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https://www.readbyqxmd.com/read/28231673/-changes-of-resistant-phenotype-and-crispr-cas-system-of-four-shigella-strains-passaged-for-90-times-without-antibiotics
#1
B Zhang, L J Hong, G C Duan, W J Liang, H Y Yang, Y L Xi
Objective: To explore the stability of resistant phenotypes and changes of clustered regularly interspaced short palindromic repeats (CRISPR)/CRISPR-associated (Cas) gene system on four Shigella strains in the absence of antibiotics. Methods: Four clinical isolated Shigella strains that resistant to different antibiotics were consecutive passaged for 90 times without antibiotics. Agar dilution method was used to determine the minimum inhibitory concentration of Shigella strains. After sequence analysis with PCR, CRISPR Finder and Clustal X 2...
February 10, 2017: Zhonghua Liu Xing Bing Xue za Zhi, Zhonghua Liuxingbingxue Zazhi
https://www.readbyqxmd.com/read/28231007/molecular-dynamics-recrystallization-behavior-and-water-solubility-of-amorphous-anticancer-agent-bicalutamide-and-its-polyvinylpyrrolidone-mixtures
#2
Justyna Szczurek, Marzena Rams-Baron, Justyna Knapik-Kowalczuk, Agata Antosik, Joanna Szafraniec, Witold Jamroz, Mateusz Dulski, Renata Jachowicz, Marian Paluch
In this paper, we investigated the molecular mobility and physical stability of amorphous bicalutamide, a poorly water-soluble drug widely used in prostate cancer treatment. Our broadband dielectric spectroscopy measurements and differential scanning calorimetry studies revealed that amorphous BIC is a moderately fragile material with strong tendency to recrystallize from amorphous state. However, mixing the drug with polymer polyvinylpyrrolidone results in a substantial improvement of physical stability attributed to antiplasticizing effect governing by polymer additive...
February 23, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28230203/water-insoluble-photosensitizer-nanocolloids-stabilized-by-supramolecular-interfacial-assembly-towards-photodynamic-therapy
#3
Yamei Liu, Kai Ma, Tifeng Jiao, Ruirui Xing, Guizhi Shen, Xuehai Yan
Nanoengineering of hydrophobic photosensitizers (PSs) is a promising approach for improved tumor delivery and enhanced photodynamic therapy (PDT) efficiency. A variety of delivery carriers have been developed for tumor delivery of PSs through the enhanced permeation and retention (EPR) effect. However, a high-performance PS delivery system with minimum use of carrier materials with excellent biocompatibility is highly appreciated. In this work, we utilized the spatiotemporal interfacial adhesion and assembly of supramolecular coordination to achieve the nanoengineering of water-insoluble photosensitizer Chlorin e6 (Ce6)...
February 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28229944/development-and-in-vivo-evaluation-of-an-innovative-hydrochlorothiazide-in-cyclodextrins-in-solid-lipid-nanoparticles-formulation-with-sustained-release-and-enhanced-oral-bioavailability-for-the-hypertension-treatment-in-pediatrics
#4
Marzia Cirri, Natascia Mennini, Francesca Maestrelli, Paola Mura, Carla Ghelardini, Lorenzo di Cesare Mannelli
An innovative pediatric oral formulation of hydrochlorothiazide (HCT) (2mg/mL), endowed with improved bioavailability and sustained release properties and suitable for the hypertension treatment in pediatric patients, was developed by combining the drug-cyclodextrin complexation and the incorporation of the complex into Solid Lipid Nanoparticles (SLN). Precirol(®)ATO5-based SLN, with two different surfactants (Pluronic(®)F68 and Tween(®)80) loaded with the drug as such or as binary system with hydroxypropyl-beta-cyclodextrin (HPβCd) and sulfobutyl-ether-beta-cyclodextrin (SBEβCd) both as physical mixture (P...
February 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28229435/design-and-pharmacodynamics-of-recombinant-nz2114-histidine-mutants-with-improved-activity-against-methicillin-resistant-staphylococcus-aureus
#5
Huixian Chen, Ruoyu Mao, Da Teng, Xiumin Wang, Ya Hao, Xingjun Feng, Jianhua Wang
NZ2114 is a promising candidate for therapeutic application owing to its potent activity to Staphylococcus aureus. Our objective was to identify NZ2114 derivatives with improved activity through substitution of His16 and His18 with residues Arginine and Lysine. Eight mutants were designed and expressed in Pichia pastoris X-33 via pPICZαA. Five of them exhibited strong antimicrobial activity against S. aureus at low minimal inhibitory concentrations (MICs) of 0.057-0.454 μM. Among them, H1, H2, and H3 showed ideal pharmacodynamic effects on methicillin-resistant S...
December 2017: AMB Express
https://www.readbyqxmd.com/read/28229357/experimental-determination-and-theoretical-calculation-of-the-eutectic-composition-of-cefuroxime-axetil-diastereomers
#6
Namita Dalal, Ira S Buckner, Peter L D Wildfong
Cefuroxime axetil (CFA), an ester prodrug of cefuroxime exists as a pair of diastereoemers, namely isomer A and isomer B. To enable phase diagram construction, crystallization of the diastereomers of CFA from the commercially available amorphous drug substance was carried out. Isomer A was separated with a purity approaching 100% whereas the maximum purity of isomer B was 85% as confirmed by solution state proton NMR spectroscopy. The crystalline forms of isomer A and isomer B were confirmed as forms AI and BI, respectively, based on differential scanning calorimetry (DSC) analysis and powder X-ray diffraction...
February 22, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28228927/computational-approaches-for-revealing-the-structure-of-membrane-transporters-case-study-on-bilitranslocase
#7
REVIEW
Katja Venko, A Roy Choudhury, Marjana Novič
The structural and functional details of transmembrane proteins are vastly underexplored, mostly due to experimental difficulties regarding their solubility and stability. Currently, the majority of transmembrane protein structures are still unknown and this present a huge experimental and computational challenge. Nowadays, thanks to X-ray crystallography or NMR spectroscopy over 3000 structures of membrane proteins have been solved, among them only a few hundred unique ones. Due to the vast biological and pharmaceutical interest in the elucidation of the structure and the functional mechanisms of transmembrane proteins, several computational methods have been developed to overcome the experimental gap...
2017: Computational and Structural Biotechnology Journal
https://www.readbyqxmd.com/read/28228214/inhibition-of-protein-tyrosine-phosphatase-non-receptor-type-2-by-ptp-inhibitor-xix-its-role-as-a-multiphosphatase-inhibitor
#8
Hien Thi Thu Le, Young-Chang Cho, Sayeon Cho
Protein tyrosine phosphatases (PTPs) play crucial roles in signal transduction and their functional alteration has been detected in many diseases. PTP inhibitors have been developed as therapeutic drugs for diseases that are related to the activity of PTPs. In this study, PTP inhibitor XIX, an inhibitor of CD45 and PTEN, was investigated whether it inhibits other PTPs. Protein tyrosine phosphatase non-receptor type 2 (PTPN2) was selectively inhibited by the inhibitor in a competitive manner. Drug affinity responsive target stability (DARTS) analysis showed that the inhibitor induces conformational changes in PTPN2...
February 23, 2017: BMB Reports
https://www.readbyqxmd.com/read/28228088/aryl-heteroaryl-substituted-celecoxib-derivatives-as-cox-2-inhibitors-synthesis-anti-inflammatory-activity-and-molecular-docking-studies
#9
Golla Madhava, Katla Venkata Ramana, Saddala Madhu Sudhana, Devineni Subba Rao, Kuntrapakam Hema Kumar, Valluru Lokanatha, Asupatri Usha Rani, Chamarthi Naga Raju
BACKGROUND: Cyclooxygenase (COX-2) inhibitors have been developed to provide better anti-inflammatory and analgesic efficacy than those of traditional NSAIDs. Several compounds having selective COX-2 inhibitors such as SC-558, Celecoxib, Rofecoxib, Valdecoxib and Etoricoxib are marketed as new generation NSAIDs and block the production of prostaglandins (PGs) in inflammatory cells. New anti-inflammatory dynamic agents with improved potency and safety profile are still needed. OBJECTIVE: As a part of our continuation research work towards the synthesis of anti-inflammatory agents, the synthesis of N-substituted aryl/heteroaryl-pyrazole-1yl benzene sulfonamide (Celecoxib) derivatives, and evaluated their anti-inflammatory activity in both methods in vitro and in vivo, and molecular docking study on COX-2 enzyme will be discussed in this study...
February 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28227226/learning-approaches-to-improve-prediction-of-drug-sensitivity-in-breast-cancer-patients
#10
Turki Turki, Zhi Wei, Turki Turki, Zhi Wei, Turki Turki, Zhi Wei
Predicting drug response to cancer disease is an important problem in modern clinical oncology that attracted increasing recent attention from various domains such as computational biology, machine learning, and data mining. Cancer patients respond differently to each cancer therapy owing to disease diversity, genetic factors, and environmental causes. Thus, oncologists aim to identify the effective therapies for cancer patients and avoid adverse drug reactions in patients. By predicting the drug response to cancer, oncologists gain full understanding of the effective treatments on each patient, which leads to better personalized treatment...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28226332/responsible-safe-and-effective-prescription-of-opioids-for-chronic-non-cancer-pain-american-society-of-interventional-pain-physicians-asipp-guidelines
#11
Laxmaiah Manchikanti, Adam M Kaye, Nebojsa Nick Knezevic, Heath McAnally, Konstantin Slavin, Andrea M Trescot, Susan Blank, Vidyasagar Pampati, Salahadin Abdi, Jay S Grider, Alan D Kaye, Kavita N Manchikanti, Harold Cordner, Christopher G Gharibo, Michael E Harned, Sheri L Albers, Sairam Atluri, Steve M Aydin, Sanjay Bakshi, Robert L Barkin, Ramsin M Benyamin, Mark V Boswell, Ricardo M Buenaventura, Aaron K Calodney, David L Cedeno, Sukdeb Datta, Timothy R Deer, Bert Fellows, Vincent Galan, Vahid Grami, Hans Hansen, Standiford Helm Ii, Rafael Justiz, Dhanalakshmi Koyyalagunta, Yogesh Malla, Annu Navani, Kent H Nouri, Ramarao Pasupuleti, Nalini Sehgal, Sanford M Silverman, Thomas T Simopoulos, Vijay Singh, Daneshvari R Solanki, Peter S Staats, Ricardo Vallejo, Bradley W Wargo, Arthur Watanabe, Joshua A Hirsch
BACKGROUND: Opioid use, abuse, and adverse consequences, including death, have escalated at an alarming rate since the 1990s. In an attempt to control opioid abuse, numerous regulations and guidelines for responsible opioid prescribing have been developed by various organizations. However, the US opioid epidemic is continuing and drug dose deaths tripled during 1999 to 2015. Recent data show a continuing increase in deaths due to natural and semisynthetic opioids, a decline in methadone deaths, and an explosive increase in the rates of deaths involving other opioids, specifically heroin and illicit synthetic fentanyl...
February 2017: Pain Physician
https://www.readbyqxmd.com/read/28226244/molecularly-organic-inorganic-hybrid-hollow-mesoporous-organosilica-nanocapsules-with-tumor-specific-biodegradability-and-enhanced-chemotherapeutic-functionality
#12
Ping Huang, Yu Chen, Han Lin, Luodan Yu, Linlin Zhang, Liying Wang, Yufang Zhu, Jianlin Shi
Based on the intrinsic features of high stability and unique multifunctionality, inorganic nanoparticles have shown remarkable potentials in combating cancer, but their biodegradability and biocompatibility are still under debate. As a paradigm, this work successfully demonstrates that framework organic-inorganic hybridization can endow the inorganic mesoporous silica nanocarriers with unique tumor-sensitive biodegradability and high biocompatibility. Based on a "chemical homology" mechanism, molecularly organic-inorganic hybridized hollow mesoporous organosilica nanocapsules (HMONs) with high dispersity and sub-50 nm particle dimension were constructed in mass production...
February 15, 2017: Biomaterials
https://www.readbyqxmd.com/read/28225601/rational-optimization-of-diphenyl-ether-binding-kinetics-to-the-enoyl-acp-reductase-fabi1-from-burkholderia-pseudomallei
#13
Carla Maya Neckles, Sandra Eltschkner, Jason Ellsworth Cummings, Maria Hirschbeck, Fereidoon Daryaee, Gopal R Bommineni, Zhuo Zhang, Lauren A Spagnuolo, Weixuan Yu, Shabnam Davoodi, Richard A Slayden, Caroline Kisker, Peter J Tonge
There is growing awareness of the link between drug-target residence time and in vivo drug activity, and there are increasing efforts to determine the molecular factors that control the lifetime of a drug-target complex. Rational alterations in drug-target residence time require knowledge of both the ground and transition states on the inhibition reaction coordinate, and we have determined the structure-kinetic relationship for 22 ethyl or hexyl substituted diphenyl ethers that are slow-binding inhibitors of bpFabI1, the enoyl-ACP reductase FabI1 from Burkholderia pseudomallei...
February 22, 2017: Biochemistry
https://www.readbyqxmd.com/read/28225570/washless-method-enables-multilayer-coating-of-an-aggregation-prone-nanoparticulate-drug-delivery-system-with-enhanced-yields-colloidal-stability-and-scalability
#14
Lamees Nayef, Rafael Castiello, Maryam Tabrizian
Aggregation is frequently encountered during coating nanoparticles, especially when the core is not solid and the coating polyelectrolytes are weak. Here, the coating of a nanoliposome with two weak polyelectrolytes, alginate and chitosan, is investigated. First, quartz crystal microbalance with dissipation, atomic force microscopy, scanning electron microscopy, and energy dispersive spectroscopy analyses confirm the feasibility of firm adsorption of up to 16 layers of weak polyelectrolytes to the liposomal surface...
February 22, 2017: Macromolecular Bioscience
https://www.readbyqxmd.com/read/28225510/effective-use-of-calcineurin-inhibitor-in-combination-therapy-for-interstitial-lung-disease-in-patients-with-dermatomyositis-and-polymyositis
#15
Yasuhiro Shimojima, Wataru Ishii, Masayuki Matsuda, Dai Kishida, Shu-Ichi Ikeda
OBJECTIVE: The current study demonstrated the potential use of calcineurin inhibitor (CNI) in combination therapy for interstitial lung disease (ILD) complicated with dermatomyositis (DM) and polymyositis (PM). METHODS: Thirty DM/PM patients with ILD were enrolled in this study. Continuous intravenous administration of cyclosporine A (IV-CsA) was simultaneously started with corticosteroid in patients presenting more than two respiratory distress factors as follows: <70 mmHg of PaO2, percentage of vital capacity <70%, and/or exertional dyspnea...
March 2017: Journal of Clinical Rheumatology: Practical Reports on Rheumatic & Musculoskeletal Diseases
https://www.readbyqxmd.com/read/28225369/long-term-outcomes-of-rituximab-therapy-in-patients-with-noninfectious-posterior-uveitis-refractory-to-conventional-immunosuppressive-therapy
#16
Andres F Lasave, Caiyun You, Lina Ma, Khawla Abusamra, Neerav Lamba, Manuel Valdes Navarro, Halea Meese, C Stephen Foster
PURPOSE: To assess long-term effectiveness of rituximab therapy for refractory noninfectious uveitis affecting the posterior segment. METHODS: Retrospective case series. Patients diagnosed with recalcitrant noninfectious posterior uveitis who were treated with rituximab intravenous infusions between 2010 and 2015 were included. Patients underwent best-corrected visual acuity testing and fluorescein angiography evidence of disk or vascular staining at 6, 12, 18, and 24 months...
February 20, 2017: Retina
https://www.readbyqxmd.com/read/28224393/coamorphous-loratadine-citric-acid-system-with-enhanced-physical-stability-and-bioavailability
#17
Jin Wang, Ruimiao Chang, Yanan Zhao, Jiye Zhang, Ting Zhang, Qiang Fu, Chun Chang, Aiguo Zeng
Coamorphous systems using citric acid as a small molecular excipient were studied for improving physical stability and bioavailability of loratadine, a BCS class II drug with low water solubility and high permeability. Coamorphous loratadine-citric acid systems were prepared by solvent evaporation technique and characterized by differential scanning calorimetry, X-ray powder diffraction, and Fourier transform infrared spectroscopy. Solid-state analysis proofed that coamorphous loratadine-citric acid system (1:1) was amorphous and homogeneous, had a higher T g over amorphous loratadine, and the intermolecular hydrogen bond interactions between loratadine and citric acid exist...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28223869/compatibility-study-of-paracetamol-chlorpheniramine-maleate-and-phenylephrine-hydrochloride-in-physical-mixtures
#18
G G G de Oliveira, A Feitosa, K Loureiro, A R Fernandes, E B Souto, P Severino
Paracetamol (PAR), phenylephrine hydrochloride (PHE) and chlorpheniramine maleate (CPM) are commonly used in clinical practice as antipyretic and analgesic drugs to ameliorate pain and fever in cold and flu conditions. The present work describes the use of thermal analysis for the characterization of the physicochemical compatibility between drugs and excipients during the development of solid dosage forms. Thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC) were used to study the thermal stability of the drug and of the physical mixture (drug/excipients) in solid binary mixtures (1:1)...
January 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28223861/biogenic-nanoparticles-bearing-antibacterial-activity-and-their-synergistic-effect-with-broad-spectrum-antibiotics-emerging-strategy-to-combat-drug-resistant-pathogens
#19
Syed Baker, Azmath Pasha, Sreedharamurthy Satish
The present study emphasizes on synthesis of bimetallic silver-gold nanoparticles from cell free supernatant of Pseudomonas veronii strain AS41G inhabiting Annona squamosa L. The synthesized nanoparticles were characterized using hyphenated techniques with UV-Visible spectra ascertained absorbance peak between 400 and 800 nm. Possible interaction of biomolecules in mediating and stabilization of nanoparticles was depicted with Fourier transform infrared spectroscopy (FTIR). X-ray diffraction (XRD) displayed Bragg's peak conferring the 1 0 0, 1 1 1, 2 0 0, and 2 2 0 facets of the face centered cubic symmetry of nanoparticles suggesting that these nanoparticles were crystalline in nature...
January 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28223517/heart-failure-drug-changes-the-mechanoenzymology-of-the-cardiac-myosin-powerstroke
#20
John A Rohde, David D Thomas, Joseph M Muretta
Omecamtiv mecarbil (OM), a putative heart failure therapeutic, increases cardiac contractility. We hypothesize that it does this by changing the structural kinetics of the myosin powerstroke. We tested this directly by performing transient time-resolved FRET on a ventricular cardiac myosin biosensor. Our results demonstrate that OM stabilizes myosin's prepowerstroke structural state, supporting previous measurements showing that the drug shifts the equilibrium constant for myosin-catalyzed ATP hydrolysis toward the posthydrolysis biochemical state...
February 21, 2017: Proceedings of the National Academy of Sciences of the United States of America
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