Resveratrol Encapsulation and Release from Pristine and Functionalized Mesoporous Silica Carriers

Resveratrol, a naturally occurring polyphenol, has attracted significant attention due to its antioxidant, cardioprotective and anticancer potential. However, its low aqueous solubility limits resveratrol bioavailability and use. In this work, different mesoporous silica matrices were used to encapsulate the polyphenol and to increase its dissolution rate. Pristine MCM-41, MCM-48, SBA-15, SBA-16, FDU-12 and MCF silica were obtained. The influence of SBA-15 functionalized with aminopropyl, isocyanate, phenyl, mercaptopropyl, and propionic acid moieties on resveratrol loading and release profiles was also assessed. The cytotoxic effects were evaluated for mesoporous carriers and resveratrol-loaded samples against human lung cancer (A549), breast cancer (MDA-MB-231) and human skin fibroblast (HSF) cell lines. The effect on apoptosis and cell cycle were assayed for selected resveratrol-loaded carriers. The polyphenol molecules are encapsulated only inside the mesopores, mostly in amorphous state. All materials containing either pristine or functionalized silica carriers increased polyphenol dissolution rate. The influence of the physico-chemical properties of the mesoporous carriers and resveratrol–loaded supports on the kinetic parameters was identified. Resv@SBA-15-SH and Resv@SBA-15-NCO samples exhibited the highest anticancer effect against A549 cells (IC50 values were 26.06 and 36.5 µg/mL, respectively) and against MDA-MB-231 (IC50 values were 35.56 and 19.30 µg/mL, respectively), which highlights their potential use against cancer.

Granulated Sugar-Containing Functional Products in Jelly Fillings

Introduction. Iodine is one of the most important elements for maintaining human health and cognitive skills. Contemporary food industry is looking for new functional foods fortified with macro- and micronutrients. Confectionery products occupy a fairly large segment of human diet. The present research objective was to substitute traditional white sugar with an experimental granulated sugar-containing product that contained maltodextrin, cane molasses, and Japanese kelp extract. This substitute could reduce the calorie content of jelly and increase its functional properties while maintaining its sensory profile, e.g. consistency, increasing its shelf-life, and simplifying the tec hnological process. Study objects and methods. Granulated sugar-containing product is a new component for the confectionery industry, but its effect on technological processes is unpredictable. The research featured an experimental granulated sugar-containing product with maltodextrin, cane molasses, and Japanese kelp. The growth rate of granules and their structure were studied by scanning microscopy and radiography, the granulometric composition and solubility – by determining the relative dissolution rate, the effect of the granulated sugar-containing product on the sensory and physicochemical parameters of jelly – by refractometry and titrometry. Results and discussion. The experimental granulated sugar-containing product contained sucrose both in crystalline and amorphous state, which affected the distribution of nutrients within the product. The growth rate of granules affected the resulting structure of the product and its solubility, which decreased by 2.5 times as the size of the granules grew. The dissolution rate decreased compared to crystalline sugar. As a result, the technological process of jelly production had to be adjusted. The developed jelly had a lower energy value and better nutritional qualities. The high content of vitamins and macro- and microelements makes it a functional product. The experimental jelly received 22.3 points for sensory profile. Its hysico-chemical parameters (soluble solids < 68%, acidity > 2.2 8%) met the standard requirements for this type of product. Conclusion. The new granulated sugar-containing product simplified the technological process and improved the sanitary, hygienic, and working conditions.

Application of Mathematical Models to Determine the Feasibility of Amorphous Drug Layering in Pan Coaters

Oral solid dosage forms that contain APIs in the amorphous state have become commonplace because of many drug substances exhibiting poor water solubility, which negatively impacts their absorption in the human GI tract. While micronization, solvent spray-drying, and hot-melt extrusion can address solubility issues, spray coating of the APIs onto beads and tablets offers another option for producing amorphous drug products. High-level comparisons between bead and tablet coating technologies have the potential for simpler equipment and operation that can reduce the cost of development and manufacturing. However, spray coating directly onto tablets is not without challenges, especially with respect to meeting uniformity acceptance value (AV) criteria, comprising accuracy (mean) and precision (variance) objectives. The feasibility of meeting AV criteria is examined, based on mathematical models for accuracy and precision. The results indicate that the main difficulty in manufacturing satisfactory drug-layered tablets by spray coating is caused by the practical limitations of achieving the necessary coating precision. Despite this limitation, it is shown that AV criteria can be consistently met by appropriate materials monitoring and control as well as processing equipment setup, operation, and maintenance.

Control of extrinsic porosities in linked metal-organic polyhedra gels by imparting coordination-driven self-assembly with electrostatic repulsion

The linkage of metal-organic polyhedra (MOPs) for the synthesis of porous soft materials is one of the promising strategies to combine processability with permanent porosity. Compared to the defined internal cavity of MOPs, it is still difficult to control the extrinsic porosities generated between crosslinked MOPs because of their random arrangements in their networks. Herein, we report a method to form linked MOP gels with controllable extrinsic porosities by introducing negative charges on the surface of MOPs that facilitates electrostatic repulsion between them. A hydrophilic rhodium-based cuboctahedral MOP (OHRhMOP) with 24 hydroxyl groups on its outer periphery can be controllably deprotonated to impart the MOP with tunable electrostatic repulsion in solution. This electrostatic repulsion between MOPs stabilizes the kinetically trapped state, in which a MOP is coordinated with various bisimidazole linkers in a monodentate fashion at a controllable link-er/MOP ratio. The heating of the kinetically trapped molecules leads to the formation of gels with similar colloidal networks but different extrinsic porosity. This strategy allows us to design the molecular-level networks and the resulting porosities even in the amorphous state.

Bioavailability Enhancement of Vitamin E TPGS Coated Liposomes of Nintedanib Esylate Formulation Developed Using Quality by Design Approach

PurposeNintedanib esylate (NE) is a kinase inhibitor designated for the cure of non-small cell lung cancer suffers from first-pass metabolism which resulted in low oral bioavailability (~4.7%). The intent of this exploration was to increase the oral bioavailability of NE by means of TPGS coated liposomes. MethodsThe NE-loaded TPGS coated liposomes were formulated by high-speed homogenization by optimizing process parameters like phospholipids: cholesterol molar ratio, drug loading and sonication time through the design of experiments. The drug's behaviour was studied using a variety of techniques, including physicochemical characterization, in-vitro and in-vivo studies. ResultsThe NE-liposomes had a particle size of 125±6.68 nm, entrapment efficiency of 88.64±4.12% and zeta potential of +46±2.75 mV. X-ray diffraction analysis revealed that NE had been converted to an amorphous state, while transmission electron microscope images showed spherical shape and smooth coating of TPGS on surface of liposomes. The formulation showed Higuchi kinetics with sustained drug release of 88.72 ± 3.40% in 24 hours. Cellular uptake of C-6 labelled liposomes was observed in A-549 cells and cytotoxicity testing revealed that NE-liposomes were more effective than marketed formulation Ofev®. Formulation remained in simulated fluids and for three months in stability chamber and. Liposomal oral bioavailability was ~6.23 times greater in sprague dawley male rats compared to marketed formulation Ofev®, according to in-vivo pharmacokinetic data. ConclusionNE-Liposomal formulations are better for oral administration compared to the marketed capsules because of the prolonged drug release and increased oral bioavailability as a result, the developed formulation can become a successful strategy in cancer chemotherapy.

Establishment and Characterization of Stable Zein/Glycosylated Lactoferrin Nanoparticles to Enhance the Storage Stability and in vitro Bioaccessibility of 7,8-Dihydroxyflavone

In this work, the lactoferrin (LF) was glycosylated by dextran (molecular weight 10, 40, and 70 kDa, LF 10K, LF 40K, and LF 70K) via Maillard reaction as a stabilizer to establish zein/glycosylated LF nanoparticles and encapsulate 7,8-dihydroxyflavone (7,8-DHF). Three zein/glycosylated LF nanoparticles (79.27–87.24 nm) with low turbidity (&lt;0.220) and polydispersity index (PDI) (&lt;0.230) were successfully established by hydrophobic interactions and hydrogen bonding. Compared with zein/LF nanoparticles, zein/glycosylated LF nanoparticles further increased stability to ionic strength (0–500 mM NaCl) at low pH conditions. Zein/glycosylated LF nanoparticles had nanoscale spherical shape and glycosylated LF changed surface morphology of zein nanoparticles. Besides, encapsulated 7,8-DHF exhibited an amorphous state inside zein/glycosylated LF nanoparticles. Most importantly, zein/glycosylated LF nanoparticles had good water redispersibility, high encapsulation efficiency (above 98.50%), favorable storage stability, and bioaccessibility for 7,8-DHF, particularly LF 40K. Collectively, the above research provides a theoretical reference for the application of zein-based delivery systems.

Влияние режима получения образцов и термообработки на локальную структуру халькогенидного полупроводника Ge-=SUB=-2-=/SUB=-Sb-=SUB=-2-=/SUB=-Te-=SUB=-5-=/SUB=-

Specifics of "amorphous state - crystal" phase transitions in dependence on the samples obtaining method and thermal processing, as well as changes in the structure and close range order in the arrangement of the atoms of Ge20Sb20.5Te51 chalcogenide semiconductors have been studied by the x-ray diffraction and Raman spectroscopy. It has been shown that Ge20Sb20.5Te51 films obtained by thermal evaporation on an unheated substrate are amorphous; after heat treatment at 220 and 400 °C, transform into a crystalline phase with a cubic and hexagonal structure. The chemical bonds and the main structural elements that form the matrix of the investigated objects, as well as the changes that occur in them during heat treatment, have been determined.

Pyrolytic Behavior of Long-Chain Alkyl Quaternary Ammonium Bromide Inside Nanopores

The pyrolytic behavior of organic matter inside nanopores was studied by simultaneous thermogravimetric/differential scanning calorimetry analyzer coupled with Fourier transform infrared spectroscopy (STA/TG-FTIR). Nanoporous silica was prepared by a hydrothermal method using long-chain alkyl quaternary ammonium bromide (CnTAB, n = 12, 14) as a template. The pyrolytic behavior of CnTAB inside nanopores with different diameters was investigated and compared with that of CnTAB inside and outside nanopores. The results showed that the pyrolytic removal process consisted of the following features: 1) CnTAB underwent carbon chain decomposition and oxidation; 2) the DSC exothermal peak of CnTAB came mainly from its oxidative combustion, and the oxidative combustion temperature decreased with increasing pore size; 3) the CnTAB inside nanopores underwent crystallization–amorphous state phase transition, and CnTAB got trapped inside the calcined nanopores. In addition, the pyrolytic behavior of CnTAB inside the calcined nanopores was found to be similar to that of the uncalcined nanopores. This study aims to understand the storage and transformation processes of organic hydrocarbons under nanopore-confinement effect.

EXPERIMENTAL METHODS FOR STUDYING THE RESOURCE VALUE OF DUMP BLAST FURNACE SLAGS

The study of the properties of blast-furnace slags requires an integrated approach, including various research methods. The purpose of the work is to substantiate the resource value of the Zaporizhstal dump blast furnace slag. The research methods were used: X-ray phase, petrographic, gamma-spectrometric analysis and electron probe microanalysis. The slag is dispersed into fractions, since the slag minerals have different hardness. Fractions (mm) were investigated in the work: >20 2.5–5, <0.63. X-ray phase analysis made it possible to reveal in the crystalline part of blast-furnace slag minerals that are technically valuable in the production of binders: 3CaO∙2SiO2, SiO2, 2CaO∙Al2O3∙SiO2, α-2CaO∙SiO2, 2CaO∙MgO∙2SiO2, α-CaO∙SiO2. Minerals akermanite, bredigite, pseudo-wollastonite have hydraulic activity. It is shown that the mass fraction of the amorphous component is half the mass of the blast furnace slag. The high content of substances in the amorphous state confirms the possibility of sorption of extraneous ions and compounds. The found elements Potassium, Sodium, Sulfur, Chlorine, Cuprum and Titanium are not part of the minerals. Slag contains less than 1% of the total amount of Fe, Ti and Cu, belonging to the 3rd class of hazardous substances. The maximum content of Potassium, Sodium and Titanium is typical for the fraction 2.5–5 mm. The most basic is the fraction <0.63 mm (pH 9.7), for the 2.5–5 mm fraction pH 9.1, the most acidic fraction >20 (pH 8.2). By the value of the toxicity index (4.3–5.4) and the III hazard class, dump blast furnace slag «Zaporizhstal» as a moderately hazardous waste can be used as a secondary raw material in the construction industry. The database on the content of natural radionuclides in technogenic raw materials has been updated. It has been proven that slag and its individual fractions contain natural radionuclides 40К, 226Ra, 232Th. The main contribution to the value of Сef is made by the 226Ra radionuclide, then by 232Th. The excess of specific activity is expressed for the 2.5–5 mm fraction. The I class of radiation hazard is defined, which allows the use of slag in construction without restrictions. Dump blast furnace slag «Zaporizhstal can be recommended in the production of inorganic binders « by the totality of chemical indicators.

Polylactic Acid Piezo-Biopolymers: Chemistry, Structural Evolution, Fabrication Methods, and Tissue Engineering Applications

Polylactide acid (PLA), as an FDA-approved biomaterial, has been widely applied due to its unique merits, such as its biocompatibility, biodegradability, and piezoelectricity. Numerous utilizations, including sensors, actuators, and bio-application—its most exciting application to promote cell migration, differentiation, growth, and protein–surface interaction—originate from the piezoelectricity effect. Since PLA exhibits piezoelectricity in both crystalline structure and an amorphous state, it is crucial to study it closely to understand the source of such a phenomenon. In this respect, in the current study, we first reviewed the methods promoting piezoelectricity. The present work is a comprehensive review that was conducted to promote the low piezoelectric constant of PLA in numerous procedures. In this respect, its chemistry and structural origins have been explored in detail. Combining any other variables to induce a specific application or to improve any PLA barriers, namely, its hydrophobicity, poor electrical conductivity, or the tuning of its mechanical properties, especially in the application of cardiovascular tissue engineering, is also discussed wherever relevant.