Development of a solid self-microemulsifying drug delivery system (SMEDDS) for solubility enhancement of naproxen

Context: Comparative evaluation of liquid and solid self-microemulsifying drug delivery systems (SMEDDS) as promising approaches for solubility enhancement.

Objective: The aim of this work was to develop, characterize, and evaluate a solid SMEDDS prepared via spray-drying of a liquid SMEDDS based on Gelucire® 44/14 to improve the solubility and dissolution rate of naproxen.

Material and methods: Various oils and co-surfactants in combination with Gelucire® 44/14 were evaluated during excipient selection study, solubility testing, and construction of (pseudo)ternary diagrams. The selected system was further evaluated for naproxen solubility, self-microemulsification ability, and in vitro dissolution of naproxen. In addition, its transformation into a solid SMEDDS by spray-drying using maltodextrin as a solid carrier was performed. Scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) were used to evaluate the physical characteristics of the solid SMEDDS obtained.

Results: The selected formulation of SMEDDS was comprised of Miglyol 812®, Peceol?, Gelucire® 44/14, and Solutol® HS 15. The liquid and solid SMEDDS formed a microemulsion after dilution with comparable average droplet size and exhibited uniform droplet size distribution. In the solid SMEDDS, liquid SMEDDS was adsorbed onto the surface of maltodextrin and formed smooth granular particles with the encapsulated drug predominantly in a dissolved state and partially in an amorphous state. Overall, incorporation of naproxen in SMEDDS, either liquid or solid, resulted in improved solubility and dissolution rate compared to pure naproxen.

Conclusion: This study indicates that a liquid and solid SMEDDS is a strategy for solubility enhancement in the future development of orally delivered dosage forms.     

Enhancing the electrical conductivity of carbon black/graphite nanoplatelets: Poly(ethylene‐butyl acrylate) composites by melt extrusion

The influence of processing parameters such as screw geometry, temperature profile, and screw speed on the electrical properties of hybrid composites consisting of graphite nanoplatelets and carbon black in ethyl butyl acrylate was studied. Two different screws were used to compound the hybrid composites at two different temperatures and two different screw speeds. A beneficial effect was noted with regard to the electrical properties when adding nanoplatelets to the filler system. The cause could be a synergistic effect due to the difference in particle shape of the two fillers. Lower percolation thresholds were obtained with the conventional screw due to less breakage of the graphite nanoplatelets compared to the barrier screw. No significant changes of the electrical properties were observed when changing the temperature profiles or the screw speeds. Furthermore, the melt viscosity of the compounds was not appreciably affected at the rather low filler contents used here. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 42897.     

Inline electron holography and VEELS for the measurement of strain in ternary and quaternary (In,Al,Ga)N alloyed thin films and its effect on bandgap energy

We present the use of (1) dark‐field inline electron holography for measuring the structural strain, and indirectly obtaining the composition, in a wurtzite, 4‐nm‐thick InAlGaN epilayer on a AlN/GaN/AlN/GaN multinano‐layer heterosystem, and (2) valence electron energy‐loss spectroscopy to study the bandgap value of five different, also hexagonal, 20–50‐nm‐thick InAlGaN layers. The measured strain values were almost identical to the ones obtained by other techniques for similarly grown materials. We found that the biaxial strain in the III‐N alloys lowers the bandgap energy as compared to the value calculated with different known expressions and bowing parameters for unstrained layers. By contrast, calculated and experimental values agreed in the case of lattice‐matched (almost unstrained) heterostructures.     

Titanium diffusion in shinbone of rats with osseointegrated implants

Dental implants are composed of commercially pure Ti (which is actually an alloy of titanium, and minor or trace components such as aluminium and vanadium). When the implant is inserted, its surface undergoes a number of chemical and mechanical processes, releasing particles of titanium to the medium. The metabolism of free ions of titanium is uncertain; the uptaking processes in the body are not well known, nor their toxic dose. In addition, physical properties of newly formed bone, such as diffusivity and activation energy, are scarce and rarely studied. In this study, we analysed the diffusion of titanium in the titanium‐implanted shinbones of six adult male Wistar rats by spatially resolved micro x‐ray fluorescence. The measurements were carried out at the microfluorescence station of the x‐ray fluorescence (XRF) beamline of the Brazilian synchrotron facility LNLS (from Portuguese ‘Laboratorio Nacional de Luz Sincrotron’). For each sample, XRF spectra were taken by linear scanning in area near the new bone formed around the Ti implant. The scanning line shows a clear effect of titanium diffusion whereas calcium intensity presents a different behaviour. Moreover, a clear correlation among the different structures of bones is observed in the Ti and Ca intensities. The results obtained in these measurements may allow determining quantitatively the parameters of diffusion rates and other physical properties of new bone like diffusion coefficients.     

Minimizing photodecomposition of flavin adenine dinucleotide fluorescence by the use of pulsed LEDs

Dynamic alterations in flavin adenine dinucleotide (FAD) fluorescence permit insight into energy metabolism‐dependent changes of intramitochondrial redox potential. Monitoring FAD fluorescence in living tissue is impeded by photobleaching, restricting the length of microfluorimetric recordings. In addition, photodecomposition of these essential electron carriers negatively interferes with energy metabolism and viability of the biological specimen. Taking advantage of pulsed LED illumination, here we determined the optimal excitation settings giving the largest fluorescence yield with the lowest photobleaching and interference with metabolism in hippocampal brain slices. The effects of FAD bleaching on energy metabolism and viability were studied by monitoring tissue pO₂, field potentials and changes in extracellular potassium concentration ([K⁺]_o). Photobleaching with continuous illumination consisted of an initial exponential decrease followed by a nearly linear decay. The exponential decay was significantly decelerated with pulsed illumination. Pulse length of 5 ms was sufficient to reach a fluorescence output comparable to continuous illumination, whereas further increasing duration increased photobleaching. Similarly, photobleaching increased with shortening of the interpulse interval. Photobleaching was partially reversible indicating the existence of a transient nonfluorescent flavin derivative. Pulsed illumination decreased FAD photodecomposition, improved slice viability and reproducibility of stimulus‐induced FAD, field potential, [K⁺]_o and pO₂ changes as compared to continuous illumination.     

Spread or backwash: The impact on population dynamics and business performance of a new road in a rural county of Galicia (Spain)

The natural experiment provided by the opening of a section that completed the A8 motorway in Mariña de Lugo, a rural area in Galicia (Spain), offers an opportunity to identify whether spread or backwash effects in economic activity are observed. The new section directly affects only a small strip of the territory—where the transition from the inland rural areas to the more dynamic coastal area takes place. This allows us to test a separate dual inner-coastal socio-economic performance after the opening of the new road—an analysis that has rarely been performed for rural areas in developed countries. We study the impact over population growth, employment and business financial results, using the differences-in-differences approach. The results we obtain are consistent with the spread hypothesis for the nearest municipality to the new road section, while the spread effects did not disseminate to the neighbouring municipalities. These global results hide a different performance at the sector level, positive for transport and manufacturing companies, and negative for retail firms and hospitality.     

Production of Ag−ZnO powders by hot mechanochemical processing

Ag–CdO composites are still one of the most commonly used electrical contact materials in low-voltage applications owing to their excellent electrical and mechanical properties. Nevertheless, considering the restriction on using Cd due to its toxicity, it is necessary to find alternative materials that can replace these composites. In this study, the synthesis of Ag?ZnO alloys from Ag?Zn solid solutions was investigated by hot mechanochemical processing. The hot mechanochemical processing was conducted in a modified attritor mill at 138 °C under flowing O₂ at 1200 cm³/min for 3.0 h. The microstructure and phase evolution were investigated using X-ray diffractometry, field emission gun scanning electron microscopy and transmission electron microscopy. The results suggest that it is possible to complete the oxidation of Ag?Zn solid solution by hot mechanochemical processing at a low temperature and short time. This novel synthesis route can produce Ag?ZnO composites with a homogeneous distribution of nanoscale ZnO precipitates, which is impossible to achieve using the conventional material processing methods. Considering the fact that the fundamental approach to improving electric contact material performance resides in obtaining uniform dispersion of the second-phase in the Ag matrix, this new processing route could open the possibility for Ag?ZnO composites to replace non-environmentally friendly Ag?CdO.     

Effect of Silicon and Graphite Degeneration on High-Temperature Oxidation of Ductile Cast Irons in Open Air

Oxidation of Metals - The use of high silicon ductile irons is increasing as they offer some advantages with respect to conventional pearlitic–ferritic grades such as high elongation at...