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European Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/29787786/preparation-of-99m-tc-levetiracetam-intranasal-microemulsion-as-the-first-radiotracer-for-spect-imaging-of-the-synaptic-vesicle-protein-sv2a
#1
Hassan M Rashed, Rehab N Shamma, Hanan A El-Sabagh
Selective receptors imaging using gamma emitting radiopharmaceuticals allows accurate diagnosis and follow up of many brain related disorders. Levetiracetam, a selective SV2A receptor antiepileptic, was successfully radiolabeled using 99m Tc. Different conditions affecting the labelling process were studied and optimum radiochemical yield of 89.8% was obtained. 99m Tc-levetiracetam was effectively formulated and characterized as microemulsion with particle size of 16.34 ± 5.58 nm and polydispersity index of 0...
May 19, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29782910/comparison-of-dissolution-time-profiles-no-similarity-but-where-is-the-difference
#2
Stefan Horkovics-Kovats
The similarity of the dissolution time profiles is routinely determined by various statistical methods, e.g. by calculating the f2 similarity factor, by calculating the multivariate statistical distance or determining the confidence interval of f2 metrics using the bootstrapping method. If the similarity of the dissolution profiles is not achieved, these methods provide no information about the possible causes of the differences in the final dosage forms. In this article it is shown that after introduction of summary parameters into the disintegration-dissolution model (DDM), such as intrinsic lifetime distribution of particles, saturation state function, drug load of the system and applying population data analysis, differences on the level of intrinsic lifetime distributions of particles of active pharmaceutical ingredient in immediately release formulations are identified...
May 18, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29778782/acyclovir-lipid-nanocapsules-gel-for-oromucosal-delivery-a-preclinical-evidence-of-efficacy-in-the-chicken-pouch-membrane-model
#3
Darine Abozaid, Alyaa Ramadan, Heba Barakat, Nawal Khalafallah
The study aimed to develop a patient-friendly acyclovir gel with improved efficacy in viral mouth infections, in response to patients' need for an intraoral acyclovir product. Acyclovir was loaded in lipid nanocapsules in gel form, and formulae were evaluated for oromucosal delivery. Lipid nanocapsules were prepared by the phase inversion method. Formulae were optimized to achieve maximum acyclovir entrapment and minimum acyclovir precipitation. Colloidal properties, and pharmaceutical performance indicators were assessed...
May 17, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29777858/cd44-targeted-plga-nanomedicines-for-cancer-chemotherapy
#4
REVIEW
Ankit Saneja, Divya Arora, Robin Kumar, Ravindra Dhar Dubey, Amulya K Panda, Prem N Gupta
In recent years scientific community has drawn a great deal of attention towards understanding the enigma of cluster of differentiation-44 (CD44) in order to deliver therapeutic agents more selectively towards tumor tissues. Moreover, its over-expression in variety of solid tumors has attracted drug delivery researchers to target this receptor with nanomedicines. Conventional nanomedicines based on biodegradable polymers such as poly(lactide-co-glycolide) (PLGA) are often associated with insufficient cellular uptake by cancer cells, due to lack of active targeting moiety on their surface...
May 16, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29777857/study-of-the-influence-of-substrate-and-spectrophotometer-characteristics-on-the-in-vitro-measurement-of-sunscreens-efficiency
#5
C Couteau, A Philippe, M-A Vibet, E Paparis, L Coiffard
All the methods used for the in vitro measurement of the SPF, the universal indicator of sunscreens efficiency, rely on a spectrophotometric analysis. What can vary about the experimental protocol used is mainly the substrate and the type of spectrophotometer chosen. We decided to work with polymethylmetacrylate plates that we analyzed using two spectrophotometers equipped with integrating spheres, the UV1000S and the UV2000 apparatus. Two marketed products were such tested, after spreading 2 mg/cm2 on the plates, using one apparatus after another...
May 16, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29777856/ocular-irritation-and-cyclosporine-a-distribution-in-the-eye-tissues-after-administration-of-solid-lipid-microparticles-in-the-rabbit-model
#6
Eliza Wolska, Małgorzata Sznitowska, Juliusz Chorążewicz, Oliwia Szerkus, Aleksandra Radwańska, Michał J Markuszewski, Roman Kaliszan, Krystyna Raczyńska
The aim of this study was to investigate the in vivo effect of Solid Lipid Microparticles (SLM), proposed for topical ocular administration of cyclosporine, on the rabbit eye. SLM carrier is an aqueous dispersion of lipid microparticles (20% w/w) with a size up to 15 μm. Cyclosporine was dissolved in the formulation in the concentration of 0.5 or 2.0% (w/w). Ocular tolerance of microsphere dispersion was assessed in rabbit model by the Draize eye test (SLM was compared with emulsion and oily solution), and cyclosporine distribution in ocular tissues was evaluated after multiple application of tested formulations (SLM dispersions, emulsions and oily solution) for 7 days...
May 16, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29777855/polymer-lipid-hybrid-nanoparticles-as-enhanced-indomethacin-delivery-systems
#7
Annalisa Dalmoro, Sabrina Bochicchio, Shamil F Nasibullin, Paolo Bertoncin, Gaetano Lamberti, Anna Angela Barba, Rouslan I Moustafine
Non-steroidal anti-inflammatory drugs (NSAIDs), i.e. indomethacin used for rheumatoid arthritis and non-rheumatoid inflammatory diseases, are known for their injurious actions on the gastrointestinal (GI) tract. Mucosal damage can be avoided by using nanoscale systems composed by a combination of liposomes and biodegradable natural polymer, i.e. chitosan, for enhancing drug activity. Aim of this study was to prepare chitosan-lipid hybrid delivery systems for indomethacin dosage through a novel continuous method based on microfluidic principles...
May 16, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29777854/dissolving-polymeric-microneedle-arrays-for-enhanced-site-specific-acyclovir-delivery
#8
Boonnada Pamornpathomkul, Tanasait Ngawhirunpat, Ismaiel A Tekko, Lalitkumar Vora, Helen O McCarthy, Ryan F Donnelly
Acyclovir is widely indicated for the treatment of herpes labialis (cold sores), typically caused by the herpes simplex virus type 1 (HSV-1). However, topical acyclovir has poor efficacy, due to its low skin permeability. The purpose of this study was, therefore, to evaluate the ability of dissolving polymeric microneedle (MN) arrays to improve the local delivery of acyclovir. Acyclovir-loaded dissolving MN arrays (0.49 cm2 ) were formulated from aqueous blends of Gantrez® S-97 with 361 needles per array (589 ± 9...
May 16, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29775655/confocal-raman-microspectroscopy-as-an-alternative-to-differential-scanning-calorimetry-to-detect-the-impact-of-emulsifiers-and-formulations-on-stratum-corneum-lipid-conformation
#9
Ziwei Zhang, Dominique Jasmin Lunter
The purpose of this study was to investigate the impact of emulsifiers and formulations on stratum corneum (SC) lipid conformation and evaluate confocal Raman microspectroscopy (CRM) as an alternative method to differential scanning calorimetry (DSC) in this research context. To this end, four different formulations were used: three conventional creams that contained ionic and/or non-ionic emulsifiers and one surfactants-free emulsion stabilized by a polymeric emulsifier. Additionally, all emulsifiers were tested in aqueous solutions/dispersions in the respective concentrations as present in the formulations...
May 15, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29772274/pharmacodynamic-and-pharmacokinetic-characteristics-of-ymr-65-a-tubulin-inhibitor-in-tumor-bearing-mice
#10
Ali Fan, Jiali Wei, Mengru Yang, Qing Zhang, Yaliang Zhang, Qingwang Liu, Ning Li, Di Zhao, Yang Lu, Junxiu Li, Jie Zhao, Shuhua Deng, Bingjie Zhang, Hailiang Zhu, Xijing Chen
YMR-65, 5-(5-bromo-1-methyl-1H-indol-3-yl)-3-(3-methoxyphenyl)-4, 5-dihydro-1H-pyrazole-1-carboxamide, is a potential tubulin inhibitor exhibiting good anticancer activity. In our study, we illustrated the biological activities in HepG2 cells and the pharmacodynamic and pharmacokinetic profiles were evaluated in murine H22 hepatoma-bearing mice. Molecular docking assay and colchicine competition assay indicated that YMR-65 could bind tightly to the colchicine binding site of tubulin. Further investigation demonstrated that YMR-65 arrested cells in the G2/M phase of cell cycle and induced apoptosis in HepG2 cells...
May 14, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29772273/effect-of-formulation-and-process-variables-on-lipid-based-sustained-release-tablets-via-continuous-twin-screw-granulation-a-comparative-study
#11
Venkata Raman Kallakunta, Roshan Tiwari, Sandeep Sarabu, Suresh Bandari, Michael A Repka
The current study's aim is to prepare lipid based sustained release tablets via a twin-screw granulation technique and compare those dosage forms with conventional techniques, namely wet granulation and direct compression. The granules were successfully manufactured in a single-step, continuous twin-screw granulation process with a low proportion of binder (Klucel™ EF, HPC SSL) using Compritol® 888 ATO, Precirol® ATO 5 and Geleol™ as sustained release agents. The granules prepared showed good flow characteristics and compaction properties...
May 14, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29763667/selection-of-a-round-convex-tablet-shape-that-mitigates-the-risk-of-chipping-and-capping-based-on-systematic-evaluation-by-utilizing-multivariate-analysis
#12
Shuichi Tanabe, Hiroshi Nakagawa, Tomoyuki Watanabe, Hidemi Minami, Shuichi Ando, Nora A Urbanetz, Regina Scherließ
Selecting a tablet shape that minimizes the risk of chipping and capping during manufacture is important in pharmaceutical industry. Here, the selection was performed based on systematic evaluation for the first time. Abrasion and stress relaxation time were utilized as indices of the occurrences of chipping and capping, respectively. Partial least square regression models that used tablet shape parameters to estimate the tablet's abrasion and stress relaxation time were utilized to develop response surface plots of the effect of the tablet shapes on the occurrence of chipping and capping systematically, and to identify an optimum tablet shape that is expected to have a low occurrence of chipping and capping...
May 12, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29752999/the-scaffold-protein-pdzk1-modulates-expression-and-function-of-the-organic-anion-transporting-polypeptide-2b1
#13
Celio Ferreira, Paul Hagen, Melanie Stern, Janine Hussner, Uwe Zimmermann, Markus Grube, Henriette E Meyer Zu Schwabedissen
The protein family of Organic Anion Transporting Polypeptides (OATPs) summarizes various transporters known to facilitate cellular uptake of xenobiotics. One member of this family is OATP2B1. This transporter is ubiquitously expressed and possesses a PDZ-binding motif at the C-terminus. PDZK1 (PDZ domain-containing 1) is a scaffold protein that influences function of different membrane proteins by sorting/stabilization of their membrane localization. It was aim of the herein reported study to investigate whether there is an interaction between OATP2B1 and PDZK1, and to further characterize its impact on transport function...
May 9, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29751102/human-and-rat-precision-cut-intestinal-slices-as-ex-vivo-models-to-study-bile-acid-uptake-by-the-apical-sodium-dependent-bile-acid-transporter
#14
Ming Li, Ivan Vokral, Bernard Evers, Inge A M de Graaf, Marina H de Jager, Geny M M Groothuis
No abstract text is available yet for this article.
May 8, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29751101/how-to-measure-release-from-nanosized-carriers
#15
REVIEW
Lisa Nothnagel, Matthias G Wacker
Novel drug delivery systems exhibit great potential in the formulation of poorly soluble compounds but also reduce the side effects of highly active drug molecules. Despite all efforts, there are only few technologies available to investigate the in vitro release of next-generation nanotherapeutics. In the following, different approaches for application of drug release testing from nanoparticles in the fields of formulation development and quality control are discussed. A variety of methods is available, starting from dialysis-based equipment, in situ measurements, flow-through and sample and separate setups...
May 8, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29746911/n-demethylation-of-n-methyl-4-aminoantipyrine-the-main-metabolite-of-metamizole
#16
Fabio Bachmann, Urs Duthaler, Deborah Rudin, Stephan Krähenbühl, Manuel Haschke
Metamizole is an old analgesic used frequently in some countries. Active metabolites of metamizole are the non-enzymatically generated N-methyl-4-aminoantipyrine (4-MAA) and its demethylation product 4-aminoantipyrine (4-AA). Previous studies suggested that 4-MAA demethylation can be performed by hepatic cytochrome P450 (CYP) 3A4, but the possible contribution of other CYPs remains unclear. Using human liver microsomes (HLM), liver homogenate and HepaRG cells, we could confirm 4-MAA demethylation by CYPs. Based on CYP induction (HepaRG cells) and CYP inhibition (HLM) we could identify CYP2B6, 2C8, 2C9 and 3A4 as major contributors to 4-MAA demethylation...
May 8, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29746912/topical-delivery-of-anthramycin-ii-influence-of-binary-and-ternary-solvent-systems
#17
Tasnuva Haque, Khondaker Miraz Rahman, David E Thurston, Jonathan Hadgraft, Majella E Lane
Anthramycin (ANT) is a member of the pyrolobenzodiazepine family and is a potent cytotoxic agent. Previously, we reported the topical delivery of ANT from a range of solvents that may also act as skin penetration enhancers (SPEs). The skin penetration and uptake was monitored for simple solutions of ANT in propylene glycol (PG), dipropylene glycol (DiPG), Transcutol P (TC), isopropyl myristate (IPM), propylene glycol monocaprylate (PGMC) and propylene glycol monolaurate (PGML). The amounts of PG, DiPG and TC that were taken up by, and that penetrated the skin were also measured, with a clear dependence of ANT penetration on the rate and extent of PG and TC permeation...
May 7, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29733979/functionalized-extracellular-vesicles-as-advanced-therapeutic-nanodelivery-systems
#18
REVIEW
Mei Lu, Haonan Xing, Zhe Xun, Tianzhi Yang, Xiaoyun Zhao, Cuifang Cai, Dongkai Wang, Pingtian Ding
Extracellular vesicles (EVs) are membrane enclosed vesicles that are shed by almost all cell types, and play a fundamental role in cell-to-cell communication. The discovery that EVs are capable of functionally transporting nucleic acid- and protein-based cargoes between cells, rapidly promotes the idea of employing them as drug delivery systems. These endogenous vesicles indeed hold tremendous promise for therapeutic delivery. However, issues associated with exogenously administered EVs, including rapid clearance by the immune system, apparent lack of targeting cell specificity, and insufficient cytoplasmic delivery efficiency, may limit their therapeutic applicability...
May 4, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29730322/salt-formation-improved-the-properties-of-a-candidate-drug-during-early-formulation-development
#19
Kalle Sigfridsson, Matti Ahlqvist, Martin Lindsjö, Stefan Paulsson
The purpose of this study was to investigate if AZD5329, a dual neurokinin NK1/2 receptor antagonist, is a suitable candidate for further development as an oral immediate release (IR) solid dosage form as a final product. The neutral form of AZD5329 has only been isolated as amorphous material. In order to search for a solid material with improved physical and chemical stability and more suitable solid-state properties, a salt screen was performed. Crystalline material of a maleic acid salt and a fumaric acid salt of AZD5329 were obtained...
May 3, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29729414/semi-mechanistic-pharmacokinetic-pharmacodynamic-model-of-three-pegylated-rhuepo-and-ior%C3%A2-epocim-in-new-zealand-rabbits
#20
G Reynaldo-Fernández, J Solozábal, D Amaro, E M Fernández-Sánchez, L Rodríguez-Vera, M Bermejo, V Mangas-Sanjuan, I F Troconiz
Marketed formulations of erythropoietin (EPO) ior®EPOCIM, MIRCERA® and two newly developed pegylated-EPO analogues (PEG-EPO 32 and 40 kDa) formulations were intravenously administered to New Zealand rabbits. A semi-mechanistic Pharmacokinetic/Pharmacodynamic (PK/PD) model describing in a simultaneous and integrated form the time course of reticulocytes, red blood cells and hemoglobin was built to account for the time course of hematopoiesis stimulation after erythropoietin administration. Data analysis was performed based on the population approach with the software NONMEM version 7...
May 2, 2018: European Journal of Pharmaceutical Sciences
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