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European Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/28636950/structural-evidence-of-quercetin-multi-target-bioactivity-a-reverse-virtual-screening-strategy
#1
Diego Carvalho, Margot Paulino, Fabio Polticelli, Florencia Arredondo, Robert J Williams, Juan A Abin-Carriquiry
The ubiquitous flavonoid quercetin is broadly recognized for showing diverse biological and health-promoting effects, such as anti-cancer, anti-inflammatory and cytoprotective activities. The therapeutic potential of quercetin and similar compounds for preventing such diverse oxidative stress-related pathologies has been generally attributed to their direct antioxidant properties. Nevertheless, accumulated evidence indicates that quercetin is also able to interact with multiple cellular targets influencing the activity of diverse signaling pathways...
June 18, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28629804/zero-order-controlled-release-delivery-of-cholecalciferol-from-injectable-biodegradable-microsphere-in-vitro-characterization-and-in-vivo-pharmacokinetic-studies
#2
Lalit Vora, Sita V G, Pradeep Vavia
Poly(lactic-co-glycolic acid) microspheres loaded with cholecalciferol (CL), more bioactive form of vitamin D was developed as an injectable controlled drug release system and was evaluated for its feasibility of once a month delivery. The CL loaded microspheres (CL-MS) were prepared by simple oil in water (O/W) emulsion-solvent evaporation technique incorporated with a stabilizer, Tocopherol Succinate (TS). Different formulation as well as process parameters were investigated namely concentration of emulsifier, concentration of stabilizer and drug: polymer mass ratios...
June 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28629803/development-of-mpc-dpa-polymeric-nanoparticle-systems-for-inhalation-drug-delivery-applications
#3
Abdul Khaliq Elzhry Elyafi, Guy Standen, Steven T Meikle, Andrew L Lewis, Jonathan P Salvage
Inhalation of nanoparticles for pulmonary drug delivery offers the potential to harness nanomedicine formulations of emerging therapeutics, such as curcumin, for treatment of lung cancer. Biocompatible nanoparticles composed of poly(2-methacryloyloxyethyl phosphorylcholine)-b-poly(2-(diisopropylamino)ethyl methacrylate) (MPC-DPA) have been shown to be suitable nanocarriers for drugs, whilst N-trimethyl chitosan chloride (TMC) coating of nanoparticles has been reported to further enhance their cellular delivery efficacy; the combination of the two has not been previously investigated...
June 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28625749/preclinical-evaluation-of-melanocortin-1-receptor-mc1-r-specific-68-ga-and-44-sc-labeled-dota-napamide-in-melanoma-imaging
#4
Gábor Nagy, Noémi Dénes, Adrienn Kis, Judit P Szabó, Ervin Berényi, Ildikó Garai, Péter Bai, István Hajdu, Dezső Szikra, György Trencsényi
PURPOSE: Alpha melanocyte stimulating hormone (α-MSH) enhances melanogenesis in melanoma malignum by binding to melanocortin-1 receptors (MC1-R). Earlier studies demonstrated that alpha-MSH analog NAPamide molecule specifically binds to MC1-R receptor. Radiolabeled NAPamide is a promising radiotracer for the non-invasive detection of melanin producing melanoma tumors by Positron Emission Tomography (PET). In this present study the MC1-R selectivity of the newly developed Sc-44-labeled DOTA-NAPamide was investigated in vitro and in vivo using melanoma tumors...
June 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28625748/comparison-of-liposomal-drug-formulations-for-transdermal-iontophoretic-drug-delivery
#5
K Malinovskaja-Gomez, S Espuelas, M J Garrido, J Hirvonen, T Laaksonen
This study was aimed to evaluate the in vitro transdermal direct/pulsed current iontophoretic delivery of an amphiphilic model compound from various lipid vesicle-encapsulated formulations compared to free-drug formulation. Conventional, pegylated, ultradeformable liposomes (transfersomes) and ethosomes loaded with a negatively charged drug diclofenac sodium (DS) were prepared and characterized. All the liposomes possessed an average size of ≈100-150nm and negative zeta potential. No changes in colloidal stability were detected after 8h incubation of any vesicle formulation under constant or pulsed iontophoretic current...
June 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28627473/glycyrrhetic-acid-but-not-glycyrrhizic-acid-strengthened-entecavir-activity-by-promoting-its-subcellular-distribution-in-the-liver-via-efflux-inhibition
#6
Qianying Chen, Hongzhu Chen, Wenjie Wang, Jiali Liu, Wenyue Liu, Ping Ni, Guowei Sang, Guangji Wang, Fang Zhou, Jingwei Zhang
Entecavir (ETV) is a superior nucleoside analogue used to treat hepatitis B virus (HBV) infection. Although its advantages over other agents include low viral resistance and the elicitation of a sharp decrease in HBV DNA, adverse effects such as hepatic steatosis, hepatic damage and lactic acidosis have also been reported. Glycyrrhizin has long been used as hepato-protective medicine. The clinical combination of ETV plus glycyrrhizin in China displays better therapeutic effects and lower rates of liver damage...
June 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28627472/molecular-dynamics-as-a-tool-for-in-silico-screening-of-skin-permeability
#7
Paolo Rocco, Francesco Cilurzo, Paola Minghetti, Giulio Vistoli, Alessandro Pedretti
Prediction of skin permeability can have manifold applications ranging from drug delivery to toxicity prediction. Along with the semi-empirical or mechanistic models proposed in the last decades, Molecular Dynamics simulations have recently become a fruitful tool for investigating membrane permeability, in particular as they allow the involved mechanisms to be modelled at a molecular level. Despite their significant structural complexity, Molecular Dynamics simulations can also be utilized to study permeation through the lipid matrix that characterizes the stratum corneum...
June 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28627471/phospholipid-drug-conjugates-as-a-novel-oral-drug-targeting-approach-for-the-treatment-of-inflammatory-bowel-disease
#8
Arik Dahan, Milica Markovic, Svetlana Epstein, Noa Cohen, Ellen M Zimmermann, Aaron Aponick, Shimon Ben-Shabat
The enzyme phospholipase A2 (PLA2) is overexpressed in the inflamed intestine in inflammatory bowel disease (IBD) patients, and in this work we aimed to exploit PLA2 as a prodrug-activating enzyme for a novel PL-drug conjugate, thereby liberating the free drug specifically in the targeted diseased tissue(s). The proposed prodrug contains a drug moiety covalently bound through a linker to the sn-2 position of a phospholipid (PL). The NSAID diclofenac was used as model molecule, and four different linker lengths (2, 4, 6 and 8 -CH2 units) were studied...
June 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28627470/investigation-of-itraconazole-ternary-amorphous-solid-dispersions-based-on-povidone-and-carbopol
#9
Fan Meng, Jordan Meckel, Feng Zhang
We investigate a ternary system that consists of itraconazole (ITZ) and two polymers: povidone K12 and Carbopol 907. The interactions between these two polymers and their effects on the properties of ternary ITZ amorphous solid dispersions (ASDs) are studied. These two polymers can form a water-insoluble complex in acidic aqueous media. The critical pH is determined to be 4.17. The weight percentage of Carbopol 907 in the interpolymer complex range from 59 to 70%, depending on the initial ratios between these two polymers in the starting solutions...
June 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28627469/modeling-and-comparison-of-release-profiles-effect-of-the-dissolution-method
#10
Sara Cascone
During the last decades, the study of the in vitro dissolution of pharmaceuticals has been strongly encouraged by the FDA in order to determine its relationship with the in vivo bioavailability of a drug. In this work immediate and extended release formulations containing diclofenac, a BCS class II drug, were studied using different dissolution methods. The release profiles obtained in USP Apparatus II and USP Apparatus IV were evaluated and compared to determine the effect of the fluid dynamic conditions on the release...
June 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28627468/a-novel-chalcone-derivative-lqfm064-induces-breast-cancer-cells-death-via-p53-p21-kit-and-pdgfra
#11
Bruna Lannuce Silva Cabral, Artur Christian Garcia da Silva, Renato Ivan de Ávila, Alane Pereira Cortez, Rangel Magalhães Luzin, Luciano Morais Lião, Eric de Souza Gil, Gérman Sanz, Boniek G Vaz, José R Sabino, Ricardo Menegatti, Marize Campos Valadares
This study shows the design, synthesis and antitumoral potential evaluation of a novel chalcone-like compound, (E)-3- (3, 5-di-ter-butyl-4-hydroxyphenyl)-1- (4-hydroxy-3-methoxyphenyl) prop-2-en-1-one [LQFM064) (4)], against human breast adenocarcinoma MCF7 cells. Some toxicological parameters were also investigated. LQFM064) (4) exhibited cytotoxic activity against MCF7 cells (IC50=21μM), in a concentration dependent-manner, and triggered significant changes in cell morphology and biochemical/molecular parameters, which are suggestive of an apoptosis inductor...
June 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28619620/development-of-a-solid-dosage-platform-for-the-oral-delivery-of-bilayer-vesicles
#12
Jitinder S Wilkhu, Sarah E Mcneil, David E Anderson, Marc Kirchmeier, Yvonne Perrie
Within this work, we develop vesicles incorporating sub-unit antigens as solid dosage forms suitable for the oral delivery of vaccines. Using a combination of trehalose, dextran and mannitol, freeze-dried oral disintegrating tablets were formed which upon rehydration release bilayer vesicles incorporating antigen. Initial studies focused on the optimisation of the freeze-dry cycle and subsequently excipient content was optimised by testing tablet hardness, disintegration time and moisture content. The use of 10% mannitol and 10% dextran produced durable tablets which offered strong resistance to mechanical damage yet appropriate disintegration times and dispersed to release niosomes-entrapping antigen...
June 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28614733/impact-of-capillary-flow-hydrodynamics-on-carrier-mediated-transport-of-opioid-derivatives-at-the-blood-brain-barrier-based-on-ph-dependent-michaelis-menten-and-crone-renkin-analyses
#13
Siti R Yusof, N Joan Abbott, Alex Avdeef
Most studies of blood-brain barrier (BBB) permeability and transport are conducted at a single pH, but more detailed information can be revealed by using multiple pH values. A pH-dependent biophysical model was applied to the mechanistic analysis of published pH-dependent BBB luminal uptake data from three opioid derivatives in rat: pentazocine (Suzuki et al., 2002a, 2002b), naloxone (Suzuki et al., 2010a), and oxycodone (Okura et al., 2008). Two types of data were processed: in situ brain perfusion (ISBP) and brain uptake index (BUI)...
June 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28614732/influence-of-the-drug-distribution-in-electrospun-gliadin-fibers-on-drug-release-behavior
#14
Ying Xu, Jiao-Jiao Li, Deng-Guang Yu, Gareth R Williams, Jun-He Yang, Xia Wang
Drug distribution within its carrier in a solid dosage form often generates a profound influence on its release profile, particularly when the physicochemical properties of the carrier are exploited to manipulate drug release behavior. In this job, two different types of distributions of a model drug ibuprofen (IBU) within a protein gliadin in their electrospun nanofibers were intentionally created. One was homogeneous distribution in the monolithic fibers fabricated using a modified coaxial process, and the other one was heterogeneous distribution in the core/shell fibers prepared through a traditional coaxial process...
June 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28606803/pharmaceutical-counselling-about-different-types-of-tablet-splitting-methods-based-on-the-results-of-weighing-tests-and-mechanical-development-of-splitting-devices
#15
O Somogyi, A Meskó, L Csorba, P Szabó, R Zelkó
The division of tablets and adequate methods of splitting them are a complex problem in all sectors of health care. Although tablet-splitting is often required, this procedure can be difficult for patients. Four tablets were investigated with different external features (shape, score-line, film-coat and size). The influencing effect of these features and the splitting methods was investigated according to the precision and "weight loss" of splitting techniques. All four types of tablets were halved by four methods: by hand, with a kitchen knife, with an original manufactured splitting device and with a modified tablet splitter based on a self-developed mechanical model...
June 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28599988/pharmacological-evaluation-and-molecular-docking-of-new-di-tert-butylphenol-compound-lqfm-091-a-new-dual-5-lox-cox-inhibitor
#16
Roberta Campos Lino, Daiany Priscila Bueno da Silva, Iziara Ferreira Florentino, Dayane Moreira da Silva, José Luís Rodrigues Martins, Daniel da Costa Batista, Karla Carneiro de Siqueira Leite, Bianca Villavicencio, Géssica A Vasconcelos, Andreia Luiza Pereira Silva, Renato Ivan de Ávila, Hugo Verli, Marize Campos Valadares, Eric de Souza Gil, Boniek G Vaz, Luciano M Lião, Ricardo Menegatti, Elson Alves Costa
Dual 5-LOX/COX inhibitors are potential new dual drugs to treat inflammatory conditions. This research aimed to design, synthesis and to evaluate the anti-inflammatory and antinociceptive effects of the new compound, which is derived from nimesulide and darbufelone lead compounds. The new dual inhibitor 5-LOX/COX has the possible advantage of gastrointestinal safety. A voltammetric experiment was conducted to observe the drug's antioxidative effect. A formalin test, a hot plate test and carrageenan-induced mechanical hyperalgesia were employed to evaluate the analgesic nature of LQFM-091...
June 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28606804/a-human-challenge-model-for-respiratory-syncytial-virus-kinetics-the-pharmacological-effect-of-a-novel-fusion-inhibitor-and-the-modeling-of-symptoms-scores
#17
Julia Korell, Bruce Green, John DeVincenzo, Dymphy Huntjens
Respiratory syncytial virus (RSV) causes acute lower respiratory tract infections, and is a major cause of hospital admissions and death in young children. Limited treatments currently exist that can prevent or minimise exacerbation of the disease. The aims of this work were: 1) to develop a population pharmacodynamic model to describe RSV kinetics (RSVK) in nasal lavage, 2) evaluate the impact of an investigational fusion inhibitor, JNJ-53718678, on RSVK, and 3) determine the relationship between RSVK and symptoms scores...
June 9, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28606802/quantification-and-modeling-of-nanomechanical-properties-of-chlorpropamide-%C3%AE-%C3%AE-and-%C3%AE-conformational-polymorphs
#18
Biljana Janković, Tatjana Joksimović, Jernej Stare, Evgeniy Losev, Viktoriya Zemtsova, Stane Srčič, Elena Boldyreva
The nanomechanical properties of the α-, β-, and γ- conformational polymorphs of chlorpropamide were determined by the dynamic contact module continuous stiffness measurement at nanoindenter. The mechanical anisotropy of the α-polymorph was confirmed by indenting different faces, and its deformational behavior was assigned as ductile. Based on the nanoindentation results, the β and γ forms are moderately hard with plastic flow at contact points. The results revealed a correlation between Young's modulus and inter-planar interaction energy with regard to crystal orientation...
June 9, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28603033/in-vivo-analysis-of-supersaturation-precipitation-absorption-behavior-after-oral-administration-of-pioglitazone-hydrochloride-salt-determinant-site-of-oral-absorption
#19
Yusuke Tanaka, Masahisa Sugihara, Ayaka Kawakami, So Imai, Takafumi Itou, Hirokazu Murase, Kazunori Saiki, Satoshi Kasaoka, Hiroshi Yoshikawa
The purpose of this study was to evaluate in vivo supersaturation/precipitation/absorption behavior in the gastrointestinal (GI) tract based on the luminal concentration-time profiles after oral administration of pioglitazone (PG, a highly permeable lipophilic base) and its hydrochloride salt (PG-HCl) to rats. In the in vitro precipitation experiment in the classic closed system, while the supersaturation was stable in the simulated gastric condition, PG drastically precipitated in the simulated intestinal condition, particularly at a higher initial degree of supersaturation...
June 9, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28603031/silk-fibroin-degumming-affects-scaffold-structure-and-release-of-macromolecular-drugs
#20
Kira Nultsch, Oliver Germershaus
Silk fibroin (SF) is a natural polymer with tremendous potential as a matrix for drug delivery systems as well as for tissue engineering. Silk sericin (SS) removal (degumming) is a critical step during SF purification, potentially affecting SF integrity and resulting in structural changes such as partial hydrolysis and inhibition of micelle formation. In addition to SF composition itself, the molecular weight and charge of encapsulated drugs may significantly affect drug release from SF matrices. The effect of these parameters on drug release was investigated by varying SF degumming time and charge of the model compound encapsulated in SF films...
June 9, 2017: European Journal of Pharmaceutical Sciences
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