Read by QxMD icon Read


Matt Shirley, Lesley J Scott
Isavuconazole is a second-generation triazole with activity against a broad spectrum of clinically important fungi. Its water-soluble prodrug, isavuconazonium sulfate (Cresemba(®)), available in interchangeable intravenous and oral formulations, is approved in the USA and EU for the treatment of adults with invasive aspergillosis and mucormycosis. In international phase III clinical trials, isavuconazole was efficacious and generally well tolerated in the treatment of these life-threatening diseases. In the phase III SECURE trial, isavuconazole was non-inferior to voriconazole for the primary treatment of invasive mould disease (primarily aspergillosis) and was associated with fewer drug-related treatment-emergent adverse events (TEAEs) than voriconazole...
October 20, 2016: Drugs
Ahmad Ainurofiq, Syaiful Choiri, Muhamad Ali Azhari, Chaterin Romauli Siagian, Bambang Budi Suryadi, Fea Prihapsara, Sholichah Rohmani
Purpose: The aim of this research was to formulate and develop an orally disintegrating tablet (ODT) that incorporated a MEL/β-CD complex, using a quality by design (QbD) approach to enhance solubility and drug release. Methods: Multiple regression linear analysis was conducted to develop the kneading process and ODT formulation. Mixing time and amount of solvent were used as independent variables in kneading process optimisation, while the superdisintegrants were used to obtain the desired formulation. Fourier transform infrared spectroscopy and differential scanning calorimetry were performed for complex characterization...
September 2016: Advanced Pharmaceutical Bulletin
Shanshan Wang, Chao Han, Sisi Wang, Lijuan Bai, Shanshan Li, Jianguang Luo, Lingyi Kong
Cu(II) complexed amino acid ionic liquid, Cu(II)-[1-butyl-3-methylimidazolium][L-Pro] (Cu(II)-[BMIm][L-Pro]), was successfully adopted as chiral ligand to improve the enantioseparation efficiency in high speed counter-current chromatography (HSCCC). For the enantioseparation of intractable naringenin (NRG) racemic mixtures, Cu(II)-[BMIm][L-Pro] coupled with hydroxypropyl-β-cyclodextrin (HP-β-CD) was successfully applied as dual chiral selectors in HSCCC. The influence of important parameters, including the concentration of the chiral selectors, the pH value, and the temperature were investigated...
October 14, 2016: Journal of Chromatography. A
Salvatore Fanali
This paper presents the state of the art concerning the separation of chiral compounds by means of nano-liquid chromatography (nano-LC). The enantiomers' separation and determination are a subject of fundamental importance in various application fields such as pharmaceutical industry, biomedicine, food, agrochemical etc. Nano-LC is a miniaturized chromatographic technique offering some advantages over conventional ones such as low consumption of mobile phase, sample volume and amount of chiral stationary phase, reduced costs etc...
October 14, 2016: Journal of Chromatography. A
Lu Wang, Xiang-Yong Liang, Li-Sheng Ding, Sheng Zhang, Bang-Jing Li
A new type of chiral magnetic nano-particles was prepared via covalently linked magnetic nano-particles (Fe3O4) and heptakis (6-O-triisopropylsilyl)-β-cyclodextrin (6-TIPS-β-CD). The resulting selectors (TIPS-β-CD-MNPs) combined the high magnetic property Fe3O4 and efficient chiral recognition ability of 6-TIPS-β-CD. The enantioselectivity of TIPS-β-CD-MNPs towards 1-(1-naphthyl) ethylamine was six times higher than that of parent β-CD modified Fe3O4 particles.
October 20, 2016: Chemistry, An Asian Journal
Suporn Charumanee, Siriporn Okonogi, Jakkapan Sirithunyalug, Peter Wolschann, Helmut Viernstein
The aim of the study was to investigate the solubility of piroxicam (Prx) depending on the inclusion complexation with various cyclodextrins (CDs) and on ethanol as a co-solvent. The phase-solubility method was applied to determine drug solubility in binary and ternary systems. The results showed that in systems consisting of the drug dissolved in ethanol-water mixtures, the drug solubility increased exponentially with a rising concentration of ethanol. The phase solubility measurements of the drug in aqueous solutions of CDs, β-CD and γ-CD exhibited diagrams of AL-type, whereas 2,6-dimethyl-β-CD revealed AP-type...
October 18, 2016: Scientia Pharmaceutica
Al-Abboodi Shakir Ashwaq, Mothanna Sadiq Al-Qubaisi, Abdullah Rasedee, Ahmad Bustamam Abdul, Yun Hin Taufiq-Yap, Swee Keong Yeap
Dentatin (DEN), purified from the roots of Clausena excavata Burm f., has poor aqueous solubility that reduces its therapeutic application. The aim of this study was to assess the effects of DEN-HPβCD (hydroxypropyl-β-cyclodextrin) complex as an anticancer agent in HT29 cancer cell line and compare with a crystal DEN in dimethyl sulfoxide (DMSO). The exposure of the cancer cells to DEN or DEN-HPβCD complex leads to cell growth inhibition as determined by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay...
October 18, 2016: International Journal of Molecular Sciences
Qiang Zhao, Zhen Lian, Xuedong Gao, Yun Yan, Jianbin Huang
The ability to modulate the amphiphilic aggregation reversibly with external stimuli, especially by light trigger, is of great importance. It makes great contribution to the development of applications by self-assembly. However, most previously described systems are based on specific molecular design and difficultly applied in light-inert aggregations. Here we develop a general and effective approach to control the morphology of amphiphilic aggregates by light, which is suitable for different assemblies such as micelle, vesicle and helix...
October 20, 2016: Langmuir: the ACS Journal of Surfaces and Colloids
Mordjane Boukhet, Fabien Piguet, Hadjer Ouldali, Manuela Pastoriza-Gallego, Juan Pelta, Abdelghani Oukhaled
The transport of macromolecules through nanopores is involved in many biological functions and is today at the basis of promising technological applications. Nevertheless the interpretation of the dynamics of the macromolecule/nanopore interaction is still misunderstood and under debate. At the nanoscale, inside biomimetic channels under an external applied voltage, electrophoresis, which is the electric force acting on electrically charged molecules, and electroosmotic flow (EOF), which is the fluid transport associated with ions, contribute to the direction and magnitude of the molecular transport...
October 20, 2016: Nanoscale
Subhadeep Saha, Aditi Roy, Kanak Roy, Mahendra Nath Roy
Host-guest inclusion complexes of β-cyclodextrin with two vitamins viz., nicotinic acid and ascorbic acid in aqueous medium have been explored by reliable spectroscopic, physicochemical and calorimetric methods as stabilizer, carrier and regulatory releaser of the guest molecules. Job's plots have been drawn by UV-visible spectroscopy to confirm the 1:1 stoichiometry of the host-guest assembly. Stereo-chemical nature of the inclusion complexes has been explained by 2D NMR spectroscopy. Surface tension and conductivity studies further support the inclusion process...
October 20, 2016: Scientific Reports
Corneille Edgar Ontsouka, Xiao Huang, Eldar Aliyev, Christiane Albrecht
Cell-based studies previously showed that the ATP-binding cassette transporter A1 (ABCA1) transfers cholesterol across mammary epithelial cells (MEC). Data for phospholipid transport are lacking, and it is unclear from which cellular source the transported cholesterol stems, whether this transport activates signaling pathways, and how lactogenic hormones regulate it. To clarify these aspects, lipid transport and expressional analyses were performed in bovine primary (bMEC) and/or immortalized (MAC-T) MEC cultures...
October 16, 2016: Molecular and Cellular Endocrinology
Ting Wei, Wenjun Zhan, Limin Cao, Changming Hu, Yangcui Qu, Qian Yu, Hong Chen
Development of a versatile strategy for antibacterial surfaces is of great scientific interest and practical significance. However, few methods can be used to fabricate antibacterial surfaces on substrates of different chemistries and structures. In addition, traditional antibacterial surfaces may suffer problems related to the attached dead bacteria. Herein, antibacterial surfaces with multifunctionality and regenerability are fabricated by a universal strategy. Various substrates are firstly deposited with multilayered films containing guest moieties, which further serve as binding sites for incorporation of biocidal "host" molecules, β-cyclodextrin (β-CD) derivatives modified with quaternary ammonium salt groups (CD-QAS)...
October 19, 2016: ACS Applied Materials & Interfaces
Dandan Wang, Guoguang Chen, Lili Ren
Amiodarone hydrochloride (AMD) is used in the treatment of a wide range of cardiac tachyarrhythmias, including both ventricular fibrillation (VF) and hemodynamically unstable ventricular tachycardia (VT). The objectives of this study were to improve the solubility and bioavailability in fasted state and to reduce the food effect of AMD by producing its inclusion complex with sulfobutylether-β-cyclodextrin (SBE-β-CD). The complex was prepared through a saturated water solution combined with the freeze-drying method and then characterized by Fourier transform infrared spectroscopy, proton nuclear magnetic resonance spectroscopy, and differential scanning calorimetry...
October 18, 2016: AAPS PharmSciTech
Monica R P Rao, Chaitanya Shirsath
Efavirenz is a non-nucleoside reverse transcriptase inhibitor which is chronically prescribed for HIV patients. However, it exhibits solubility-limited bioavailability. Aim of this work was to enhance the solubility and dissolution of the Biopharmaceutical Classification System (BCS) class II drug efavirenz, using beta-cyclodextrin-based nanosponges. Nanosponges have high drug loading capacity and are effective for solubility enhancement. Beta-cyclodextrin was crosslinked with carbonates in different ratios to prepare nanosponges...
October 18, 2016: AAPS PharmSciTech
Takeshi Funakoshi, Toshihiko Aki, Masateru Tajiri, Kana Unuma, Koichi Uemura
Aberrant cellular accumulation of cholesterol is associated with neuronal lysosomal storage disorders such as Niemann-Pick disease Type C (NPC). We have shown previously that l-norephedrine (l-Nor), a sympathomimetic amine, induces necrotic cell death associated with massive cytoplasmic vacuolation in SH-SY5Y human neuroblastoma cells. To reveal the molecular mechanism underling necrotic neuronal cell death caused by l-Nor, we examined alterations in the gene expression profile of cells during l-Nor exposure...
October 18, 2016: Journal of Biological Chemistry
R Onnainty, E M Schenfeld, J P Petiti, M R Longhi, A Torres, M A Quevedo, G E Granero
Here, a novel drug delivery system was developed for the hydrochlorothiazide (HCT):ß-cyclodextrin (ßCD) inclusion complex loaded into chitosan (CS) nanoparticles (NPs)[CS/HCT:ßCD NPs]. It was found, for the first time, that exposure of the intestinal mucosa to free HCT resulted in an increased and abnormal intestinal permeability associated with several injuries to the intestinal epithelium. Nevertheless, the HCT delivery system obtained ameliorated the damage of the intestinal epithelium induced by HCT...
October 18, 2016: Molecular Pharmaceutics
Mariana Certal, Adriana Vinhas, Aurora Barros-Barbosa, Fátima Ferreirinha, Maria Adelina Costa, Paulo Correia-de-Sá
Nucleotides released during heart injury affect myocardium electrophysiology and remodelling through P2 purinoceptors activation in cardiac myofibroblasts. ATP and UTP endorse [Ca(2) +]i accumulation and growth of DDR-2/a-SMA-expressing myofibroblasts from adult rat ventricles via P2Y4 and P2Y2 receptors activation, respectively. Ventricular myofibroblasts also express ADP-sensitive P2Yi, P2Yi2 and P2Yi3 receptors as demonstrated by immunofluorescence confocal microscopy and western blot analysis, but little information exists on ADP effects in these cells...
October 18, 2016: Journal of Cellular Physiology
Natalia Miękus, Ilona Olędzka, Alina Plenis, Piotr Kowalski, Ewa Bień, Aleksandra Miękus, Małgorzata Anna Krawczyk, Elżbieta Adamkiewicz-Drożyńska, Tomasz Bączek
The unbalanced secretion of biogenic amines (BAs) is considered to be a relevant biochemical biomarker in the screening for neuroendocrine tumors, such as: neuroblastoma and pheochromocytoma. However, there is still a need to improve the bioanalytical procedures for BA determination in biological samples due to their instability (photo- and thermosensitivity, easy oxidation) and low concentration in the body fluids. In this study, the primary analytical challenge was to optimize the method of extraction of seven compounds from among BAs and their precursors from urine samples...
October 11, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Haitham Alrabiah, Abdulrahman Al-Majed, Mohammed Abounassif, Gamal A E Mostafa
The fabrication and development of two polyvinyl chloride (PVC) membrane sensors for assaying phenobarbitone sodium are described. Sensors 1 and 2 were fabricated utilizing β- or γ-cyclodextrin as ionophore in the presence of tridodecylmethylammonium chloride as a membrane additive, and PVC and dioctyl phthalate as plasticizer. The analytical parameters of both sensors were evaluated according to the IUPAC guidelines. The proposed sensors showed rapid, stable anionic response (-59.1 and -62.0 mV per decade) over a relatively wide phenobarbitone concentration range (5...
December 1, 2016: Acta Pharmaceutica
Yuki Daimon, Noriyasu Kamei, Kohsaku Kawakami, Mariko Takeda-Morishita, Hironori Izawa, Yuki Takechi-Haraya, Hiroyuki Saito, Hideki Sakai, Masahiko Abe, Katsuhiko Ariga
The effect of carrier morphology on the intestinal absorption of insulin was investigated using a morphology-tunable polymeric carrier, β-cyclodextrin-grafted chitosan (BCC). The insulin-BCC complexes were prepared either in acetate and citrate buffer solutions, followed by dilution with phosphate buffer for the administration. The complex had a molecular network structure in the acetate buffer, whereas nanoparticles formed in the citrate buffer. The network structure in the acetate buffer was maintained even after dilution with a phosphate buffer, but the nanoparticles in the citrate buffer caused aggregation after dilution...
October 17, 2016: Molecular Pharmaceutics
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"