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European Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/28223236/effect-of-hyaluronic-acid-binding-to-lipoplexes-on-intravitreal-drug-delivery-for-retinal-gene-therapy
#1
Thomas F Martens, Karen Peynshaert, Thaís Leite Nascimento, Elias Fattal, Marcus Karlstetter, Thomas Langmann, Serge Picaud, Jo Demeester, Stefaan C De Smedt, Katrien Remaut, Kevin Braeckmans
Intravitreal administration of nanomedicines could be valuable for retinal gene therapy, if their mobility in the vitreous and therapeutic efficacy in the target cells can be guaranteed. Hyaluronic acid (HA) as an electrostatic coating of polymeric gene nanomedicines has proven to be beneficial on both accounts. While electrostatic coating provides an easy way of coating cationic nanoparticles, the stability of electrostatic complexes in vivo is uncertain. In this study, therefore, we compare electrostatic with covalent coating of gene nanocarriers with HA for retinal gene therapy via intravitreal administration...
February 18, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28219748/improved-antitumor-activity-and-reduced-toxicity-of-doxorubicin-encapsulated-in-poly-%C3%AE%C2%B5-caprolactone-nanoparticles-in-lung-and-breast-cancer-treatment-an-in-vitro-and-in-vivo-study
#2
Laura Cabeza, Raul Ortiz, Jose Prados, Ángel V Delgado, Maria J Martín-Villena, Beatriz Clares, Gloria Perazzoli, Jose M Entrena, Consolación Melguizo, Jose L Arias
Poly(ε-caprolactone) (PCL) nanoparticles (NPs) offer many possibilities for drug transport because of their good physicochemical properties and biocompatibility. Doxorubicin-loaded PCL NPs have been synthesized to try to reduce the toxicity of doxorubicin (DOX) for healthy tissues and enhance its antitumor effect in two tumor models, breast and lung cancer, which have a high incidence in the global population. PCL NPs were synthesized using a modified nanoprecipitation solvent evaporation method. The in vitro toxicity of PCL NPs was evaluated in breast and lung cancer cell lines from both humans and mice, as was the inhibition of cell proliferation and cell uptake of DOX-loaded PCL NPs compared to free DOX...
February 17, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28216342/near-infrared-monitoring-of-roller-compacted-ribbon-density-investigating-sources-of-variation-contributing-to-noisy-spectral-data
#3
Mary Ellen Crowley, Avril Hegarty, Michael A P McAuliffe, Graham E O'Mahony, Luke Kiernan, Kevin Hayes, Abina M Crean
The aim of this study was to highlight how variability in roller compacted ribbon quality can impact on NIR spectral measurement and to propose a simple method of data selection to remove erroneous spectra. The use of NIR spectroscopy for monitoring ribbon envelope density has been previously demonstrated, however to date there has been limited discussion as to how spectral data sets can contain erroneous outliers due to poor sample presentation to the NIR probes. In this study compacted ribbon of variable quality was produced from three separate blends of microcrystalline cellulose (MCC)/lactose/magnesium stearate at 8 Roll Force settings (2-16kN/cm)...
February 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28214545/potential-of-amphiphilic-graft-copolymer-%C3%AE-tocopherol-succinate-g-carboxymethyl-chitosan-in-modulating-the-permeability-and-anticancer-efficacy-of-tamoxifen
#4
Sunil K Jena, Sanjaya K Samal, Shamandeep Kaur, Mahesh Chand, Abhay T Sangamwar
Recent studies showed an enhanced oral bioavailability of tamoxifen (TMX) by hydrophobically modified α-tocopherol succinate-g-carboxymethyl chitosan (Cmc-TS) micelles. As a continued effort, here we evaluated TMX-loaded polymeric micelles (TMX-PMs) for its enhanced permeability with increased anticancer efficacy and decreased hepatotoxicity. We employed co-solvent evaporation technique to encapsulate TMX into Cmc-TS. Apparent permeability assay of TMX-PMs was performed on Caco-2 cell line. The absorptive transport of TMX increased significantly about 3...
February 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28214546/effect-of-cyclophosphamide-on-the-solid-form-of-mannitol-during-lyophilization
#5
Krupaliben Patel, Bhushan Munjal, Arvind K Bansal
Mannitol is a commonly used bulking agent in lyophilized formulations. It can crystallize into multiple solid forms during lyophilization thereby exhibiting phase heterogeneity and variability in product performance. In this manuscript, we studied the effect of cyclophosphamide (CPA), an anticancer drug, on the solid form of mannitol during lyophilization from aqueous solutions. Freeze-concentration studies were performed in the DSC while lyophilization was performed in a lab scale freeze dryer. DSC experiments revealed two-stage crystallization of mannitol (1...
February 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28212981/development-of-solid-sedds-vi-effect-of-precoating-of-neusilin%C3%A2-us2-with-pvp-on-drug-release-from-adsorbed-self-emulsifying-lipid-based-formulations
#6
Suhas G Gumaste, Beatryz O S Freire, Abu T M Serajuddin
Adsorption of lipid-based formulations, which are usually liquid, onto silicas has been extensively investigated in the past decade to convert them into solid dosage forms. There are conflicting reports on the ability of commercially available porous silicas, like Neusilin® US2, to release lipid formulations completely, especially after long-term storage. In this study, the release of a model drug, probucol, from different formulations of medium chain lipids and a surfactant, Kolliphor EL (Cremophor EL) or polysorbate 80, were studied after adsorbing them onto Neusilin® US2...
February 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28193537/preparation-characterization-and-in-vivo-evaluation-of-a-combination-delivery-system-based-on-hyaluronic-acid-jeffamine-hydrogel-loaded-with-phbv-plga-blend-nanoparticles-for-prolonged-delivery-of-teriparatide
#7
Nika Bahari Javan, Hamed Montazeri, Leila Rezaie Shirmard, Nersi Jafary Omid, Ghullam Reza Barbari, Mohsen Amini, Mohammad Hossein Ghahremani, Morteza Rafiee-Tehrani, Farid Abedin Dorkoosh
In the current study, biodegradable PHBV/PLGA blend nanoparticles (NPs) containing Teriparatide were loaded in hyaluronic acid/jeffamine (HA-JEF ED-600) hydrogel to prepare a combination delivery system (CDS) for prolonged delivery of Teriparatide. The principal purpose of the present study was to formulate an effective and prolonged Teriparatide delivery system in order to reduce the frequency of injection and thus enhance patient's compliance. Morphological properties, swelling behaviour, crosslinking efficiency and rheological characterization of HA-JEF ED-600 hydrogel were evaluated...
February 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28215944/cd44-cancer-cell-induced-metastasis-a-feasible-neck-metastasis-model
#8
Tian-Fu Wu, Lei Chen, Lin-Lin Bu, Jie Gao, Wen-Feng Zhang, Jun Jia
Neck metastasis of oral squamous cell carcinoma (OSCC) indicates a poor prognosis. Few neck metastasis models are currently available for drug trials and clinical research on OSCC. This study constructed a feasible animal model of neck metastasis by using CD44+ stem cell-like cancer cells. Real-time PCR was used to determine the expression levels of several reported cancer stem cell (CSC) markers, including CD44, CD133, ALDH1 and OCT4, in three OSCC cell lines. Magnetic sorting and DiO/DiD labelling were used to isolate subpopulations of cells and monitor cancer cell migration...
February 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28215943/all-trans-retinoic-acid-enhances-gemcitabine-cytotoxicity-in-human-pancreatic-cancer-cell-line-aspc1-by-up-regulating-protein-expression-of-deoxycytidine-kinase
#9
Hiroki Kuroda, Masanori Tachikawa, Yasuo Uchida, Koetsu Inoue, Hideo Ohtsuka, Sumio Ohtsuki, Michiaki Unno, Tetsuya Terasaki
We previously showed that gemcitabine resistance in pancreatic cancer chemotherapy correlates with suppressed expression of deoxycytidine kinase (dCK), which catalyzes the rate-limiting step of gemcitabine activation. The purpose of the present study was to find a drug that might be useful to enhance the cytotoxicity of gemcitabine by increasing dCK expression in gemcitabine-resistant human pancreatic cancer cell line AsPC1. Screening of 40 prescription drugs identified 35 with no intrinsic cytotoxicity towards AsPC1 cells...
February 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28215942/how-to-identify-and-eliminate-compounds-with-a-risk-of-high-clinical-dose-during-the-early-phase-of-lead-optimisation-in-drug-discovery
#10
Simon Teague, Klara Valko
An alternative approach has been developed to estimate the clinical dose of new drug molecules at an early stage in the drug discovery process. This approach has been compared to traditional methods using the clinical dose as indicated on the drug label of 136 marketed drugs. At the early stages of drug discovery only in silico predictions or some initial in vitro screening data are normally available, typically parameters such as affinity/potency (pXC50)from isolated enzymes or receptors, measured albumin and phospholipid binding using biomimetic HPLC measurements, and in vitro clearance using P450 enzymes or liver microsomes...
February 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28193538/multifunctional-luv-liposomes-decorated-for-bbb-and-amyloid-targeting-a-in-vitro-proof-of-concept
#11
Konstantina Papadia, Eleni Markoutsa, Spyridon Mourtas, Anastassios D Giannou, Barabara La Ferla, Fransesco Nicotra, Mario Salmona, Pavlos Klepetsanis, Georgios T Stathopoulos, Sophia G Antimisiaris
Multifunctional LUV liposomes (mf-LIPs) were developed, having a curcumin-lipid ligand (TREG) with affinity towards amyloid species, together with ligands to target the transferrin and the LDL receptors of the blood-brain-barrier (BBB), on their surface. mf-LIPs were evaluated for their brain targeting, on hCMEC/D3 monolayers, and for their ability to inhibit Aβ-peptide aggregation. The transport of mf-LIP across hCMEC/D3 monolayers was similar to that of BBB-LIPs, indicating that the presence of TREG on their surface does not reduce their brain targeting potential...
February 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28192168/novel-benzophenone-3-derivatives-with-promising-potential-as-uv-filters-relationship-between-structure-photoprotective-potential-and-phototoxicity
#12
María Teresa Páez González, Fernando Fumagalli, Carolina Gomes Benevenuto, Flavio da Silva Emery, Lorena Rigo Gaspar
Benzophenone-3 (BP-3) is a UV filter with absorption at the UVB and UVA wavelengths which has not been extensively studied in experiments involving its absorbing effects and toxicity. We synthetized four BP-3 derivatives and characterized their photoprotective potential by UV absorption and photodegradation, their phototoxicity potential by 3T3 Neutral Red Uptake (3T3 NRU PT) and their photoreactivity by the reactive oxygen species (ROS) assay. The UV absorption, photodegradation, phototoxicity and photoreactivity of the four BP-3 derivatives (BP-3 carbonate, BP-3 carbazole, BP-3 phenylamine and BP-3 methoxy-phenylamine) were evaluated and compared to those of BP-3...
February 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28192167/re-programming-pullulan-for-targeting-and-controlled-release-of-doxorubicin-to-the-hepatocellular-carcinoma-cells
#13
Anna Balasso, Stefano Salmaso, Patrizia Pontisso, Antonio Rosato, Santina Quarta, Alessio Malfanti, Francesca Mastrotto, Paolo Caliceti
A novel bioconjugate for hepatocellular carcinoma (HCC) targeting was obtained by pullulan re-programming, which involves the backbone oxidation and conjugation of targeting peptide and doxorubicin (Doxo) through a releasable linker. Preliminary in vivo studies showed that the oxidation of 40 glucopyranose units (GPU) out of 100 remarkably reduced the pullulan unspecific liver tropism. This oxidized polymer was functionalized with PreS1 to selectively target the HCC and with rhodamine (Rhod) as label to perform in vitro cell up-take investigations...
February 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28189817/insight-into-stereoselective-disposition-of-enantiomers-of-a-potent-antithrombotic-agent-s002-333-following-administration-of-the-racemic-compound-to-mice
#14
Manisha Bhateria, Ramakrishna Rachumallu, Sahithi Yerrabelli, Anil K Saxena, Rabi Sankar Bhatta
S002-333 [2-(4-methoxy-benzenesulfonyl)-2,3,4,9-tetrahydro-1H-b-carboxylic acid amide], a potent antithrombotic agent developed by CSIR-CDRI, is a racemic mixture of two enantiomers (S004-1032 (R)-isomer and S007-1558 (S)-isomer). Despite extensive research, little is known about the pharmacokinetics of S002-333 enantiomers. Given that mouse is an established model for anti-platelet/antithrombotic activity and interspecies differences exists in the direction of stereoselectivity in pharmacokinetic processes, we investigated the pharmacokinetic disposition of S002-333 enantiomers in mice...
February 9, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28189816/screening-of-inhibitors-of-angiotensin-converting-enzyme-ace-employing-high-performance-liquid-chromatography-electrospray-ionization-triple-quadrupole-mass-spectrometry-hplc-esi-qqq-ms
#15
Syed Ghulam Musharraf, Muhammad Salman Bhatti, Muhammad Iqbal Choudhary, Atta-Ur Rahman
Angiotensin-converting enzyme (ACE) plays a key role in regulating blood pressure in the body by converting the angiotensin I (AI) into angiotensin II (AII). Angiotensin II is a potent vaso-active peptide that causes arterioles to constrict, resulting in increased blood pressure. A rapid and sensitive method for the identification of inhibitors of ACE was developed, and optimized employing HPLC-ESI-QqQ-MS. In this assay, angiotensin I substrate was converted into the product angiotensin II with the catalytic action of ACE...
February 9, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28189815/antioxidant-activity-and-protective-effect-of-suramin-against-oxidative-stress-in-collagen-induced-arthritis
#16
Debasis Sahu, Shikha Sharma, Rajeev K Singla, Amulya Kumar Panda
It is imperative to interrupt the link between arthritis and regulation of oxidative stress with the administration of antioxidants. Suramin is known for its anti-inflammatory, antineoplastic and antiangiogenic activities implying its possible antioxidant property. In this study, the antioxidant activity of suramin in cell free system was found to be higher than l-ascorbic acid (l-AA) with respect to its scavenging effect on nitric oxide (NO), hypochlorous acid and hydrogen peroxide radicals. Besides, suramin was found to be nontoxic to cultured RAW cells even at high concentrations along with marked inhibition of NO production...
February 9, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28189814/optimization-of-paeonol-loaded-poly-butyl-2-cyanoacrylate-nanocapsules-by-central-composite-design-with-response-surface-methodology-together-with-the-antibacterial-properties
#17
Jingjing Yao, Yangxin Zhang, Qiming Hu, Decheng Zeng, Fang Hua, Wei Meng, Weiyun Wang, Guan-Hu Bao
With the aim to enhance dissolution rate and bioavailability of paeonol, paeonol-loaded poly(butyl-2-cyanoacrylate) nanocapsules (Pae@PNCs) were prepared by interfacial spontaneous polymerization for the first time. Herein, a rotatable central composite design (RCCD) with three-factor five-level was applied to evaluate the optimization experiments. To the maximum percentage encapsulation efficiency (EE%) and minimum particle size (nm) of the Pae@PNCs, a quadratic polynomial model was generated to predict and evaluate the independent variables with respect to the dependent variables...
February 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28188911/a-rational-approach-to-elucidate-human-monoamine-oxidase-molecular-selectivity
#18
Giuseppe Felice Mangiatordi, Domenico Alberga, Leonardo Pisani, Domenico Gadaleta, Daniela Trisciuzzi, Roberta Farina, Andrea Carotti, Gianluca Lattanzi, Marco Catto, Orazio Nicolotti
Designing highly selective human monoamine oxidase (hMAO) inhibitors is a challenging goal on the road to a more effective treatment of depression and anxiety (inhibition of hMAO-A isoform) as well as neurodegenerative diseases (inhibition of hMAO-B isoform). To uncover the molecular rationale of hMAOs selectivity, two recently prepared 2H-chromene-2-ones, namely compounds 1 and 2, were herein chosen as molecular probes being highly selective toward hMAO-A and hMAO-B, respectively. We performed molecular dynamics (MD) studies on four different complexes, cross-simulating one at a time the two hMAO-isoforms (dimer embedded in a lipid bilayer) with the two considered probes...
February 7, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28188910/expression-and-splicing-of-abc-and-slc-transporters-in-the-human-blood-brain-barrier-measured-with-rnaseq
#19
Adam M Suhy, Amy Webb, Audrey C Papp, Ethan G Geier, Wolfgang Sadee
The blood-brain barrier (BBB) expresses numerous membrane transporters that supply needed nutrients to the central nervous system (CNS), consisting mostly of solute carriers (SLC transporters), or remove unwanted substrates via extrusion pumps through the action of ATP binding cassette (ABC) transporters. Previous work has identified many BBB transporters using hybridization arrays or qRT-PCR, using targeted probes. Here we have performed next-generation sequencing of the transcriptome (RNAseq) extracted from cerebral cortex tissues and brain microvessel endothelial cells (BMEC) obtained from two donors...
February 7, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28188909/extensive-preclinical-evaluation-of-an-infliximab-biosimilar-candidate
#20
M A Velasco-Velázquez, N Salinas-Jazmin, E Hisaki-Itaya, L Cobos-Puc, W Xolalpa, G Gonzalez, A Tenorio-Calvo, N Piña-Lara, L C Juarez-Bayardo, L F Flores-Ortiz, E Medina-Rivero, N O Pérez, S M Pérez-Tapia
Infliximab is therapeutic monoclonal antibody (mAb) against TNF-α employed in the treatment of immunoinflammatory diseases. The development of biosimilar mAbs is a global strategy to increase drug accessibility and reduce therapy-associated costs. Herein we compared key physicochemical characteristics and biological activities produced by infliximab and infliximab-Probiomed in order to identify functionally relevant differences between the mAbs. Binding of infliximab-Probiomed to TNF-α was specific and had kinetics comparable to that of the reference product...
February 7, 2017: European Journal of Pharmaceutical Sciences
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