Intracellular pH‐sensitive dextran‐based micelles as efficient drug delivery platforms

As drug delivery systems, stimuli‐responsive polymer micelles hold great potential in cancer chemotherapeutics to improve therapeutic efficiency and eliminate organism adverse effects. Here, pH‐sensitive polymeric micelles based on dextran‐g‐benzimidazole were designed and used for intracellular anticancer drug delivery. The anticancer drug doxorubicin (DOX) was effectively loaded into the micelles via hydrophobic interactions. In vitro release studies demonstrated that the release of loaded DOX was greater and faster under acid conditions such as in carcinomatous areas (pH < 6.8) than in physiological conditions (pH 7.4). MTT assays and flow cytometric analyses showed that DOX‐loaded micelles had higher cellular proliferation inhibition towards HeLa and HepG2 cells than pH‐insensitive controls. These pH‐sensitive micelles with significant efficiency for intracellular drug release will be beneficial to the future of in vivo biomedical applications. © 2014 Society of Chemical Industry     

换能器结构参数对聚合物超声塑化黏弹生热的影响

为研究超声换能器结构参数对聚合物超声塑化过程黏弹性生热的影响，首先确定超声黏弹性生热系统的组成，进行纵振超声换能器结构设计；然后分析超声黏弹性生热过程及超声黏弹性生热原理；最后采用单一变量法分析超声换能器的主要结构参数对其纵振频率及工具头前端质点最大振幅的影响，将其实际输出的纵振激励加载于熔融聚合物，研究其结构参数对聚合物超声黏弹性生热过程及达到聚合物玻璃化转变温度所用时间的影响。结果表明，随纵振激励作用时间的增加，聚合物温度非线性升高；放大比对聚合物温度变化影响最大，前盖板厚度和工具头长度次之，影响最小的是变幅杆长度。     

核电站放射性污染液压扭力扳手的去污实践

核电站在日常生产及大修过程中,放射性污染设备和场地的检修作业会产生一定量的污染检修工具,其中包含价值高、体积大、去污难度大的液压扭力扳手。因液压扭力扳手结构复杂、主子部件较多、且热点多淤积在死角位置,导致其放射性去污难度较大,国内核电站多作放射性固体废物处理为主。液压扭力扳手作为高价值专用工具,大量放射性污染检修工具报废给核电站成本管控、放射性废物最小化管理和电站辐射防护最优化带来了较大的压力。针对此问题, 电站开展了多项放射性污染液压扭力扳手深度去污试验,采用化学去污、机械去污、泡沫去污、超声波去污等多种组合工艺,经过四个阶段的深度去污试验,最终将多台放射性污染液压扭力扳手全部去污合格,并全部实现现场复用。此次深度去污试验研究总结的“放射性污染液压扭力扳手深度去污方法”,去污因子超过10³,去污试验各项指标效果良好,方法可行、有效、实用,可为业内同行提供参考。     

超声波辅助插层-剥离法制备煤系高岭土微粉的研究

我国煤系高岭土储量丰富,为满足造纸、纺织等行业个性化的需求,通常要对其进行深加工。以山西朔州煤系高岭土为原料,分别在恒温磁力搅拌和超声波作用下探究了煤系高岭土/二甲基亚砜(DMSO)插层复合物制备的最佳条件,在插层复合物的基础上对煤系高岭土进行超声辅助剥离,制备得到高岭土微粉,并利用XRD、SEM、BET、TG-DSC等方法分析表征样品。正交实验结果表明在磁力搅拌条件下DMSO用量、插层时间以及插层温度均对插层率具有一定的影响,引入超声波有利于高岭土插层率的提升。插层复合物经超声辅助剥离后晶粒厚度明显减小,高岭土片层状结构大体上呈现碎片化,仅保留少部分大的片状结构,其边缘碎化,整体上也出现碎裂的趋势。剥离样品的比表面积和孔径均大幅度增加,为硬质高岭土的剥离和超微细粉体的制备提供了新的思路。     

辅助电流对Cu/Al大功率超声波焊接的影响

为获得更高质量的Cu/Al异质金属接头，开展了Cu/Al电流辅助大功率超声波焊接工艺试验，研究了辅助电流对Cu/Al超声波焊接的界面温度、材料塑性流动、界面中间相分布及接头力学性能的影响。结果表明，复合焊件成型良好，其接头抗拉剪力为3030 N，接头的断裂模式为韧性-脆性复合断裂。在同样的焊接时间0.2 s内，随着电流的增大，Cu/Al界面温度增加，金属塑性流动以及界面扩散也随之增强，这说明辅助电流能明显促进界面冶金；相比长时间0.4 s的超声波焊接，辅助电流能在保证界面温度、材料塑性变形的前提下，能明显减薄了界面IMC层的厚度，这是电流增强Cu/Al接头的主要物理机制。研究结果为优化Cu/Al复合焊接头强度提供了参考。     

Kinetics of ultrasonic extraction of polyphenols,anthocyanins and tannins from five different New Zealand grape pomaces

Polyphenols were extracted from five kinds of New Zealand grape pomace (Sauvignon Blanc, Pinot Gris, Gerwurztraminer, Merlot and Pinot Noir) at 30, 50 and 70 °C in an ultrasonic generator. The extraction kinetics for total phenol, anthocyanin and tannin were determined. The results of dynamics study showed that the extraction of total polyphenols, anthocyanin and tannin followed first-order reaction kinetics during the extraction at 30, 50 and 70 °C. The total phenolic content, anthocyanin conten, and tannin content of water–ethanol extracts from grape pomaces were compared, and the parameters in the extraction kinetics equations were determined. The extraction results showed that the Pinot Noir pomace extract had the highest total phenolic content of 59.95 mg GAE g⁻¹ pomace and tannin content of 79.93 mg EE g⁻¹ pomace. The anthocyanin content in Merlot pomace extract was the highest, which was 4.50 CE g⁻¹ pomace. The results might be of great significance for the development of grape pomace or its polyphenol and/or anthocyanin components as an antioxidant source with natural and inexpensive benefits.     

Experimental Treatment with Favipiravir for COVID-19: An Open-Label Control Study

There is currently an outbreak of respiratory disease caused by a novel coronavirus. The virus has been named severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and the disease it causes has been named coronavirus disease 2019 (COVID-19). More than 16% of patients developed acute respiratory distress syndrome, and the fatality ratio was 1%–2%. No specific treatment has been reported. Herein, we examined the effects of favipiravir (FPV) versus lopinavir (LPV)/ritonavir (RTV) for the treatment of COVID-19. Patients with laboratory-confirmed COVID-19 who received oral FPV (Day 1: 1600 mg twice daily; Days 2–14: 600 mg twice daily) plus interferon (IFN)-α by aerosol inhalation (5 million international unit (IU) twice daily) were included in the FPV arm of this study, whereas patients who were treated with LPV/RTV (Days 1–14: 400 mg/100 mg twice daily) plus IFN-α by aerosol inhalation (5 million IU twice daily) were included in the control arm. Changes in chest computed tomography (CT), viral clearance, and drug safety were compared between the two groups. For the 35 patients enrolled in the FPV arm and the 45 patients in the control arm, all baseline characteristics were comparable between the two arms. A shorter viral clearance median time was found for the FPV arm versus the control arm (4 d (interquartile range (IQR): 2.5–9) versus 11 d (IQR: 8–13), P < 0.001). The FPV arm also showed significant improvement in chest CT compared with the control arm, with an improvement rate of 91.43% versus 62.22% (P = 0.004). After adjustment for potential confounders, the FPV arm also showed a significantly higher improvement rate in chest CT. Multivariable Cox regression showed that FPV was independently associated with faster viral clearance. In addition, fewer adverse events were found in the FPV arm than in the control arm. In this open-label before-after controlled study, FPV showed better therapeutic responses on COVID-19 in terms of disease progression and viral clearance. These preliminary clinical results provide useful information of treatments for SARS-CoV-2 infection.     

Pharmacokinetic Parameters of HIV-1 Protease Inhibitors

Since the beginning of the HIV epidemic, research has been carried out to control the virus. Understanding the mechanisms of replication has given access to the various classes of drugs that over time have transformed AIDS into a manageable chronic disease. The class of protease inhibitors (PIs) gained notice in anti-retroviral therapy, once it was found that peptidomimetic molecules act by blocking the active catalytic center of the aspartic protease, which is directly related to HIV maturation. However, mutations in enzymatic internal residues are the biggest issue for these drugs, because a small change in biochemical interaction can generate resistance. Low plasma concentrations of PIs favor viral natural selection; high concentrations can inhibit even partially resistant enzymes. Food-drug/drug-drug interactions can decrease the bioavailability of PIs and are related to many side effects. Therefore, this review summarizes the pharmacokinetic properties of current PIs, the changes when pharmacological boosters are used and also lists the major mutations to help understanding of how long the continuous treatment can ensure a low viral load in patients.     

承压设备插入式接管角焊缝超声相控阵检测工艺

插入式接管角焊缝的特殊结构和焊缝形式,增加了常规A型超声波对其检测的难度和工艺的复杂性。针对承压设备插入式接管角焊缝容易出现的几类典型缺陷,通过CIVA软件仿真制定检测工艺,同时采用以色列ISONIC 2009相控阵设备对模拟试块进行检测,并与CIVA仿真结果进行了比对。结果表明,插入式接管角焊缝的超声相控阵检测工艺具有良好的检测效果,验证了工艺的有效性,为相控阵检测技术在插入式接管角焊缝中的推广应用提供了相关经验。