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European Journal of Pharmaceutical Sciences

Shan Wang, Chengyu Liu, Yuejie Chen, Zhen Zhang, Alan Zhu, Feng Qian
Hydroxypropyl methylcellulose acetate succinate (HPMC-AS) is one of the most widely used polymers used in amorphous solid dispersions (ASD) for solubility and bioavailability enhancement of poorly water-soluble drugs. Once released from ASDs, HPMC-AS was often found to be highly effective in maintaining drug supersaturation, and this capability is dependent on the concentration and substitution types of this pH-dependent polymer. Therefore, accurate quantification of different grades of HPMC-AS allows us to better understand the release and supersaturation mechanisms of HPMC-AS based ASDs...
July 10, 2018: European Journal of Pharmaceutical Sciences
Adriana Port, Magda Bordas, Raquel Enrech, Rosalia Pascual, Martí Rosés, Clara Ràfols, Xavier Subirats, Elisabeth Bosch
In the present study three different procedures have been compared for the determination of the lipophilicity of the unionized species (log Po/w ) of neutral, acidic, basic, amphoteric, and zwitterionic drugs. Shake-flask, potentiometric and chromatographic approaches have been assayed in a set of 66 representative compounds in different phases of advanced development. An excellent equivalence has been found between log Po/w values obtained by shake-flask and potentiometry, while the chromatographic approach is less accurate but very convenient for screening purposes when a high-throughput is required...
July 10, 2018: European Journal of Pharmaceutical Sciences
Jens Van Den Abeele, Maissa Rayyan, Ilse Hoffman, Els Van de Vijver, Wei Zhu, Patrick Augustijns
This work aimed to (i) expand the dataset on gastric fluid composition in the paediatric population (0-18 years old) and (ii) improve our understanding of age-dependent changes in gastric fluid characteristics involved in gastrointestinal drug disposition. For this purpose, gastric fluids from preterm neonates, term neonates, infants, children and adolescents were collected during routine medical procedures. Gastric fluid constituents relevant for gastrointestinal drug disposition were characterized i.e., pH, osmolality and bile salts (concentration + composition)...
July 10, 2018: European Journal of Pharmaceutical Sciences
Maja Bjelošević, Katarina Bolko Seljak, Uroš Trstenjak, Manca Logar, Boris Brus, Pegi Ahlin Grabnar
Freeze-drying is the method of choice to dry formulations with biopharmaceutical drugs, to enhance protein stability. This is usually done below the glass transition temperature of maximally freeze-concentrated solutions (Tg '), to avoid protein aggregation, preserve protein activity, and obtain pharmaceutically 'elegant' cakes. Unfortunately, this is a lengthy and energy-consuming process. However, it was recently shown that drying above Tg ' or even above the collapse temperature (Tc ) is not necessarily detrimental for stability of biopharmaceuticals, and hence provides an attractive option for freeze-drying cycle optimisation...
July 10, 2018: European Journal of Pharmaceutical Sciences
Maryam Ghaffari, Gholamreza Dehghan, Fereydoon Abedi-Gaballu, Soheila Kashanian, Behzad Baradaran, Jafar Ezzati Nazhad Dolatabadi, Dusan Losic
Dendrimers are nano-sized and three-dimensional macromolecules with well-defined globular architecture and are widely used in various aspects such as drug and gene delivery owing to multivalent and host-guest entrapment properties. However, dendrimers like other nanomaterials have some disadvantages for example rapid clearance by reticuloendothelial system, toxicity due to interaction of amine terminated group with cell membrane, low transfection efficiency and lack of controlled release behavior, which reduce their therapeutic efficiency...
July 9, 2018: European Journal of Pharmaceutical Sciences
Tamás Pálla, Gergő Tóth, Márta Kraszni, Arash Mirzahosseini, Béla Noszál
Populations, protonation constants and octanol-water partition coefficients were determined and assigned specifically to fast interconverting individual conformers, exemplified in baclofen and pregabalin, the GABA-related drug molecules of biaxial, double rotations. Rotamer statuses along both axes in water and octanol were elucidated from 1 H NMR vicinal coupling constants. Conformer abundances were obtained by the appropriate combination of the rotamer populations in the two adjacent moieties in the molecule...
July 5, 2018: European Journal of Pharmaceutical Sciences
Guillermo Nicolás Tocchetti, Camila Juliana Domínguez, Felipe Zecchinati, Maite Rocío Arana, María Laura Ruiz, Silvina Stella Maris Villanueva, Aldo Domingo Mottino, Johanna Weiss, Juan Pablo Rigalli
Multidrug resistance-associated protein 2 (MRP2) plays a key role in hepatic and intestinal disposition of endo- and xenobiotics. Several therapeutic agents modulate MRP2 activity resulting in pharmacological interactions. Nomegestrol acetate (NMGA) is a progestogen increasingly used in contraceptive formulations. The aim of this work was to evaluate the effect of NMGA on MRP2 activity in HepG2 and Caco-2 cells as models of human hepatocytes and enterocytes, respectively. NMGA (5, 50 and 500 nM; 48 h) decreased MRP2-mediated transport of 2,4-dinitrophenyl-S-glutathione in HepG2 cells, with no effect on MRP2 protein expression...
July 5, 2018: European Journal of Pharmaceutical Sciences
Tamer M Sakr, O M Khowessah, M A Motaleb, A Abd El-Bary, M T El-Kolaly, Mohamed M Swidan
Nanotechnology may be applied in medicine where the utilization of nanoparticles (≤100 nm) for the delivery and targeting of theranostic agents is at the forefront of projects in cancer nano-science. This study points a novel one step synthesis approach to build up polyethylene glycol capped silver nanoparticles doped with I-131 radionuclide (131 I-doped Ag-PEG NPs). The formula was prepared with average hydrodynamic size 21 nm, zeta potential - 25 mV, radiolabeling yield 98 ± 0.76%, and showed good in-vitro stability in saline and mice serum...
July 5, 2018: European Journal of Pharmaceutical Sciences
Manasa Kongot, Neeraj Dohare, Vishal Singh, Nitin Kumar Singhal, Rajan Patel, Amit Kumar
In the efforts to develop a biocompatible transition metal complex as a drug alike for some of the prevailing non-communicable diseases (NCDs) and communicable diseases (CDs), a novel binuclear NiII compound [{NiII (hpdbal-sbdt)}2 ] (2) has been synthesized by the reaction of Ni(OAc)2 .4H2 O and H2 hpdbal-sbdt (1) [1 is a dibasic tridentate ONS2- donor Schiff base ligand obtained by the condensation of 2-hydroxy-5-(phenyldiazenyl)benzaldehyde (Hhpdbal) and S-benzyldithiocarbazate (Hsbdt)]. Both ligand 1 and compound 2 were structurally characterized in the solid and solution state using various spectroscopic techniques like ATIR, 1 H NMR, 13 C NMR, TGA, FESEM, EDS and CHNS analysis...
July 5, 2018: European Journal of Pharmaceutical Sciences
M Lengyel, E Balogh, D Szerőczei, Cs Dobó-Nagy, Zs Pápay, V Stömmer, I Klebovich, I Antal
As surfactants are capable of influencing the droplet formation, our study primarily aims the investigation of the effect of a nonionic surfactant e.g. Polysorbate 80 on the formation of microspheres on the course of vibrating nozzle method with coacervation. The experiments also concern the impact of the different process parameters (e.g. vibration frequency, feed rate and voltage) on the shape and size distribution of microspheres characterized by laser diffraction size determination completed with particle image analysis...
July 5, 2018: European Journal of Pharmaceutical Sciences
Margarida Miranda, João José Sousa, Francisco Veiga, Catarina Cardoso, Carla Vitorino
Hitherto, for the approval of a topical generic drug product, the majority of the regulatory agencies require clinical endpoint studies to prove its therapeutic equivalence in relation to a reference product. Pharmacodynamic studies are also available to support bioequivalence, however, these are solely applicable for corticosteroids. The first strategy is considered the "gold standard", since it can be applied to all drug products. Nevertheless, the high variability intrinsic to topical drug delivery makes this analysis relatively insensitive, costly, time-consuming, besides requiring a large number of subjects...
July 4, 2018: European Journal of Pharmaceutical Sciences
Yu-Chih Lin, Chwan-Fwu Lin, Ahmed Alalaiwe, Pei-Wen Wang, Yi-Ping Fang, Jia-You Fang
The UVA absorbers such as avobenzone are widely used for sunlight protection; however, they show a significant skin penetration. The aim of the present study was to formulate UVA absorbers into mesoporous silicas (MSs) for enhanced UVA protection with reduced percutaneous absorption. Two MSs prepared with different structure-directing agents (Pluronic P123 as single MS and combined Pluronic P123-Pluronic F68 as hybrid MS) were synthesized in this study. The hybrid MS exhibited higher specific surface area (853 m2 /g) than the single MS (764 m2 /g)...
July 4, 2018: European Journal of Pharmaceutical Sciences
Guo Li, Yanfang Yang, Rui Zhou, Fayan Meng, Xuehua Li
Cancer cell targeted therapy using a biocompatible targeted drug delivery system can increase the therapeutic effects of cellular cancer therapy. Here, we report a Folic Acid (FA) and polyethyleneimine (PEI) functionalized Graphene Oxide (GO) nanocarrier, FA-PEI-GO, used to deliver two new Copper complexes into the folate-receptor-positive nasopharyngeal carcinoma cell line. GO was prepared by modified Hummers method and then decorated by PEI and FA. Afterwards, the material was characterized by the X-ray photoelectron spectra (XPS), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEM), and atomic force microscope (AFM)...
July 4, 2018: European Journal of Pharmaceutical Sciences
Shymaa Hatem, Maha Nasr, Noha H Moftah, Maha H Ragai, Ahmed S Geneidi, Seham A Elkheshen
The present study aimed to develop vitamin C based nanovesicles (aspasomes) loaded with the antioxidant melatonin, as a novel cosmeceutical to be used for clinical treatment of androgenic alopecia (AGA). Aspasomes were assessed regarding their particle size, charge, drug entrapment, anti-oxidant potential, physical stability, in vitro release, surface morphology, and ex-vivo skin deposition. Clinically, melatonin aspasomes were tested on AGA patients, and assessed by evaluating the degree of improvement through conduction of hair pull test, histometric analysis and dermoscopic evaluation...
July 4, 2018: European Journal of Pharmaceutical Sciences
Mohyeddin Assali, Ramzi Shawahna, Safa' Dayyeh, Mays Shareef, Imad-Aldin Alhimony
Inflammation is a nonspecific response of tissues to diverse stimuli and/or insults associated with the release of various mediators that induce pain, fever, and general sense of illness. Such responses can be reduced by the administration of non-steroidal or steroidal anti-inflammatory drugs. These anti-inflammatory drugs are associated with various side effect. However, the combination of non-steroidal anti-inflammatory drugs (NSAIDs) with glucocorticoids provides a synergistic anti-inflammatory and pain relief with less side effects...
July 4, 2018: European Journal of Pharmaceutical Sciences
Ayse N Oktay, Alptug Karakucuk, Sibel Ilbasmis-Tamer, Nevin Celebi
Flurbiprofen (FB) is the one of the non-steroidal anti-inflammatory drugs (NSAIDs) which has low water solubility and dissolution. Nanosuspensions are promising drug delivery systems consisting pure drug particles to overcome poor water solubility issues. Recently, design of experiment (DoE) approaches have often been used to develop new formulations include nanosuspensions. The main objective of this study was to prepare FB nanosuspensions in existence of Plantacare 2000 (PL) as stabilizer using DoE approach to evaluate the critical formulation attributes (CFAs) and critical process parameters (CPPs)...
July 4, 2018: European Journal of Pharmaceutical Sciences
Shansen Xu, Yanan Chen, Mingming Zhao, Yingjie Guo, Zhanyou Wang, Limei Zhao
Valproic acid (VPA) is a first-line anti-epileptic drug that is used in the treatment of generalized and partial seizures. Gene variants had been proved to influence the pharmacokinetics (PK) of VPA and contribute to its inter-individual variability (IIV). The aim of this study was to systematically investigate the effects of candidate gene variants (CYPs, UGTs, ABC transporters, and nuclear receptors) on VPA PK in Chinese children with epilepsy. A total of 1065 VPA serum trough concentrations at steady state were collected from 264 epileptic pediatric patients aged 3 months to 16 years...
July 4, 2018: European Journal of Pharmaceutical Sciences
Gergely Völgyi, Dóra Csicsák, Krisztina Takács-Novák
No abstract text is available yet for this article.
June 30, 2018: European Journal of Pharmaceutical Sciences
Maria José de Jesús Valle, Paula Coutinho, Maximiano Prata Ribeiro, Amparo Sánchez Navarro
The present work deals with the rational design and in vitro evaluation of vaginal tablets for focal delivery of fluconazole (FLZ) and itraconazol (ITZ). Drug loaded liposomes with and without d-alpha-tocopheryl polyethylene glycol 1000 succinate (vit E TPGS) were prepared by direct sonication of the components and mixed with albumin to obtain albusomes. Tablets were obtained by direct compression of the lyophilized cake. The influence of vit E TPGS on size, zeta potential and entrapment efficiency (EE%) of liposomes and albusomes was evaluated...
June 30, 2018: European Journal of Pharmaceutical Sciences
Twana Mohammed M Ways, Wing Man Lau, Keng Wooi Ng, Vitaliy V Khutoryanskiy
In this study, we synthesised thiolated silica nanoparticles using 3-mercaptopropyltrimethoxysilane and functionalised them with either 5 kDa methoxy polyethylene glycol maleimide (PEG) or 5 kDa alkyne-terminated poly(2-ethyl-2-oxazoline) (POZ). The main objectives of this study are to investigate the effects of pH on the size and ξ-potential of these nanoparticles and evaluate their mucoadhesive properties ex vivo using rat intestinal mucosa. The sizes of thiolated, PEGylated and POZylated silica nanoparticles were 53 ± 1, 68 ± 1 and 59 ± 1 nm, respectively...
June 30, 2018: European Journal of Pharmaceutical Sciences
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