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European Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/28716758/oral-delivery-of-vancomycin-by-tetraether-lipid-liposomes
#1
Philipp Uhl, Silvia Pantze, Philip Storck, Johannes Parmentier, Dominik Witzigmann, Götz Hofhaus, Jörg Huwyler, Walter Mier, Gert Fricker
Despite the outstanding progress in modern medicine, the oral delivery of peptide drugs is limited until today due to their instability in the gastrointestinal tract and low mucosa penetration. To overcome these hurdles, liposomes containing the specific tetraether lipid GCTE (glycerylcaldityltetraether lipid) were examined. For this purpose, the glycopeptide antibiotic vancomycin was used as model substance and liposomes were prepared by DAC (dual assymetric centrifugation). These liposomes showed a size and polydispersity index comparable to standard liposomes...
July 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28716757/saturated-phosphatidylcholine-as-matrix-former-for-oral-extended-release-dosage-forms
#2
Marina Kolbina, Roland Bodmeier, Martin Körber
The aim of this study was to evaluate the suitability of saturated phosphatidylcholine (Phospholipon® 90H) as extended release excipient in matrix tablets for three model drugs with different aqueous solubility (theophylline, caffeine and diprophylline). The tablets could be prepared by direct compression because of the favorable phospholipid powder flow properties (Carr's index: 12.64 and angle of repose: 28.85) and good compactibility. Tablets of low porosity were formed already at low pressure of 40MPa and with drug loadings up to 70% due to high plasticity of the phospholipid...
July 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28711715/novel-peptide-motifs-from-lysozyme-suppress-pro-inflammatory-cytokines-in-macrophages-by-antagonizing-toll-like-receptor-and-lps-scavenging-action
#3
Hisham R Ibrahim, Kosuke Hamasaki, Takeshi Miyata
Lysozyme is commonly found in spots where bacterial infections are most likely to enter the body. Earlier we found that lysozyme possesses five antimicrobial peptide motifs in its N-terminal region which can be generated by newborn pepsin. In this study, we explore the role of these peptides in the anti-inflammatory activity of lysozyme. The five peptides, helix1 (H1), helix2 (H2), H1 and H2 connected with a loop (HLH), H2 extended with either 2 β-strands (H2-S12) or 3 β-strands (H2-S13), were synthesized and examined for anti-inflammatory action...
July 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28711714/review-an-update-on-the-use-of-oral-phospholipid-excipients
#4
Peter van Hoogevest
The knowledge and experiences obtained with oral phospholipid excipients is increasing continuously. Nevertheless the present number of oral products using these excipients as essential excipient is very limited. This is remarkable to note, since phospholipids play a significant role in the food uptake mechanisms of the GI tract and these mechanisms could be translated into suitable dosage forms and corresponding drug delivery strategies. In addition, phospholipid excipients are multifunctional biodegradable, non-toxic excipients, which can be used in oral dosage forms as wetting agents, emulsifier, solubilizer and matrix forming excipients...
July 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28711713/surprisingly-high-stability-of-the-a%C3%AE-oligomer-eliminating-all-d-enantiomeric-peptide-d3-in-media-simulating-the-route-of-orally-administered-drugs
#5
Anne Elfgen, Beatrix Santiago-Schübel, Lothar Gremer, Janine Kutzsche, Dieter Willbold
The aggregation of the amyloid β protein (Aβ) plays an important role in the pathology of Alzheimer's disease. Previously, we have developed the all-d-enantiomeric peptide D3, which is able to eliminate neurotoxic Aβ oligomers in vitro and improve cognition in a transgenic Alzheimer's disease mouse model in vivo even after oral administration. d-Peptides are expected to be more resistant against enzymatic proteolysis compared to their l-enantiomeric equivalents, and indeed, a pharmacokinetic study with tritiated D3 revealed the oral bioavailability to be about 58%...
July 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28711712/ex-vivo-and-in-vivo-evaluation-of-microemulsion-based-transdermal-delivery-of-e-coli-specific-t4-bacteriophage-a-rationale-approach-to-treat-bacterial-infection
#6
Vaibhav Rastogi, Pragya Yadav, Anurag Verma, Jayanta K Pandit
This study is focused on the development and evaluation of transdermal delivery of E. coli-specific T4 bacteriophages both ex-vivo and in-vivo using microemulsion as delivery carrier in eradicating the infection caused by E. coli. Microemulsions were prepared by mixing selected oil, surfactants and aqueous phase containing bacteriophages. The formulations were subjected to physicochemical characterization, ex-vivo and in-vivo permeation, stability studies, histological and immunofluorescence examination. The colloidal system exhibits a uniform size distribution, of finite size (150-320nm)...
July 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28709911/increased-drug-load-and-polymer-compatibility-of-bilayered-orodispersible-films
#7
J Carolina Visser, Oekie A F Weggemans, René J Boosman, Katja U Loos, Henderik W Frijlink, Herman J Woerdenbag
The addition of enalapril maleate to a casting solution for orodispersible films (ODFs) containing hypromellose and carbomer 974P as film forming agents (standard casting solution, SCS) caused a dose dependent reduction of the viscosity. This phenomenon was a serious problem in the preparation of ODFs with an increased enalapril load (>1mg per ODF) when using the solvent casting method. The aim of the present work was twofold. Firstly, the influence of enalapril on the viscosity of SCS was studied in more detail...
July 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28709912/excipient-mediated-alteration-in-drug-bioavailability-in-the-rat-model-depends-on-the-sex-of-the-animal
#8
Yang Mai, Francisco Afonso-Pereira, Sudaxshina Murdan, Abdul Basit
The pharmaceutical excipient, polyethylene glycol 400 (PEG 400), unexpectedly alters the bioavailability of the BCS class III drug ranitidine in a sex-dependent manner. As ranitidine is a substrate for the efflux transporter P-glycoprotein (P-gp), we hypothesized that the sex-related influence could be due to interactions between PEG 400 and P-gp. In this study, we tested this hypothesis by: i) measuring the influence of PEG 400 on the oral bioavailability of another P-gp substrate (ampicillin) and of a non-P-gp substrate(metformin); and ii) measuring the effect of PEG 400 on drug bioavailability in the presence of a P-gp inhibitor (cyclosporine A) in male and female rats...
July 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28709910/silicon-zinc-glycerol-hydrogel-a-potential-immunotropic-agent-for-topical-application
#9
Tat'yana G Khonina, Maria V Ivanenko, Oleg N Chupakhin, Alexander P Safronov, Ekaterina A Bogdanova, Maxim S Karabanalov, Vasily V Permikin, Leonid P Larionov, Lyudmila I Drozdova
Nanoparticles synthesized using sol-gel method are promising agents for biomedical applications, in particular for the therapy and diagnosis of various diseases. Using silicon and zinc glycerolates as biocompatible precursors we synthesized by the sol-gel method a new bioactive silicon-zinc-containing glycerohydrogel combining the positive pharmacological properties of the precursors. In the present work the structural features of silicon-zinc-containing glycerohydrogel and its immunotropic properties were studied...
July 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28709909/pemetrexed-conjugated-with-gold-nanoparticles-synthesis-characterization-and-a-study-of-noncovalent-interactions
#10
Elżbieta U Stolarczyk, Krzysztof Stolarczyk, Marta Łaszcz, Marek Kubiszewski, Andrzej Leś, Olga Michalak
Gold nanoparticles (AuNPs) have been widely used as nanocarriers in drug delivery application. However, the binding mechanism between AuNPs and drug bases still remains a puzzle. Our study included: (i) optimization of three synthesis of the AuNPs-pemetrexed (PE) nanocomposites formation which was monitored by UV-Vis spectroscopy, (ii) identification of PE in gold nanocomposites and mechanism of PE interaction with gold nanoparticles by electrochemistry, NMR and Raman measurements, (iii) characterization of the three nanocomposites by TEM, DSL, ESL, zeta potential, XRPD and TGA analysis...
July 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28693957/follicle-stimulating-hormone-encapsulation-in-the-cholesterol-modified-chitosan-nanoparticles-via-molecular-dynamics-simulations-and-binding-free-energy-calculations
#11
Mohammad Yahyaei, Faramarz Mehrnejad, Hossein Naderi-Manesh, Ali Hossein Rezayan
Follicle-stimulating hormone (FSH) is widely applied in the modern ovarian stimulation techniques. However, it must be administered daily because of its short half-life. Recently, the cholesterol (CS) modified chitosan (CTS) nanogels have attracted significant interest as promising controlled release protein delivery because of their ability to minimize the aggregation and irreversible denaturation of proteins. Herein, we report a molecular dynamics (MD) simulation investigation on the molecular mechanisms of FSH encapsulation in the CS-CTS nanogels...
July 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28693956/mechanistic-insights-of-the-enhancement-effect-of-sorbitan-monooleate-on-olanzapine-transdermal-patch-both-in-release-and-percutaneous-absorption-processes
#12
Ning Li, Peng Quan, XiaoCao Wan, Chao Liu, Xiaochang Liu, Liang Fang
In this paper, based on the optimized formulation of olanzapine (OLN) transdermal patch, the role of sorbitan monooleate (SP) in OLN release and percutaneous absorption processes was probed in vitro and in vivo. Rheological test, DSC, FT-IR and molecular modeling were conducted to elucidate the effect of SP on the release process of OLN from transdermal patch. Additionally, the action of SP on the percutaneous absorption process was probed using tape stripping transdermal experiment, confocal laser scanning microscopy (CLSM), ATR-FTIR and molecular docking...
July 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28690099/electrospun-polymeric-nanofibers-new-horizons-in-drug-delivery
#13
REVIEW
Shreya Thakkar, Manju Misra
Nanofibers obtained using electrospinning technique are being used since ages especially in fields of textile industry, sensors, filters, protective clothing and tissue engineering. Their use as drug delivery system is an emerging platform in the field of pharmaceuticals and now-a-days formulation scientists are paying great attention to the technology due to several advantages prime being easy modulation of drug release profile depending upon the properties of polymer/polymeric blends/other materials used...
July 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28687529/design-synthesis-and-biological-evaluation-of-2-4-dihydropyrano-2-3-c-pyrazole-derivatives-as-autotaxin-inhibitors
#14
Tatu Pantsar, Prosanta Singha, Tapio J Nevalainen, Igor Koshevoy, Jukka Leppänen, Antti Poso, Juha M A Niskanen, Sanna Pasonen-Seppänen, Juha R Savinainen, Tuomo Laitinen, Jarmo T Laitinen
Inhibition of Autotaxin (ATX) is a potential treatment strategy for several diseases, including tumors with elevated ATX-lysophosphatidic acid (LPA) signaling. Combining structure-based virtual screening together with hen egg-white Autotaxin (ewATX) activity assays enabled the discovery of novel small-molecule ATX inhibitors with a 2,4-dihydropyrano[2,3-c]pyrazole scaffold. These compounds are suggested to bind to the lipophilic pocket, leaving the active site unrestrained. Our most potent compound, (S)-6-amino-4-(3,4-dichlorophenyl)-3-(4-[(4-fluorobenzyl)oxy]phenyl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile [(S)-25], inhibited human ATX (hATX) with an IC50-value of 134nM...
July 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28687530/comparison-of-segmental-dependent-permeability-in-human-and-in-situ-perfusion-model-in-rat
#15
Ruiz-Picazo Alejandro, Lozoya-Agullo Isabel, Ortiz-Azcarate Miguel, Merino-Sanjuán Matilde, González-Álvarez Marta, González-Álvarez Isabel, Bermejo Marival
Nowadays, alternative methods have been developed to predict intestinal permeability values in human as in vitro, in situ or ex vivo methods. They were developed by the necessity to avoid the problems of the human permeability experiments. However, determination of human permeability is needed to properly validate the alternative methods. For this reason, recently, Dahlgren et al. published an indirect method based on a deconvolution technique to estimate the human permeability in different gastrointestinal segments (jejunum, ileum and colon)...
July 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28687528/selection-of-effective-cocrystals-former-for-dissolution-rate-improvement-of-active-pharmaceutical-ingredients-based-on-lipoaffinity-index
#16
Piotr Cysewski, Maciej Przybyłek
New theoretical screening procedure was proposed for appropriate selection of potential cocrystal formers possessing the ability of enhancing dissolution rates of drugs. The procedure relies on the training set comprising 102 positive and 17 negative cases of cocrystals found in the literature. Despite the fact that the only available data were of qualitative character, performed statistical analysis using binary classification allowed to formulate quantitative criterions. Among considered 3679 molecular descriptors the relative value of lipoaffinity index, expressed as the difference between values calculated for active compound and excipient, has been found as the most appropriate measure suited for discrimination of positive and negative cases...
July 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28684136/open-innovation-towards-sharing-of-data-models-and-workflows
#17
Daniela J Conrado, Mats O Karlsson, Klaus Romero, Céline Sarr, Justin J Wilkins
Sharing of resources across organisations to support open innovation is an old idea, but which is being taken up by the scientific community at increasing speed, concerning public sharing in particular. The ability to address new questions or provide more precise answers to old questions through merged information is among the attractive features of sharing. Increased efficiency through reuse, and increased reliability of scientific findings through enhanced transparency, are expected outcomes from sharing...
July 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28679107/macrophage-selective-photodynamic-therapy-by-meta-tetra-hydroxyphenyl-chlorin-loaded-polymeric-micelles-a-possible-treatment-for-cardiovascular-diseases
#18
Jos W H Wennink, Yanna Liu, Petri I Mäkinen, Francesca Setaro, Andrès de la Escosura, Meriem Bourajjaj, Jari P Lappalainen, Lari P Holappa, Joep B van den Dikkenberg, Mina Al Fartousi, Panagiotis N Trohopoulos, Seppo Ylä-Herttuala, Tomas Torres, Wim E Hennink, Cornelus F van Nostrum
Selective elimination of macrophages by photodynamic therapy (PDT) is a new and promising therapeutic modality for the reduction of atherosclerotic plaques. m-Tetra(hydroxyphenyl)chlorin (mTHPC, or Temoporfin) may be suitable as photosensitizer for this application, as it is currently used in the clinic for cancer PDT. In the present study, mTHPC was encapsulated in polymeric micelles based on benzyl-poly(ε-caprolactone)-b-methoxy poly(ethylene glycol) (Ben-PCL-mPEG) using a film hydration method, with loading capacity of 17%...
July 2, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28673756/in-vitro-simulation-of-realistic-gastric-pressure-profiles
#19
Felix Schneider, Regine Beeck, Melanie Hoppe, Mirko Koziolek, Werner Weitschies
Novel in vitro dissolution tools can aid the development of orally administered drugs by explaining dosage form related in vivo phenomena that are not explainable with standard test apparatuses. Such novel tools are able to mimic various parameters in accordance with gastrointestinal conditions. Hereby, in vivo occurring pressure events were shown to be of major importance since they largely affect dosage form disintegration, drug dissolution and subsequently resulting drug plasma concentration profiles. The aim of the present study was to investigate the feasibility of producing biorelevant pressure events with standard test apparatuses and with the dynamic open flow through test apparatus...
June 30, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28669637/editorial-iapc-5-special-issue
#20
EDITORIAL
Zoran Mandic, Kin Tam
No abstract text is available yet for this article.
June 29, 2017: European Journal of Pharmaceutical Sciences
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