotechnological relevance. The amino acid sequence of 10 putative lipases, obtained by in silico translation, ranged between 389 and 773 amino acids. Two of the analysed putative proteins showed a signal peptide, 25 and 33 amino acids long for KmYJR107Wp and KmLIP3p, and a molecular weight of 44.53 and 58.23 kDa, respectively. The amino acid alignment of KmLIP3p and KmYJR107Wp with the crystallized lipases from a patatin and the YlLip2 lipase from Yarrowia lipolytica, respectively, revealed the presence of the hydrolase characteristic motifs. From the 3D models of putative extracellular K. marxianus L-2029 lipases, the conserved pentapeptide of each was determined, being GTSMG for KmLIP3p and GHSLG for KmYJR107Wp; besides, the genes of these two enzymes (LIP3 and YJR107W) are apparently regulated by oleate response elements. The phylogenetic analysis of all K. marxianus lipases revealed evolutionary affinities with lipases from abH15.03, abH23.01, and abH23.02 families.     

Impact of adhesive ingredients on adhesion between rubber and brass-plated steel wire in tire

Proficiency on underlying mechanism of rubber-metal adhesion has been increased significantly in the last few decades. Researchers have investigated the effect of various ingredients, such as hexamethoxymethyl melamine, resorcinol, cobalt stearate, and silica, on rubber-metal interface. The role of each ingredient on rubber-metal interfacial adhesion is still a subject of scrutiny. In this article, a typical belt skim compound of truck radial tire is selected and the effect of each adhesive ingredient on adhesion strength is explored. Out of these ingredients, the effect of cobalt stearate is found noteworthy. It has improved adhesion strength by 12% (without aging) and by 11% (humid-aged), respectively, over control compound. For detailed understanding of the effect of cobalt stearate on adhesion, scanning electron microscopy and energy dispersive spectroscopy are utilized to ascertain the rubber coverage and distribution of elements. X-ray photoelectron spectroscopy results helped us to understand the impact of Cu_XS layer depth on rubber-metal adhesion. The depth profile of the Cu_XS layer was found to be one of the dominant factors of rubber-metal adhesion retention. Thus, this study has made an attempt to find the impact of different adhesive ingredients on the formation of Cu_XS layer depth at rubber-metal interface and establish a correlation with adhesion strength simultaneously.     

On Application of Carbon-Containing Electrode Materials in Technology of Electrospark Alloying: Part 1. Peculiarities of Coating Formation Using Electrospark Treatment of Titanium Alloy OT4-1

Electrospark treatment of OT4-1 titanium alloy was performed sequentially with a STIM-20N hard-alloy electrode (TiC–20% Ni) and carbon-containing material (graphite and carbon-based composite materials). Kinetics of the mass transfer of the hard-alloy electrode was studied. The cathode mass loss during the first minute of the treatment was established. The kinetics results were processed using the methods of mathematical statistics. The erosion resistance of the applied carbon-containing materials was determined. Phase composition and relief of the coatings formed were analyzed. It was found that the application of the carbon-containing material increases the content of refractory phases in the coatings. Increase in the time of the treatment using the carbon-containing materials decreases the roughness of the coatings.     

Effect of focused ion beam sample preparation on the phase composition of zirconia

The investigation of phase transformations in metastable ceramic systems such as zirconia often requires local phase analysis within the areas of interest. Electron backscatter diffraction is a suitable method in combination with focused ion beam sample preparation. The interaction between ion beam and sample has to be carefully considered. In case of metastable Y-PSZ and Mg-PSZ, phase transformations were observed after FIB preparation with 30?kV, 30?nA and 5° incidence angle. Damage was the dominating effect for angles of 72°. The expected local temperature increase due to the ion bombardment with 30?kV and 30?nA is 700?K for ZrO₂. Thus, the observed phase transformations can be explained on the basis of the temperature increase in the corresponding Y-PSZ phase diagram. In case of Mg-PSZ, the transition temperature is 1083?°C. The local temperature increase was obviously lower. The excitation energy for the observed phase transformation was smaller than expected from the phase diagrams of the thermodynamic equilibrium. Using 5?kV, 4.8?nA and 5° incidence angle, no phase transformations and no damage were observed. Thus, these conditions are well suited for the FIB preparation of metastable zirconia.     

Compressive properties of pristine and SiC-Te-added MgB2 powders,green compacts and spark-plasma-sintered bulks

Pristine and (SiC+Te)-added MgB₂ powders, green and spark plasma sintered (SPS) compacts were investigated from the viewpoint of quasi-static and dynamic (Split-Hopkinson Pressure Bar, SHPB) compressive mechanical properties The amount of the additive (SiC+Te) was selected to be the optimum one for maximization of the superconducting functional parameters. Pristine and added MgB₂ show very similar compressive parameters (tan δ, fracture strength, Vickers hardness, others) and fragment size in the SHPB test. However, for the bulk SPSed samples the ratio of intergranular to transgranular fracturing changes, the first one being stronger in the added sample. This is reflected in the quasi-static K_IC that is higher for the added sample. Despite this result, sintered samples are brittle and have roughly similar fragmentation behavior as for brittle engineering ceramics. In the fragmentation process, the composite nature of our samples should be considered with a special focus on MgB₂ blocks (colonies) that show the major contribution to fracturing. The Glenn-Chudnovsky model of fracturing under dynamic load provides the closest values to our experimental fragment size data.     

Effect of waste serpentine on the properties of basic insulating refractories

Basic insulating refractories were fabricated by the pressing route using dead-burned magnesia, pure calcined alumina, expanded perlite, and calcined waste serpentine as starting raw materials in four compositions from F1 to F4. Periclase and forsterite were major phases in F1 and F2 compositions, while spinel was also detected in the XRD patterns of F3 and F4 samples. Quantitative phase analysis showed that F4 sample sintered at 1450?°C has the highest forsterite content among all other samples. On the other hand, it has lower thermal conductivity compared to F1 to F3, and even lower than aluminosilicate IFBs with the same bulk density. It is concluded that forsterite is a highly insulating material, compared to periclase, corundum, periclase-spinel, aluminosilicates, such as mullite, etc.     

Surface structural and solar absorptance features of nitrate-based copper-cobalt oxides composite coatings: Experimental studies and molecular dynamic simulation

The copper and cobalt oxides composites coatings on aluminum substrates have been successfully synthesized via sol-gel method using nitrate-based sol precursors. The composites were characterized by X-ray Diffraction (XRD), X-ray photoelectron spectroscopy (XPS), Field Emission Scanning Electron Microscopy (FESEM), Atomic Force Microscopy (AFM), and UV–Vis–NIR spectrophotometry. The sol-gel reactions were discussed and Molecular Dynamics (MD) simulation was integrated into the study to predict molecules assembly properties. The XRD analyses revealed that the CuO and the Co₃O₄ composites were formed after the annealing process with the average difference of the calculated lattice parameters compared to ICDDs was 1.17%. The surface electronic structure was mainly consisted of tetrahedral Cu(I), octahedral Cu(II), tetrahedral Co(II), octahedral Co(III) as well as surface, sub-surface and lattice oxygen O^?. The XRD, XPS and MD simulation results showed that there was minimal (or possibly non-existing) indication of copper-cobalt mixed phase oxides formations. FESEM and AFM surveys revealed that the coating had a porous surface composed of interlinked nanoparticles in the range of ~?10 to ~?40?nm. UV–Vis–NIR reflectance spectra showed that the sol precursors concentration and the dip-drying cycle significantly influenced the absorptance value with optimum absorptance (α) of 88.7% exhibited by coating synthesized using sol concentration of 0.1?M and 10 dip-drying cycles. High absorptance value and simplicity in the synthesis process render the coatings to be very promising candidates for solar selective absorber (SSA) applications.     

Reexamination of the Ergothioneine Biosynthetic Methyltransferase EgtD from Mycobacterium tuberculosis as a Protein Kinase Substrate

Ergothioneine has emerged as a crucial cytoprotectant in the pathogenic lifestyle of Mycobacterium tuberculosis. Production of this antioxidant from primary metabolites may be regulated by phosphorylation of Thr213 in the active site of the methyltransferase EgtD. The structure of mycobacterial EgtD suggests that this post-translational modification would require a large-scale change in conformation to make the active-site residue accessible to a protein kinase. In this report, we show that, under in vitro conditions, EgtD is not a substrate of protein kinase PknD.