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European Journal of Pharmaceutical Sciences

Francesco Cilurzo, Umberto M Musazzi, Silvia Franzé, Guido Fedele, Paola Minghetti
Transdermal patches and medicated plasters are designed to sustain efficacious systemic or loco-regional drug concentrations, respectively. In both cases, drug skin permeation is a critical attribute from the early stage of the pharmaceutical development. In 2014, the EMA introduced the guideline "on the quality of transdermal patches", in which the importance of equivalence of drug fluxes in vitro skin permeation study was particularly emphasized to generic or abridged applications for the marketing authorization or manage dossier variations during the product cycle life...
September 17, 2018: European Journal of Pharmaceutical Sciences
Wenli Zhang, Zhiyu Wang, Chenchen Wu, Ya Jin, Xinyue Liu, Zimei Wu, Jianping Liu
In cholesterol/DSPE-PEG2000 /DPPC systems, nano-disks could evolve between liposomes and spherical micelles in a certain range of PEG-lipids. How cholesterol or drug influences this evolution and what about the properties of discoidal micelles as drug carrier are still not clear. Aiming at this, nanocarriers with different contents of cholesterol and DSPE-PEG2000 were prepared by thin-film-hydration method. Firstly, the bilayer fluidity of nanocarriers was investigated and proved to decrease with the increase of cholesterol, and the cooperative degree between phospholipids was also related to cholesterol content in an order of 30 > 40 > 15 > 0 mol%...
September 17, 2018: European Journal of Pharmaceutical Sciences
Caren Tatiane de David Antoniazzi, Samira Dal Toé De Prá, Paula Ronsani Ferro, Mariane Arnoldi Silva, Gabriela Adamante, Amanda Spring de Almeida, Camila Camponogara, Cássia Regina da Silva, Gustavo de Bem Silveira, Paulo Cesar Lock Silveira, Sara Marchesan Oliveira, Flávia Karine Rigo, Francesco De Logu, Romina Nassini, Gabriela Trevisan
Thermal injury promotes tissue inflammation and pain, which is difficult to control. Different peripheral mechanisms seem to be involved in burn pain, such as free radical-induced damage, but further study is still needed to understand how oxidant substances induced nociceptor sensitization. The transient receptor potential ankyrin 1 (TRPA1) is an ion channel activated by oxidants substances, and it could be sensitized after tissue inflammation. This study evaluated the TRPA1 involvement in nociception and inflammation produced by a thermal injury model...
September 17, 2018: European Journal of Pharmaceutical Sciences
P Ronnander, L Simon, H Spilgies, A Koch
A mathematical model was developed to predict the transport of sumatriptan molecules across the skin followed by absorption into the bloodstream. The drug was encapsulated in dissolving polyvinylpyrrolidone-based microneedles shaped in the form of pyramids. Mass balance equations were derived to simulate the dissolution and transport of the pharmaceutical ingredient. The theoretical framework made it possible to assess and predict the effects of key parameters on the release profile. The skin concentration increased with the loading dose and the height of the microneedle...
September 14, 2018: European Journal of Pharmaceutical Sciences
Rudradip Pattanayak, Atish Barua, Amlan Das, Tanima Chatterjee, Adrija Pathak, Pritha Choudhury, Srikanta Sen, Prosenjit Saha, Maitree Bhattacharyya
KRAS, a frequently mutated G-quadruplex forming proto-oncogene is responsible for almost every type of cancer which can form a parallel G-quadruplex structure in the promoter region. G-quadruplex structure is one of the most important drug targets for modern cancer therapy for their unique structure and specificity. Here, we have screened several synthetic porphyrin-based compounds as potential KRAS G-quadruplex stabilizing ligands, using molecular modeling and docking studies. Two novel porphyrins: Porphyrin-1(Cobalt containing) and Porphyrin-2 (Palladium containing) evidenced high affinity towards KRAS-promoter/G-quadruplex...
September 14, 2018: European Journal of Pharmaceutical Sciences
Vijay A Pawar, Arehalli S Manjappa, Prashant R Murumkar, Tejal K Gajaria, Ranjisinh V Devkar, Anil K Mishra, Mange Ram Yadav
Drug-fortified cationic liposomes of 6‑methoxy‑2‑naphthylacetic acid (6‑MNA) were prepared and characterized by various techniques. The residence time of drug-fortified liposomes in joint cavity was evaluated by intra-articular (IA) administration of the radio-labeled (99m Tc) liposomal formulation in the inflamed joints in rats. The cationic liposomal formulation composed of 6‑MNA (3) as an active agent, its double salt (4) with the lipid 1,2‑distearoyl‑sn‑glycero‑3‑phosphoethanolamine (DSPE), and pharmaceutically acceptable excipients such as hydrogenated soyabean phospatidylcholine (HSPC) and 1,2‑dioleyloxy‑3‑trimethylammoniumpropane chloride (DOTAP) were developed using thin film hydration technique...
September 13, 2018: European Journal of Pharmaceutical Sciences
Johan W Mouton
BACKGROUND: The Minimum Inhibitory Concentration (MIC) is a reference value for susceptibility testing of bacteria. However, the MIC is a net result of growth and killing after a certain duration of exposure under standardized favourable in vitro conditions. Killing and growth characteristics of a drug may yield more information on its activity and help to explain discrepancies between efficacy observed in vitro and in vivo. METHODS: The MIC of meropenem was determined for P...
September 12, 2018: European Journal of Pharmaceutical Sciences
Mahua Sarkar, Robert G Grossman, Elizabeth G Toups, Diana S-L Chow
Enterally administered riluzole is currently being investigated in a Phase II/III clinical trial for the treatment of acute spinal cord injury (SCI). Many SCI patients suffer from severe motor dysfunction and exhibit swallowing difficulties and cannot swallow riluzole tablets. The purpose of the present study was to develop a liquid solution formulation of riluzole, which can be administered more easily to this patient population with the capability to adjust the dose if needed. Riluzole was solubilized using water miscible organic solvents, namely, polyethylene glycol 400, propylene glycol and glycerin...
September 8, 2018: European Journal of Pharmaceutical Sciences
Kathrin Locher, Jens M Borghardt, Herbert Wachtel, Kerstin J Schaefer, Karl G Wagner
Biphasic dissolution models were proposed to provide good predictive power for in vivo absorption kinetics. However, up to date the impact of hydrodynamics in mini-scale models are not well understood. Consequently, the aim of this work was to investigate different setups of a previously published mini-scale biphasic dissolution model (miBIdi-pH-II) to better understand the relevance of hydrodynamics for evaluating kinetic parameters and to simultaneously increase the robustness of the experimental model. As a first step, the hydrodynamics within the aqueous phase were characterized by in silico simulations of the flow patterns...
September 6, 2018: European Journal of Pharmaceutical Sciences
Andrew M Ayoob, Marcello Peppi, Vishal Tandon, Robert Langer, Jeffrey T Borenstein
Measurement of drug distribution in the inner ear has important roles in the design of local delivery methods, such as direct, intracochlear delivery, and in assessment of emerging drug candidates in preclinical animal models. Sampling methods have been used in the past to measure drug concentrations in the cochlear fluids, but these methods provide no direct information about drug distribution in the cochlear tissues. In this work, we evaluated four fluorescent markers that simulate drug distribution in the organ of Corti after intracochlear delivery to the cochlea's scala tympani compartment...
September 6, 2018: European Journal of Pharmaceutical Sciences
Yasmine Korteby, Yassine Mahdi, Kamel Daoud, Géza Regdon
No abstract text is available yet for this article.
September 6, 2018: European Journal of Pharmaceutical Sciences
Jamie Anne Lugtu-Pe, Alireza Ghaffari, Kuan Chen, Anil Kane, Xiao Yu Wu
The amorphous solid dispersion (ASD) technique has been employed to formulate poorly-soluble drugs, however, development of solid dosage forms with ASD is challenging due to the high propensity of amorphous drug to precipitate upon dissolution. Thus this work aimed to explore the potential of controlled release amorphous solid dispersion (CRASD) systems using polyvinyl acetate (PVAc) as a release-retarding excipient to mitigate the drug precipitation during dissolution of poorly water-soluble drugs. A number of solid oral CRASD dosage forms in different shapes and structures were prepared to contain spray-dried SD powders of a model BCS Class II drug, celecoxib (CEL), polyvinylpyrrolidone (PVP) and polyvinyl acetate (PVAc) which was incorporated in varying ways...
September 6, 2018: European Journal of Pharmaceutical Sciences
Reham Mokhtar Aman, Irhan Ibrahim Abu Hashim, Mahasen Mohamed Meshali
Apocynin (APO), a specific NADPH oxidase inhibitor, is a bioactive phytochemical that exhibits versatile pharmacological activities. However, its rapid elimination and poor bioavailability represent great challenges to pharmaceutical scientists. Accordingly, novel chitosan-based APO-loaded solid lipid nanoparticles (CS,APO - loaded SLNS ) were developed to address such obstacles. A full 24 factorial design of experiment approach was employed to evaluate the individual and combined effect of critical process parameters namely; the amount of glycerol tristearate (GTS, XA ) and sucrose mono palmitate (SMP, XB ) as well as the concentration of chitosan (CS, XC ) and polyvinyl alcohol (PVA, XD ), on different critical quality attributes...
September 5, 2018: European Journal of Pharmaceutical Sciences
Jingxin Gou, Yuheng Liang, LinLin Miao, Yanhui Chao, Yu Zhang, Tian Yin, Haibing He, Xing Tang
Enteric polymers have been found with absorption promotion effect on nanoparticles. To study the role of enteric polymers played in the process of oral nanoparticle delivery, Eudragit L100-55 (EU) and sodium alginate (SA) were selected as model enteric polymers and larotaxel (LTX) as model drug. Suspensions composed of LTX-loaded nanoparticles, HPMC and different enteric polymers (EU and SA) were prepared (NP@EU, NP@SA). And aspects like precipitate morphology upon contact with acid, nanoparticle encapsulation capability, in vitro drug release, intestinal residence and in vivo oral bioavailability were studied...
September 5, 2018: European Journal of Pharmaceutical Sciences
Yifei Guo, Ting Wang, Shuang Zhao, Hanhong Qiu, Meihua Han, Zhengqi Dong, Xiangtao Wang
Drug-loaded nanoparticles utilizing amphiphilic molecules as nanocarriers were developed broadly for nanoscale drug delivery system. Linear amphiphilic molecule (PEG45 C18 ) based on PEG and alkyl chain was designed and synthesized. To study the influence of alkyl chain on antitumor activity, 10-hydroxycamptothecin (HCPT) was selected as the hydrophobic drug, amphiphilic molecule (PEG45 C18 ) and hydrophilic PEG (PEG45 ) were applied as nanocarriers to form HCPT-loaded nanoparticles (HCPT/PEG45 C18 NPs and HCPT/PEG45 NPs)...
September 4, 2018: European Journal of Pharmaceutical Sciences
Tong Liu, Xiaojing Zhang, Yidan Zhang, Jiuzhou Hou, Dong Fang, Hua Sun, Qin Li, Songqiang Xie
This study aimed to investigate the cellular disposition of liquiritigenin via the sulfonation pathway and the role of efflux transporters in liquiritigenin sulfate excretion. The sulfonation disposition of liquiritigenin was investigated using SULT1A3 overexpressed HEK293 cells (HEK-SULT1A3 cells). Liquiritigenin generated one mono-sulfate metabolite (7-O-sulfate) in HEK-SULT1A3 cell lysate. And the sulfonation followed the Michaelis-Menten kinetic (Vmax  = 0.84 nmol/min/mg and Km  = 7.12 μM)...
August 31, 2018: European Journal of Pharmaceutical Sciences
Tejal Rawal, Snehal Patel, Shital Butani
The purpose of the present research work was to explore chitosan nanoparticles (NPs) of a novel anti-tubercular drug, bedaquiline (BDQ) in order to reduce dose and side effects associated with oral BDQ formulation. The NPs were fabricated using ionic gelation method and evaluated for particle size, zeta potential, entrapment efficiency and drug loading. Plackett Burman was used as screening design. Two level three-factor factorial design was applied for optimization. Following freeze drying of NPs, the powder obtained was mixed with lactose pre-blend to obtain a respirable powder...
August 31, 2018: European Journal of Pharmaceutical Sciences
Carolin Auch, Meike Harms, Karsten Mäder
The predictability of preformulation screening tools for polymer selection in amorphous solid dispersions (ASD) regarding supersaturation and precipitation was systematically examined. The API-polymer combinations were scaled up by means of hot-melt extrusion and spray-drying to verify the predictions. As there were discrepancies between a solvent-based screening and performance of ASD, a new screening tool with improved predictability at minimal investments of time and material is presented. The method refinement resulted in a better correlation between the screening and ASD prototypes...
August 30, 2018: European Journal of Pharmaceutical Sciences
Bianca D van Groen, Evita van de Steeg, Miriam G Mooij, Marola M H van Lipzig, Barbara A E de Koning, Robert M Verdijk, Heleen M Wortelboer, Roger Gaedigk, Chengpeng Bi, J Steven Leeder, Ron H N van Schaik, Joost van Rosmalen, Dick Tibboel, Wouter H Vaes, Saskia N de Wildt
BACKGROUND: Hepatic membrane transporters are involved in the transport of many endogenous and exogenous compounds, including drugs. We aimed to study the relation of age with absolute transporter protein expression in a cohort of 62 mainly fetus and newborn samples. METHODS: Protein expressions of BCRP, BSEP, GLUT1, MCT1, MDR1, MRP1, MRP2, MRP3, NTCP, OCT1, OATP1B1, OATP1B3, OATP2B1 and ATP1A1 were quantified with LC-MS/MS in isolated crude membrane fractions of snap-frozen post-mortem fetal and pediatric, and surgical adult liver samples...
August 30, 2018: European Journal of Pharmaceutical Sciences
A Işılay Özdoğan, Gülçin Akca, Sevda Şenel
In recent years, statin group drugs have been widely investigated in treatment of periodontal diseases due to their anti-inflammatory effect. The efficacy of statins can be enhanced by local administration into the periodontal pocket by appropriate delivery systems. The aim of our study was to develop a bioadhesive delivery system for local delivery of atorvastatin in treatment of periodontal disease. For this purpose, gel formulations were prepared using different types of chitosan (base and water soluble) and viscosity, bioadhesivity and syringeability of the gels as well as in vitro drug release properties were investigated vitro...
August 29, 2018: European Journal of Pharmaceutical Sciences
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