Improved Controlled Release and Brain Penetration of the Small Molecule S14 Using PLGA Nanoparticles

Phosphodiesterase 7 (PDE7) is an enzyme responsible for the degradation of cyclic adenosine monophosphate (cAMP), an important cellular messenger. PDE7’s role in neurotransmission, expression profile in the brain and the druggability of other phosphodiesterases have motivated the search for potent inhibitors to treat neurodegenerative and inflammatory diseases. Different heterocyclic compounds have been described over the years; among them, phenyl-2-thioxo-(1H)-quinazolin-4-one, called S14, has shown very promising results in different in vitro and in vivo studies. Recently, polymeric nanoparticles have been used as new formulations to target specific organs and produce controlled release of certain drugs. In this work, we describe poly(lactic-co-glycolic acid) (PLGA)-based polymeric nanoparticles loaded with S14. Their preparation, optimization, characterization and in vivo drug release profile are here presented as an effort to improve pharmacokinetic properties of this interesting PDE7 inhibitor.     

Concepts,processing, and recent developments in encapsulating essential oils

By the virtue of their olfactory, physicochemical, and biological characteristics, essential oils (EOs) have drawn wide attention as additives in daily chemicals like perfume or personal care products. Nevertheless, they are physicochemically unstable and susceptible to degradation or loss. Microencapsulation offers a feasible strategy to stabilize and prolong release of EO. This review summarizes the recognized benefits and functional properties of various preparation and characterization methods, wherein innovative fabrication strategies and their formation mechanisms are especially emphasized. Progress in combining detecting/measuring technologies with kinetic modelling are discussed, to give an integral approach of controlling the dynamic release of encapsulated EOs. Moreover, new development trends of EOs capsules are also highlighted.     

缓香型玉米醇溶蛋白微胶囊乳液的制备及应用

为改善皮革的特殊气味并提升其应用性能,该研究以玉米醇溶蛋白（Zein）、艾叶香精（AAE）以及普兰尼克F127等为原料,通过反溶剂法制备缓香型玉米醇溶蛋白微胶囊（AAE@ZMs）乳液,再将AAE@ZMs乳液与成膜剂己内酰胺改性酪素复配后应用于皮革涂饰。结果表明,Zein与F127、AAE和戊二醛通过化学交联和氢键相互作用,同时F127和AAE可使Zein中的氨基酸重排并发生荧光猝灭;制得的AAE@ZMs乳液中微胶囊平均粒径约为298.6 nm且具有较好的分散性和稳定性;AAE@ZMs的包覆率和负载率分别可以达到73.2%和5.8%,在良溶剂中释放120 h时的AAE累积释放率约为83.1%。将AAE@ZMs应用于皮革涂饰后,涂饰革样中AAE的释放周期为6周,对金黄色葡萄球菌和大肠杆菌均具有较好的抑制效果,同时涂饰革样还展现出较好的机械性能。     

负载活性组分的核壳结构纤维膜的制备及性能

采用同轴静电纺丝技术将蛛丝蛋白（Ss）和美洲大蠊提取物（PAE）分别负载于纳米纤维的壳层与核层。随着Ss的增加,纤维直径从350 nm降至280 nm,核层直径由120nm升至140 nm,壳层厚度由115 nm降至70 nm。Ss的加入使纳米纤维膜具有良好的机械性能和亲水性,纳米纤维膜的拉伸强度可达到4.31 MPa,溶胀率可达到150%,水蒸气透过率可达到1834 g/(m2?24h),水接触角减小到 32.7 ?。纳米纤维膜核壳结构能够有效抑制药物突释,实现药物长效释放,7天内药物释放可达77%;纳米纤维膜能够有效抑制细菌生长,促进细胞增殖,相较于未负载Ss的纳米纤维膜,负载20%Ss的纤维膜的细胞增殖效果提高25%,说明Ss和PAE在伤口愈合过程中能够起到协同作用。     

Poly(chitosan-ester-ether-urethane) Hydrogels as Highly Controlled Genistein Release Systems

Polymeric hydrogels play an increasingly important role in medicine, pharmacy and cosmetology. They appear to be one of the most promising groups of biomaterials due to their favorable physicochemical properties and biocompatibility. The objective of the presented study was to synthesize new poly(chitosan-ester-ether-urethane) hydrogels and to study the kinetic release of genistein (GEN) from these biomaterials. In view of the above, six non-toxic hydrogels were synthesized via the Ring-Opening Polymerization (ROP) and polyaddition processes. The poly(ester-ether) components of the hydrogels have been produced in the presence of the enzyme as a biocatalyst. In some cases, the in vitro release rate of GEN from the obtained hydrogels was characterized by near-zero-order kinetics, without “burst release” and with non-Fickian transport. It is important to note that developed hydrogels have been shown to possess the desired safety profile due to lack of cytotoxicity to skin cells (keratinocytes and fibroblasts). Taking into account the non-toxicity of hydrogels and the relatively highly controlled release profile of GEN, these results may provide fresh insight into polymeric hydrogels as an effective dermatological and/or cosmetological tool.     

Facile Fabrication of Povidone Iodine-Embedded Polytetrafluoroethylene Superhydrophobic Films with Improved Antiadhesive and Bactericidal Properties in Bacterial Environments

It remains a challenge to maintain the antiadhesion properties of superhydrophobic films after exposure to bacterial environments. In this work, superhydrophobic bactericidal polymer films via the simple incorporation of polyvinylpyrrolidone-iodine (PVP-I) or iodine into polytetrafluoroethylene (PTFE) are fabricated to improve their antiadhesive and antibacterial capability. Superhydrophobic iodine-embedded films, polytetrafluoroethylene/polyvinylpyrrolidone-iodine and polytetrafluoroethylene-iodine (PTFE/PVP-I and PTFE-I), show excellent antiadhesive and bactericidal performances even post exposure to bacterial solutions as compared to iodine-free counterparts by controlling the release of iodine. Especially, superhydrophobic PTFE/PVP-I films display a more sustained iodine release profile and significant antibacterial properties against gram-positive (S. aureus, methicillin-resistant S. aureus (MRSA)) and gram-negative (E. coli) bacteria. Such a facile combination of antiseptic agents and superhydrophobic surface could be widely used for antiseptic biomedical applications.     

Hypoxia/Temperature/pH Triple Stimuli–Responsive Block Copolymers: Synthesis,Self-Assembly,and Controlled Drug Release

The amphiphilic block copolymer poly(methacrylic acid-co-2-nitroimidazole acrylate)-b-poly(2-(N,N-dimethylamino)ethyl methacrylate) (P(MAA-co-NIMA)-b-PDMAEMA) with the hypoxia/temperature/pH triple responsiveness is synthesized by reversible addition-fragmentation chain transfer polymerization (RAFT), hydrolysis, and 3-(3-dimethylaminopropyl)-1-ethylcarbodiimide (EDC) reactions, and successfully self-assembled into micelles. The hypoxia response in vitro is realized, and then the sensitivity of the self-assembled micelles to the hypoxia condition is studied by controlling the grafting amount of aminated 2-nitroimidazole. Because 2-(N,N-dimethylamino) ethyl methacrylate (DMAEMA) is a typical material sensitive to temperature and pH conditions, the self-assembled micelles are also responsive to temperature and different acidic/basic conditions. In addition, the cumulative release rate of doxorubicin (DOX) at 42 °C, pH = 6.0, and hypoxic conditions increases significantly, and verifies the synergistic promotion effect of the above stimulations. This intelligent polymer with triple response mechanism improves the controllability and efficiency of drug release, and is expected to be a drug carrier for cancer treatment.     

中小电机新能效等级对无取向电工钢需求的影响

电机新能效等级标准的实施,对硅钢产品提出了更高的要求。本文结合中小电机、无取向电工钢的发展,分析了电机的损耗与硅钢性能的关系,并提出了新能效等级标准实施后对无取向电工钢的需求预测。     

基于PCA-RBF网络模型的硫化矿自燃安全性研究

为了更加准确地预测硫化矿自燃安全性,综合考虑硫化矿自燃倾向性及火灾后果严重性,将硫化矿自燃安全性划分为9个等级,并选取矿山含硫量、矿山含碳量、矿石温度、矿石堆放时间、采场人员数量、氧气浓度和采场矿层厚度作为评价因素集。利用主成分分析法（Principal Component Analysis,PCA）对94个采场样本数据进行降维处理,得到包含70%以上原始信息的3个主成分。将降维后的84组数据作为基于径向基函数神经网络（Radial Basis Function Neural Network,RBF）预测模型的训练样本,10组数据作为检验样本进行硫化矿自燃安全性预测。最后分别利用十折交叉验证法和留一法对94组检验样本的自燃安全性预测结果进行检验,得到硫化矿自燃安全性预测准确率分别为92.55%和91.49%。研究结果表明：PCA-RBF网络模型对硫化矿自燃安全性的预测性能良好,且优于未经主成分分析的结果。     

B级钢中频感应熔炼用镁砂坩埚的失效与防护

根据B级钢中频感应熔炼过程中镁砂坩埚的工作环境特点,指出坩埚失效的主要形式:热应力开裂、侵蚀变薄、表层剥落、钢液渗透、表面结渣等,并对其失效机理进行分析。通过调整镁砂的颗粒级配,采用多相复合技术,在坩埚的特定区域使用特定坩埚材料的分区捣筑、合理安排烧结工艺、精心操作、精心修补。从而提高了坩埚使用寿命。