Surface modification of poly(lactide-co-glycolide) nanoparticles by d-α-tocopheryl polyethylene glycol 1000 succinate as potential carrier for the delivery of drugs to the brain

The potential health benefits of vitamin E (d-α-tocopheryl polyethylene glycol 1000 succinate, TPGS), particularly, in curing of the neurological symptoms associated with vitamin E deficiency have been reported. Hence, vitamin E containing carriers for delivery of drugs to the brain might be useful from different points of view. Herein, in order to obtain desired surface morphology and particle size of poly(lactide-co-glycolide) (PLGA) nanoparticles (NPs) and high emulsifying effects, TPGS-modified PLGA NPs were optimized as a potential carrier for the delivery of drugs to the brain. The particle sizes, surface morphology, phase composition correlated with different emulsifiers and different stirring times were characterized. Also, the in vitro cytotoxicity of the samples using PC12 cell line was investigated. According to the obtained results, by increasing the percentages of TPGS, the average particle size decreased and the distribution of particle diameters came closer by further addition, and the larger particles did not create. In addition, no obvious cytotoxicity was observed at various TPGS amounts, and the modified PLGA NPs were considered biocompatible since they show little decrease in cellular viability. With the increase of TPGS ratio, more effective in vitro therapeutic effects could be observed, which achieved the highest cell viability, because the degradation of NPs may release the most amounts of TPGS components that have synergistic activity. Furthermore, it was found that TPGS as a water-soluble derivative of natural source of vitamin E could be a perfect emulsifier for making PLGA NPs as potential carrier for delivery of drugs to the brain.     

Ultrasound mediated efficient ring opening of epoxides by in situ generated dithiocarbamates in green reaction media

Ultrasound accelerated a safe, clean and environmentally benign one-pot, three-component synthesis of 2-hydroxy dithiocarbamate, from amine, carbon disulfide and epoxide in good to excellent yields and short reaction time with excellent chemo-, regio-, and stereoselectivities in green reaction media (water, deep eutectic solvent [DES] and polyethylene glycol [PEG]). The one-pot, three-component condensation of primary and secondary amine with carbon disulfide and epoxides under ultrasonic irradiation was developed as a green and fast protocol for the rapid high-yielding preparation of 2-hydroxy dithiocarbamate in green reaction media without organic solvent and tedious workup.     

Diastereoselective synthesis of fused [1,3]thiazolo[1,3]oxazins and [1,3]oxazino[2,3-b][1,3]benzothiazoles

An efficient diastereoselective synthesis of 7-ethyl 5,6-dialkyl 7H-[1,3]thiazolo[2,3-b][1,3]oxazin-5,6, 7-tricarboxylates and 2-ethyl 3,4-dialkyl 2H-[1,3]oxazino [2,3-b][1,3]benzothiazole-2,3,4-tricarboxylates via reaction of thiazole and benzothiazole with dialkyl acetylenedicarboxylates in the presence of ethyl pyruvate is described.     

DFT investigation on some nitrogen-doped fullerenes with more antiradical and antioxidant activities than C60

Structural Chemistry - Although fullerene C60 is a strong scavenger for alkyl radicals, it is insusceptible toward peroxyl radicals. Substitution of carbon atoms in the fullerene cage by...     

Analysis of complexes pairing hydroperoxyl radical with peroxyformic acid

Ab initio quantum calculations are used to analyze the binding of complexes pairing OOH with HOOCHO. Six minima are located on the potential energy surface, all of cyclic geometry. Of particular interest are the OH...O and CH...O H-bonds that arise in the complexes and the manner in which these interactions influence the internal properties of the subunits. The analysis is complicated by the presence of an intramolecular H-bond in the unperturbed HOOCHO molecule, which must be broken in order to form the pair of intermolecular H-bonds that are responsible for the binding in the most stable complex. The CH bond of HOOCHO is contracted, and its stretching frequency undergoes a blue shift, when this group participates in a H-bond.     

Electro-Organic Synthesis of 2-Amino-3-cyano-benzofuran Derivatives Using Hydroquinones and Malononitrile

Abstract

In this work, electrochemical oxidation of hydroquinones has been studied in the presence of malononitrile as a nucleophile in aqueous solution using cyclic voltammetry and controlled potential coulometry. The results indicate that the quinones derived from hydroquinones participate in Michael addition and then intramolecular nucleophilic addition to yield benzofuran derivatives. The electrochemical synthesis of these new 2-amino-3-cyano-benzofuran derivatives has been performed successfully at a carbon-rod electrode in an undivided cell in good to excellent yields at room temperature.     

Synthesis and Characterization of Tungsten Trioxide/Polyaniline/Polyacrylonitrile Composite Nanofibers for Application as a Counter Electrode of DSSCs

Russian Journal of Electrochemistry - —Electrospinning and spin-coating techniques were used for the fabrication of polyacrylonitrile/polyaniline/WO3 (PAN/PANI/WO3) nanocomposite nanofibers...     

Green biosynthesis of silver nanoparticles using Callicarpa maingayi stem bark extraction

Different biological methods are gaining recognition for the production of silver nanoparticles (Ag-NPs) due to their multiple applications. The use of plants in the green synthesis of nanoparticles emerges as a cost effective and eco-friendly approach. In this study the green biosynthesis of silver nanoparticles using Callicarpa maingayi stem bark extract has been reported. Characterizations of nanoparticles were done using different methods, which include; ultraviolet-visible spectroscopy (UV-Vis), powder X-ray diffraction (XRD), transmission electron microscopy (TEM), scanning electron microscopy (SEM), energy dispersive X-ray fluorescence (EDXF) spectrometry, zeta potential measurements and Fourier transform infrared (FT-IR) spectroscopy. UV-visible spectrum of the aqueous medium containing silver nanoparticles showed absorption peak at around 456 nm. The TEM study showed that mean diameter and standard deviation for the formation of silver nanoparticles were 12.40 ± 3.27 nm. The XRD study showed that the particles are crystalline in nature, with a face centered cubic (fcc) structure. The most needed outcome of this work will be the development of value added products from Callicarpa maingayi for biomedical and nanotechnology based industries.     

One-pot synthesis of highly functionalized 1,2-dihydropyridines from primary alkylamines, alkyl isocyanides, and acetylenic esters

A novel one-pot isocyanide-based cascade four-component reaction between primary alkylamines, acetylenic esters, and alkyl isocyanides led to tetraalkyl 1-alkyl(aryl)-4-alkylamino-1,2-dihydropyridine-2,3,5,6-tetracarbxylates in good yields.