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European Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/28330769/difference-in-the-core-shell-dynamics-of-polyethyleneimine-and-poly-l-lysine-dna-polyplexes
#1
Elina Vuorimaa-Laukkanen, Ekaterina S Lisitsyna, Tiia-Maaria Ketola, Emmanuelle Morin-Pickardat, Huamin Liang, Martina Hanzlíková, Marjo Yliperttula
Electrostatic polymer-DNA complexes (polyplexes) have been widely investigated for DNA delivery, and remarkable differences in transfection efficacy have been seen among the materials. For example, polyethyleneimine (PEI) mediates DNA transfection more effectively than poly(l-lysine) (PLL). Biophysical properties of the polyplexes may explain their different properties in gene delivery. We investigated the structural dynamics in DNA polyplexes, especially the material exchange between the core and shell regions of the PEI and PLL polyplexes...
March 18, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28323119/cumulative-evidence-of-the-low-reliability-of-frozen-thawed-pig-skin-as-a-model-for-in-vitro-percutaneous-permeation-testing
#2
LETTER
Amnon C Sintov
Porcine skin has frequently been used as a model in in vitro permeation studies being considered as an excellent alternative for human skin due to biochemical similarities. The use of frozen skin after thawing is particularly more convenient for these studies since it is available whenever needed. Even though several researchers have noticed that freezing and then thawing the tissue result in enhancement of drug permeation, many published articles have still described studies using frozen pig skin for bioequivalence and transdermal evaluation of drug products...
March 18, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28323118/mixed-poly-vinyl-pyrrolidone-based-drug-loaded-nanomicelles-shows-enhanced-efficacy-against-pancreatic-cancer-cell-lines
#3
Anisha Veeren, Archana Bhaw-Luximon, Debabrata Mukhopadhyay, Dhanjay Jhurry
We report in this paper on the enhanced efficacy of a physical mixture of two single anti-cancer loaded nanomicelles against PANC-1 and BxPC-3. Poly(vinyl pyrrolidone-b-polycaprolactone) (PVP-b-PCL) and poly(vinyl pyrrolidone-b-poly(dioxanone-co-methyl dioxanone)) (PVP-b-P(DX-co-MeDX)) were synthesized and successfully loaded with various anti-cancer drugs - gemcitabine (GEM), doxorubicin.HCl (DOX.HCl), doxorubicin.NH2 (DOX), 5-fluorouracil (5-FU) and paclitaxel (PTX). Spherical micelles of size 160-477 nm were obtained as characterized by DLS while sizes determined by TEM were in the range 140-250 nm...
March 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28323117/absorption-metabolism-and-excretion-of-the-glp-1-analogue-semaglutide-in-humans-and-nonclinical-species
#4
Lene Jensen, Hans Helleberg, Ad Roffel, Jan Jaap van Lier, Inga Bjørnsdottir, Palle Jacob Pedersen, Everton Rowe, Julie Derving Karsbøl, Mette Lund Pedersen
Semaglutide is a human glucagon-like peptide-1 analogue in clinical development for the treatment of type 2 diabetes. The absorption, metabolism and excretion of a single 0.5mg/450μCi [16.7MBq] subcutaneous dose of [(3)H]-radiolabelled semaglutide was investigated in healthy human subjects and compared with data from nonclinical studies. Radioactivity in blood, plasma, urine and faeces was determined in humans, rats and monkeys; radioactivity in expired air was determined in humans and rats. Metabolites in plasma, urine and faeces were quantified following profiling and radiodetection...
March 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28323116/the-effect-of-g3-pamam-dendrimer-conjugated-with-b-group-vitamins-on-cell-morphology-motility-and-atp-level-in-normal-and-cancer-cells
#5
Łukasz Uram, Magdalena Szuster, Maria Misiorek, Aleksandra Filipowicz, Stanisław Wołowiec, Elżbieta Wałajtys-Rode
In a search for the safe vitamin carrier the PAMAM G3 dendrimer covalently substituted with 9 and 10 molecules of vitamin B7 (biotin) and B6 (pyridoxal), respectively (BC-PAMAM) was investigated. Dendrimer substitution with B-group vitamins significantly alters its biological properties as compared to native form. Observed effects on investigated cell parameters including morphology, adhesion, migration and ATP level were different for normal human fibroblasts (BJ) and squamous cell carcinoma (SCC-15) cell lines...
March 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28323115/gene-transfection-efficiency-into-dendritic-cells-is-influenced-by-the-size-of-cationic-liposomes-dna-complexes
#6
Yoshikazu Inoh, Mie Nagai, Kayo Matsushita, Mamoru Nakanishi, Tadahide Furuno
Cationic liposomes have attracted recent attention as DNA vaccine carriers that can target dendritic cells (DCs). In general, cationic liposome/DNA complexes (lipoplexes) are taken up by various cells via clathrin-mediated endocytosis, caveolae-mediated endocytosis, macropinocytosis, or phagocytosis, with the mode of endocytosis determining further intracellular trafficking pathways. Moreover, the physicochemical properties of cationic lipoplexes, including lipid composition, shape, size, and charge, influence transfection efficiency, affecting uptake and subsequent intracellular pathways...
March 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28315463/in-vitro-biphasic-dissolution-tests-and-their-suitability-for-establishing-in-vitro-in-vivo-correlations-a-historical-review
#7
REVIEW
Aude Pestieau, Brigitte Evrard
For many decades, one of the most critical issues in the pharmaceutical industry has been the poor solubility of some drugs. Indeed, a prerequisite for drug absorption is the presence of dissolved drug at the absorption site and this can be challenging for compounds with low aqueous solubility such as BCS class II (low solubility, high permeability) and IV (low solubility, low permeability) compounds. If the development of oral delivery formulations of these compounds is frequently challenging to formulation scientists in the pharmaceutical industry, the in vitro evaluation of these new formulations is also a great challenge...
March 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28315467/hce-t-cell-based-permeability-model-a-well-maintained-or-a-highly-variable-barrier-phenotype
#8
Marina Juretić, Bisera Jurišić Dukovski, Iva Krtalić, Stephan Reichl, Biserka Cetina-Čižmek, Jelena Filipović-Grčić, Jasmina Lovrić, Ivan Pepić
The most extensively characterized human-derived cell line used in transcorneal permeability studies, in terms of passive transcellular and paracellular transport, transporter expression and metabolic enzymes, is the immortalized human corneal epithelial cell line (HCE-T). The purpose of this study is to describe the changes in the HCE-T barrier phenotype in vitro when valid cultivation conditions, in accordance with the standardized HCE-T cell-based model protocol, were employed. Evaluation of the structural and functional barrier properties revealed two different HCE-T barrier phenotypes, depending on the polycarbonate membrane pore size...
March 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28315466/innovative-approach-for-identifying-root-causes-of-glass-defects-in-sterile-drug-product-manufacturing
#9
Lukas Eberle, Alexander Svensson, Andreas Graser, Joerg Luemkemann, Hirokazu Sugiyama, Rainer Schmidt, Konrad Hungerbuehler
In sterile drug product manufacturing, scratched and broken glass containers (i.e., vials) cause product losses, glass particles, equipment contamination and additional cleaning efforts. However, mechanical resistance and exposure of vials to mechanical stress are not sufficiently understood, and no systematic approach for reducing glass-related losses is established. Manufacturers may tackle glass-related losses more rationally if (i) frequencies for inflicting disqualifying damages to drug product containers are known for given forces, (ii) actual exposure in industrial filling lines is quantified and (iii) process enhancements are derived based on collected information...
March 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28315465/early-preclinical-evaluation-of-dihydropyrimidin-thi-ones-as-potential-anticonvulsant-drug-candidates
#10
Mariana Matias, Gonçalo Campos, Samuel Silvestre, Amílcar Falcão, Gilberto Alves
Although significant advances are occurring in epilepsy research, about 30% of epileptic patients are still inadequately controlled by standard drug therapy. For this reason, it continues to be important to develop new chemical entities through which epilepsy could be effectively controlled. In this study, the anticonvulsant activity of forty-two dihydropyrimidin(thi)ones was explored and their efficacy was evaluated in rodents against the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole tests...
March 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28315464/a-novel-nanosuspension-of-andrographolide-preparation-characterization-and-passive-liver-target-evaluation-in-rats
#11
Ligang Guo, Le Kang, Xinrong Liu, Xiangyun Lin, Donghua Di, Yong Wu, Dexian Kong, Yihui Deng, Yanzhi Song
Andrographolide (Andro) is an excellent anti-inflammatory bicyclic diterpene γ-lactone. However, the poor solubility limits its application as injection for the treatment of acute inflammation. To meet the clinical needs for emergency, the Andro nanosuspensions injection was first prepared by the wet milling technique. The Andro nanosuspensions were composed of 3% Andro, 5% poloxamer 188 as the non-ionic stabilizer, 0.05% sodium deoxycholate or 0.1% sodium tauroursodeoxy cholate as the ionic stabilizer, and prepared by 350rpm speed and 12cycles of grinding with 0...
March 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28302396/supercritical-antisolvent-co-precipitation-of-rifampicin-and-ethyl-cellulose
#12
Rania Djerafi, Andri Swanepoel, Christelle Crampon, Lonji Kalombo, Philip Labuschagne, Elisabeth Badens, Yasmine Masmoudi
Rifampicin-loaded submicron-sized particles were prepared through supercritical anti-solvent process using ethyl cellulose as polymeric encapsulating excipient. Ethyl acetate and a mixture of ethyl acetate/dimethyl sulfoxide (70/30 and 85/15) were used as solvents for both drug and polymeric excipient. When ethyl acetate was used, rifampicin was crystallized separately without being embedded within the ethyl cellulose matrix while by using the ethyl acetate/dimethyl sulfoxide mixture, reduced crystallinity of the active ingredient was observed and a simultaneous precipitation of ethyl cellulose and drug was achieved...
March 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28300611/surface-area-volume-and-shape-descriptors-as-a-novel-tool-for-polymer-lead-design-and-discovery
#13
Jonatan Riis Christensen, Helena Meng-Lund, Holger Grohganz, Antti Poso, Tuomo Laitinen, Ossi Korhonen, Lene Jørgensen, Jari Pajander
In recent years, the demand and interest for functionalized polymers have increased for drug delivery purposes. Because of the increased interest, methods that can be used to predict physical and chemical properties of polymers prior to synthesis would be of high value for the design and development of novel polymer structures. Through use of molecular descriptors and Principal Component Analysis, this study explores the possibilities of using in silico methods for polymer design and characterization for property prediction...
March 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28288854/irinotecan-induced-bile-acid-malabsorption-is-associated-with-down-regulation-of-ileal-asbt-slc10a2-in-mice
#14
A-Xi Shi, Yan Zhou, Xiao-Yi Zhang, Yan-Shu Zhao, Hong-Yan Qin, Yan-Ping Wang, Xin-An Wu
Irinotecan, (CPT-11), an antitumor agent primarily used for the treatment of solid tumors, has often compromised clinical application due to the inducement of severe delay-onset diarrhea. Bile acid malabsorption (BAM) is widely accepted as the common cause of diarrhea. However, whether CPT-11-induced diarrhea has correlation with BAM is unknown. The aim of this study was to investigate the effect of CPT-11 on the bile acid homeostasis in mice. The mice were administrated with CPT-11 intravenously for four consecutive days...
March 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28286289/mechanistic-investigation-of-the-negative-food-effect-of-modified-release-zolpidem
#15
Cord J Andreas, Xavier Pepin, Constantinos Markopoulos, Maria Vertzoni, Christos Reppas, Jennifer Dressman
AIMS: When administered orally as either an immediate or modified release dosage form, zolpidem demonstrates a negative food effect, i.e. decrease in Cmax and AUC. The aim of the study was to arrive at a better understanding of the absorption of this BCS class I compound, in vivo and to simulate the observed plasma profiles using in vitro and in silico methods. METHODS: Pharmacokinetic profiles of zolpidem are presented from a bioavailability (8mg intravenous; 10mg immediate release Stilnox®; 10mg and 12...
March 9, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28285174/a-computational-study-suggests-that-replacing-peg-with-pmoz-may-increase-exposure-of-hydrophobic-targeting-moiety
#16
Aniket Magarkar, Tomasz Róg, Alex Bunker
In a previous study we showed that the cause of failure of a new, proposed, targeting ligand, the AETP moiety, when attached to a PEGylated liposome, was occlusion by the poly(ethylene glycol) (PEG) layer due to its hydrophobic nature, given that PEG is not entirely hydrophilic. At the time we proposed that possible replacement with a more hydrophilic protective polymer could alleviate this problem. In this study we have used computational molecular dynamics modelling, using a model with all atom resolution, to suggest that a specific alternative protective polymer, poly(2-methyloxazoline) (PMOZ), would perform exactly this function...
March 9, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28285173/peptide-dendrimer-conjugates-of-ketoprofen-synthesis-and-ex-vivo-and-in-vivo-evaluations-of-passive-diffusion-sonophoresis-and-iontophoresis-for-skin-delivery
#17
Aswathi R Hegde, Prarthana V Rewatkar, Jyothsna Manikkath, Karnaker Tupally, Harendra S Parekh, Srinivas Mutalik
The aim of this study was to evaluate skin delivery of ketoprofen when covalently tethered to mildly cationic (2(+) or 4(+)) peptide dendrimers prepared wholly by solid phase peptide synthesis. The amino acids glycine, arginine and lysine formed the dendrimer with ketoprofen tethered either to the lysine side-arm (Nε) or periphery of dendrimeric branches. Passive diffusion, sonophoresis- and iontophoresis-assisted permeation of each peptide dendrimer-drug conjugate (D1-D4) was studied across mouse skin, both in vitro and in vivo...
March 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28285172/multifunctional-luv-liposomes-decorated-for-bbb-and-amyloid-targeting-b-in-vivo-brain-targeting-potential-in-wild-type-and-app-ps1-mice
#18
Konstantina Papadia, Anastasios D Giannou, Eleni Markoutsa, Christian Bigot, Greejte Vanhoute, Spyridon Mourtas, Annemie Van der Linded, Georgios T Stathopoulos, Sophia G Antimisiaris
Multifunctional liposomes (mf-LIPs) having a curcumin-lipid ligand (to target amyloids) together with two ligands to target the transferrin, and the low-density apolipoprotein receptor of the blood-brain-barrier (BBB) on their surface, were previously studied (in vitro) as potential theranostic systems for Alzheimer's disease (AD) (Papadia et al., 2017, Eur. J. Pharm. Sciences; 101:140-148). Herein, the targeting potential of mf-LIPs was compared to that of BBB-LIPs (liposomes having only the two BBB-specific ligands) in FVB mice (normal), as well as in double transgenic mice (APP/PS1) and their corresponding littermates (WT), by live-animal (in vivo) and explanted organ (ex vivo) imaging...
March 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28279762/process-optimization-by-use-of-design-of-experiments-application-for-liposomalization-of-fk506
#19
Hiroyasu Toyota, Tomohiro Asai, Naoto Oku
Design of experiments (DoE) can accelerate the optimization of drug formulations, especially complexed formulas such as those of drugs, using delivery systems. Administration of FK506 encapsulated in liposomes (FK506 liposomes) is an effective approach to treat acute stroke in animal studies. To provide FK506 liposomes as a brain protective agent, it is necessary to manufacture these liposomes with good reproducibility. The objective of this study was to confirm the usefulness of DoE for the process-optimization study of FK506 liposomes...
March 7, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28279761/evaluation-of-caax-prenyl-protease-ii-of-leishmania-donovani-as-potential-drug-target-infectivity-and-growth-of-the-parasite-is-significantly-lowered-after-the-gene-knockout
#20
Ruchika Bhardwaj, Mousumi Das, Shalini Singh, Adarsh Kumar Chiranjivi, Sitraraau Vijaya Prabhu, Sanjeev Kumar Singh, Vikash Kumar Dubey
Prenylation pathway is responsible for post translational modification of various signal proteins, including proteins of Ras superfamily. CAAX prenyl proteases are known to be key players in prenylation pathway. In the current study, we have evaluated CAAX prenyl protease II as a possible drug target against Leishmania donovani parasite, the causative agent of visceral leishmaniasis. Gene knockout strategy was employed to target CAAX prenyl protease II and subsequent effects were studied. CAAX prenyl protease II knockout resulted in significant decrease in growth and infectivity...
March 7, 2017: European Journal of Pharmaceutical Sciences
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