Site-Specific PEGylation of Therapeutic Proteins

The use of proteins as therapeutics has a long history and is becoming ever more common in modern medicine. While the number of protein-based drugs is growing every year, significant problems still remain with their use. Among these problems are rapid degradation and excretion from patients, thus requiring frequent dosing, which in turn increases the chances for an immunological response as well as increasing the cost of therapy. One of the main strategies to alleviate these problems is to link a polyethylene glycol (PEG) group to the protein of interest. This process, called PEGylation, has grown dramatically in recent years resulting in several approved drugs. Installing a single PEG chain at a defined site in a protein is challenging. Recently, there is has been considerable research into various methods for the site-specific PEGylation of proteins. This review seeks to summarize that work and provide background and context for how site-specific PEGylation is performed. After introducing the topic of site-specific PEGylation, recent developments using chemical methods are described. That is followed by a more extensive discussion of bioorthogonal reactions and enzymatic labeling.     

Assessment of spray quality from an external mix nozzle and its impact on SQL grinding performance

Spray quality is the critical factor which decides the efficacy of Small Quantity Lubrication (SQL) technology in a high specific energy involved machining process like grinding. Yet, the understanding about spray quality, the actual process mechanics and its effect on machining performance is inadequate. The present work is an attempt to establish a correlation between the spray input variables, quality of the spray and machining performance of SQL grinding through modelling and experiments. Using computational fluid dynamic techniques, the variation of droplet size, droplet velocity, number of droplets and heat transfer coefficient have been analysed at different input parameters and the computed trends have been verified and validated. CFD modelling of spray indicates that it is possible to produce aerosol medium with high heat dissipation ability at moderately high air pressure and low flow rate. It also shows that any increase in atomising air pressure favourably leads to notable increase in wetting area and also results in substantial enhancement in heat dissipation ability. Reduction of residual stress is thus remarkably good. On the other hand, grinding fluid flow rate, if increased, offers significantly better lubricity and reduces the grinding force which also reduces tensile residual stress. Short spell grinding test results are found to be in good agreement with CFD results.     

Nature of heterophase inclusions in high-purity optical fiber materials as studied with 3D laser ultramicroscopy

3D laser ultramicroscopy (3D LUM) is intended specially for determining the concentration and size distribution of submicron inclusions in the bulk samples of high-purity materials for visible and IR fiber optics. In this work the 3D LUM technique is shown to be able to identify the nature of individual inclusions detected. The measurement of the light scattered by an inclusion at a varied probe beam wavelength and polarization and at a varied scattered light collection angle makes it possible to determine the inclusion refractive index. The 3D LUM possibilities are illustrated by the example of studying the inclusion nature in the As₂S₃ glass samples prepared by the direct synthesis from elements in a quartz container at elevated temperatures.     

Effects of structural characteristics on microwave dielectric properties of low-loss (Zn1-xNix)ZrNbTaO8 ceramics

Low-loss (Zn_1-xNi_x)ZrNbTaO₈ (0.02?≤?x?≤?0.10) ceramics possessing single wolframite structure are initiatively synthesized by solid-state route. Based on the results of Rietveld refinement, complex chemical bond theory is used to establish the correlation between structural characteristics and microwave performance in this ceramic system. A small amount of Ni²⁺ (x?=?0.06) in A-site with the fixed substitution of Ta⁵⁺ in B-site can effectually raise the Q?×?f value of ZnZrNb₂O₈ ceramic, embodying a dense microstructure and high lattice energy. The dielectric constant and τ_f are mainly affected by bond ionicity and the average octahedral distortion. The (Zn_0.94Ni_0.06)ZrNbTaO₈ ceramic sample sintered at 1150?°C for 3?h exhibits an outstanding combination of microwave dielectric properties: ε_r =?27.88, Q?×?f?=?128,951?GHz, τ_f =?–39.9?ppm/°C. Thus, it is considered to be a candidate material for the communication device applications at high frequency.     

Preparation and characterization of Fe‐Tetranitro phthalocyanine/polyurethane blends

In this article, Fe‐Tetranitro phthalocyanine (Fe‐TNPc)/polyurethane (PU) blends were prepared by solution blending. The mechanical properties of the samples were studied by tensile tests. The results showed that the tensile strength and the elongation at break of the samples increased with increasing Fe‐TNPc content. The improved mechanical properties for the samples containing Fe‐TNPc was attributed to the increased microphase separation degree of PU, which was further investigated by dynamic mechanical analysis (DMA) and Fourier transform infrared analysis. The lower T_g of the soft segments and the higher T_g of the hard segments for the samples containing Fe‐TNPc indicated an increase of microphase separation degree of PU. The increased hydrogen bonded carbonyl groups in the samples with increasing Fe‐TNPc content also proved the conclusion. Quantitative evaluation of the interaction between Fe‐TNPc and PU was also investigated by analyzing the physical crosslinking density of the samples. The results indicated that the physical crosslinking density of the samples increased with increasing Fe‐TNPc content. The antibacterial properties of the samples were investigated. The results showed that the percentage bacterial inactivation toward S. aureus and E. coli of the samples were 98.9% and 90.9%, respectively, when Fe‐TNPc was added to 1%. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 41284.     

Study of Compatibilized Liquid Crystalline Polymer/Cyclic Olefin Copolymer Blends

The technology to produce compatibilized blends of liquid crystalline polymer and highly amorphous cyclic olefin copolymers through two novel approaches were studied. The first approach was to use silane-functionalized halloysite nanotube as nonspecific compatibilizer and the second method was reactive compatibilization. The study of blends and their resulting microstructure; their thermal, mechanical, and viscoelastic properties were investigated. The kinetic study of blends compatibilized through both routes was performed.     

《化学制药单元操控》工学结合课程的教学探索

《化学制药单元操控》是一门新开发的将情景教学、实验操作和仿真实训相结合的工学结合课程。其中,引入化工仿真教学这一新型的教学方式,即通过在非常逼真的操作环境中进行技能训练,使学生对实际生产装置有更加感性的了解和认识。本文对《化学制药单元操控》工学结合课程开发与实施应用过程进行分析和总结得到几点经验,同时分享对该门课程教学改革中的一些心得。     

Mechanism of smoke suppression by melamine in rigid polyurethane foam

The smoke suppression of rigid polyurethane foam (RPUF) modified by melamine was investigated based on three sections: the condensed phase, the carbon layer, and the gas phase. In the condensed phase, the results of thermogravimetry, X‐ray photoelectron spectroscopy (XPS) N1S spectrum, and Fourier transform infrared spectroscopy indicated that melamine could suppress the degradation of RPUF by reacting with the aromatic hydrocarbons. It also reduced the smoke generation because the volatilizable aromatic hydrocarbons were the principal smoke precursors in a fire. In the carbon layer, the decrease from 38.50% to 24.76% of the inner layer oxygen content identified by XPS full‐spectrum and C1S spectrum indicated that melamine could prevent oxygen from transferring into the inner foam by the formation of an enhanced surface carbon layer, and the enhanced carbon layer could also block the release of smoke precursors. In the gas phase, the content of total aromatic hydrocarbons declined to 59.12% according to pyrolysis gaseous chromatography mass spectroscopy and indicated that melamine could reduce the smoke precursors. The results of smoke density chamber and cone calorimeter tests revealed that the addition of the melamine could decrease the smoke density of burning RPUF. Copyright © 2014 John Wiley & Sons, Ltd.