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N Willecke, A Szepes, M Wunderlich, J P Remon, C Vervaet, T De Beer
The overall objective of this work is to understand how excipient characteristics influence the drug product quality attributes and process performance of a continuous twin screw wet granulation process. The knowledge gained in this study is intended to be used for Quality by Design (QbD)-based formulation design and formulation optimization. Three principal components which represent the overarching properties of 8 selected pharmaceutical fillers were used as factors, whereas factors 4 and 5 represented binder type and binder concentration in a design of experiments (DoE)...
April 20, 2018: International Journal of Pharmaceutics
Christoph A Umbricht, Martina Benesova, Roger Schibli, Cristina Müller
The treatment of metastatic castration-resistant prostate cancer (mCRPC) remains challenging with current treatment options. The development of more effective therapies is, therefore, urgently needed. Targeted radionuclide therapy with prostate-specific membrane antigen (PSMA)-targeting ligands has revealed promising clinical results. In an effort to optimize this concept, it was the aim of this study to design and investigate PSMA ligands comprising different types of albumin binders. PSMA-ALB-53 and PSMA-ALB-56 were designed by combining the glutamate-urea PSMA-binding entity, a DOTA chelator and an albumin binder based on the 4-(p-iodophenyl)-moiety or p-(tolyl)-moiety...
April 23, 2018: Molecular Pharmaceutics
Dingtao Ma, Yongliang Li, Hongwei Mi, Shan Luo, Peixin Zhang, Zhiqun Lin, Jianqing Li, Han Zhang
The sluggish sodium reaction kinetics, unstable Sn/Na2O interface and large volume expansion are major obstacles that markedly impede practical applications of SnO2-based electrodes for sodium-ion batteries (SIBs). Herein, we report the crafting of homogeneously confined oxygen vacancy-containing SnO2-x nanoparticles with well-defined void space in porous carbon nanofibers (denoted SnO2-x/C composites) that address the issues noted above for advanced SIBs. Notably, SnO2-x/C composites can be readily exploited as the working electrode, dispensing with the need for the use of binders and conductive additives...
April 23, 2018: Angewandte Chemie
Changsheng Shan, Kaifeng Wu, Hung-Ju Yen, Claudia Narvaez Villarrubia, Tom Nakotte, Xiangjie Bo, Ming Zhou, Gang Wu, Hsing-Lin Wang
For first time, we report that graphene oxide (GO) can be used as a new "dual-role" binder for Si nanoparticles (SiNPs) -based lithium ion batteries (LIBs). GO not only provides a graphene-like porous 3D framework for accommodating the volume changes of SiNPs during charging/discharging cycles, but also acts as a polymer-like binder that forms strong chemical bonds with SiNPs through its Si-OH functional groups to trap and stabilize SiNPs inside the electrode. Leveraging this unique dual-role of GO binder, we fabricated GO/SiNPs electrodes with remarkably improved performances as compared to using the conventional polyvinylidene fluoride (PVDF) binder...
April 23, 2018: ACS Applied Materials & Interfaces
Sudheer Nambiar, Unnikrishnan Kunjan Pillai, Joe Devasahayam, Tony Oliver, Asha Karippot
End stage renal disease (ESRD) population account for 1.9 per patient year of hospital admissions annually. ESRD population are at increased risk of bleeding secondary to use of anticoagulation during hemodialysis and uremia induced platelet dysfunction. Gastrointestinal bleeding accounts for 3-7% of all deaths in ESRD population. Lower gastrointestinal bleeding refers to blood loss from a site in the gastrointestinal tract distal to the ligament of Treitz. It is usually suspected when a patient complains of hematochezia...
2018: Case Reports in Nephrology
Nathalie M Scheers, Dora I A Pereira, Nuno Faria, Jonathan J Powell
Ferric chelates may be used as oral iron supplements or phosphate binders but both ferric citrate and ferric EDTA have been shown to promote tumor burden in murine models of colon cancer. Here we studied their effects on cancer cell growth, at typical supplemental iron levels encountered in the gastrointestinal tract (0.01-0.2 mM). Caco-2 and/or Hutu-80 cells were exposed to these forms of chelated iron or to ferrous sulfate and outcomes were assessed using cell proliferation assays, proteome profiler arrays, western blot, and ELISA...
March 30, 2018: Oncotarget
Hui Wen Ng, Carmine Leggett, Sugunadevi Sakkiah, Bohu Pan, Hao Ye, Leihong Wu, Chandrabose Selvaraj, Weida Tong, Huixiao Hong
The detrimental health effects associated with tobacco use constitute a major public health concern. The addiction associated with nicotine found in tobacco products has led to difficulty in quitting among users. Nicotinic acetylcholine receptors (nAChRs) are the targets of nicotine and are responsible for addiction to tobacco products. However, it is unknown if the other >8000 tobacco constituents are addictive. Since it is time-consuming and costly to experimentally assess addictive potential of such larger number of chemicals, computationally predicting human nAChRs binding is important for in silico evaluation of addiction potential of tobacco constituents and needs structures of human nAChRs...
March 30, 2018: Oncotarget
Mehdi Hatami
Poly(amic acid), the precursor of polyimide (PI), was used for the preparation of PI/CeO2 nanocomposites (NC)s by ultrasonic assisted technique via insertion of the surface modified CeO2 nanoparticles (NP)s into PI matrix. In the preparation stages, in the first, the modifications of CeO2 NPs by using hexadecyltrimethoxysilane (HDTMS) as a binder were targeted using ultrasonic waves. In the second step, newly designed PI structure was formed from the sonochemical imidization process as a molecular hook. In this step two different reactions were occurred...
June 2018: Ultrasonics Sonochemistry
E Papastavrou, P Breedon, D Fairhurst
Low-temperature deposition modeling (LDM), otherwise termed freeze-form extrusion fabrication or rapid freeze prototyping, involves dispensing an aqueous-based ceramic paste or polymeric hydrogel along predefined paths in subzero ambient temperatures, followed by freeze-drying. The solidification of the material after the deposition of each layer enables large parts to be built without the need for organic binders, which can often have cytotoxic effects. Freeze-dried parts obtained from LDM typically exhibit pores with openings that range in average between 1 and 40 μm...
2018: Methods in Molecular Biology
Leandra C Constantino, Luisa B Binder, Samuel Vandresen-Filho, Giordano G Viola, Fabiana K Ludka, Mark W Lopes, Rodrigo B Leal, Carla I Tasca
N-methyl D-aspartate (NMDA) preconditioning is evoked by the administration of a subtoxic dose of NMDA and is protective against neuronal excitotoxicity. This effect may involve a diversity of targets and cell signaling cascades associated to neuroprotection. Phosphatidylinositol-3 kinase/protein kinase B (PI3K/Akt) and mitogen-activated protein kinases (MAPKs) such as extracellular regulated protein kinase 1/2 (ERK1/2) and p38MAPK pathways play a major role in neuroprotective mechanisms. However, their involvement in NMDA preconditioning was not yet fully investigated...
April 20, 2018: Neurotoxicity Research
Youn Cheol Joe, K Prasanna, Suk Hyun Kang, Yong Nam Jo, Chang Woo Lee
The electrophoretic deposition (EPD) process enables more uniform coating layers and saves time over the traditional laminating (LN) process. LiNi0.8Co0.1Mn0.1O2 (NCM811) is prepared by EPD and LN processes in this study. The electrode materials, which are composed of active materials, conductive agents, and binders, are more uniformly dispersed on the substrate by the EPD process when compared with the LN process. Since the weight ratio of NCM811 can be changed through the EPD process, the specific capacity is calculated by weighing the deposited active materials after the process...
September 1, 2018: Journal of Nanoscience and Nanotechnology
Mario Giess, Anna Witte, Julia Jasper, Oliver Koch, Daniel Summerer
5-methylcytosine (5mC) and its oxidized derivatives are regulatory elements of mammalian genomes involved in development and disease. These nucleobases do not selectively modulate Watson-Crick pairing, preventing their programmable targeting and analysis by traditional hybridiza-tion probes. Transcription-activator-like effectors (TALEs) can be engineered for use as programmable probes with epi-genetic nucleobase selectivity. However, only partial selectivi-ties for oxidized 5mC have been achieved so far, preventing unambiguous target binding...
April 20, 2018: Journal of the American Chemical Society
Julia J Scialla
PURPOSE OF REVIEW: Treatment of mineral metabolism is a mainstay of dialysis care including some of its most widely used and costly pharmaceuticals. Although many mineral metabolites are associated with increased risk of mortality, cardiovascular disease, and other morbidities, few clinical trials are available to guide therapy and most focus on single drug approaches. In practice, providers manage many aspects of mineral metabolism simultaneously in integrated treatment approaches that incorporate multiple agents and changes in the dialysis prescription...
April 6, 2018: Current Opinion in Nephrology and Hypertension
Attila Kormos, Christine Koehler, Eszter Fodor, Zsófia Rutkai, Maddison Martin, Gábor Mező, Edward Lemke, Péter Kele
Fluorogenic probes are capable of minimizing background fluorescence of unreacted and non-specifically adsorbed reagents. The preceding years have brought substantial developments in the design and synthesis of bioorthogonally applicable fluorogenic systems mainly based on the quenching effects of azide and tetrazine moieties. The modulation power exerted by these bioorthogonal motifs typically becomes less efficient on more conjugated systems, i.e. on probes with red-shifted emission wavelength. In order to reach efficient quenching, i...
April 20, 2018: Chemistry: a European Journal
Saskia Roesch, Thomas Lindner, Max Sauter, Anastasia Loktev, Paul Flechsig, Martin Müller, Walter Mier, Rolf Warta, Gerhard Dyckhoff, Christel Herold-Mende, Uwe Haberkorn, Annette Altmann
Alpha v beta 6 (αvβ6) integrin is overexpressed by several carcinomas, and thus considered as target for diagnostic imaging and anti-cancer therapies. Recently, we presented SFITGv6 as a novel potential tracer for imaging and targeted therapy of αvβ6 integin-positive carcinomas. Here, we analyzed affinity and specificity of five native αvβ6 integrin-specific binders in comparison to SFITGv6. Methods: Sunflower trypsin inhibitor (SFTI)-1-based peptides containing arginine-glycine-aspartic acid (RGD) motif-spanning octamers of fibronectin (SFFN1), tenascin C (SFTNC), vitronectin (SFVTN), and latency-associated peptides (LAP) 1 (SFLAP1), and 3 (SFLAP3) were synthesized and their binding potential to αvβ6 integrin-expressing head and neck squamous cell carcinoma (HNSCC) cell lines was evaluated...
April 19, 2018: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
Alexandra M Koenig, Laura Ramo-Fernández, Christina Boeck, Maria Umlauft, Markus Pauly, Elisabeth B Binder, Clemens Kirschbaum, Harald Gündel, Alexander Karabatsiakis, Iris-Tatjana Kolassa
BACKGROUND: The inconsistency in results of cortisol alterations after childhood maltreatment (CM) might arise due to the fact that no study so far considered the effects of environmental factors such as maltreatment load and genetic factors such as the influence of FKBP5 genotype on stress hormone regulation. This study analyzed the interaction between the single nucleotide polymorphism rs1360780 within the FKBP5 gene and the severity of maternal CM experiences (maltreatment load) on hair steroid levels of mother-infant-dyads...
April 5, 2018: Psychoneuroendocrinology
Liewei Qiu, Yiding Shen, Huabo Fan, Xiaowu Yang, Chen Wang
The rheology of carboxymethyl fenugreek gum (CFG) is characterized and applied it as a binder for the silicon anode of lithium-ion batteries (LIBs). First, a series of carboxymethyl fenugreek gum (namely CFG-1, CFG-2 and CFG-3) was prepared and characterized by Fourier transform infrared spectrophotometer and hydrogen nuclear magnetic resonance spectrometry studies. In rheological measurements, the CFG solutions show higher flowability, weaker viscoelastic behavior and better thixotropy than that of fenugreek gum (FG) solution...
April 16, 2018: International Journal of Biological Macromolecules
Hirotaka Komaba, Takatoshi Kakuta, Takehiko Wada, Miho Hida, Takao Suga, Masafumi Fukagawa
Background: Hyperphosphatemia and poor nutritional status are associated with increased mortality. Lanthanum carbonate is an effective, calcium-free phosphate binder, but little is known about the long-term impact on mineral metabolism, nutritional status and survival. Methods: We extended the follow-up period of a historical cohort of 2292 maintenance hemodialysis patients that was formed in late 2008. We examined 7-year all-cause mortality according to the serum phosphate levels and nutritional indicators in the entire cohort and then compared the mortality rate of the 562 patients who initiated lanthanum with that of the 562 propensity score-matched patients who were not treated with lanthanum...
April 16, 2018: Nephrology, Dialysis, Transplantation
Mona Kusch, Sarah Gillessen, Jochen Saliger, Hans Karbe, Ellen Binder, Gereon R Fink, Simone Vossel, Peter H Weiss
OBJECTIVE: Reduced awareness for motor or cognitive impairments has mainly been studied in relation to right-hemispheric deficits such as left-sided hemiparesis. However, recent studies suggest that also left hemisphere (LH) stroke can lead to reduced awareness for neurological/neuropsychological deficits, for example, aphasia. The aim of the current study was to characterize reduced awareness for apraxic as well as aphasic deficits in patients suffering from LH stroke. METHOD: After the assessment of apraxia and aphasia, patients (n = 32) were asked to rate their performance on a 1- to 5-point rating scale...
April 19, 2018: Neuropsychology
Sangeet Dhillon-Jhattu, Stuart M Sprague
Hyperphosphatemia is a common complication of CKD. Prior to development of overt hyperphosphatemia, there are several adaptive mechanisms that occur to maintain normal phosphorus equilibrium in patients with CKD. These include an early and progressive rise in fibroblast growth factor 23 (FGF 23), followed by an increase in parathyroid hormone (PTH) with a decrease in 1,25-dihydroxyvitamin D (1,25 Vit D). Over the last 20 years, a large number of studies have shown that hyperphosphatemia is a strong predictor of adverse clinical outcomes including increased incidence of vascular calcification, cardiovascular disease, and all-cause mortality in both individuals with CKD as well as those with normal kidney function...
April 19, 2018: Seminars in Dialysis
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