Cup-shaped E,E-stilbenophane: synthesis,crystal structure and supramolecular chemistry

A new E,E-stilbenophane was synthesised and characterised. The crystal structure of this cyclophane shows that this molecule has a cup-shaped structure, which hosts a phenyl ring of neighbouring molecule as guest in its cavity with a π–π distance of about 3.7 Å. Moreover, the NMR spectra and theoretical analysis (gauge-independent atomic orbitals (GIAO) and quantum theory of atoms in molecules (QTAIM)) suggest that the silver recognition by E,E-stilbenophane host molecules is based on cation–π interactions in which the π-electrons of the double bonds play a major role.     

Screening Anti-Cancer Drugs against Tubulin using Catch-and-Release Electrospray Ionization Mass Spectrometry

Tubulin, which is the building block of microtubules, plays an important role in cell division. This critical role makes tubulin an attractive target for the development of chemotherapeutic drugs to treat cancer. Currently, there is no general binding assay for tubulin–drug interactions. The present work describes the application of the catch-and-release electrospray ionization mass spectrometry (CaR-ESI-MS) assay to investigate the binding of colchicinoid drugs to αβ-tubulin dimers extracted from porcine brain. Proof-of-concept experiments using positive (ligands with known affinities) and negative (non-binders) controls were performed to establish the reliability of the assay. The assay was then used to screen a library of seven colchicinoid analogues to test their binding to tubulin and to rank their affinities.

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Synthesis of high-modulus thermoset PUs of PCL-PTMG/CNW biomaterials with different soft domain architecture and composition for high shape memory performance

Cellulose - In this research work, a series of thermoset polyurethane (tPU) nanocomposites and a thermoplastic PU (TPPU) were synthesized using semi-crystalline polyols. Poly(ε-caprolactone)...     

The effect of solvent composition on vancomycin hydrochloride and free base vancomycin release from in situ forming implants

In situ forming drug delivery systems that are formed by solvent‐induced phase inversion have attracted extensive attention in sustained delivery of peptides and proteins. Based on the findings of our previous studies, N‐methyl‐2‐pyrrolidone (NMP) and acetone are two solvents that could improve the release profile of vancomycin from in situ forming systems based on poly(D,L‐lactide‐co‐glycolic acid). In this study, the effect of different compositions of these solvents on the release profile of hydrochloride and free base forms of vancomycin was investigated. To this end, several formulations with vancomycin (either hydrochloride or free base form) and different proportions of NMP and acetone were prepared. The cumulative drug release at specified time was determined and tested against conventional kinetic models. The surface and cross‐sectional morphology of implants were investigated by SEM. The experimental results showed that as solvent composition changed, the amount of vancomycin release during the first 12 h changed, too. The use of free base vancomycin resulted in an extended vancomycin release profile with less initial burst release. The formulation containing free base vancomycin and mixed solvents of acetone and NMP in 2:1 ratio released 70% of loaded drug in 6 weeks with near zero‐order kinetic. The best kinetic model to fit the in vitro release profiles was found to be Peppas–Sahlin model. Copyright © 2016 John Wiley & Sons, Ltd.     

Characterizing colloidal behavior of non-ionic emulsifiers in non-polar solvents using electrical impedance spectroscopy

Colloidal behavior of a widely used non-ionic emulsifier, sorbitan monooleate (Span80), was investigated in non-polar solvents (cyclohexane and xylene) using electrical impedance spectroscopy (EIS). The electrical characteristics of the colloidal mixtures were measured with frequency scans ranging from 1 Hz to 200 kHz. The conductances at low frequencies were found to increase with an increase in Span80 concentration. The source of conductivity for non-polar solvents using non-ionic emulsifiers is usually attributed to ionic impurities either in the Span80 or in the non-polar solvents. The measured electrical characteristics for pure Span80 and pure non-polar solvents revealed that the source of ionic conduction is impurities in Span80. It was confirmed that the ionic impurities in the non-polar solvents are in form of aggregate of ions, ion-pairs, and triple ions which is unaffected with the emulsifier concentration. Analyses using equivalent electrical circuits confirmed that the critical Maxwell-Wagner frequency is 0.6–1.8 Hz for the mixtures. The conductance-concentration profiles for the mixtures at 1 Hz showed transitions from a square root to a linear concentration dependence at the CMC. This indicated that the dissociation model holds below the CMC, while the fluctuation model applies above the CMC. The conductance profiles enabled estimates of the relative hydrophilic core radius and the fraction of charged micelles in both non-polar solvents. Figure

CMC determination of non-ionic emulsifier in non-polar solvents     

Electrical impedance spectroscopy study of piezoelectric PVDF membranes

Piezoelectric poly (vinylidene fluoride) (PVDF) membranes were prepared from pre-fabricated membranes by electrically poling in an intense electric field. The electrical impedance of PVDF membranes measured over a frequency range of 10^?2–10⁵ Hz before and after poling is presented. The effect of pressure on the impedance characteristics of un-poled and poled PVDF membranes was also studied. A four element model circuit, including a constant phase element (CPE) was fitted to the impedance spectra. The elements of the circuit fitted to the poled sample were more conductive compared with those of the un-poled sample. Stronger CPE elements in the circuit were detected in the poled samples under pressure suggesting that the piezoelectric activity of PVDF is the major contributor to the constant phase angle seen at low frequencies.