Preparation of Co-Processed Excipients for Controlled-Release of Drugs Assembled with Solid Lipid Nanoparticles and Direct Compression Materials

The purpose of the study was to develop a novel, directly compressible, co-processed excipient capable of providing a controlled-release drug system for the pharmaceutical industry. A co-processed powder was formed by adsorption of solid lipid nanoparticles (SLN) as a controlled-release film onto a functional excipient, in this case, dicalcium phosphate dihydrate (DPD), for direct compression (Di-Tab^®). The co-processed excipient has advantages: easy to implement; solvent-free; industrial scaling-up; good rheological and compressibility properties; and the capability to form an inert platform. Six different batches of Di-Tab^®:SLN weight ratios were prepared (4:0.6, 3:0.6, 2:0.6, 1:0.6, 0.5:0.6, and 0.25:0.6). BCS class III ranitidine hydrochloride was selected as a drug model to evaluate the mixture’s controlled-release capabilities. The co-processed excipients were characterized in terms of powder rheology and dissolution rate. The best Di-Tab^®:SLN ratio proved to be 2:0.6, as it showed high functionality with good flow and compressibility properties (Carr Index = 16 ± 1, Hausner Index = 1.19 ± 0.04). This ratio could control release for up to 8 h, so it fits the ideal profile calculated based on biopharmaceutical data. The compressed systems obtained using this powder mixture behave as a matrix platform in which Fickian diffusion governs the release. The Higuchi model can explain their behavior.     

Intrinsic Apyrase-Like Activity of Cerium-Based Metal–Organic Frameworks (MOFs): Dephosphorylation of Adenosine Tri- and Diphosphate

Apyrase is an important family of extracellular enzymes that catalyse the hydrolysis of high-energy phosphate bonds (HEPBs) in ATP and ADP, thereby modulating many physiological processes and driving life activities. Herein, we report an unexpected discovery that cerium-based metal–organic frameworks (Ce-MOFs) of UiO-66(Ce) have intrinsic apyrase-like activity for ATP/ADP-related physiological processes. The abundant Ce^III/Ce^IV couple sites of Ce-MOFs endow them with the ability to selectively catalyse the hydrolysis of HEPBs of ATP and ADP under physiological conditions. Compared to natural enzymes, they could resist extreme pH and temperature, and present a broad range of working conditions. Based on this finding, a significant inhibitory effect on ADP-induced platelet aggregation was observed upon exposing the platelet-rich plasma (PRP) to the biomimetic UiO-66(Ce) films, prefiguring their wide application potentials in medicine and biotechnology.     

Enantioselective Approach for Expanding the Three-Dimensional Space of Tetrahydroquinoline to Develop BET Bromodomain Inhibitors**

The pharmaceutical industry has a pervasive need for chiral specific molecules with optimal affinity for their biological targets. However, the mass production of such compounds is currently limited by conventional chemical routes, that are costly and have an environmental impact. Here, we propose an easy access to obtain new tetrahydroquinolines, a motif found in many bioactive compounds, that is rapid and cost effective. Starting from simple raw materials, the procedure uses a proline-catalyzed Mannich reaction followed by the addition of BF₃ ⋅ OEt₂, which generates a highly electrophilic aza-ortho-quinone methide intermediate capable of reacting with different nucleophiles to form the diversely functionalized tetrahydroquinoline. Moreover, this enantioselective one-pot process provides access for the first time to tetrahydroquinolines with a cis-2,3 and trans-3,4 configuration. As proof of concept, we demonstrate that a three-step reaction sequence, from simple and inexpensive starting compounds and catalysts, can generate a BD2-selective BET bromodomain inhibitor with anti-inflammatory effect.     

The Morphology and Mechanical Properties of Isotactic Polypropylene Injection-Molded Samples with the Presence of β-Nucleation Agent and Periodical Shear Field

The pressure vibration injection molding (PVIM) method was used to prepare β-nucleated isotactic polypropylene samples (PVIM β-iPP samples); a relatively low, periodical shear was imposed on the polymer melt in the mold at the filling and packing stages. The crystal structures and crystal orientation of the PVIM β-iPP samples were investigated by polarizing light microscopy (PLM), scanning electron microscopy (SEM), and synchrotron two-dimensional wide-angle X-ray diffraction (2D-WAXD). The PLM observations indicated that a cylindrite layer, rather than the transition layer, was found in PVIM β-iPP samples, which is different from the conventional injection-molded (CIM) samples. In addition, the thickness of the oriented layer of the PVIM samples was obviously greater than that of the CIM samples. The SEM observations demonstrated that a large amount of shish-kebab structures appeared in the shear layer of the PVIM β-iPP samples; at the same time, numerous β-spherulites were formed in the core layer. The 2D-WAXD data indicated that orientation homogeneity, to some degree, could be obtained by the periodical shear during PVIM. As a result, the above-mentioned morphology of the PVIM β-iPP samples leads to potentially useful prominent reinforcement and toughening of the material.     

Crystal structure of decacalcium tetrapotassium hexakis (pyrophosphate) nonahydrate

The crystal structure of Ca₁₀K₄(P₂O₇)₆·9H₂O has been determined by single crystal X-ray diffraction. Crystals are hexagonal, space group P6₃cm witha=11.761(1),c=9.770(1) Å, andZ=1. The structure was refined toR=0.028 andR _w=0.037 for 468 reflections withI3(I). The structure consists of a compact assembly of Ca and P₂O₇ ions arranged in layers perpendicular to thec-axis in a hexagonal array with relatively large open channels along thec-axis. The K ions and the water molecules are located in these open channels and are disordered.Certain commercial materials and equipments are identified in this paper to specify the experimental procedure. In no instance does such identification imply recommendation or endorsement by the National Institute of Standards and Technology or the ADA Health Foundation or that the material or equipment identified is necessarily the best available for the purpose.     

Carbonyl polymeric electrode materials for metal-ion batteries

This review presents the recent progress in carbonyl polymeric electrode materials for lithium-ion batteries, sodium-ion batteries and magnesiumion batteries. This comprehensive review is expected to be helpful for arousing more interest of organic materials for metal-ion batteries and designing novel battery materials with high performance.     

High-performance organic electrolyte supercapacitors based on intrinsically powdery carbon aerogels

Powdery carbon aerogel with an ideal hierarchical pore structure shows impressive capacitive performances when utilized as electrodes for organic electrolyte supercapacitors.     

Structural and spectroscopic studies of LaPO4:Ce/Tb@LaPO4@SiO2 nanorods: Synthesis and role of surface coating

Highly fluorescent LaPO₄:Ce/Tb@LaPO₄@SiO₂ (core/shell/Si) nanorods(NRs) were fabricated with an average length 100 nm by co-precipitation process at low temperature. X-ray diffraction (XRD), Transmission electron microscopy (TEM), energy dispersive X-ray analysis, Fourier transform infrared, optical absorption and photoluminescence spectral techniques were applied to investigate the crystal structure, phase purity, morphology, surface chemistry and optical properties of the as-prepared samples. XRD results confirmed the formation of highly crystalline with single phase, monoclinic type structure. TEM image illustrates the poly-dispersed, narrow size distributed, irregular size rod-shaped nanostructures, with mean diameters of 20 nm and average lengths up to 140 nm. FTIR spectral analysis confirmed the silica surface modification. The comparative emission spectral study shows highest luminescence intensity of core/shell NRs, due to a reduction in nonradiative transition rate. The emission intensity enhancement proves that growing of an inert LaPO₄ layer on the surface of luminescent core-NRs was an effective way to suppress surface related quenching mechanism. These well crystalline, highly aqueous soluble along with extraordinary colloidal stability core/shell/Si NRs were extremely suitable material in fluorescent bio-labeling applications.     

A new method of using supercritical carbon dioxide as a green solvent for synthesis and purification of 5,5‴-bis(tridecafluorohexyl)-2,2′:5′,2″:5″,2‴-quaterthiophene,which is one of n-type organic semiconducting materials

We have investigated synthesis as well as purification of 5,5?-bis(tridecafluorohexyl)-2,2′:5′,2″:5″,2?-quaterthiophene (BFH-4?T, n-type organic semiconducting material) using supercritical carbon dioxide (scCO₂) as a green solvent. BFH-4T was obtained in good selectivity and high yield by TDAE/PdCl₂-catalyzed reductive coupling reaction of 5-bromo-5′-(tridecafluorohexyl)-2,2′-bithiophene in scCO₂. We have also successfully established purification of the reaction mixture by passing scCO₂ in the reaction vessel. The product was yellow powder of BFH-4T with purity of more than 99% and Pd catalyst was not contained.     

Solution-processable high-efficiency bis(trifluoromethyl)phenyl functionalized phosphorescent neutral iridium(III) complex for greenish yellow electroluminescence

A novel and highly efficient bis(trifluoromethyl)phenyl functionalized iridium(III) complex is designed and synthesized. The complex shows intensive greenish yellow phosphorescence (525?nm with 563?nm as shoulder), high photoluminescence efficiency (0.90) and moderate full width at half maximum (72?nm). The bulky bis(trifluoromethyl)phenyl moiety introduced into the complex provides the excellent solubility and effective steric hindrance for solution-processed organic light-emitting diodes. The maximum power efficiency and current efficiency of electroluminescence are 4.13?lm/W and 9.54?cd/A, respectively.