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European Journal of Pharmaceutics and Biopharmaceutics

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https://www.readbyqxmd.com/read/28729179/global-regression-model-for-moisture-content-determination-using-near-infrared-spectroscopy
#1
Matthieu Clavaud, Yves Roggo, Klara Degardin, Pierre-Yves Sacré, Philippe Hubert, Eric Ziemons
Near-infrared (NIR) global quantitative models were evaluated for the moisture content (MC) determination of three different freeze-dried drug products. The quantitative models were based on 3822 spectra measured on two identical spectrometers to include variability. The MC, measured with the reference Karl Fischer (KF) method, were ranged from 0.05% to 4.96%. Linear and non-linear regression models using Partial Least Square (PLS), Decision Tree (DT), Bayesian Ridge Regression (Bayes-RR), K-Nearest Neighbors (KNN), and Support Vector Regression (SVR) algorithms were created and evaluated...
July 17, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28720487/pdms-b-pmoxa-polymersomes-for-hepatocyte-targeting-and-assessment-of-toxicity
#2
Klara Kiene, Susanne H Schenk, Fabiola Porta, Alexandra Ernst, Dominik Witzigmann, Philip Grossen, Jörg Huwyler
Nanoparticles, such as polymersomes, can be directed to the hepatic asialoglycoprotein receptor to achieve targeted drug delivery. In this study, we prepared asialofetuin conjugated polymersomes based on the amphiphilic di-block copolymer poly(dimethylsiloxane)-b-poly(2-methyloxazoline) (PDMS-b-PMOXA). They had an average diameter of 150nm and formed monodisperse vesicles. Drug encapsulation and sustained release was monitored using the hydrophilic model compound carboxyfluorescein. Asialoglycoprotein receptor specific uptake by HepG2 cells in vitro was energy dependent and could be competitively inhibited by the free targeting ligand...
July 15, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28713018/effect-of-increased-surface-hydrophobicity-via-drug-conjugation-on-the-clearance-of-inhaled-pegylated-polylysine-dendrimers
#3
Shadabul Haque, Victoria M McLeod, Seth Jones, Sandy Fung, Michael Whittaker, Michelle McIntosh, Colin Pouton, David J Owen, Christopher J H Porter, Lisa M Kaminskas
PEGylated polylysine dendrimers are attractive and well tolerated inhalable drug delivery platforms that have the potential to control the release, absorption kinetics and lung retention time of conjugated drugs. The clinical application of these systems though, would likely require partial substitution of surface PEG groups with drug molecules that are anticipated to alter their lung clearance kinetics and clearance pathways. In the current study, we therefore evaluated the impact of increased surface hydrophobicity via substitution of 50% surface PEG groups with a model hydrophobic drug (α-carboxyl OtButylated methotrexate) on the lung clearance of a Generation 5 PEGylated polylysine dendrimer in rats...
July 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28709903/targeted-delivery-of-cyclosporine-a-by-polymeric-nanocarriers-improves-the-therapy-of-inflammatory-bowel-disease-in-a-relevant-mouse-model
#4
Ana Melero, Christina Draheim, Steffi Hansen, Elisa Giner, Juan José Carreras, Raquel Talens-Visconti, Teresa María Garrigues, José Esteban Peris, Ma Carmen Recio, Rosa Giner, Claus-Michael Lehr
The therapy of inflammatory bowel diseases is still rather inefficient, and about 80% of patients require surgery at some stage. Improving the treatments by more efficient medication is, therefore, an urgent medical need. The objective of this project was to demonstrate targeted delivery of Cyclosporine-A (CYA) to the inflamed areas of the intestinal mucosa after oral administration, enabling improved alleviation of the symptoms and, at the same time, reduced systemic drug absorption and associated adverse effects...
July 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28694161/cxcr4-targeted-dendrimer-for-anti-cancer-drug-delivery-and-breast-cancer-cell-migration-inhibition
#5
Chuda Chittasupho, Songyot Anuchapreeda, Narong Sarisuta
CXCR4 and its ligand CXCL12 play a critical role in the metastasis of various types of cancer including breast cancer. Breast tumors preferentially metastasize to the lung, bones and distant lymph nodes, secreting high levels of CXCL12. We hypothesized that targeted inhibition of CXCR4 in breast cancer cells should suppress CXCR4-positive tumor cells toward secondary metastatic sites. In the present study, the efficacy of CXCR4 targeted dendrimers carrying DOX (LFC131-DOX-D4) on cellular binding, cytotoxicity, and migration of BT-549-Luc and T47D breast cancer cells was investigated...
July 7, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28694160/artificial-neural-network-based-particle-size-prediction-of-polymeric-nanoparticles
#6
John Youshia, Mohamed Ehab Ali, Alf Lamprecht
Particle size of nanoparticles and the respective polydispersity are key factors influencing their biopharmaceutical behavior in a large variety of therapeutic applications. Predicting these attributes would skip many preliminary studies usually required to optimize formulations. The aim was to build a mathematical model capable of predicting the particle size of polymeric nanoparticles produced by a pharmaceutical polymer of choice. Polymer properties controlling the particle size were identified as molecular weight, hydrophobicity and surface activity, and were quantified by measuring polymer viscosity, contact angle and interfacial tension, respectively...
July 7, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28690201/neurotensin-receptor-1-facilitates-intracellular-and-transepithelial-delivery-of-macromolecules
#7
Joanna L Bird, Rachael Simpson, Driton Vllasaliu, Alan D Goddard
G protein-coupled receptors are expressed on the surface of eukaryotic cells and internalise in response to ligand binding. The actions of the hormone and neurotransmitter neurotensin (NT) are predominantly mediated by specific interactions with one such receptor. Neurotensin receptor 1 (NTS1), which is upregulated in a variety of cancers, including pancreatic and breast tumours. NTS1 could therefore serve as a target for selective delivery of therapeutics. This study characterised the expression of NTS1 in HEK293 cells, as well as both polarised and non-polarised intestinal epithelial Caco-2 cells...
July 6, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28690200/functional-electrospun-fibers-for-the-treatment-of-human-skin-wounds
#8
REVIEW
Jing Wang, Maike Windbergs
Wounds are trauma induced defects of the human skin involving a multitude of endogenous biochemical events and cellular reactions of the immune system. The healing process is extremely complex and affected by the patient́s physiological conditions, potential implications like infectious pathogens and inflammation as well as external factors. Due to increasing incidence of chronic wounds and proceeding resistance of infection pathogens, there is a strong need for effective therapeutic wound care. In this context, electrospun fibers with diameters in the nano- to micrometer range gain increasing interest...
July 6, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28690199/high-concentration-protein-formulations-how-high-is-high
#9
Patrick Garidel, Alexander B Kuhn, Lars V Schäfer, Anne R Karow-Zwick, Michaela Blech
High-concentration protein formulation (HCPF) is a term that is used to describe protein formulations, mostly monoclonal antibody (mAb) drugs, at high protein concentration. The concentration is rarely defined, with typical ranges varying between 50 and 150 mg/ml for mAbs. The term HCPF is meant to include and express specific solution properties of formulations that are prone to appear at high protein concentrations such as high viscosity, high opalescence, phase separation, gel formation or the increased propensity for protein particle formation...
July 6, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28684278/zeta-potential-changing-self-emulsifying-drug-delivery-systems-containing-phosphorylated-polysaccharides
#10
Janine Griesser, Stephanie Burtscher, Saskia Köllner, Isabelle Nardin, Felix Prüfert, Andreas Bernkop-Schnürch
AIM: The aim of the study was to develop novel zeta potential changing self-emulsifying drug delivery systems (SEDDS) containing phosphorylated polysaccharides. METHODS: Starch and hydroxypropyl starch (HPS) were phosphorylated by utilizing phosphorus pentoxide. The modified starches, starch phosphate (SP) and hydroxypropyl starch phosphate (HPSP), were loaded into SEDDS and investigated regarding particle size, zeta potential, stability and cell viability. The release of immobilized phosphate by intestinal alkaline phosphatase (IAP) was analyzed via malachite green assay...
July 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28669796/alginate-hydrogel-improves-anti-angiogenic-bevacizumab-activity-in-cancer-therapy
#11
Natália N Ferreira, Leonardo M B Ferreira, Vera Miranda-Gonçalves, Rui M Reis, Thiago V Seraphim, Júlio César Borges, Fátima Baltazar, Maria Palmira D Gremião
Anti-vascular endothelial growth factor (anti-VEGF) therapy applied to solid tumors is a promising strategy, yet, the challenge to deliver these agents at high drug concentrations together with the maintenance of therapeutic doses locally, at the tumor site, minimizes its benefits. To overcome these obstacles, we propose the development of a bevacizumab-loaded alginate hydrogel by electrostatic interactions to design a delivery system for controlled and anti-angiogenic therapy under tumor microenvironmental conditions...
June 29, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28669795/downstream-processing-of-hyperforin-from-hypericum-perforatum-root-cultures
#12
Paul Haas, Mariam Gaid, Ajmal Zarinwall, Ludger Beerhues, Stephan Scholl
Hyperforin is a major metabolite of the medicinal plant Hypericum perforatum (St. John's Wort) and has recently been found in hormone induced root cultures. The objective of this study is to identify a downstream process for the production of a hyperforin-rich extract with maximum extraction efficiency and minimal decomposition. The maximum extraction time was found to be 60min. The comparison of two equipment concepts for the extraction and solvent evaporation was performed employing two different solvents...
June 29, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28655665/effect-of-amphiphilic-graft-co-polymer-carrier-on-physical-stability-of-bosentan-nanocomposite-assessment-of-solubility-dissolution-and-bioavailability
#13
Prakash N Kendre, Pravin D Chaudhari
Bosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary arterial hypertension (PAH). But the solubility and bioavailability of this drug are poor, which has restricted the design and development of dosage forms for efficient and successful therapy. The present study was carried out to develop nanocomposites using an amphiphilic graft co-polymer (Soluplus®) as a carrier to enhance the solubility and bioavailability of bosentan. The graft co-polymer-based nanocomposite formulation was prepared using the single-emulsion technique...
June 24, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28655664/protection-of-hydrophobic-amino-acids-against-moisture-induced-deterioration-in-the-aerosolization-performance-of-highly-hygroscopic-spray-dried-powders
#14
Jiaqi Yu, Hak-Kim Chan, Thomas Gengenbach, John A Denman
BACKGROUND: Inhalable particles containing amorphous form of drugs or excipients may absorb atmospheric moisture, causing powder aggregation and recrystallization, adversely affecting powder dispersion and lung deposition. The present study aims to explore hydrophobic amino acids for protection against moisture in spray-dried amorphous powders, using disodium cromoglycate (DSCG) as a model drug. MATERIALS AND METHODS: DSCG powders were produced by co-spray drying with isoleucine (Ile), valine (Val) and methionine (Met) in various concentrations (10, 20 and 40% w/w)...
June 24, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28652141/andrographolide-loaded-nanoparticles-for-brain-delivery-formulation-characterisation-and-in-vitro-permeability-using-hcmec-d3-cell-line
#15
Clizia Guccione, Mouhssin Oufir, Vieri Piazzini, Daniela Elisabeth Eigenmann, Evelyn Andrea Jähne, Volha Zabela, Maria Teresa Faleschini, Maria Camilla Bergonzi, Martin Smiesko, Matthias Hamburger, Anna Rita Bilia
Andrographolide (AG) is a major diterpenoid of the Asian medicinal plant Andrographis paniculata which has shown exciting pharmacological potential for the treatment of inflammation-related pathologies including neurodegenerative disorders. Conversely, the low bioavailability of AG still represents a limiting factor for its use. To overcome these limitations, AG was loaded into human serum albumin based nanoparticles (HSA NPs) and poly ethylcyanoacrylate nanoparticles (PECA NPs). HSA NPs were prepared by thermal (HSAT AG NPs) and chemical cross-linking (HSAC AG NPs), while PECA AG NPs were produced by emulsion-polymerization...
June 23, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28648864/impact-of-plasma-protein-binding-on-cargo-release-by-thermosensitive-liposomes-probed-by-fluorescence-correlation-spectroscopy
#16
Judith J Mittag, Barbara Kneidl, Tobias Preiß, Martin Hossann, Gerhard Winter, Stefan Wuttke, Hanna Engelke, Joachim O Rädler
Thermosensitive liposomes (TSLs) whose phase-transition temperature (Tm) lies slightly above body temperature are ideal candidates for controlled drug release via local hyperthermia. Recent studies, however, have revealed disruptive shifts in the release temperature Tr in mouse plasma, which are attributed to undefined interactions with blood proteins. Here, we study the effects of four major plasma proteins - serum albumin (SA), transferrin (Tf), apolipoprotein A1 (ApoA1) and fibrinogen (Fib) - on the temperature-dependent release of fluorescein di-β-D-galactopyranoside (FDG) from TSLs...
June 22, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28648863/two-phase-amorphous-amorphous-solid-drug-dispersion-with-enhanced-stability-solubility-and-bioavailability-resulting-from-ultrasonic-dispersion-of-an-immiscible-system
#17
Luz María Martínez, Marcelo Videa, Tania López Silva, Samuel Castro, Adolfo Caballero, Víctor J Lara-Díaz, Fabiola Castorena-Torres
Amorphization of active pharmaceutical ingredients (APIs) and the preparation of solid dispersions are strategies that can be synergized to improve the solubility of oral drugs. Immiscibility between an API and a carrier in the molten state that could be perceived as a problem in the preparation of solid dispersions, may actually introduce an advantage. In the present work, a two-phase amorphous-amorphous solid dispersion (AASD) was prepared by ultrasonicating a molten immiscible mixture of indomethacin (IND) and glucose (GLU) prior quenching...
June 22, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28648862/octacosanol-educes-physico-chemical-attributes-release-and-bioavailability-as-modified-nanocrystals
#18
Surashree Sen Gupta, Mahua Ghosh
Octacosanol is a lesser known nutraceutical with the potential for treatment of several inflammatory diseases, high cholesterol, Parkinson's symptoms and tumour growth along with the capacity to improve athletic performance. But its lipophilicity and large structure inhibits extended solubility in water resulting in poor absorption and a low bioavailability. In the present work, sodium salt of octacosyl sulfate was synthesized. It displayed improved water solubility. Its nanocrystals, synthesized by means of nanoprecipitation technique, enhanced diffusion velocity, antioxidant capacity, shelf-life, penetrability and bioavailability...
June 22, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28647443/dermal-and-transdermal-delivery-of-pharmaceutically-relevant-macromolecules
#19
REVIEW
S Münch, J Wohlrab, R H H Neubert
The skin offers an attractive way for dermal and transdermal drug delivery that is why the drug still needs certain qualities to transcend the outermost layer of the skin, the stratum corneum. The requirements are: drugs with a maximum molecular weight of 1kDa, high lipophilicity and a certain polarity. This would restrict the use of a transdermal delivery of macromolecules, which would make the drug more effective in therapeutic administration. Various studies have shown that macromolecules without support do not penetrate the human skin...
June 21, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28633956/a-time-adjustable-pulsatile-release-system-for-ketoprofen-in-vitro-and-in-vivo-investigation-in-a-pharmacokinetic-study-and-an-ivivc-evaluation
#20
Haiying Wang, Lizhen Cheng, Haoyang Wen, Caiyan Li, Yuenan Li, Xiaoyu Zhang, Yongfei Wang, Yanyan Wang, Tuanjie Wang, Weisan Pan, Xinggang Yang
A time-adjustable pulsatile release system (TAPS) containing ketoprofen (KF) as an active pharmaceutical agent was developed having been designed for bedtime dosing and releasing drug in the early morning to control the symptoms of rheumatoid arthritis (RA). The formulation involved a tablet core (KF) and a control-release layer, and the coating membrane was composed of EC and Eudragit L100. A single-factor study, a central composite design and a response surface method were selected to optimize the formula and the optimum prescription was as follows: tablet core (KF 50mg, MCC 70mg, lactose 40mg, L-HPC 38mg), and film (EC 7...
June 17, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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