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European Journal of Pharmaceutical Sciences

Kitti Szőke, Attila Czompa, István Lekli, Péter Szabados-Fürjesi, Mihály Herczeg, Magdolna Csávás, Anikó Borbás, Pál Herczegh, Árpád Tósaki
Ischemic heart conditions are among the main causes of sudden cardiac death worldwide. One of the strategies for avoiding myocardial infarction is the low-dose, prophylactic use of acetylsalicylic acid (ASA), an inhibitor of platelet aggregation. To avoid the gastrointestinal damage, ASA prodrugs bearing nitric oxide (NO)-donating moiety covalently conjugated to ASA have been synthesized and evaluated extensively worldwide. Herein the synthesis of a new hybrid ASA ester covalently attached to the NO donor linsidomine, an active metabolite of molsidomine (MOL) is reported...
February 16, 2019: European Journal of Pharmaceutical Sciences
Huili Li, Huanjie Li, Wei Yu, Shengnan Huang, Ying Liu, Ningxia Zhang, Jinxiu Yuan, Xin Xu, Shaofeng Duan, Yurong Hu
In recent years, cancer treatment has been facing the challenge of increasing antitumor efficiency and avoiding severe adverse effects simultaneously. In this study, we designed a controlled release drug delivery system, doxorubicin (Dox)-loaded and hyaluronic acid (HA)-modified PEGylated gold nanocages (AuNCs), which was designated as PEG-HAn-AuNCs/Dox (n represented 10n HA repeating units were modified on each AuNC). In this system, AuNCs were applied as the photothermal cores, Dox was employed as the model drug, HA was applied as the tumor-microenvironment responsive switch to achieve controlled release, and poly (ethylene glycol) (PEG) was used as the stealth polymer to prolong systemic circulation time...
February 16, 2019: European Journal of Pharmaceutical Sciences
Adam S Darwich, Howard J Burt, Amin Rostami-Hodjegan
Physiologically-based pharmacokinetic (PBPK) models provide a framework for in vitro-in vivo extrapolation of metabolic drug clearance. Many of the concepts in PBPK can have consequential impact on more mechanistic systems pharmacology models. In the gut wall, turnover of enzymes and enterocytes are typically lumped into one rate constant that describes the time dependent enzyme activity. This assumption may influence predictability of any sustained and dynamic effects such as mechanism-based inhibition (MBI), particularly when considering translation from healthy to gut disease...
February 15, 2019: European Journal of Pharmaceutical Sciences
Vinay R Sonawane, Mohd Usman Mohd Siddique, Linda Gatchie, Ibidapo S Williams, Sandip B Bharate, Venkatesan Jayaprakash, Barij N Sinha, Bhabatosh Chaudhuri
Microsomal cytochrome P450 (CYP) enzymes, isolated from recombinant bacterial/insect/yeast cells, are extensively used for drug metabolism studies. However, they may not always portray how a developmental drug would behave in human cells with intact intracellular transport mechanisms. This study emphasizes the usefulness of human HEK293 kidney cells, grown in 'suspension' for expression of CYPs, in finding potent CYP1A1/CYP1B1 inhibitors, as possible anticancer agents. With live cell-based assays, quinazolinones 9i/9b were found to be selective CYP1A1/CYP1B1 inhibitors with IC50 values of 30/21 nM, and > 150-fold selectivity over CYP2/3 enzymes, whereas they were far less active using commercially-available CYP1A1/CYP1B1 microsomal enzymes (IC50 , >10/1...
February 15, 2019: European Journal of Pharmaceutical Sciences
Tian Yang, Yue Shi, Chengjiang Lin, Chengda Yan, Donghu Zhang, Jianyang Lin
JCC-02, N-(3,5-dimethyladamantan-1-yl)-N'-(3-chlorophenyl) urea, has been developed as a novel N-methyl-d-aspartate (NMDA) receptor inhibitor for the treatment of Alzheimer's disease (AD). In this study, a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed to determine the concentration of JCC-02 in rat plasma and different tissues to investigate its pharmacokinetic behavior in vivo and distribution character in organs. The matrix samples were prepared by protein precipitation method with acetonitrile using gliclazide as the internal standard (IS)...
February 15, 2019: European Journal of Pharmaceutical Sciences
Angela Abruzzo, Teresa Cerchiara, Federica Bigucci, Giampaolo Zuccheri, Cristina Cavallari, Bruno Saladini, Barbara Luppi
The aim of this work was to prepare new mucoadhesive nasal decongestant nanoparticles obtained by direct crosslinking between the cationic polymer chitosan and the anionic drug cromolyn. Different chitosan/cromolyn molar ratios were used in order to obtain nanoparticles of suitable size, encapsulation efficiency/drug loading and mucoadhesion. Moreover, the ability of the nanoparticles to deliver cromolyn into and through the nasal mucosa was evaluated. The obtained positively charged nanoparticles, sized 180-400 nm, showed interesting properties in terms of yield, mucoadhesion, encapsulation efficiency and drug loading...
February 13, 2019: European Journal of Pharmaceutical Sciences
Florian Laubé, Andy Poupon, Philippe Zinck, Christel Müller-Goymann, Stephan Reichl, Véronique Nardello-Rataj
The human nail, like any biological material, is not readily available in large amounts and shows some variability from one individual to another. Replacing it by synthetic models is of great interest to perform reproducible and reliable tests in order to assess drug diffusion or nail lacquer adhesion for example. Keratin films, produced at the lab scale from natural hair, and the commercially available Vitro-nail® sheets have been proposed as models of human nails. In this study, we have investigated in detail these two materials...
February 13, 2019: European Journal of Pharmaceutical Sciences
Mohamed H Solayman, Taimour Y Langaee, Yan Gong, Mohamed H Shahin, Stephen T Turner, Arlene B Chapman, John G Gums, Eric Boerwinkle, Amber L Beitelshees, Manal El-Hamamsy, Lamia El-Wakeel, Rhonda M Cooper-DeHoff, Osama A Badary, Julie A Johnson
β-blockers show variable efficacy as antihypertensives. Herein, we evaluated plasma miRNAs as biomarkers for defining antihypertensive response to β-blockers. Expression of 22 β-blocker pharmacodynamics-related miRNAs was assessed in baseline plasma samples from 30 responders and 30 non-responders to metoprolol from the PEAR-2 study (Discovery). Logistic regression was performed to identify miRNAs significantly associated with metoprolol response. Those miRNAs were profiled in baseline plasma samples from 25 responders and 25 non-responders to atenolol from the PEAR study (validation)...
February 9, 2019: European Journal of Pharmaceutical Sciences
Tiziana Di Francesco, Emmanuelle Sublet, Gerrit Borchard
The assessment of interchangeability of nanomedicines and nanosimilars is required for ensuring the safety, quality and efficacy of these complex drugs. Since 2011, regulatory agencies and researchers focused their attention on the characterization of iron sucrose, a colloidal solution parenterally used for the treatment of iron deficiency anemia, as well as on their follow-on versions, the so-called iron sucrose similars (ISSs). The purpose of this study was the evaluation of the size and size distribution of both IS and ISSs after dilution in polypropylene bags containing saline, mimicking the preparation of ready-to-use infusions to be administered in a hospital environment...
February 8, 2019: European Journal of Pharmaceutical Sciences
Betul Suyumbike Yagci, Sedat Odabas, Eda Ayse Aksoy
In this study, novel elastomeric biodegradable bone regenerative films were developed from metformin (Met) and polyurethane (PU). Metformin was selected due to its osteogenic properties and proper chemical structure to react with PU prepolymer. Metformin was integrated into PU macromolecular structure as chain extender after the synthesis of PU prepolymer via condensation polymerization of polycaprolactone diol and hexamethylene diisocyanate. Chemical, thermal, viscoelastic properties of PU-Met films where characterized and discussed in terms of structure-property relationships...
February 8, 2019: European Journal of Pharmaceutical Sciences
Willy Smeralda, Marc Since, Sophie Corvaisier, Rémi Legay, Anne-Sophie Voisin-Chiret, Aurélie Malzert-Freon
Lipophilicity must be necessarily determined in drug discovery since this physicochemical property will directly influence the pharmacokinetics of a drug as its pharmacodynamics profile. Pyridoclax is an original lead, recently identified as very promising in treatment of chemoresistant cancers. The partition coefficient (Kp) of this anticancer drug was determined by microplate assays, well adapted in drug discovery, since being rapid, and requiring only poor drug amounts. The analytical approach was performed either by UV derivative spectrophotometry after validation thanks to a set of basic, neutral and acid reference substances, or originally, by raw fluorescence spectrophotometry by taking advantage of the pyridoclax intrinsic fluorescence...
February 8, 2019: European Journal of Pharmaceutical Sciences
Tong An, Zhixiang Liu, Zhiqiang Zhang, Jia Zhou, Mingming Wang, Meijuan Zou, Gang Cheng
The aim of the present study was to develop a new marker for correcting water flux in the in situ single-pass intestinal perfusion (SPIP) model. The new marker was designed and synthesized based on the application of both polyethylene glycol-4000 (PEG-4000) and phenol red as non-absorbable markers. The new marker mPEG-PR was obtained by combining phenol red with polyethylene glycol monomethyl ether-4000 (mPEG-4000) and verified by nuclear magnetic resonance (NMR), ultraviolet (UV) spectra, gel permeability chromatograph (GPC) and differential scanning calorimetry (DSC)...
February 5, 2019: European Journal of Pharmaceutical Sciences
Panagiotis Barmpalexis, Anna Karagianni, Konstantinos Katopodis, Elisavet Vardaka, Kyriakos Kachrimanis
A realistic molecular description of amorphous drug-polymer-plasticizer matrices, suitable for the preparation of amorphous solid dispersions (ASDs) with the aid of fusion-based techniques, was evaluated. Specifically, the incorporation of two model drugs (i.e. ibuprofen, IBU, and carbamazepine, CBZ) having substantially different thermal properties and glass forming ability, on the molecular representation of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (SOL)/polyethylene glycol (PEG, working as a plasticizer) molecular and thermal properties were evaluated with the aid of classical molecular dynamics (MD) and docking simulations...
February 5, 2019: European Journal of Pharmaceutical Sciences
Qiang Li, Qianqian Zhao, Qiufang Jing, Xiaosi Ma, Ning Chen, Guobin Ren, Defang Ouyang, Fuzheng Ren
Molecular interactions between drug and polymeric carriers are believed to be the key for high drug loading and better physical stability of micro-particles. However, molecular interactions between drug and polymer are still difficult to investigate using only experimental tools. In this study, high-loaded glipizide (GLP)/hydroxypropyl methylcellulose acetate succinate (HPMCAS) (1/1 w/w) micro-particles were prepared using an in situ pH-dependent solubility method. Molecular interactions within the micro-particles were investigated by integrated experimental and modeling techniques...
February 5, 2019: European Journal of Pharmaceutical Sciences
Shakeel Ahmad, Saquib Jalil, Sumera Zaib, Sana Aslam, Matloob Ahmad, Azhar Rasul, Muhammad Nadeem Arshad, Sadia Sultan, Abdul Hameed, Abdullah M Asiri, Jamshed Iqbal
We report the synthesis and biological evaluation of two new series of 2-amino-6-benzyl-4-phenyl-4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine-3‑carbonitrile 5,5-dioxides and 2-amino-6-methyl-4-phenyl-4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine-3‑carbonitrile 5,5-dioxides. The synthetic methodology involves a multistep reaction starting with methyl anthranilate which was coupled with methane sulfonyl chloride. The product of the reaction was subjected to N-benzylation and N-methylation reactions followed by ring closure with sodium hydride resulting in the formation of respective 2,1-benzothiazine 2,2-dioxides...
February 5, 2019: European Journal of Pharmaceutical Sciences
Puxvadee Chaikul, Nuntawat Khat-Udomkiri, Kochchawan Iangthanarat, Jiradej Manosroi, Aranya Manosroi
Physicochemical characteristics and in vitro anti-skin aging activity of gallic acid loaded in niosomes were investigated. Gallic acid was loaded in neutral (Brij 52/cholesterol at 7:3) and cationic CTAB niosomes (Brij 52/cholesterol/cetyltrimethylammonium bromide at 7:3:0.65). The maximum loading capacity and entrapment efficiency of gallic acid were 3.5, 4.48 ± 2.10 in neutral and 50%, w/w, 10.94 ± 0.78% in cationic CTAB niosomes, respectively. All gallic acid loaded in niosomes showed the unilamellar structure under transmission electron microscope with size range of 131...
February 5, 2019: European Journal of Pharmaceutical Sciences
Darshan R Telange, Shivendra B Nirgulkar, Milind J Umekar, Arun T Patil, Anil M Pethe, Nikhil R Bali
In the present study, umbelliferone - phospholipids complex - loaded matrix film (UPLC - MF) was developed with a goal of improving transdermal permeation and anti-inflammatory potential of umbelliferone (UMB). Umbelliferone - phospholipids complex (UPLC) was prepared using solvent evaporation method. UPLC-MF was prepared by simple and reproducible solvent casting method. Prepared UPLC and UPLC-MF were both physico-chemically characterized by Fourier transforms infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD), proton nuclear magnetic resonance spectroscopy (1 H NMR), weight variation, thickness, tensile strength, folding endurance, % elongation, moisture content and uptake Functional characterization of UPLC and UPLC-MF was carried out by solubility analysis, in vitro dissolution, diffusion, and ex vivo permeation via dialysis and biological membrane...
February 5, 2019: European Journal of Pharmaceutical Sciences
Rosalba Patiño-Herrera, José Francisco Louvier-Hernández, Eleazar M Escamilla-Silva, Julie Chaumel, Alma Gabriela Palestino Escobedo, Elías Pérez
Mesoporous silica nanoparticles (MSNPs) were synthesized and loaded with metformin hydrochloride (Metf), its adsorption has studied at different concentrations and pHs, optimal adsorption conditions were determined. Hybrid MSNPs-Metf were mixed with chitosan to compress them and form quasi-spherical pellets, were coated with five chitosan layers as a barrier to prolong metformin release. It showed that this pellet is useful for metformin controlled release since drug over time was significantly delayed by the chitosan coating and then, as metformin is electrostatically linked to MSNPs, it also controls the release of drug, releasing 170 mg after 17 h of exposure at pH 1...
February 5, 2019: European Journal of Pharmaceutical Sciences
Claudia Kirbs, Franziska Kluwe, Franziska Drescher, Edith Lackner, Peter Matzneller, Johanna Weiss, Markus Zeitlinger, Charlotte Kloft
Voriconazole, a broad-spectrum antifungal drug used to prevent and treat invasive fungal infections, shows complex pharmacokinetics and is primarily metabolised by various CYP enzymes. An adequate unbound antibiotic concentration-time profile at the target-site of an infection is crucial for effective prophylaxis or therapy success. Therefore, the aim was to evaluate the pharmacokinetics of voriconazole after the approved sequence dosing in healthy volunteers in interstitial space fluid, assessed by microdialysis, and in plasma...
February 4, 2019: European Journal of Pharmaceutical Sciences
Pratibha Anchi, Amit Khurana, Debasish Swain, Gananadhamu Samanthula, Chandraiah Godugu
Curcumin (cur) is a well known plant flavonoid with pleiotropic pharmacological activities. However, due to its poor bioavailability those therapeutic benefits are still out of reach for patient community. The main aim of our study was to prepare sustained release cur microparticles (CuMPs) with Poly (lactic-co-glycolic acid) (PLGA), an FDA approved biodegradable polymer and to assess their pharmacological potential in multiple low doses streptozotocin (MLD-STZ) induced type 1 diabetes mellitus (T1DM). CuMPs were formulated and characterized for size (12...
February 4, 2019: European Journal of Pharmaceutical Sciences
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