Development of docetaxel nanocapsules for improving in vitro cytotoxicity and cellular uptake in MCF-7 cells

The aim of this study was to fabricate docetaxel loaded nanocapsules (DTX-NCs) with a high payload using Layer-by-Layer (LbL) technique by successive coating with alternate layers of oppositely charged polyelectrolytes. Developed nanocapsules (NCs) were characterized in terms of morphology, particle size distribution, zeta potential (ζ-potential), entrapment efficiency and in vitro release. The morphological characteristics of the NCs were assessed using transmission electron microscopy (TEM) that revealed coating of polyelectrolytes around the surface of particles. The developed NCs successfully attained a submicron particle size while the ζ-potential of optimized NCs alternated between (+) 34.64?±?1.5 mV to (?) 33.25?±?2.1 mV with each coating step. The non-hemolytic potential of the NCs indicated the suitability of the developed formulation for intravenous administration. A comparative study indicated that the cytotoxicity of positively charged NCs (F4) was significant higher (p?in vitro on MCF-7 cells. Furthermore, cell uptake studies evidenced a higher uptake of positive NCs (≥1.2 fold) in comparison to negative NCs. In conclusion, formulated NCs are an ideal vehicle for passive targeting of drugs to tumor cells that may result in improved efficacy and reduced toxicity of encapsulated drug moiety.     

Voltage Assisted Control of Spin-Transfer Nano-Oscillators

The spin-transfer nano-oscillator(STNO) has recently acquired a huge amount of research interest, due to its promising easy tunability along with the miniature size. The output frequency control of an STNO through magnetic field and current has been examined almost to its full extent; however, there are issues that still need to be addressed. Here, we propose a novel way of voltage control of the output frequency of an STNO, and alongside reducing its power requirement.     

Experimental study on combustion stability and performance of hydrogen-enriched compressed natural gas of a free-piston linear generator

Free Piston linear Generator (FPLG) engine fueled by compressed natural gas (CNG) has recently gained increased research attention. However, due to the low-velocity burning and poor lean limit of CNG fuel, the FPLG engine combustion stability, performance, and efficiency are still low. Hydrogen has a greater burning velocity with wider flame limits that could extend the lean burn limits and combustion characteristics of CNG. This paper compares pure CNG and 10% hydrogen-enriched CNG at various ignition speeds (0.6 ms, 0.8 m/s, and 1 m/s), injection positions (0 mm, 5 mm, 10 mm and 15 mm), and lambda ratios (0.9, 1.4 and 1.7) on the combustion characteristics, performance, and conversion efficiency are duly discussed. The findings show that the FPLG combustion stability limits increase with the hydrogen addition into the CNG. The CNG in-cylinder pressure increases significantly when the injection position is advanced, whereas the hydrogen addition reduces the influence of the injection position. The heat release rate increases by 15.62% and 23.72% with hydrogen addition, corresponding to the advanced and retarded injection positions. Consequently, the hydrogen addition increases the power RMS to 209.21 W and 232.64 W with an increment of 3.46% and 3.13%, respectively. Conclusively, the hydrogen addition into the CNG evidently shortens the combustion duration while improving the heat release rate, combustion stability, power RMS, Cycle-to-Cycle variation, and conversion efficiency.     

含膦酸酯结构单元的磺胺衍生物合成与抗菌活性

为了寻找抗菌候选化合物,采用基于片段的药物发现方法,以氨基膦酸酯和磺酰氯为原料,设计合成了15个含膦酸酯结构单元的磺胺衍生物,经IR、1HNMR和13CNMR确认结构。采用两倍稀释法测定目标化合物的MIC(最小抑菌浓度)。结果表明:部分目标化合物呈潜在的抗菌活性,对所测试标准菌和耐药菌均有抑制活性。其中,化合物Ⅱf〔N-[(二乙氧基膦酰基)-4-氟苯甲基]-4-甲氧基苯磺酰胺〕对金黄色葡萄球菌(S. aureus)、大肠埃希菌(E. coli)、耐甲氧西林金黄色葡萄球菌(MRSA)及耐氟喹诺酮类大肠杆菌(MREC)的MIC分别为32、64、128和128μg/mL,化合物Ⅱl〔N-[(二乙氧基膦酰基)-4-氟苯甲基]-4-氟苯磺酰胺〕对S. aureus、E. coli、MRSA及MREC的MIC分别为32、32、64和64μg/mL,抗菌活性优于对照药磺胺嘧啶。     

Survey on Passivity Based Control of Induction Machine

Induction machines (IM) constitute a theoretically interesting and practically important class of nonlinear systems. They are frequently used as wind generators for their power/cost ratio. They are described by a fifth‐order nonlinear differential equation with two inputs and only three state variables available for measurement. The control task is further complicated by the fact that IM are subject to unknown (load) disturbances and the parameters can be of great uncertainty. One is then faced with the challenging problem of controlling a highly nonlinear system, with unknown time‐varying parameters, where the regulated output, besides being unmeasurable, is perturbed by an unknown additive signal. Passivity‐based control (PBC) is a well‐established structure‐preserving design methodology which has shown to be very powerful to design robust controllers for physical systems described by Euler‐Lagrange equations of motion. PBCs provide a natural procedure to "shape" the potential energy yielding controllers with a clear physical interpretation in terms of interconnection of the system with its environment and are robust vis á vis to unmodeled dissipative effects. One recent approach of PBC is the Interconnection and Damping Assignment Passivity‐Based Control (IDA‐PBC) which is a very useful technique to control nonlinear systems assigning a desired (Port‐Controlled Hamiltonian) structure to the closed‐loop. The aim of this paper is to give a survey on different PBC of IM. The originality of this work is that the author proves that the well known field oriented control of IM is a particular case of the IDA‐PBC with disturbance.     

A Strategy for Discovering Heterochiral Bioactive Peptides by Using the OB2nP Library and SPOTs Method

d -Amino acid containing peptides are promising as drug lead compounds because of their expected higher stability in vivo. A heterochiral random peptide library called the one-bead–2ⁿ-peptide (OB2ⁿP) library, which can display 2ⁿ peptide diastereomers per bead, has been developed. Through screening of the OB2ⁿP library and subsequent binding assay among the peptide diastereomers synthesized in parallel by means of the SPOTs method, new heterochiral mimotopes for the anti-β-endorphin monoclonal antibody have been obtained. One mimotope was a new ligand for the μ-opioid receptor. The screening strategy enabled d -amino acid containing drug leads to be obtained efficiently by expanding searchable chemical space without increasing the experimental scale.     

Efficacious Doxorubicin Delivery Using Glutathione-Responsive Hollow Non-phospholipid Vesicles Bearing Lipoyl Cholesterols

In this study, we developed redox-sensitive vesicles using synthesised lipoyl cholesterol derivatives, a non-ionic surfactant and an optimum level of free cholesterol. Interestingly, concentration-dependent self-assembly was observed by scanning electron microscopy, wherein vesicles manifested as hollow spherical (at 0.15 mm ) and triangular (0.50 mm ). The redoxresponsive characteristics of the vesicles was probed in the presence of dithiothreitol; they underwent a clear increase in size as observed by dynamic light scattering measurements. These vesicles could easily encapsulate an anticancer drug, doxorubicin, and were observed to be stable in the presence of serum. They showed substantial release of the drug in response to biologically relevant stimulus, that is, glutathione. A toxicity assessment on HeLa and HepG2 cancer cells demonstrated activities of the drug-loaded vesicles comparable to that of free drug, whereas significantly enhanced toxicity and apoptotic induction were observed against drug-resistant HeLa cells, which was determined by studying the cellular internalisation of doxorubicin.