As small molecule drugs become harder to develop and less cost effective for patient use, efficient strategies for their property improvement become increasingly important to global health ...initiatives. Improvements in the physical properties of Active Pharmaceutical Ingredients (APIs), without changes in the covalent chemistry, have long been possible through the application of binary component solids. This was first achieved through the use of pharmaceutical salts, within the last 10–15years with cocrystals and more recently coamorphous systems have also been consciously applied to this problem. In order to rationally discover the best multicomponent phase for drug development, intermolecular interactions need to be considered at all stages of the process. This review highlights the current thinking in this area and the state of the art in: pharmaceutical multicomponent phase design, the intermolecular interactions in these phases, the implications of these interactions on the material properties and the pharmacokinetics in a patient.
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Rice bran oil bodies (RBOBs), as natural oil-in-water emulsions, can be used as a good carrier for delivering hydrophobic functional ingredients. In this work, the lutein ester-loaded rice bran oil ...body (LRBOB) emulsions were successfully prepared by restructuring the RBOBs natural structure through heat treatment and high-pressure homogenization. The physicochemical properties, photostability, and in vitro digestion of LRBOB emulsions with different oil body concentrations were investigated. The LRBOB emulsion with 50% RBOBs had maximum lutein ester encapsulation efficiency (94%) with larger mean particle size (566.44 ± 18.05 nm) and zeta potential (−43.87 ± 0.8 mV), exhibiting good physical stability and an amorphous structure of lutein ester. Meanwhile, the emulsion droplets formed a network structure through mutual adsorption, as observed by CLSM. Moreover, the apparent viscosity of LRBOB emulsion was increased with the increase of RBOBs concentration, showing a shear thinning behavior. Within the linear viscoelastic range, the emulsions mainly displayed elastic rheological characteristics. Furthermore, the photooxidation studies showed that the LRBOB emulsion retained a maximum of 37% lutein ester after 96 h of UV irradiation, and the half-life was extended to 58.89 h. Meanwhile, a higher amount of RBOBs effectively reduced lipid and protein oxidation and minimized color difference, indicating that RBOBs could effectively improve the stability of lutein ester. Based on the results of in vitro simulated digestion, LRBOB emulsion showed higher free fatty acid release (32%) and lutein ester bioaccessibility (40.17%) in the adult model, but is not recommended for infant diets. This work will provide a new delivery vehicle for the utilization of raw lutein materials, expanding the potential applications of natural plant oil bodies.
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•Lutein ester-loaded rice bran oil body (LRBOB) emulsions are successfully prepared.•The best lutein ester encapsulation efficiency and physical stability are optimized at 50% oil bodies.•LRBOB emulsions significantly enhanced the photostability of lutein ester.•Bioaccessibility of lutein ester was improved in the simulated adult digestion model.
This review discusses the imminent threat that microplastics (MPs) associated with pharmaceuticals represent to the aquatic environment and public health. We initially focused upon recognizing and ...stressing that MPs are ubiquitous pollutants. The influence of environmental factors, such as pH, mechanical stress, and photodegradation, are examined, aiming to elucidate how both substances might associate, what are their simultaneous degradation pathways and, to understand the interactions between MPs and pharmaceuticals. Mathematical tools, such as modeling and simulations, are presented in detail, aiming to improve how information is interpreted. Furthermore, it is exhibited that MPs sorption and interaction behavior towards organic contaminants play an important role in understanding its dynamics in the environment, as well as their possible interactions with pharmaceuticals that are summarized. At last, MPs and pharmaceuticals toxicity and bioaccumulation are presented.
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•Weathering heavily influence MPs sorption of organic contaminants.•Understanding MPs sorption modeling can improve further data interpretation.•MPs and pharmaceuticals, when combined, present increased toxicity.•MPs influence on pharmaceuticals degradation in the environment remains unclear.
Birefringent materials play indispensable roles in modulating the polarization of light and are vital in the laser science and technology. Currently, the design of birefringent materials operating in ...the deep-ultraviolet region (DUV, λ ≤200 nm) is still a great challenge. In this work, we developed a new DUV birefringent crystal LiBO
based on BO
infinite chains in the Li-B-O system, which simultaneously achieves the shortest UV cutoff edge (164 nm) and the largest birefringence (≥0.168 at 266 nm) among all the reported borate-based DUV birefringent materials. Single crystals of LiBO
with dimensions up to Ø55 × 34 mm
were grown by the Czochralski method, providing access to large-sized single crystal with low cost. Moreover, it has a high laser damage threshold and stable physicochemical properties. These outstanding characters unambiguously support that LiBO
can be an excellent birefringent material for DUV application.
•Green banana flour contains high amounts of resistant starch and phenolics.•Extrusion cooking of green banana flour changes physicochemical properties.•Properties of extruded green banana flour were ...influenced by feed moisture and screw speed.•Storing of extruded flours at 4°C increased the resistant starch content.
Green banana flour was extruded through a co-rotating twin-screw extruder with constant barrel temperature. The objectives of this study were to determine the effect of extrusion cooking variables (feed moisture, FM, 20% and 50%; screw speed, SS, 200 and 400rpm) and storing of the extruded flours at 4°C for 24h on the physicochemical properties, resistant starch (RS), pasting properties and antioxidant capacities. Extrusion cooking at higher FM and lower SS increased the amylose content, which was expressed in highest RS content. Water adsorption index (WAI) and pasting properties were increased, while water solubility index (WSI), total phenolic content (TPC) and antioxidant activities (FRAP, ABTS+, DPPH) in free and bound phenolics were decreased compared to the other extruded samples. Storing the extruded flours at 4°C for 24h prior to oven drying was the main factor leading to a further increase in the content of amylose, RS, TPC and WSI values, as well as pasting properties – in particular peak viscosity. Compared to native banana flour, extrusion cooking caused significant changes in all studied properties of the extruded flours, except for soluble DF and antioxidant capacity (ABTS+ and DPPH) of bound phenolics.
Tetrazoles via Multicomponent Reactions Neochoritis, Constantinos G; Zhao, Ting; Dömling, Alexander
Chemical reviews,
02/2019, Letnik:
119, Številka:
3
Journal Article
Recenzirano
Odprti dostop
Tetrazole derivatives are a prime class of heterocycles, very important to medicinal chemistry and drug design due to not only their bioisosterism to carboxylic acid and amide moieties but also to ...their metabolic stability and other beneficial physicochemical properties. Although more than 20 FDA-approved drugs contain 1H- or 2H-tetrazole substituents, their exact binding mode, structural biology, 3D conformations, and in general their chemical behavior is not fully understood. Importantly, multicomponent reaction (MCR) chemistry offers convergent access to multiple tetrazole scaffolds providing the three important elements of novelty, diversity, and complexity, yet MCR pathways to tetrazoles are far from completely explored. Here, we review the use of multicomponent reactions for the preparation of substituted tetrazole derivatives. We highlight specific applications and general trends holding therein and discuss synthetic approaches and their value by analyzing scope and limitations, and also enlighten their receptor binding mode. Finally, we estimated the prospects of further research in this field.
In this study, the effect of temperature (160–180 °C) and time (15–35 min) on functional properties, antioxidant activity, total phenolic content, the fatty acid composition of chia seed (Salvia ...hispanica L) flours were evaluated. Results showed roasting significantly increased the oil absorption capacity, water absorption index, water solubility index, water absorption capacity, and browning index and decreased moisture content of flours. Omega-3 (α-linoleic acid) was the main fatty acid detected in both raw and roasted chia seed flours followed with linoleic and oleic acids. Based on obtained results, at 180 °C, increasing the roasting time (15 to 25 min) significantly decreased the amount of chlorogenic acid and pyrocatechol from 0.15 (mg/g) and 1.5 (mg/g) in the raw sample to 0.11 (mg/g) and 1.25 (mg/g) in the chia seed flours roasted at 180 °C for 25 min, respectively. Fourier-transform infrared spectra showed roasting reduced the amount of polysaccharide (1740–1750 cm−1) and protein/lipid (2800–3000 cm−1) in samples. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis photograph showed roasting reduced the amounts of globulins S 7 and S 11 of chia seed flours. The current study explains the roasting at 180 °C for 35 min improved functional properties and total phenol content of chia seed flours.
The objective of this study was to investigate the impact of high-intensity ultrasound treatment (sonication) on the molecular, physicochemical, and functional properties of walnut protein isolate. ...Aqueous walnut protein suspensions were sonicated at varying power levels (200, 400 or 600 W) and times (15 or 30 min), and then any alternations in protein structure and properties were determined. SDS-PAGE demonstrated that there were no changes in protein electrophoretic patterns, indicating that sonication did not break covalent bonds. Circular dichroism spectroscopy indicated a small change in protein secondary structure after sonication, with a decrease in α-helix and increase in β-sheet, β-turn, and random coil content. There was an increase in surface free sulfhydryl (SH) groups and a decrease in fluorescence intensity after sonication, indicating that appreciable changes in tertiary structure occurred. Ultrasound reduced the size of the particles in aqueous walnut protein dispersions as confirmed by static light scattering and scanning electron microscopy, suggesting that sonication dissociated protein aggregates. Moreover, the water-solubility (+22%), emulsifying activity index (+26%), and emulsifying stability index (+41%) all increased after sonication. These results suggest that sonication is a valuable tool for improving the functional attributes of walnut proteins.
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•The impact of sonication on the properties of walnut protein isolate (WNPI) was evaluated.•SDS-PAGE showed that sonication did not alter the molecular weight of WNPI.•Circular dichroism and fluorescence indicated that sonication altered the structure of WNPI.•The water-solubility and emulsifying properties of WNPI were improved by sonication.•These results suggest that sonication may be used to improve walnut protein functionality.
This review systematically reports the pyrolysis of oily sludge (OS) from petroleum industry in regards to its dual features of the energy recovery potential and the environmental risks. The ...petroleum hydrocarbons are the nonbiodegradable fractions in OS that possess hazardous properties, i.e. ignitability and toxicity. Besides, complicated hazardous elements (i.e. N, S and Cl) and heavy metals inherently existing in OS further aggravate the environmental risks. However, the high oil content and heating value of OS contribute to its huge energy resource potential. Considering the energy demand and the environmental pressure, the ultimate purposes of the OS management are to enhance the oil recovery efficiency to minimize the oil content as well as to stabilize the hazardous elements and heavy metals into the solid residue. Among various OS management technologies, pyrolysis is the most suitable approach to reach both targets. In this review paper, the pyrolysis principle, the kinetics and the product distribution in three-phases are discussed firstly. Then the effects of operating parameters of the pyrolysis process on the quality and the application potential of the three-phase products, as well as the hazardous element distribution are discussed. To further solve the dominant concerns, such as the oil content in the solid residue, the pyrolytic oil quality and the migration of hazardous elements and heavy metals, the potentials of the catalytic pyrolysis and the co-pyrolysis with additives are also summarized. Also, the typical pyrolysis reactors are then presented. From the perspective of the energy efficiency and the non-hazardous disposal, the integrated technology combining the pyrolysis and the combustion for the OS management is recommended. Finally, the remaining challenges of OS pyrolysis encountered in the research and the industrial application are discussed and the related outlooks are itemized.
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•Energy recovery and non-hazardous disposal are dual targets for OS pyrolysis.•The OS characteristics with energy potential and environmental risk are summarized.•This review focuses on valuable products distribution and harmful components flow.•The advantages and future challenges for OS pyrolysis are proposed and outlooked.
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