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European Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/28088372/nanoformulation-of-dual-bexarotene-tailed-phospholipid-conjugate-with-high-drug-loading
#1
Ruiyu He, Yawei Du, Longbing Ling, Muhammad Ismail, Yongpeng Hou, Chen Yao, Xinsong Li
Bexarotene (Bex), a synthetic retinoid X receptor-selective activator, has been proved to be an efficacious chemotherapeutic agent. But, its clinical application is limited due to the poor solubility. In this report, dual bexarotene-tailed phospholipid (DBTP) conjugate based nanovesicles were prepared in order to develop new nanoformulation. DBTP conjugate was first synthesized by conjugating two Bex molecules with glycerophosphorylcholine (GPC) through facial esterification. The amphiphilic DBTP nanovesicles were prepared without any additive by reverse-phase evaporation method...
January 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28088371/a-quality-by-design-qbd-study-on-enoxaparin-sodium-loaded-polymeric-microspheres-for-colon-specific-delivery
#2
Dana Hales, Laurian Vlase, Sebastian Alin Porav, Andreea Bodoki, Lucian Barbu-Tudoran, Marcela Achim, Ioan Tomuță
The aim of this study was to apply quality by design (QbD) for pharmaceutical development of enoxaparin sodium microspheres for colon-specific delivery. The Process Parameters (CPPs) and Critical Quality Attributes (CQAs) were identified. A central composite experimental design was used in order to develop the design space of microspheres for colon-specific delivery that have the desired Quality Target Product Profile (QTPP). The CPPs studied were Eudragit® FS-30D/Eudragit® RS-PO ratio, poly(vinyl alcohol) (PVA) concentration and sodium chloride (NaCl) concentration...
January 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28087355/generation-of-quercetin-cellulose-acetate-phthalate-systems-for-delivery-by-supercritical-antisolvent-process
#3
I García-Casas, A Montes, C Pereyra, E J Martínez de la Ossa
Supercritical antisolvent process (SAS) has been used to precipitate microparticles of quercetin, a plant pigment found in many foods and used for medical treatments, pharmaceutical and cosmetic industries, together with nanoparticles of cellulose acetate phthalate (CAP), a polymer quite frequently used in drug delivery. Previously, precipitation of nanoparticles of CAP by the same process was studied at different conditions of pressure, temperature, CO2and solution flow rates, nozzle diameter and initial concentration of the solution...
January 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28087354/effect-of-piroxicam-on-lipid-membranes-drug-encapsulation-and-gastric-toxicity-aspects
#4
Natalia Wilkosz, Sami Rissanen, Małgorzata Cyza, Renata Szybka, Maria Nowakowska, Alex Bunker, Tomasz Róg, Mariusz Kepczynski
Uptake of piroxicam, a non-steroidal anti-inflammatory drug, from the intestines after oral intake is limited due to its low solubility and its wide use is associated with several side effects related to the gastrointestinal tract. In this study, all-atom molecular dynamics (MD) simulations and fluorescent spectroscopy were employed to investigate the interaction of piroxicam in neutral, zwitterionic, and cationic forms with lipid bilayers composed of phosphatidylcholine, cholesterol, and PEGylated lipids. Our study was aimed to assess the potential for encapsulation of piroxicam in liposomal carriers and to shed more light on the process of gastrointestinal tract injury by the drug...
January 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28087353/thiolated-polymers-as-mucoadhesive-drug-delivery-systems
#5
REVIEW
Sarah Duggan, Wayne Cummins, Orla O' Donovan, Helen Hughes, Eleanor Owens
Mucoadhesion is the process of binding a material to the mucosal layer of the body. Utilising both natural and synthetic polymers, mucoadhesive drug delivery is a method of controlled drug release which allows for intimate contact between the polymer and a target tissue. It has the potential to increase bioavailability, decrease potential side effects and offer protection to more sensitive drugs such as proteins and peptide based drugs. The thiolation of polymers has, in the last number of years, come to the fore of mucoadhesive drug delivery, markedly improving mucoadhesion due to the introduction of free thiol groups onto the polymer backbone while also offering a more cohesive polymeric matrix for the slower and more controlled release of drug...
January 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28087352/engineering-hot-melt-extruded-solid-dispersion-for-controlled-release-of-hydrophilic-drugs
#6
Shuli Zhang, Xuan Meng, Zheng Wang, Aiping Fan, Guocheng Wang, Yanjun Zhao, Yu Tang
It is often challenging to precisely manipulate the release behavior of hydrophilic drugs that is believed to be crucial for a satisfactory therapeutic outcome. The aim of this work was to regulate the dissolution of hydrophilic drug from hot-melt extruded solid dispersion via rational screening of the pore-forming agents. Venlafaxine hydrochloride and Compritol® 888 ATO was selected as the model drug and carrier excipient, respectively. Hydrophilic polyethylene glycol (PEG 6000) and polyvinylpyrolidone (PVP K30) were chosen as the transient pore-forming agents...
January 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28077276/in-vitro-prediction-of-gastrointestinal-absorption-of-novel-%C3%AE-hydroxy-%C3%AE-arylalkanoic-acids-using-pampa-technique
#7
Jelena Savić, Vladimir Dobričić, Katarina Nikolic, Sote Vladimirov, Sanda Dilber, Jasmina Brborić
Prediction of gastrointestinal absorption of thirteen newly synthesized β-hydroxy-β-arylalkanoic acids (HAA) and ibuprofen was performed using PAMPA test. The highest values of PAMPA parameters (%T and Papp) were calculated for 1C, 1B and 2C and these parameters were significantly lower in comparison to ibuprofen. QSPR analysis was performed in order to identify molecular descriptors with the highest influence on %T and -logPapp and to create models which could be used for the design of novel HAA with improved gastrointestinal absorption...
January 7, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28069427/fabrication-of-topical-metered-dose-film-forming-sprays-for-pain-management
#8
Sneha Ranade, Amrita Bajaj, Vaishali Londhe, Najib Babul, Danny Kao
Topical film-forming metered dose spray formulations were designed for management of pain. Ropivacaine, a local anesthetic is explored for its topical efficacy in alleviating pain. Metered dose spray containers, organic solvents, film forming polymers and permeation enhancers were utilized to fabricate the Metered Dose topical spray. Factors like viscosity, spray pattern, spray angle, volume of actuation, droplet size distribution of the metered dose spray formulation and drying time, flexibility and wash-ability of the film formed after spraying were assessed...
January 6, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28065853/sitagliptin-inhibit-human-lymphocytes-proliferation-and-th1-th17-differentiation-in-vitro
#9
Marcelo Maia Pinheiro, Caroline Lais Stoppa, Claudete Justina Valduga, Cristina Eunice Okuyama, Renata Gorjão, Regina Mara Silva Pereira, Susana Nogueira Diniz
Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of anti-diabetic agents that are widely used in clinical practice to improve glycemic control in patients with type 2 diabetes. DPP-4 is also known as lymphocyte cell surface protein, CD26, and plays an important role in T-cell immunity. Recent studies suggest that DPP-4 inhibitors improve beta-cell function and attenuate autoimmunity in type 1 diabetic mouse models. To investigate the direct effect of DPP4 in immune response, human peripheral blood mononuclear cells (PBMC) from healthy volunteers were obtained by Ficoll gradient and cultivated in the absence (control) or presence of phytohemagglutinin (PHA), or stimulated with PHA and treated with sitagliptin...
January 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28063969/hii-mesophase-as-a-drug-delivery-system-for-topical-application-of-methyl-salicylate
#10
Xin Liang, Yu-Lin Chen, Xiao-Jing Jiang, Sheng-Mei Wang, Ji-Wen Zhang, Shuang-Ying Gui
The main objective of this study was to develop reversed hexagonal (HII) mesophase for transdermal delivery of methyl salicylate. The formulation was prepared, characterized and evaluated for its skin penetration in vitro and skin retention in vivo. Preliminary pharmacodynamics and skin irritation were also investigated. The formulation was identified as hexagonal structure. In vitro study exhibited that HII mesophase enhanced the skin permeation by delivering 2.61 times more methyl salicylate than the commercially available cream...
January 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28063968/lack-of-genetic-association-between-oct1-abcb1-and-ugt2b7-variants-and-morphine-pharmacokinetics
#11
L M Nielsen, E Sverrisdóttir, T B Stage, S Feddersen, K Brøsen, L L Christrup, A M Drewes, A E Olesen
AIM: A high inter-individual variation in the pharmacokinetics and pharmacodynamics of morphine has been observed. Genetic polymorphisms in genes encoding the organic cation transporter isoform 1 (OCT1), the efflux transporter p-glycoprotein (ABCB1), and the UDP-glucuronosyltransferase-2B7 (UGT2B7) may influence morphine pharmacokinetics and thus, also pharmacodynamics. The aim of this study was to evaluate the association between OCT1, ABCB1, and UGT2B7 variants, and morphine pharmacokinetics and -dynamics in healthy volunteers...
January 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28063967/an-innovative-polysaccharide-nanobased-nail-formulation-for-improvement-of-onychomycosis-treatment
#12
Fernanda C Flores, Roberta S Rosso, Letícia Cruz, Ruy C R Beck, Cristiane B Silva
Tioconazole-loaded nanocapsule suspensions and its coating with a cationic polymer were developed for nail drug delivery. The colloidal systems presented a nanometric size around 155nm for uncoated nanoparticles and 162nm for those with the cationic coating, with negative and positive zeta potential values, respectively. Both nanosuspensions showed drug content close to theoretical values (1mgmL(-1)), association efficiency close to 100% (HPLC) and were able to control tioconazol release. The developed formulations showed in vitro antifungal activity (agar diffusion method) against C...
January 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28063966/linking-organic-anion-transporting-polypeptide-1b1-and-1b3-oatp1b1-and-oatp1b3-interaction-profiles-to-hepatotoxicity-the-hyperbilirubinemia-use-case
#13
Eleni Kotsampasakou, Sylvia E Escher, Gerhard F Ecker
Hyperbilirubinemia is a pathological condition of excessive accumulation of conjugated or unconjugated bilirubin in blood. It has been associated with neurotoxicity and non-neural organ dysfunctions, while it can also be a warning of liver side effects. Hyperbilirubinemia can either be a result of overproduction of bilirubin due to hemolysis or dyserythropoiesis, or the outcome of impaired bilirubin elimination due to liver transporter malfunction or inhibition. There are several reports in literature that inhibition of organic anion transporting polypeptides 1B1 and 1B3 (OATP1B1 and OATP1B3) might lead to hyperbilirubinemia...
January 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28063965/a-calix-4-arene-derivativeand-itsselectiveinteractionwithdrugs-clofibric-acid-diclofenac-andaspirin
#14
Angela F Danil de Namor, Maan Al Nuaim, Jose A Villanueva Salas, Sophie Bryant, Brendan Howlin
The synthesis and characterisation of a partially substituted calix[4]arene, namely, 5,11,17,23-tetra-tert-butyl,25,27-bis[aminoethoxy] 26,28-dihydroxycalix[4]arene are reported. Its interaction with commonly used pharmaceuticals (clofibric acid, diclofenac and aspirin) was investigated by spectroscopic ((1)H NMR and UV), electrochemical (conductance measurements) and thermal (titration calorimetry) techniques. It is concluded on the basis of the experimental work and molecular simulation studies that the receptor interacts selectively with these drugs...
January 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28062260/effect-of-differential-surface-anisotropy-on-performance-of-two-plate-shaped-crystals-of-aspirin-form-i
#15
Tanshu Jain, Sneha Sheokand, Sameer R Modi, Bharat Ugale, Ram Naresh Yadav, Navin Kumar, C M Nagaraja, Arvind K Bansal
Differential surface anisotropy of different crystals of the same API can have a significant impact on their pharmaceutical performance. The present work investigated the impact of differential surface anisotropy of two plate-shaped crystals of aspirin (form I) on their hygroscopicity, stability and compaction behavior. These crystals differed in their predominant facets (100) and (001) and were coded as AE-100 & E-001. (100) facets exposed polar carbonyl groups which provided hydrophilicity to the facets. In contrast, (001) facets possessed hydrophobicity as they exposed non-polar aryl and methyl groups...
January 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28062259/preparation-of-curcumin-loaded-pcl-peg-pcl-triblock-copolymeric-nanoparticles-by-a-microchannel-technology
#16
Fangyuan Guo, Dingjia Guo, Wei Zhang, Qinying Yan, Yan Yang, Weiyong Hong, Gensheng Yang
Biodegradable polymeric nanoparticles (NPs) have potential therapeutic applications; however, preparing NPs of a specific diameter and uniform size distribution is a challenge. In this work, we fabricated a microchannel system for the preparation of curcumin (Cur)-loaded NPs by the interfacial precipitation method, which rapidly and consistently generated stable NPs with a relatively smaller diameter, narrow size distribution, and higher drug-loading capacity and entrapment efficiency. Poly(ε-caprolactone)-poly(ethylene glycol)-poly (ε-caprolactone) triblock copolymers(PCEC) used as the carrier material was synthesized and characterized...
January 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28057551/metabolite-inactive-etomidate-analogues-alleviating-suppression-on-adrenal-function-in-beagle-dogs
#17
Jun Yang, Yi Kang, Bin Wang, Linghui Yang, Jin Liu, Wensheng Zhang
Owing to rapid generation in body, the metabolites of etomidate softdrug are able to accumulate in either the brain or periphery and subsequently affect the recovery from anaesthesia or cause corticosteroid suppression. This study was designed to investigate the ability of two etomidate analogues (ET-26, ET-42) with inactive metabolites to provide anaesthesia with lesser corticosteroid suppression. The 50% effective dose (ED50) of ET-26, ET-42, Etomidate, MOC-ET (an etomidate softdrug) and CPMM (an improved etomidate softdrug) required to induce anaesthesia intravenously in Beagle dogs were 1...
January 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28057549/novel-amphiphilic-chitosan-nanocarriers-for-sustained-oral-delivery-of-hydrophobic-drugs
#18
Marjan Motiei, Soheila Kashanian
Chitosan (CS) has been investigated for its ability to be modified hydrophobically and self-assembled into nanocarriers. They can encapsulate drugs and protect them in a promising approach. However, loss of carrier stability against biological environments induces low bioavailability of encapsulated drugs after oral administration. The objective of this work was to develop and characterize a novel self-assembled nanocarrier using cross-linker under acidic condition to enhance oral absorption of a hydrophobic model drug such as Letrozole (LTZ)...
January 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28057547/intracellular-signaling-modifications-involved-in-the-anti-inflammatory-effect-of-4-alkoxy-6-9-dichloro-1-2-4-triazolo-4-3-a-quinoxalines-on-macrophages
#19
Antonio J Ruiz-Alcaraz, María Tristán-Manzano, Antonio Guirado, Jesús Gálvez, María Martínez-Esparza, Pilar García-Peñarrubia
Inflammation is part of a complex biological response directed by the immune system to fight pathogens and maintain homeostasis. Dysregulation of the inflammatory process leads to development of chronic inflammatory or autoimmune diseases. Several cell types, such as macrophages, and cytokines such as interleukin 6 (IL-6) and tumor necrosis factor alpha (TNF-α) are involved in the regulation of inflammation. The important role played by these cytokines as mediators of the inflammatory process and the side effects of current therapies have promoted the search of new therapeutic alternatives...
January 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28057550/pharmacokinetics-of-lbpt-and-its-primary-metabolites-as-well-as-tolerability-in-the-first-in-human-study
#20
Hongyun Wang, Hongzhong Liu, Ming Liu, Wenjie Wang, Liya Zhu, Haihong Huang, Pei Hu, Ji Jiang
BACKGROUND: LBPT is a novel platelet-activating factor (PAF) receptor antagonist that is developed for the treatment of rheumatoid arthritis. The purpose of this first-in-human study was to evaluate the tolerability and safety of LBPT, to investigate the pharmacokinetics of LBPT and its primary metabolites, as well as to assess the food effect on the pharmacokinetics in healthy Chinese subjects. MATERIALS AND METHODS: LBPT was evaluated in 2 clinical studies. The first study was a double blind, placebo-controlled and ascending dose study...
January 2, 2017: European Journal of Pharmaceutical Sciences
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