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European Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/28822757/quercetin-exerts-synergetic-anti-cancer-activity-with-10-hydroxy-camptothecin
#1
Qin Tang, Fangling Ji, Jingyun Wang, Lianying Guo, Yachen Li, Yongming Bao
Quercetin (Qu) is known as a dietary antioxidant with numerous bioactivities, but its function in anti-cancer has not been fully investigated. Here, we show that Qu at low doses (≤10μM) significantly enhances the inhibition of 10-hydroxy camptothecin (HCPT) on the proliferation of MCF7, BGC823 and HepG2 cells. A plasmid DNA relaxation assay indicates that the inhibition of HCPT on the catalytic activity of topoisomerase I (Topo I) is increased by Qu at 10μM. Compared to the treatment by Qu or HCPT alone, phosphorylation at Ser(139) of γH2A...
August 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28821439/effect-of-alcohol-on-skin-permeation-and-metabolism-of-an-ester-type-prodrug-in-yucatan-micropig-skin
#2
Makiko Fujii, Rieko Ohara, Azusa Matsumi, Kayoko Ohura, Naoya Koizumi, Teruko Imai, Yoshiteru Watanabe
We studied the effect that three alcohols, ethanol (EA), propanol (PA), and isopropanol (IPA), have on the skin permeation of p-hydroxy benzoic acid methyl ester (HBM), a model ester-type prodrug. HBM was applied to Yucatan micropig skin in a saturated phosphate buffered solution with or without 10% alcohol, and HBM and related materials in receptor fluid and skin were determined with HPLC. In the absence of alcohol, p-hydroxy benzoic acid (HBA), a metabolite of HBM, permeated the skin the most. The three alcohols enhanced the penetration of HBM at almost the same extent...
August 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28821438/effect-of-lipid-emulsion-infusion-on-paliperidone-pharmacokinetics-in-the-acute-overdose-rat-model-a-potential-emergency-treatment-for-paliperidone-intoxication
#3
Tomoyuki Enokiya, Erquan Zhang, Kenji Ikemura, Yuichi Muraki, Yoshiaki Iwashita, Takuya Iwamoto, Hiroshi Imai, Kazuo Maruyama, Masahiro Okuda
Paliperidone prolongs cardiac repolarization in a concentration-dependent manner. Meanwhile, continuous infusion of intravenous lipid emulsion (ILE) has been established as a detoxification therapy for lipophilic drugs. However, this change in pharmacokinetics of various drugs following ILE administration remains to be clarified. Our objective is to clarify the effect of continuous intravenous infusion of lipid emulsion (ILE) on the pharmacokinetics of overdosed paliperidone in rats. Paliperidone (20mg/kg) was administered orally to free-moving male Wistar rats...
August 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28821437/particle-sizing-of-pharmaceutical-aerosols-via-direct-imaging-of-particle-settling-velocities
#4
Rami Fishler, Frank Verhoeven, Wilbur de Kruijf, Josué Sznitman
We present a novel method for characterizing in near real-time the aerodynamic particle size distributions from pharmaceutical inhalers. The proposed method is based on direct imaging of airborne particles followed by a particle-by-particle measurement of settling velocities using image analysis and particle tracking algorithms. Due to the simplicity of the principle of operation, this method has the potential of circumventing potential biases of current real-time particle analyzers (e.g. Time of Flight analysis), while offering a cost effective solution...
August 16, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28821436/carbon-quantum-dot-tailored-calcium-alginate-hydrogel-for-ph-responsive-controlled-delivery-of-vancomycin
#5
Niladri Sarkar, Gyanaranjan Sahoo, Rashmita Das, Gyanaranjan Prusty, Sarat K Swain
Herein, we demonstrate the preparation of highly luminescent carbon quantum dots (CQDs) from Aloe vera leaf gel; in just 2h at 250°C through carbonization pathway. The prepared CQDs are structurally characterized with high resolution transmission electron microscopy (HRTEM), hydrodynamic diameter and surface polarity, Fourier transform infrared spectroscopy (FTIR), X-ray photoelectron spectroscopy (XPS), Raman, UV-visible absorption spectrophotometry and fluorescence spectroscopy. The functional carbon nanoparticles are observed as non-cytotoxic materials...
August 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28821435/model-based-population-pk-pd-analysis-of-furosemide-for-bp-lowering-effect-a-comparative-study-in-primary-and-secondary-hypertension
#6
Mahendra Shukla, Moustafa M A Ibrahim, Moon Jain, Swati Jaiswal, Abhisheak Sharma, Kashif Hanif, Jawahar Lal
Though numerous reports have demonstrated multiple mechanisms by which furosemide can exert its anti-hypertensive response. However, lack of studies describing PK-PD relationship for furosemide featuring its anti-hypertensive property has limited its usage as a blood pressure (BP) lowering agent. Serum concentrations and mean arterial BP were monitored following 40 and 80mgkg(-1) multiple oral dose of furosemide in spontaneously hypertensive rats (SHR) and DOCA-salt induced hypertensive (DOCA-salt) rats. A simultaneous population PK-PD relationship using Emax model with effect compartment was developed to compare the anti-hypertensive efficacy of furosemide in these rat models...
August 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28818531/the-position-of-fluorine-in-cp-118-954-affects-ache-inhibition-potency-and-pet-imaging-quantification-for-ache-expression-in-the-rat-brain
#7
Byung Chul Lee, Byung Seok Moon, Hyun Soo Park, Jae Ho Jung, Hyun Sik Park, Do Dam Park, Modesto de Candia, Nunzio Denora, Cosimo D Altomare, Sang Eun Kim
The in vitro inhibition potency against acetylcholinesterase (AChE) of fluorinated derivatives of CP-118,954 (1) has been shown to depend upon the position of aromatic fluorine (F) substitution on the N-benzyl moiety. Indeed, the meta-F-substituted compound 3 (IC50=1.4nM) shows similar potency with the parent compound 1 (IC50=1.2nM), whereas the ortho-F derivative 2 (IC50=3.2nM) and para-F derivative 4 (IC50=10.8nM) were found to be less potent AChE inhibitors. A comparative in vivo microdialysis study in rats showed that 3 has the strongest effect on the neuropharmacological properties as AChE inhibitor...
August 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28818532/myricetin-solid-lipid-nanoparticles-stability-assurance-from-system-preparation-to-site-of-action
#8
Dina M Gaber, Noha Nafee, Osama Y Abdallah
Myricetin - a natural flavonoid - has attracted a great interest due to its antioxidant and free-radical scavenging potential. However, its physicochemical instability critically impairs its dosage form design, evaluation and administration. In an attempt to protect from degradation, MYR was encapsulated into Gelucire-based solid lipid nanoparticles (SLNs). The impact of medium pH, processing temperature and different additives on the drug degradation either in free or nanoencapsulated form was assessed. MYR stability was further monitored in essential biorelevant fluids...
August 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28811131/assessment-of-translational-risk-in-drug-research-role-of-biomarker-classification-and-mechanism-based-pkpd-concepts
#9
Sandra A G Visser, Tjerk J H Bueters
In 2005, Danhof and coauthors proposed a new biomarker classification in the context of the application of mechanism-based PKPD modeling. They defined the term 'biomarker' as a measure that characterizes a drug-induced response, which is on the causal path between drug administration and clinical outcome. The biomarker classification identified seven categories that provide different insights into the kinetics of drug action, such as target site distribution, target engagement, or into the impact of the drug on physiology or disease...
August 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28811130/comparative-study-on-stabilizing-ability-of-food-protein-non-ionic-surfactant-and-anionic-surfactant-on-bcs-type-ii-drug-carvedilol-loaded-nanosuspension-physicochemical-and-pharmacokinetic-investigation
#10
Tianjiao Geng, Parikshit Banerjee, Zhangdi Lu, Abdelmoumin Zoghbi, Tiantian Li, Bo Wang
Carvedilol (CAR) in its pure state has low aqueous solubility and extremely poor bioavailability which largely limit its clinical application. The aim of the study is to improve the dissolution rate and the bioavailability of CAR via preparing nanosuspensions with different stabilizers. Antisolvent precipitation-ultrasonication technique was used here. Attempts have been made to use food protein- Whey protein isolate (WPI) as a stabilizer in CAR loaded nanosuspension and also to compare its stabilizing potential with conventional nanosuspension stabilizers such as non-ionic linear copolymer-poloxamer 188 (PLX188) and anionic surfactant-sodium dodecyl sulfate (SDS)...
August 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28803922/studying-furosemide-solubilization-using-an-in-vitro-model-simulating-gastrointestinal-digestion-and-drug-solubilization-in-neonates-and-young-infants
#11
Mette Klitgaard, Philip Jonas Sassene, Arzu Selen, Anette Müllertz, Ragna Berthelsen
OBJECTIVE: The aim of the present study was to study the oral performance of furosemide in neonates and young infants using a newly developed in vitro model simulating digestion and drug solubilization in the gastrointestinal (GI) tract of the human neonate and young infant population (age 0-2months). METHODS: The utilized in vitro model was designed to mimic the digestion and drug solubilization processes occurring in the stomach, and the small intestine of the neonate and young infant population, using physiologically relevant media, volumes and digestive enzymes...
August 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28801274/mannich-base-approach-to-5-methoxyisatin-3-4-isopropylphenyl-hydrazone-a-water-soluble-prodrug-for-a-multitarget-inhibition-of-cholinesterases-beta-amyloid-fibrillization-and-oligomer-induced-cytotoxicity
#12
Leonardo Pisani, Annalisa De Palma, Nicola Giangregorio, Daniela V Miniero, Paolo Pesce, Orazio Nicolotti, Francesco Campagna, Cosimo D Altomare, Marco Catto
Targeting protein aggregation for the therapy of neurodegenerative diseases remains elusive for medicinal chemists, despite a number of small molecules known to interfere in amyloidogenesis, particularly of amyloid beta (Aβ) protein. Starting from previous findings in the antiaggregating activity of a class of indolin-2-ones inhibiting Aβ fibrillization, 5-methoxyisatin 3-(4-isopropylphenyl)hydrazone 1 was identified as a multitarget inhibitor of Aβ aggregation and cholinesterases with IC50s in the low μM range...
August 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28782609/prodrugs-recent-approvals-and-a-glimpse-of-the-pipeline
#13
REVIEW
Jarkko Rautio, Jussi Kärkkäinen, Kenneth B Sloan
Prodrugs offer a versatile strategy to overcome flaws of viable drug candidates or clinically approved drugs. However, the strategic importance of prodrugs in the pharmaceutical industry has often been challenged, and prodrugs are often considered as the last option after lead optimization and when the selected drug candidate has faced significant pharmaceutical and pharmacokinetic limitations. Based on recent success in marketed drugs, prodrug strategy should clearly be considered already in early stages of lead optimization...
August 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28778465/direct-comparison-of-udp-glucuronosyltransferase-and-cytochrome-p450-activities-in-human-liver-microsomes-plated-and-suspended-primary-human-hepatocytes-from-five-liver-donors
#14
Shalenie P den Braver-Sewradj, Michiel W den Braver, Audrey Baze, Joachim Decorde, Massimiliano Fonsi, Philippe Bachellier, Nico P E Vermeulen, Jan N M Commandeur, Lysiane Richert, J Chris Vos
UDP-glucuronosyltransferases (UGTs) and cytochrome P450s (CYPs) are the major enzymes involved in hepatic metabolism of drugs. Hepatic drug metabolism is commonly investigated using human liver microsomes (HLM) or primary human hepatocytes (PHH). We describe the development of a sensitive assay to phenotype activities of six major hepatic UGT isoforms (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9 and UGT2B7) in intact PHH by analysis of glucuronidation of selective probe substrates. The non-selective, general substrate 7-hydroxycoumarin was included for comparison...
August 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28778464/a-phase-i-randomized-clinical-trial-testing-the-safety-tolerability-and-preliminary-pharmacokinetics-of-the-mglur5-negative-allosteric-modulator-get-73-following-single-and-repeated-doses-in-healthy-volunteers
#15
Carolina L Haass-Koffler, Kimberly Goodyear, Victoria M Long, Harrison H Tran, Antonella Loche, Roberto Cacciaglia, Robert M Swift, Lorenzo Leggio
Preclinical work suggests that the metabotropic glutamate receptor subtype 5 (mGlu5) may represent a novel target to treat neuropsychiatric disorders, including alcohol use disorder and obesity. The goal of this first-in-man study was to evaluate the safety, tolerability and pharmacokinetics (PK) of GET 73 (PubChem SID: 329974174), a novel mGluR5 negative allosteric modulator. This was a double-blind, placebo-controlled, ascending dose, Phase I study conducted in healthy male volunteers in two experiments. GET 73 was administered as single ascending doses (N=48; Experiment 1; 10, 30, 100, 300, 450, 600-mg) or multiple ascending doses (N=32; Experiment 2; 100, 300, 450, 450-mg twice a day)...
August 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28774813/virtual-bioequivalence-for-achlorhydric-subjects-the-use-of-pbpk-modelling-to-assess-the-formulation-dependent-effect-of-achlorhydria
#16
Kosuke Doki, Adam S Darwich, Nikunjkumar Patel, Amin Rostami-Hodjegan
Majority of bioequivalence studies are conducted in healthy volunteers. It has been argued that bioequivalence may not necessarily hold true in relevant patient populations due to a variety of reasons which affect one formulation more than the other for instance in achlorhydric patients where elevated gastric pH may lead to differential effects on formulations which are pH-sensitive with respect to release or dissolution. We therefore examined achlorhydria-related disparity in bioequivalence of levothyroxine and nifedipine formulations using virtual bioequivalence within a physiologically-based pharmacokinetic (PBPK) modelling framework...
August 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28774812/cytochrome-p450-inhibition-by-three-licorice-species-and-fourteen-licorice-constituents
#17
Guannan Li, Charlotte Simmler, Luying Chen, Dejan Nikolic, Shao-Nong Chen, Guido F Pauli, Richard B van Breemen
The potential of licorice dietary supplements to interact with drug metabolism was evaluated by testing extracts of three botanically identified licorice species (Glycyrrhiza glabra L., Glycyrrhiza uralensis Fish. ex DC. and Glycyrrhiza inflata Batalin) and 14 isolated licorice compounds for inhibition of 9 cytochrome P450 enzymes using a UHPLC-MS/MS cocktail assay. G. glabra showed moderate inhibitory effects against CYP2B6, CYP2C8, CYP2C9, and CYP2C19, and weak inhibition against CYP3A4 (testosterone). In contrast, G...
July 31, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28774811/the-interaction-of-dendrimer-doxorubicin-conjugates-with-a-model-pulmonary-epithelium-and-their-cosolvent-free-pseudo-solution-formulations-in-pressurized-metered-dose-inhalers
#18
Qian Zhong, Bruno V Humia, Alisha R Punjabi, Francine F Padilha, Sandro R P da Rocha
Oral inhalation (OI) of nano-chemotherapeutics holds great potentials in the treatment of lung cancers as it enables direct targeting of drugs to lung tissues, spatial and temporal control of drug release, and decrease in drug-associated systemic and local lung toxicity. Therefore, the design of chemistry of the nanocarriers and their OI formulations for chemotherapeutics delivery to the peripheral lungs and extrapulmonary tissues of relevance such as lymph nodes, may thus afford new opportunities for treating such relevant diseases...
July 31, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28768147/production-of-human-recombinant-phenylalanine-hydroxylase-in-lactobacillus-plantarum-for-gastrointestinal-delivery
#19
Aura María Ramírez, Alexander Rodriguez-López, Andrea Ardila, Laura Beltran, Camilo Andres Patarroyo, Adelina Del Pilar Melendez, Oscar Fernando Sánchez, Carlos Javier Alméciga-Díaz
Phenylketonuria (PKU) is an autosomal recessive disorder caused by a defective phenylalanine hydroxylase (PAH), which catalyzes the hydroxylation of l-phenylalanine (l-Phe) to l-tyrosine (l-Tyr) in presence of the cofactor tetrahydrobiopterin (BH4). Defective PAH causes accumulation of phenylalanine, which has neurotoxic effects and leads to dermatological, behavioral, and neurocognitive problems. Treatments for this disease consist in life-long diets that are hard for patients to keep, or supplementation with BH4...
July 30, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28760594/s-oxiracetam-protect-against-ischemic-stroke-via-alleviating-blood-brain-barrier-dysfunction-in-rats
#20
Liangliang Huang, Erxin Shang, Wenxiang Fan, Xiang Li, Binbin Li, Shucheng He, Yuxin Fu, Yizhi Zhang, Yunman Li, Weirong Fang
The blood brain barrier (BBB) maintains the basic stability of the brain tissue under physiological conditions, while destroys and exaggerates brain edema and inflammatory response after ischemic stroke. In this study, we researched S-oxiracetam (S-ORC), a nootropic drug, alleviates BBB dysfunction and protects against ischemic stroke in rats. Middle cerebral artery occlusion(MCAO)/reperfusion in rats is applied to mimic ischemic stroke. One hour after reperfusion, rats are administered intravenously with different dose (0...
July 29, 2017: European Journal of Pharmaceutical Sciences
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