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.     

Macrophage Immunomodulation Through New Polymers that Recapitulate Functional Effects of Itaconate as a Power House of Innate Immunity

Itaconate (ITA) is an emerging powerhouse of innate immunity with therapeutic potential that is limited in its ability to be administered in a soluble form. A library of polyester materials that incorporate ITA into polymer backbones resulting in materials with inherent immunoregulatory behavior is developed. Harnessing hydrolytic degradation release from polyester backbones, ITA polymers result in the mechanism specific immunoregulatory properties on macrophage polarization in vitro. In a functional assay, the polymer-released ITA inhibits bacterial growth on acetate. Translation to an in vivo model of biomaterial associated inflammation, intraperitoneal injection of ITA polymers demonstrate a rapid resolution of inflammation in comparison to a control polymer silicone, demonstrating the value of sustained biomimetic presentation of ITA.     

An image watermarking based on the pdf modeling and quantization effects in the wavelet domain

An image watermarking technique based on the concept of JPEG2000 algorithm is proposed. Biorthogonal wavelet 9/7 transform is used to provide a set of coefficients suitable for watermark embedding. The statistical properties of different subbands are analyzed in order to choose the number of decomposition levels and position of subbands, which will assure the best compromise between the watermark transparency and robustness. The JPEG2000 quantization is applied to avoid insignificant wavelet coefficients, while the remaining ones are used for watermarking. The optimal and blind watermark detection is based on the nonlinear score function and appropriate model of coefficients distribution. The performance of the proposed procedure is tested on examples with various images, showing robustness under different attacks, while maintaining high image quality.     

Simultaneous electrolytic production of xylitol and xylonic acid from xylose

A new electrocatalytic process for simultaneous electrolytic production of xylitol and xylonic acid or the corresponding xylonate salts directly from -d-xylose in alkaline solutions of neutral salt as supporting electrolyte has been developed and presented. An electrocatalytically active cathode coating with essentially hydridic features has been employed to enhance Faradaic yields in xylitol production at low current densities by heterogeneous reaction of hydrogenation with H-adatoms, and the entire mechanism has been proved by experimental evidence. An anionic selective anodic coating for titanium substrate was also used to suppress oxygen evolution and optimize the xylonic acid production by direct oxidation with anodically generated bromine, and to carry out the electrode process at almost equilibrium potential. The kinetic effect of specifically adsorbable anions for decreasing cathodic current yields in xylitol production and the resulting necessity for membrane separation of catholyte from anolyte, with proper optimization of the supporting neutral salt composition, has also been emphasized.Paper partly presented at 39th and 40th ISE-Meetings at Glasgow UK, 1988 and Kyoto, Japan, 1989.     

Bee colony optimization for the p-center problem

Bee colony optimization (BCO) is a relatively new meta-heuristic designed to deal with hard combinatorial optimization problems. It is biologically inspired method that explores collective intelligence applied by the honey bees during nectar collecting process. In this paper we apply BCO to the p-center problem in the case of symmetric distance matrix. On the contrary to the constructive variant of the BCO algorithm used in recent literature, we propose variant of BCO based on the improvement concept (BCOi). The BCOi has not been significantly used in the relevant BCO literature so far. In this paper it is proved that BCOi can be a very useful concept for solving difficult combinatorial problems. The numerical experiments performed on well-known benchmark problems show that the BCOi is competitive with other methods and it can generate high-quality solutions within negligible CPU times.     

Thermally Induced Microstructural Transformations of Fe72Si15B8V4Cu1 Alloy

Thermal stability, mechanism, and kinetics of thermally induced microstructural transformations and their effects on magnetic permeability of Fe₇₂Si₁₅B₈V₄Cu₁ alloy with combined amorphous/nanocrystalline structure were studied. DTA curves revealed two separated thermally activated exothermic events in the temperature ranges from 740 K to 820 K (467 °C to 547 °C) and 870 K to 930 K (597 °C to 657 °C). Crystalline phases present in the as-prepared and thermally treated alloy samples were identified, and their microstructural parameters were determined using XRD, while, to gain further insight into the mechanism of microstructural transformations, AFM and SEM–EDS analyses were performed. Deconvolution of the complex DTA peak into individual steps was conducted, and, in correlation with the results of microstructural analysis, kinetic triplets corresponding to individual transformation steps were determined, allowing for the estimation of the lifetimes of the alloy at different temperatures. Magnetic permeability measurements showed that, in spite of the influence of microstructural transformations on magnetic properties of the alloy, the favorable magnetic properties are retained over relatively a wide temperature range.

     

Determination of 200 °C Isothermal Section of Al-Ag-Ga Phase Diagram by Microanalysis,X-ray Diffraction,Hardness and Electrical Conductivity Measurements

Ternary Al-Ag-Ga system at 200 °C was experimentally and thermodynamically assessed. Isothermal section was extrapolated using optimized thermodynamic parameters for constitutive binary systems. Microstructure and phase composition of the selected alloy samples were analyzed using light microscopy, scanning electron microscopy combined with energy-dispersive spectrometry and x-ray powder diffraction technique. The obtained experimental results were found to be in a close agreement with the predicted phase equilibria. Hardness and electrical conductivity of the alloy samples from four vertical sections Al-Ag₈₀Ga₂₀, Al-Ag₆₀Ga₄₀, Ag-Al₈₀Ga₂₀ and Ag-Al₆₀Ga₄₀ of the ternary Al-Ag-Ga system at 200 °C were experimentally determined using Brinell method and eddy current measurements. Additionally, hardness of the individual phases present in the microstructure of the studied alloy samples was determined using Vickers microhardness test. Based on experimentally obtained results, isolines of Brinell hardness and electrical conductivity were calculated for the alloys from isothermal section of the ternary Al-Ag-Ga system at 200 °C.