Instillation of Ophthalmic Formulation Containing Nilvadipine Nanocrystals Attenuates Lens Opacification in Shumiya Cataract Rats

We developed ophthalmic formulations based on nilvadipine (NIL) nanocrystals (NIL-NP dispersions; mean particle size: 98 nm) by using bead mill treatment and investigated whether the instillation of NIL-NP dispersions delivers NIL to the lens and prevents lens opacification in hereditary cataractous Shumiya cataract rats (SCRs). Serious corneal stimulation was not detected in either human corneal epithelial cells or rats treated with NIL-NP dispersions. The NIL was directly delivered to the lens by the instillation of NIL-NP dispersions, and NIL content in the lenses of rats instilled with NIL-NP dispersions was significantly higher than that in the ophthalmic formulations based on NIL microcrystals (NIL-MP dispersions; mean particle size: 21 µm). Moreover, the supply of NIL prevented increases in Ca2+ content and calpain activity in the lenses of SCRs and delayed the onset of cataracts. In addition, the anti-cataract effect in the lens of rats instilled with NIL-NP dispersions was also significantly higher than that in NIL-MP dispersions. NIL-NPs could be used to prevent lens opacification.

Balance of Drug Residence and Diffusion in Lacrimal Fluid Determine Ocular Bioavailability in In Situ Gels Incorporating Tranilast Nanoparticles

We previously designed ophthalmic formulations (nTRA) containing tranilast nanoparticles (Tra-NPs) with high uptake into ocular tissues. In this study, we used in situ gel (ISG) bases comprising combinations of pluronic F127 (F127) and methylcellulose (MC/F127), pluronic F68 (F68/F127), and Carbopol (Car/F127), and we developed in situ gels incorporating Tra-NPs (Tra-NP-incorporated ISNGs) such as nTRA-F127, nTRA-MC/F127, nTRA-F68/F127, and nTRA-Car/F127. Moreover, we demonstrated the therapeutic effect on conjunctival inflammation using lipopolysaccharide-induced rats. Each Tra-NP-incorporated ISNG was prepared by the bead mill method, the particle size was 40–190 nm, and the tranilast release and diffusion from formulation were nTRA > nTRA-F127 > nTRA-F68/F127 > nTRA-Car/F127 > nTRA-MC/F127. In the Tra-NP-incorporated ISNGs, the tranilast residence time in the lacrimal fluid, cornea, and conjunctiva was prolonged, although the Cmax was attenuated in comparison with nTRA. On the other hand, no significant difference in conjunctival inflammation between non- and nTRA-F127-instilled rats was found; however, the nTRA-F68/F127, nTRA-Car/F127, and nTRA-MC/F127 (combination-ISG) attenuated the vessel leakage, nitric oxide, and tumor necrosis factor-α expression. In particular, nTRA-F68/F127 was significant in preventing the conjunctival inflammation. In conclusion, we found that the combination-ISG base prolonged the residence time of Tra-NPs; however, Tra-NP release from the formulation was attenuated, and the Tmax was delayed longer than that in nTRA. The balance of drug residence and diffusion in lacrimal fluid may be important in providing high ocular bioavailability in formulations containing solid nanoparticles.

Preparation of the heat-resistant superhydrophobic coating with a nanostructured finish layer based on a suspension of silicon dioxide in a fluorinated film-former and its properties

The processes of obtaining compositions based on organosilicon resin for a heat-resistant coating of accelerated drying, as well as its hydrophobization by creating an isotropic nano-microstructure on the surface, are studied. It is shown that the chemical nature, the content of the ingredients and the thickness of the coatings have the greatest influence on the physicochemical properties of heat-resistant coatings. The methods of obtaining a composition for heat-resistant coatings using a dissolver and a bead mill in various modes of operation were studied, which allowed us to develop a technological process for manufacturing heat-resistant paint and varnish material. The composition and technology of obtaining a final hydrophobic layer based on a suspension of aerosil HDK 12H and carbon nanoparticles in a fluorine-containing varnish LF 32LN was developed in order to obtain a complex heat-resistant, superhydrophobic and anticorrosive coating for the protection of metal products and its properties were investigated.

Nanocrystalline Suspensions of Irbesartan Enhance Oral Bioavailability by Improving Drug Solubility and Leading Endocytosis Uptake into the Intestine

We attempted to design irbesartan nanocrystalline (IRB-NC) suspensions by the bead mill method, and we evaluated the bioavailability (BA) in the oral administration of the nanocrystalline drug. The mean particle size of the IRB-NC suspensions was approximately 140 nm, and the crystalline structure of irbesartan in these suspensions was different using the bead mill method. The aggregation and degradation of irbesartan were not observed for one month, and the solubility increased. Moreover, the inclusion complex formation of IRB-NC suspensions with 2-hydroxypropyl-β-cyclodextrin was higher than that in traditional IRB powder (IRB-P). In addition, the intestinal absorption of IRB-NC suspensions was higher than that of IRB-P suspensions, and the reducing effect on blood pressure in spontaneously hypertensive SHR-SP rats orally administered IRB-NC suspensions was significantly higher than in those administered IRB-P suspensions. On the other hand, the intestinal penetration of IRB-NC suspensions was attenuated by the inhibitors of clathrin-dependent endocytosis (CME). In conclusion, we improved the low oral BA of irbesartan by preparing IRB-NC suspensions and showed that both the solubility and CME are related to the enhanced intestinal absorption of IRB-NC suspensions, resulting in an increase in their antihypertensive effect. These findings provide significant information for the development of oral nanomedicines.

The Places of Products Localization and the Influence of this Factor on the Technological Characteristics

The search for optimal conditions for the method of synthesis of copper (II) salts to create a unified one-step method for obtaining salts from natural raw materials was the purpose of this work. During the process of salt production, it is desirable that the product accumulates in the solid phase and is easily separated by phase separation methods. The study of the direct interaction of copper (II) oxide with acids in organic liquid media using a bead mill as a reactor and grinding agent of different nature showed that besides the usual places of localization of product that take place in practice, we can meet unusual places of localization of product, such as the surface of a foreign solid phase in the reactor zone, for example, the surface of the grinding agent, reactor elements, etc. It was found that in some cases, localization on a solid surface could be a favorable localization option in terms of the speed of the process. But it happens not always, because it requires specific methods of separation of film from surface, which can be very expensive. Often, the localization of the product on the solid surfaces is an extremely unfavorable localization option. It was found that different variants of product localization of interaction CuO with acids which were implemented in different proportions, prevented the creation of a unified method for producing salts in such systems

Towards Efficient Luminescent Solar Energy Concentrator Using Cuprorivaite Infrared Phosphor (CaCuSi4O10)—Effect of Dispersing Method on Photoluminescence Intensity

Cuprorivaite, also known as Egyptian blue (EB), CaCuSi4O10, has been utilized as an important blue pigment for thousands of years. It shows a 430–800 nm broad excitation band and an intense 910–920 nm near-infrared (NIR) emission peak at room temperature. The application that motivates the current research is for luminescent solar concentrator (LSC) usage. Current technology for this purpose relies on high near-infrared reflectance. This article addresses the investigation of the relationship between dispersing methods and photoluminescence (PL) intensity. Mechanical grinding methods investigated in the study were: horizontal bead mill, exfoliation and three-roll mill. The initial aim of the study was to verify if the proposed methods do not damage PL. To the surprise of the authors, three-roll mill treatment enhanced PL by nearly 50% without altering the morphology of the powder. An X-ray diffraction study suggested slight alterations in the crystal lattice.

Energy-Dependent Endocytosis Is Responsible for Skin Penetration of Formulations Based on a Combination of Indomethacin Nanoparticles and l-Menthol in Rat and Göttingen Minipig

We previously designed a Carbopol gel formulation (N-IND/MEN) based on a combination of indomethacin solid nanoparticles (IND-NPs) and l-menthol, and we reported that the N-IND/MEN showed high transdermal penetration. However, the detailed mechanism for transdermal penetration of IND-NPs was not clearly defined. In this study, we investigated whether endocytosis in the skin tissue of rat and Göttingen minipig is related to the transdermal penetration of IND-NPs using pharmacological inhibitors of endocytosis. The pharmacological inhibitors used in this study are as follows: 54 µM nystatin, a caveolae-mediated endocytosis (CavME) inhibitor; 40 µM dynasore, a clathrin-mediated endocytosis (CME) inhibitor; and 2 µM rottlerin, a micropinocytosis (MP) inhibitor. The N-IND/MEN was prepared by a bead mill method, and the particle size of solid indomethacin was 79–216 nm. In both rat and Göttingen minipig skin, skin penetration of approximately 80% IND-NPs was limited by the stratum corneum (SC), although the penetration of SC was improved by the combination of l-menthol. On the other hand, the treatment of nystatin and dynasore decreased the transdermal penetration of indomethacin in rats and Göttingen minipigs treated with N-IND/MEN. Moreover, in addition to nystatin and dynasore, rottlerin attenuated the transdermal penetration of IND-NPs in the Göttingen minipigs’ skin. In conclusion, we found that l-menthol enhanced the SC penetration of IND-NPs. In addition, this study suggests that the SC-passed IND-NPs are absorbed into the skin tissue by energy-dependent endocytosis (CavME, CME, and/or MP pathways) on the epidermis under the SC, resulting in an enhancement in transdermal penetration of IND-NPs. These findings provide significant information for the design of nanomedicines in transdermal formulations.

Y2O3:Eu3+ Nanophosphor-Coated Mica or TiO2/Mica as Red-Emitting Pearl Pigment: Coating Factors, Luminescent and Gloss Properties

Red-emitted Y2O3:Eu3+ nanophosphor coated on a mica flake (Y2O3:Eu@MF) or on TiO2 having a rutile crystalline mica flake (Y2O3:Eu@TMF) has been prepared by an electrostatic interaction with the wet-coating method for the purpose of a pigment with luminescent and gloss properties. Aggregated Y2O3:Eu3+, prepared by the template method, was dispersed into nanosol by a controlled bead-mill wet process. The (+) charged Y2O3:Eu3+ nanosol was effectively coated on the (-) charged mica flake (MF) or the TiO2/mica flake (TMF) by an electrostatic interaction between the Y2O3:Eu3+ nanoparticles and MF or TMF at pH 6–8. The coating factors of Y2O3:Eu@MF were also studied and optimized by controlling the pH, stirring temperature, calcination temperature, and coating amount of Y2O3:Eu3+. The Y2O3:Eu3+ was partially coated and optimized on the MF or TMF surface with a coating coverage of about 40–50% or 60–70%, respectively. Y2O3:Eu@MF and Y2O3:Eu@TMF were exhibiting the luminescent property of a red color under a 254 nm wavelength, and had a color purity of over 95% according to CIE chromaticity coordinates. These materials were characterized by X-ray diffraction, FE-SEM, zeta potential, and a fluorescence spectrometer. These materials with luminescent and gloss properties prepared in this work potentially meet their applications for security purposes.

Optimization of cell wall disruption and lipid extraction methods by combining different solvents from wet microalgae

Microalgae have emerged as one of the most promising options for biodiesel production over the past few decades. Lipid extraction from microalgae for biodiesel production as a bottleneck of biodiesel production technology was the main purpose of this study. In this study different methods of the cell wall disruption were compared. Then, two methods of ultrasound and bead mill were used as methods of the cell wall disruption. The maximum lipid extracted by ultrasound was 17.10% and by bead mill was 15.16% (based on microalgae biomass dry weight). After the cell wall disruption of microalgae, for lipid extraction, chloroform-methanol solvent combination was used as a high extraction method and hexane-ethanol solvent combination was used as an environmentally friendly method. In this regard, the effect of solvent to biomass ratio, temperature and extraction time was investigated and the optimal results for chloroform-methanol solvent combination were 8 ml/g, 45°C and 60 minutes, respectively, and for hexane-ethanol combination were 6 ml/g, 35◦C and 73 minutes, respectively. Under these optimal conditions, the highest amount of extracted lipid from Chlorella vulgaris with a moisture content of 87.50%, and ultrasound as a cell wall disruption method were obtained 20.39% and 16.41% (based on microalgae dry weight) with a combination of chloroform-methanol solvents and hexane-ethanol respectively. Also the highest extraction rates of 17.63% and 13.85% were obtained for the combination of chloroform-methanol and hexane-ethanol solvents, respectively by bead milling as cell wall disruption method