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https://www.readbyqxmd.com/read/28335253/soft-interaction-in-liposome-nanocarriers-for-therapeutic-drug-delivery
#1
REVIEW
Domenico Lombardo, Pietro Calandra, Davide Barreca, Salvatore Magazù, Mikhail A Kiselev
The development of smart nanocarriers for the delivery of therapeutic drugs has experienced considerable expansion in recent decades, with the development of new medicines devoted to cancer treatment. In this respect a wide range of strategies can be developed by employing liposome nanocarriers with desired physico-chemical properties that, by exploiting a combination of a number of suitable soft interactions, can facilitate the transit through the biological barriers from the point of administration up to the site of drug action...
June 25, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335215/rapamycin-loaded-solid-lipid-nanoparticles-as-a-new-tool-to-deliver-mtor-inhibitors-formulation-and-in-vitro-characterization
#2
Alice Polchi, Alessandro Magini, Jarosław Mazuryk, Brunella Tancini, Jacek Gapiński, Adam Patkowski, Stefano Giovagnoli, Carla Emiliani
Recently, the use of mammalian target of rapamycin (mTOR) inhibitors, in particular rapamycin (Rp), has been suggested to improve the treatment of neurodegenerative diseases. However, as Rp is a strong immunosuppressant, specific delivery to the brain has been postulated to avoid systemic exposure. In this work, we fabricated new Rp loaded solid lipid nanoparticles (Rp-SLN) stabilized with polysorbate 80 (PS80), comparing two different methods and lipids. The formulations were characterized by differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), wide angle X-ray scattering (WAXS), cryo-transmission electron microscopy (cryo-TEM), dynamic light scattering (DLS) and particle tracking...
May 9, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335023/qbd-driven-development-and-validation-of-liquid-chromatography-tandem-mass-spectrometric-method-for-the-quantitation-of-sildenafil-in-human-plasma
#3
M Saquib Hasnain, Shaukat Ali Ansari, Shireen Rao, Mohammad Tabish, Mukul Singh, Mohammad Syafiq Abdullah, Mohammed Tahir Ansari
The present work was employing the Quality by Design approach for the development and validation of a LC-MS-MS method to support the clinical advancement in determination of sildenafil in human plasma using lorazepam as an internal standard. Sample preparation involved solid phase extraction and calibration range observed between 3 and 1,700 ng/mL. The method was systematically optimized by employing Box-Behnken design and used mobile phase flow rate, pH and composition of mobile phase as the critical factors, and assessing the design for retention time and peak area as the responses...
February 27, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28334762/missense-uros-mutations-causing-congenital-erythropoietic-porphyria-reduce-uros-homeostasis-that-can-be-rescued-by-proteasome-inhibition
#4
Jean-Marc Blouin, Ganeko Bernardo-Seisdedos, Emma Sasso, Julie Esteve, Cécile Ged, Magalie Lalanne, Arantza Sanz-Parra, Pedro Urquiza, Hubert de Verneuil, Oscar Millet, Emmanuel Richard
Congenital erythropoietic porphyria (CEP) is an inborn error of heme biosynthesis characterized by uroporphyrinogen III synthase (UROS) deficiency resulting in deleterious porphyrin accumulation in blood cells responsible for hemolytic anemia and cutaneous photosensitivity. We analyzed here the molecular basis of UROS impairment associated with twenty nine UROS missense mutations actually described in CEP patients. Using a computational and biophysical joint approach we predicted that most disease-causing mutations would affect UROS folding and stability...
February 21, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28334528/why-prodrugs-and-propesticides-succeed
#5
John E Casida
What are the advantages of bioactivation in optimizing drugs and pesticides? Why are there so many prodrugs and propesticides? These questions are examined here by considering compounds selected on the basis of economic value or market success. The 100 major drugs and 90 major pesticides are divided into ones acting directly and those definitely or possibly requiring bioactivation. Established or candidate prodrugs accounted for 19% of the total drug sales with corresponding values of 20, 37 and 17% for proinsecticides, proherbicides and profungicides...
March 23, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28334523/transformable-nanomaterials-as-artificial-extracellular-matrix-for-inhibiting-tumor-invasion-and-metastasis
#6
Xiao-Xue Hu, Ping-Ping He, Guo-Bin Qi, Yu-Juan Gao, Yao-Xin Lin, Chao Yang, Pei-Pei Yang, Hongxun Hao, Lei Wang, Hao Wang
Tumor metastasis is one of the big challenges in cancer treatment and is often associated with high patient mortality. Until now, there is an agreement that tumor invasion and metastasis are related to degradation of extracellular matrix (ECM) by enzymes. Inspired by the formation of natural ECM and the in situ self-assembly strategy developed in our group, herein, we in situ constructed an artificial extracellular matrix (AECM) based on transformable Laminin (LN)-mimic peptide 1 (BP-KLVFFK-GGDGR-YIGSR) for inhibition of tumor invasion and metastasis...
March 23, 2017: ACS Nano
https://www.readbyqxmd.com/read/28333681/long-term-stability-of-vancomycin-hydrochloride-in-oral-solution-the-brand-name-versus-a-generic-product
#7
Sophie Huvelle, Marie Godet, Jean-Daniel Hecq, Patricia Gillet, Jacques Jamart, Laurence M Galanti
Vancomycin hydrochloride is often used for antibiotherapy in oral solution for hospitalized patients. Preparation of this solution in advance could improve time management or cost savings of drug delivery. Brand and generic products of vancomycin hydrochloride are now commercially available. The aim of this study was to investigate the long-term stability of the vancomycin hydrochloride brand name Vancocin versus the generic Vancomycine at 5°C ± 3°C. Five vials of each oral solution of 1.25 g/100 mL Vancocin and Vancomycine were stored up to 57 days at 5°C ± 3°C...
July 2016: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28333680/physical-and-chemical-stability-of-urapidil-in-0-9-sodium-chloride-in-elastomeric-infusion-pump
#8
Cristina Tomasello, Anna Leggieri, Franco Rabbia, Franco Veglio, Lorena Baietto, Chiara Fulcheri, Amedeo De Nicolò, Giovanni De Perri, Antonio D'Avolio
Urapidil is an antihypertensive agent, usually administered through intravenous bolus injection, slow-intravenous infusion, or continuous-drug infusion by perfusor. Since to date no evidences are available on drug stability in elastomeric pumps, patients have to be hospitalized. The purpose of this study was to validate an ultra-performance liquid chromatographic method to evaluate urapidil stability in an elastomeric infusion pump, in order to allow continuous infusion as home-care treatment. Analyses were conducted by diluting urapidil in an elastomeric pump...
July 2016: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28333675/basics-of-compounding-compounding-films
#9
Loyd V Allen
Films, which are a dosage form designed to dissolve on contact with a wet surface within a very short time, are thin sheets placed in the oral cavity for dissolution and absorption of the active drug. This dosage form is gaining popularity because of its convenience. Discussed within this article are the applications, advantages/disadvantages, composition, preparation, physicochemical considerations, quality control, packaging/labeling/storage, stability, and formulation considerations as they relate to films...
July 2016: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28333664/compatibility-of-norepinephrine-bitartrate-with-levofloxacin-and-moxifloxacin-during-simulated-y-site-administration
#10
Vicky Mody, Samit Shah, Jaymin Patel, Michael C Thomas
The purpose of this study was to determine the physical compatibility and chemical stability of norepinephrine bitartrate with selected fluoroquinolones during simulated intravenous Y-site administration. Simulation of Y-compatibility of intravenous fluids can be experimentally demonstrated by mixing equal volumes of two drugs of interest. Hence, we prepared 1:1 mixture of norepinephrine bitartrate and levofloxacin or moxifloxacin by mixing 64 .g/mL of norepinephrine bitartrate individually with clinically relevant concentrations of levofloxacin (5 mg/mL) and moxifloxacin (1...
May 2016: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28333661/does-your-drug-expertise-include-clinical-pharmaceutics
#11
David W Newton
Whose job is it to protect patients from harm from drug instabilities and incompatibilities and other aspects of clinical pharmaceutics? Pharmacists are better educated via multiple required general and organic chemistry prerequisite and professional curricula medicinal chemistry and pharmaceutics courses. Therefore, no healthcare professional other than pharmacists are nicknamed drug experts or are better formally educated to master drug chemistry in the bottle (i.e., injection stability and compatibility/incompatibility clinical pharmaceutics) as a prerequisite for drug administration to cause safe and effective drug chemistry in the body (i...
May 2016: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28333109/angiotensin-i-converting-enzyme-ace-inhibitory-peptides-from-plants
#12
REVIEW
Ceren Daskaya-Dikmen, Aysun Yucetepe, Funda Karbancioglu-Guler, Hayrettin Daskaya, Beraat Ozcelik
Hypertension is an important factor in cardiovascular diseases. Angiotensin-I-converting enzyme (ACE) inhibitors like synthetic drugs are widely used to control hypertension. ACE-inhibitory peptides from food origins could be a good alternative to synthetic drugs. A number of plant-based peptides have been investigated for their potential ACE inhibitor activities by using in vitro and in vivo assays. These plant-based peptides can be obtained by solvent extraction, enzymatic hydrolysis with or without novel food processing methods, and fermentation...
March 23, 2017: Nutrients
https://www.readbyqxmd.com/read/28332824/indole-substituted-benzothiazoles-and-benzoxazoles-as-selective-and-reversible-mao-b-inhibitors-for-treatment-of-parkinson-s-disease
#13
Min-Ho Nam, Moosung Park, Hyeri Park, Youngjae Kim, Seulki Yoon, Vikram Shahaji Sawant, Ji Won Choi, Jong-Hyun Park, Ki Duk Park, Sun-Joon Min, Changjoon Justin Lee, Hyunah Choo
To develop a novel, selective, and reversible MAO-B inhibitors for safer treatment of Parkinson's disease, benzothiazole and benzoxazole derivatives with indole moiety were designed and synthesized. Most of the synthesized compounds showed inhibitory activities against MAO-B and selectivity over MAO-A. The most active compound was Compound 5b, 6-fluoro-2-(1-methyl-1H-indol-5-yl)benzo[d]thiazole with an IC50 value of 29 nM with no apparent effect on MAO-A activity at 10 M. Based on the reversibility assay, Compound 5b turned out to be a fully reversible with over 95% of recovery of enzyme activity after washout of the compound...
March 23, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28332820/kinetic-landscape-of-a-peptide-bond-forming-prolyl-oligopeptidase
#14
Clarissa Melo Czekster, James H Naismith
Prolyl oligopeptidase B from Galerina marginata (GmPOPB) has recently been discovered as a peptidase capable of breaking and forming peptide bonds to yield a cyclic peptide. Despite the relevance of prolyl oligopeptidases in human biology and disease, a kinetic analysis pinpointing rate-limiting steps for a member of this enzyme family is not available. Macrocyclase enzymes are currently exploited to produce cyclic peptides with potential therapeutic applications. Cyclic peptides are promising drug-like molecules due to their stability and conformational rigidity...
March 23, 2017: Biochemistry
https://www.readbyqxmd.com/read/28331326/lithium-in-late-life-mania-a-systematic-review
#15
REVIEW
Pasquale De Fazio, Raffaele Gaetano, Mariarita Caroleo, Maria Pavia, Giovanbattista De Sarro, Andrea Fagiolini, Cristina Segura-Garcia
The prevalence of mania among >65-year-olds ranges from 0.1% to 0.4% and its treatment is a particular challenge for clinicians. Although lithium is the treatment of choice for bipolar disorder (BD), its use in elderly population was recently questioned. This study provides a comprehensive review of literature on the efficacy and tolerability of lithium as a pharmacologic treatment for mania in elderly BD patients. We conducted a systematic review, based on PRISMA guidelines, of articles published between 1970 and August 2016 and indexed in the following databases: EMBASE, MEDLINE, Cochrane Library Databases and PsycINFO...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28330874/high-resolution-3d-nmr-structure-of-the-kras-proto-oncogene-promoter-reveals-key-features-of-a-g-quadruplex-involved-in-transcriptional-regulation
#16
Abdelaziz Kerkour, Julien Marquevielle, Stefaniia Ivashchenko, Liliya A Yatsunyk, Jean-Louis Mergny, Gilmar F Salgado
Non-canonical base pairing within guanine-rich DNA and RNA sequences can produce G-quartets, whose stacking leads to the formation of a G-quadruplex (G4). G4s can coexist with canonical duplex DNA in the human genome and have been suggested to suppress gene transcription, and much attention has therefore focused on studying G4s in promotor regions of disease-related genes. For example, the human KRAS proto-oncogene contains a nuclease-hypersensitive element (1) located upstream of the major transcription start site...
March 22, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28330735/vancomycin-loaded-nanobubbles-a-new-platform-for-controlled-antibiotic-delivery-against-methicillin-resistant-staphylococcus-aureus-infections
#17
Monica Argenziano, Giuliana Banche, Anna Luganini, Nicole Finesso, Valeria Allizond, Giulia Rossana Gulino, Amina Khadjavi, Rita Spagnolo, Vivian Tullio, Giuliana Giribaldi, Caterina Guiot, Anna Maria Cuffini, Mauro Prato, Roberta Cavalli
Vancomycin (Vm) currently represents the gold standard against methicillin-resistant Staphylococcus aureus (MRSA) infections. However, it is associated with low oral bioavailability, formulation stability issues, and severe side effects upon systemic administration. These drawbacks could be overcome by Vm topical administration if properly encapsulated in a nanocarrier. Intriguingly, nanobubbles (NBs) are responsive to physical external stimuli such as ultrasound (US), promoting drug delivery. In this work, perfluoropentane (PFP)-cored NBs were loaded with Vm by coupling to the outer dextran sulfate shell...
March 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28330413/molecular-dynamic-simulation-and-dft-study-on-the-drug-dna-interaction-crocetin-as-an-anticancer-and-dna-nanostructure-model
#18
Ebrahim Azarhazin, Mohammad Izadyar, Mohammad Reza Housaindokht
In this research, the interaction of Crocetin as an anticancer drug and a Dickerson DNA has been investigated. 25 ns molecular dynamic simulations of Crocetin and DNA composed of twelve base pairs and a sequence of d(CGCGAATTCGCG)2 were done in water. Three definite parts of the B-DNA were considered in analyzing the best interactive site from the thermodynamic point of view. Binding energy analysis showed that van der Waals interaction is the most important part related to the reciprocal O and H atoms of the Crocetin and DNA...
March 22, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28330072/molecular-dynamic-simulations-of-escherichia-coli-l-asparaginase-to-illuminate-its-role-in-deamination-of-asparagine-and-glutamine-residues
#19
Rajeswara Reddy Erva, Satish Babu Rajulapati, Chandrasai Potla Durthi, Mayuri Bhatia, Madhuri Pola
Acute lymphocytic leukemia (ALL) is an outrageous disease worldwide. L-Asparagine (L-Asn) and L-Glutamine (L-Gln) deamination play a crucial role in ALL treatment. Role of Elspar(®) (L-asparaginase from Escherichia coli) in regulation of L-Asn and L-Gln has been confirmed by the other researchers through experimental studies. Therapeutic research against ALL remained elusive with the lack of information on molecular interactions of Elspar(®) with amino acid substrates. In the present study, using different docking tools binding cavities, key residues in binding and ligand binding mechanisms were identified...
June 2016: 3 Biotech
https://www.readbyqxmd.com/read/28329390/high-rates-of-transmission-of-drug-resistant-hiv-in-aruba-resulting-in-reduced-susceptibility-to-the-who-recommended-first-line-regimen-in-nearly-half-of-newly-diagnosed-hiv-infected-patients
#20
L Marije Hofstra, Elena Sánchez Rivas, Monique Nijhuis, Leonie E A Bank, Eduan Wilkinson, Karina Kelly, Tania Mudrikova, Rob Schuurman, Tulio de Oliveira, Jaclyn de Kort, Annemarie M J Wensing
Background.: In Western countries emergence of human immunodeficiency virus (HIV) drug resistance has tremendously decreased, and transmission of drug resistance has merely stabilized in recent years. However, in many endemic settings with limited resources rates of emerging and transmitted drug resistance are not regularly assessed. Methods.: We performed a survey including all HIV-infected individuals who received resistance testing in 2010-2015 in Aruba, a highly endemic HIV area in the Caribbean...
March 9, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
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