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European Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/28442440/impact-of-dose-and-surface-features-on-plasmatic-and-liver-concentrations-of-biodegradable-polymeric-nanocapsules
#1
Líliam Teixeira Oliveira, Mônica Auxiliadora de Paula, Bruno Mendes Roatt, Giani Martins Garcia, Luan Silvestro Bianchini Silva, Alexandre Barbosa Reis, Carina Silva de Paula, José Mário Carneiro Vilela, Margareth Spangler Andrade, Gwenaelle Pound-Lana, Vanessa Carla Furtado Mosqueira
The effect of polymeric nanocapsule dose on plasmatic and liver concentrations 20min after intravenous administration in mice was evaluated. Nanocapsules were prepared with different polymers, namely, poly(D,L-lactide) (PLA), polyethylene glycol-block-poly(D,L-lactide) (PLA-PEG), and PLA with chitosan (PLA-Cs) and compared with a nanoemulsion. These formulations were labelled with a phthalocyanine dye for fluorescent detection. The nanostructures had narrow size distributions upon separation by asymmetric flow field flow fractionation with static and dynamic light scattering detection, with average hydrodynamic diameters in the 130-300nm range, negative zeta potentials, except PLA-Cs nanocapsules, which had a positive zeta potential...
April 22, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435078/preformulation-studies-of-ceftriaxone-for-pediatric-non-parenteral-administration-as-an-alternative-to-existing-injectable-formulations
#2
Tina Kauss, Mathieu Marchivie, Thida Phoeung, Alexandra Gaubert, Amélie Désiré, Giovanni Tonelli, Chantal Boyer, Marie-Hélène Langlois, Anthony Cartwright, Melba Gomes, Nicholas White, Karen Gaudin
Ceftriaxone, a third generation cephalosporin, has a wide antibacterial spectrum that has good CNS penetration, which makes it potentially suitable for initial treatment of severe neonatal pediatric infections providing suitable formulation. We evaluated its physicochemical and technical characteristics to assess its potential for development as a non-parenteral dosage form. As ceftriaxone is marked only for injectable use, these data are not available. Using HPLC and Karl Fischer titration, sensitivity of ceftriaxone to water, feasibility and impact of pharmaceutical processes and compatibility with common pharmaceutical excipients were assessed...
April 20, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435077/improving-blend-content-uniformity-via-dry-particle-coating-of-micronized-drug-powders
#3
Zhonghui Huang, Wannan Xiong, Kuriakose Kunnath, Sayani Bhaumik, Rajesh N Davé
Content uniformity of low dose blends with fine active pharmaceutical ingredients (API) is adversely impacted due to API agglomeration caused by high powder cohesion. Dry coating using high-intensity vibratory mixing is employed to reduce API cohesion and granular Bond number as well as agglomeration as predicted by contact models, hence improve blend content uniformity (CU). Micronized acetaminophen (mAPAP) (~10μm), a model API, was dry coated with nano-silica R972P (20nm), and mixed with Avicel 102. The amount of silica was varied from 0 to 2...
April 20, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435076/design-synthesis-biological-evaluation-and-molecular-modelling-of-2-2-aryloxyphenyl-1-4-dihydroisoquinolin-3-2h-ones-a-novel-class-of-tspo-ligands-modulating-amyloid-%C3%AE-induced-mptp-opening
#4
Ahmed Elkamhawy, Jung-Eun Park, Ahmed H E Hassan, Ae Nim Pae, Jiyoun Lee, Beoung-Geon Park, Sora Paik, Jimin Do, Jong-Hyun Park, Ki Duk Park, Bongjin Moon, Woo Kyu Park, Heeyeong Cho, Dae Young Jeong, Eun Joo Roh
Translocator protein (TSPO) is involved in modulating mitochondrial permeability transition pore (mPTP) opening/closure leading to either apoptotic cell death via opening of mPTP or cell protection mediated by mPTP blocking and hence intercepting mPTP induced apoptosis. Herein, 2-(2-aryloxyphenyl)-1,4-dihydroisoquinolin-3(2H)-one derivatives have been designed and synthesized as new modulators for amyloid-β-induced mPTP opening. Among all, compound 7c remarkably enhanced mPTP opening while compound 7e showed the highest mPTP blocking activity...
April 20, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435075/development-of-oral-lyophilisates-containing-meloxicam-nanocrystals-using-qbd-approach
#5
Sonia Iurian, Cătălina Bogdan, Ioan Tomuță, Piroska Szabó-Révész, Anita Chvatal, Sorin E Leucuța, Mirela Moldovan, Rita Ambrus
The aim of this study was to develop oral lyophilisates with improved meloxicam (MEL) dissolution, optimizing each step of the preparation by design of experiments. First, meloxicam nanosuspensions were prepared by high-pressure homogenization (HPH), using PVP, Poloxamer or PEG as stabilizers and were subjected to freeze-drying using mannitol as cryoprotectant. The effects of the stabilizers and cryoprotectant were assessed and an optimal formulation was generated within the Design Space where the particle sizes and the PDIs are at their lowest values...
April 20, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28433750/nanoemulsion-based-electrolyte-triggered-in-situ-gel-for-ocular-delivery-of-acetazolamide
#6
Nadia Morsi, Magdy Ibrahim, Hanan Refai, Heba El Sorogy
In the present work the antiglaucoma drug, acetazolamide, was formulated as an ion induced nanoemulsion-based in situ gel for ocular delivery aiming a sustained drug release and an improved therapeutic efficacy. Different acetazolamide loaded nanoemulsion formulations were prepared using peanut oil, tween 80 and/or cremophor EL as surfactant in addition to transcutol P or propylene glycol as cosurfactant. Based on physicochemical characterization, the nanoemulsion formulation containing mixed surfactants and transcutol P was selected to be incorporated into ion induced in situ gelling systems composed of gellan gum alone and in combination with xanthan gum, HPMC or carbopol...
April 19, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28433749/novel-sulphur-containing-imatinib-metabolites-found-by-untargeted-lc-hrms-analysis
#7
Ivo Vrobel, David Friedecký, Edgar Faber, Lukáš Najdekr, Kateřina Mičová, Radana Karlíková, Tomáš Adam
Untargeted metabolite profiling using high-resolution mass spectrometry coupled with liquid chromatography (LC-HRMS), followed by data analysis with the Compound Discoverer 2.0™ software, was used to study the metabolism of imatinib in humans with chronic myeloid leukemia. Plasma samples from control (drug-free) and patient (treated with imatinib) groups were analyzed in full-scan mode and the unknown ions occurring only in the patient group were then, as potential imatinib metabolites, subjected to multi-stage fragmentation in order to elucidate their structure...
April 19, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28416470/block-ionomer-micellar-nanoparticles-from-double-hydrophilic-copolymers-classifications-and-promises-for-delivery-of-cancer-chemotherapeutics
#8
REVIEW
S S Abolmaali, A M Tamaddon, M Salmanpour, S Mohammadi, R Dinarvand
A class of double hydrophilic copolymers comprising ionic and nonionic water-soluble blocks, which are also called block ionomers, represent an interesting type of polymer assembly forming stable, homogeneous core-corona dispersions. They exhibit the solution behavior of normal polyelectrolytes, whereas assembly into micelle, vesicle or disk morphology happens by an external stimulus (pH, temperature or ionic strength) or complex formation with metal ions, ionic surfactants, polyelectrolytes, etc. Temperature, pH, redox or salt sensitivity affords a unique opportunity to control the triggered release of payloads accommodated through electrostatic interaction, coordination or chemical conjugation...
April 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28412483/effect-of-micro-environment-modification-and-polymer-type-on-the-in-vitro-dissolution-behavior-and-in-vivo-performance-of-amorphous-solid-dispersions
#9
Weiwei Sun, Baoliang Pan
This study investigates the effects of micro-environment modification and polymer type on the in-vitro dissolution behavior and in-vivo performance of micro-environment pH modifying solid dispersions (pHM-SD) for the poorly water-soluble model drug Toltrazuril (TOL). Various pHM-SDs were prepared using Ca(OH)2 as a pH-modifier in hydrophilic polymers, including polyethylene glycol 6000 (PEG6000), polyvinylpyrrolidone k30 (PVPk30) and hydroxypropyl methylcellulose (HPMC). Based on the results of physicochemical characterizations and in-vitro dissolution testing, the representative ternary (Ca(OH)2:TOL:PEG6000/HPMC/PVPk30=1:8:24, w/w/w) and binary (TOL:PVPk30=1:3, w/w) solid dispersions were selected and optimized to perform in-vivo pharmacokinetic study...
April 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28412482/dapagliflozin-citric-acid-cocrystal-showing-better-solid-state-properties-than-dapagliflozin
#10
Jun-Hui Deng, Tong-Bu Lu, Changquan Calvin Sun, Jia-Mei Chen
Dapagliflozin (DAP) is a potent and selective sodium-glucose contransporter-2 inhibitor, for treating type 2 diabetes. DAP propanediol monohydrate (DAP-PDO-H2O, 1:1:1) is the solid form used in the current tablet product to address the severe hygroscopicity problem of DAP free form. DAP-PDO-H2O, however, suffers the problem of instability when exposed to high temperature, which renders it amorphous. In this work, we report on the preparation and evaluation of a new 1:1 cocrystal between DAP and citric acid (DAP-CA)...
April 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28412485/cancer-nanotheranostics-a-review-of-the-role-of-conjugated-ligands-for-overexpressed-receptors
#11
REVIEW
Lydia Ramzy, Maha Nasr, Abdelkader A Metwally, Gehanne A S Awad
Cancer treatment using chemotherapy has many drawbacks because of its non-specificity, in which the chemotherapeutic agent attacks both normal and cancerous cells, leading to severe damage to the normal cells, especially rapidly proliferating ones. Cancer targeting enables the drug to kill only tumor cells without adversely affecting healthy tissues, which leads to the improvement of the patient's well-being. Nanoparticles offer several advantages in drug delivery such as enhancing the solubility of hydrophobic drugs, sustaining their release and prolonging their circulation time...
April 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28412484/impact-of-demographics-and-disease-progression-on-the-relationship-between-glucose-and-hba1c
#12
Anetta Claussen, Jonas B Møller, Niels R Kristensen, Søren Klim, Maria C Kjellsson, Steen H Ingwersen, Mats O Karlsson
CONTEXT: Several studies have shown that the relationship between mean plasma glucose (MPG) and glycated haemoglobin (HbA1c) may vary across populations. Especially race has previously been referred to shift the regression line that links MPG to HbA1c at steady-state (Herman & Cohen, 2012). OBJECTIVE: To assess the influence of demographic and disease progression-related covariates on the intercept of the estimated linear MPG-HbA1c relationship in a longitudinal model...
April 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28408348/design-and-in-vivo-evaluation-of-solid-lipid-nanoparticulate-systems-of-olanzapine-for-acute-phase-schizophrenia-treatment-investigations-on-antipsychotic-potential-and-adverse-effects
#13
Emil Joseph, Satish Reddi, Vibhu Rinwa, Garima Balwani, Ranendra Saha
The present paper discusses the design, characterization and in vivo evaluation of glyceryl monostearate nanoparticles of Olanzapine, an atypical antipsychotic drug for acute schizophrenia treatment, during which hospitalization is mandatory and adverse effects are at its peak. The solid lipid nanoparticulate system was obtained by emulsification-ultra sonication technique wherein three factors such as solid lipid content, concentration of surfactant and drug: solid lipid ratio were selected at three different levels in order to study their influence on significant characteristic responses such as particle size, encapsulation efficiency and drug content...
April 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28400285/development-and-evaluation-of-a-cedrol-loaded-nanostructured-lipid-carrier-system-for-in-vitro-and-in-vivo-susceptibilities-of-wild-and-drug-resistant-leishmania-donovani-amastigotes
#14
Nabanita Kar, Shreyasi Chakraborty, Asit Kumar De, Santanu Ghosh, Tanmoy Bera
Leishmaniasis is an epidemic in various countries, and the parasite Leishmania donovani is developing resistance against available drugs. In the present study the antileishmanial action of cedrol was evaluated in vitro and in vivo. Activity potentiation was achieved via nanostructured lipid carrier (NLC) complexation of cedrol. Cedrol-loaded NLC was prepared through the hot-melting emulsification-ultrasonication method. The cedrol- NLC prepared did not require the use of any organic solvents. The characterization of NLC-C1 and NLC-C2 revealed that particle size was 46...
April 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28392494/fluoride-loaded-polymeric-nanoparticles-for-dental-delivery
#15
Sanko Nguyen, Carlos Escudero, Nadia Sediqi, Gro Smistad, Marianne Hiorth
The overall aim of the present paper was to develop fluoride loaded nanoparticles based on the biopolymers chitosan, pectin, and alginate, for use in dental delivery. First, the preparation of nanoparticles in the presence of sodium fluoride (NaF) as the active ingredient by ionic gelation was investigated followed by an evaluation of their drug entrapment and release properties. Chitosan formed stable, spherical, and monodisperse nanoparticles in the presence of NaF and tripolyphoshate as the crosslinker, whereas alginate and pectin were not able to form any definite nanostructures in similar conditions...
April 7, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28392493/the-efficacy-of-probiotics-as-pharmacological-treatment-of-cutaneous-wounds-meta-analysis-of-animal-studies
#16
REVIEW
Christos G Tsiouris, Martha Kelesi, Georgios Vasilopoulos, Ioannis Kalemikerakis, Effie G Papageorgiou
The aim of the current meta-analysis of animal studies was to evaluate the efficacy of probiotics as pharmacological treatment of cutaneous wounds. A systematic electronic literature search was conducted and in total six animal studies which undertake twelve experiments met our inclusion criteria. We used the percentage (%) of wound area at the end of the first week after initial wounding to evaluate the efficacy of the probiotic treatment. The heterogeneity was estimated as statistically significant (p<0...
April 7, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28392495/cocrystal-solubility-product-analysis-dual-concentration-ph-mass-action-model-not-dependent-on-explicit-solubility-equations
#17
Alex Avdeef
A novel general computational approach is described to address many aspects of cocrystal (CC) solubility product (Ksp) determination of drug substances. The CC analysis program, pDISOL-X, was developed and validated with published model systems of various acid-base combinations of active pharmaceutical ingredients (APIs) and coformers: (i) carbamazepine cocrystal systems with 4-aminobenzoic acid, cinnamic acid, saccharin, and salicylic acid, (ii) for indomethacin with saccharin, (iii) for nevirapine with maleic acid, saccharin, and salicylic acid, and (iv) for gabapentin with 3-hydroxybenzoic acid...
April 6, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28390837/the-influence-of-mannitol-on-morphology-and-disintegration-of-spray-dried-nano-embedded-microparticles
#18
Afra Torge, Philipp Grützmacher, Frank Mücklich, Marc Schneider
Nano-embedded microparticles represent a promising approach to deliver nanoparticles to the lungs. Microparticles with an appropriate aerodynamic diameter enable an application by dry powder inhaler and the transport of nanoparticles into the airways. By disintegration after deposition, nanoparticles can be released to exhibit their advantages such as a sustained drug release and delivery of the drug across the mucus barrier. The use of an appropriate matrix excipient to embed the nanoparticles is essential for the necessary disintegration and release of nanoparticles...
April 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28389275/effect-of-oxymatrine-hspc-liposomes-on-improving-bioavailability-liver-target-distribution-and-hepatoprotective-activity-of-oxymatrine
#19
Meifeng Liu, Sha Jin, Hao Yan, Song Du
Oxymatrine (OMT) and matrine (MT) are two naturally occurring alkaloids, both of them provide anti-hepatitis effects. However OMT effect was heavily limited due to its low bioavailability, short half-life and whole body distribution. Herein, we investigated hydrogenated soybean phosphatidylcholine (HSPC) liposomes made by pH gradient active loading to understand the improved hepatoprotective effect mechanisms. Pharmacokinetics researches demonstrated the half-life time of OMT HSPC liposomes was 17.10h in mice...
April 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28389274/significance-of-breath-hold-time-in-dry-powder-aerosol-drug-therapy-of-copd-patients
#20
Alpár Horváth, Imre Balásházy, Gábor Tomisa, Árpád Farkas
Aerosol drugs are effectively used to treat chronic respiratory diseases. The efficiency of the therapy depends also on the amount and distribution of drug deposited within the airways. The objective of this study is to apply numerical techniques to analyse the effect of the duration of breath-hold after the inhalation of six different commercialized dry powder drugs on their lung deposition. For this purpose a computational airway deposition model has been adapted and validated to the special case of therapeutic aerosols...
April 4, 2017: European Journal of Pharmaceutical Sciences
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