5,476,811 results match your criteria Drug Design Development and Therapy [Journal]

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[New drugs for horses and production animals in 2018].

Tierarztl Prax Ausg G Grosstiere Nutztiere 2019 Apr 18;47(2):116-120. Epub 2019 Apr 18.

Institut für Pharmakologie, Pharmazie und Toxikologie, Veterinärmedizinische Fakultät der Universität Leipzig.

In 2018, no new active pharmaceutical ingredients were released on the German market for horses or food-producing animals. One established veterinary active pharmaceutical ingredient became available for an additional species: the inhalant anesthetic Isoflurane (Isofluran Baxter vet) from the group of halogenated hydrocarbon compounds was additionally authorized for pigs (piglets). With Acepromazine, Mepivacaine and Oxyclozanide, three temporarily non-available active ingredients were reapproved in new drugs. Read More

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http://dx.doi.org/10.1055/a-0858-7380DOI Listing

The Degree of Multidimensional Severity of Alcohol Use Disorder among Treatment-Seeking Patients: Is There an Additive Effect of Parental Alcohol Use Disorder?

Eur Addict Res 2019 Apr 18:1-7. Epub 2019 Apr 18.

Unit for Clinical Alcohol Research, Unit for Psychiatric Research, Department of Clinical Research, University of Southern, Odense, Denmark.

Background: The additive effect of parental alcohol use disorders (AUD) is conventionally defined as an increasing risk of the offspring developing AUD relative to family history negative, < family history positive with 1 parent (FHP1), < FHP2. The few studies on the additive effect of parental AUD have focused on the risk of development of offspring AUD and not on the degree of multidimensional AUD addiction severity.

Aims: The aims of the present study were to examine the frequency of treatment-seeking outpatients exposed to FHP1 and FHP2 and whether addiction severity was impacted by the additive effect of parental AUD among AUD female and male offspring. Read More

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http://dx.doi.org/10.1159/000499935DOI Listing
April 2019
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Multimorbidity in Asthma, Allergic Conditions and COPD Increase Disease Severity, Drug Use and Costs: The Finnish Pharmacy Survey.

Int Arch Allergy Immunol 2019 Apr 18:1-8. Epub 2019 Apr 18.

Skin and Allergy Hospital, Helsinki University Hospital, University of Helsinki, Helsinki, Finland.

Background: Asthma, allergic conditions, and COPD overlap, but the effect of them and their combinations on disease severity, need for drugs, use of healthcare, and costs is poorly known.

Objective: To study how different allergic diseases co-occur in asthma and allergy patients and evaluate the use of medication well as drug and healthcare costs.

Methods: Nationwide Allergy Barometer Survey was carried out in the Finnish pharmacies during 1 week in September 2016. Read More

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http://dx.doi.org/10.1159/000498861DOI Listing

Sex Influence on the Efficacy and Safety of Sacubitril/Valsartan.

Cardiology 2019 Apr 18;142(2):73-78. Epub 2019 Apr 18.

Servicio de Cardiología, Hospital Universitario Gregorio Marañón, CIBERCV, Madrid, Spain,

Background: Women are underrepresented in sacubitril/valsartan (SV) clinical trials. The aim of this study was to assess sex-specific differences in efficacy, tolerability, and safety of SV in real-world heart failure with reduced ejection fraction (HFrEF) patients.

Methods: A prospective registry in 10 centers including all patients who started SV during the last 6 months was analyzed in this study. Read More

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http://dx.doi.org/10.1159/000498984DOI Listing

Influence of Gamma-Hydroxybutyric Acid-Use and Gamma-Hydroxybutyric Acid-Induced Coma on Affect and the Affective Network.

Eur Addict Res 2019 Apr 18:1-9. Epub 2019 Apr 18.

Department of Psychiatry, Amsterdam Neuroscience, Amsterdam UMC, University of Amsterdam, Amsterdam, The Netherlands.

Background: Gamma-hydroxybutyric acid (GHB) is a drug of abuse associated with increased emergency room attendances, due to GHB-induced comas. Withdrawal from GHB often increases social anxiety and is linked to alterations in emotion processing. However, little is known about the effects of GHB-use and GHB-induced comas on affect regulation in humans. Read More

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http://dx.doi.org/10.1159/000497381DOI Listing

MADD silencing enhances anti-tumor activity of TRAIL in anaplastic thyroid cancer.

Endocr Relat Cancer 2019 Jun;26(6):551-563

Department of Microbiology and Immunology, University of Illinois College of Medicine, Chicago, Illinois, USA.

ATC is an aggressive disease with limited therapeutic options due to drug resistance. TRAIL is an attractive anti-cancer therapy that can trigger apoptosis in a cancer cell-selective manner. However, TRAIL resistance is a major clinical obstacle for its use as a therapeutic drug. Read More

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https://erc.bioscientifica.com/view/journals/erc/26/6/ERC-18
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http://dx.doi.org/10.1530/ERC-18-0517DOI Listing
June 2019
1 Read
4.805 Impact Factor

UHPLC assisted simultaneous separation of apigenin and prednisolone and its application in the pharmacokinetics of apigenin.

J Chromatogr B Analyt Technol Biomed Life Sci 2019 Apr 3;1117:58-65. Epub 2019 Apr 3.

Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, P.O. Box: 2457, Saudi Arabia. Electronic address:

A new ultra-high performance liquid chromatography-mass spectrometry-mass spectrometry (UHPLC-MS/MS) system has been formulated for the resolution of closely related drugs apigenin (API, a bioflavinoid) and prednisolone (PRD) from their mixture. This developed method comprised of a "BEH™ C column (50 mm × 2.1 mm, 1. Read More

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http://dx.doi.org/10.1016/j.jchromb.2019.04.006DOI Listing

Intraoperative ultrasonography (ioUS) characteristics of focal cortical dysplasia (FCD) type II b.

Seizure 2019 Mar 12;69:80-86. Epub 2019 Mar 12.

Department of Neurosurgery, Fondazione IRCCS Istituto Neurologico C. Besta, Milan, Italy; Department of Neurological Surgery, Johns Hopkins Medical School, Baltimore, MD, USA.

Purpose: Focal cortical dysplasia (FCD) is one of the major causes of drug-resistant epilepsy. Surgery has proved to be the treatment of choice, however up to a third of patients experience only partial resection. Ill-defined borders and lesions embedded in eloquent areas are two of the main drawbacks of FCD surgery. Read More

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http://dx.doi.org/10.1016/j.seizure.2019.02.020DOI Listing

Parental views on state cannabis laws and marijuana use for their medically vulnerable children.

Drug Alcohol Depend 2019 Feb 14;199:59-67. Epub 2019 Feb 14.

Division of Adolescent and Young Adult Medicine, Boston Children's Hospital, Boston, MA, United States; Department of Pediatrics, Harvard Medical School, Boston, MA, United States.

Background: Given a rapidly changing policy landscape, we sought to characterize the effects of state marijuana laws on parents' views of marijuana use by their teenage children.

Methods: Data are from 595 respondents to a nationally administered, web-based survey of parents of adolescents (ages 13-18 years) with any of three chronic conditions (type 1 diabetes, rheumatic disease, attention-deficit/hyperactivity disorder). Multivariate ordinal logistic regression was used to model the effects of parents' reports of state cannabis laws on their views toward marijuana use by their child. Read More

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http://dx.doi.org/10.1016/j.drugalcdep.2018.12.027DOI Listing
February 2019

Potent and selective EGFR inhibitors based on 5-aryl-7H-pyrrolopyrimidin-4-amines.

Bioorg Chem 2019 Apr 11;88:102918. Epub 2019 Apr 11.

Department of Chemistry, Norwegian University of Science and Technology (NTNU), NO-7491 Trondheim, Norway. Electronic address:

The epidermal growth factor receptor represents an important target in cancer therapy, and low molecular weight inhibitors based on quinazolines have reached the marked. Herein we report on a new scaffold, 5-aryl-7H-pyrrolo[2,3-d]pyrimidin-4-amines, and show that when employing (S)-phenylglycinol as C-4 substituent, potent inhibitors can be made. The two most active inhibitors have suitable druglike properties, were equipotent with Erlotinib in Ba/F3 cell studies, and showed lower cross reactivity than Erlotinib in a panel of 50 kinases. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.102918DOI Listing

Changes in chemsex and sexual behaviour over time, among a cohort of MSM in London and Brighton: Findings from the AURAH2 study.

Int J Drug Policy 2019 Apr 15;68:54-61. Epub 2019 Apr 15.

UCL Centre for Population research in Sexual Health and HIV, Institute for Global Health, UCL, London, United Kingdom. Electronic address:

Background: Recent evidence has suggested that chemsex (the use of mephedrone, crystal methamphetamine and γ -hydroxybutyrate/ γ -butryolactone (GHB/GBL) to enable, enhance and prolong sexual interactions) has increased among men having sex with men (MSM) attending sexual health clinics in large UK cities. To date there has been no data from the UK or Europe that describes changes in chemsex over time within a cohort of MSM.

Methods: The prospective cohort study, Attitudes to and Understanding Risk of Acquisition of HIV over Time (AURAH2), collected online questionnaire data from HIV negative or undiagnosed MSM (at enrolment) from 2015 to 2018, recruited from sexual health clinics. Read More

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http://dx.doi.org/10.1016/j.drugpo.2019.03.021DOI Listing

Application of conducting polymers to wound care and skin tissue engineering: A review.

Biosens Bioelectron 2019 Apr 6;135:50-63. Epub 2019 Apr 6.

Nanyang Environment and Water Research Institute, Residues and Resource Reclamation Center, 1 Cleantech Loop, CleanTech, Singapore, 637141, Singapore; School of Civil and Environmental Engineering, Nanyang Technological University, 50 Nanyang Avenue, Singapore, 639798, Singapore. Electronic address:

The use of intrinsically conducting polymers (CPs) in wound care and skin tissue engineering presents a novel opportunity for accelerated wound healing, enhanced antibacterial activity and the potential for controlled drug delivery. Through their increased electrical conductivity, CPs can facilitate the application of electrical stimulation directly to the wound area, which has been linked to faster wound healing. The release of drugs or biological agents to the wound site can likewise be modulated through the use of an external electrical stimuli. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09565663193028
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http://dx.doi.org/10.1016/j.bios.2019.04.001DOI Listing
April 2019
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Discovery of 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk).

Eur J Med Chem 2019 Mar 26;173:167-183. Epub 2019 Mar 26.

State Key Laboratory of Chemical Oncogenomics, Engineering Laboratory for Chiral Drug Synthesis, School of Chemical Biology and Biotechnology, Shenzhen Graduate School, Peking University, Shenzhen, 518055, China. Electronic address:

Interleukin-2-inducible T-cell kinase (Itk) plays an important role in multiple signal transduction pathways in T and mast cells, and is a potential drug target for treating inflammatory diseases, autoimmune diseases, and T cell leukemia/lymphoma. Herein, we describe the discovery of a series of covalent Itk inhibitors based on the 7H-pyrrolo[2,3-d]pyrimidine scaffold. Placing an appropriate substitution group at a hydration site of the ATP binding pocket of Itk and using a saturated heterocyclic ring as a linker to the reactive group were crucial for selectivity. Read More

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http://dx.doi.org/10.1016/j.ejmech.2019.03.055DOI Listing

Ghrelin signalling within the rat nucleus accumbens and skilled reach foraging.

Psychoneuroendocrinology 2019 Apr 8;106:183-194. Epub 2019 Apr 8.

Department of Pharmacology, Institute of Neuroscience and Physiology, The Sahlgrenska Academy at the University of Gothenburg, Gothenburg, Sweden. Electronic address:

Motivation alters behaviour in a complex manner and nucleus accumbens (NAc) shell has been implied as a key structure regulating such behaviour. Recent studies show that acute ghrelin signalling enhances motivation when assessed in a simple motor task. The aim of the present study was to define the role of ghrelin signalling on motivation in a more complex motor behaviour. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03064530193012
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http://dx.doi.org/10.1016/j.psyneuen.2019.04.008DOI Listing
April 2019
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G-quadruplex and duplex DNA binding studies of novel Ruthenium(II) complexes containing ascididemin ligands.

J Inorg Biochem 2019 Apr 6;196:110681. Epub 2019 Apr 6.

Shanghai Key Laboratory of Chemical Assessment and Sustainability, School of Chemical Science and Engineering, Tongji University, Shanghai 200092, PR China. Electronic address:

In this paper, three new Ruthenium(II) polypyridyl complexes containing ascididemin (ASC) as main ligand have been synthesized and characterized. Their interactions with different G-quadruplex (Htelo, c-myc and c-kit) (Htelo: human telomeric DNA, c-myc: cellular-myelocytomatosis viral oncogene, c-kit: oncogene c-kit promoter sequences) and duplex (ds26) DNA sequences were comparatively studied with the free ligand ASC by a series of spectroscopic techniques including UV-vis (ultraviolet-visible) spectroscopy, FID (fluorescent intercalator displacement) assay, and FRET (fluorescence resonance energy transfer) melting assay. Molecular docking studies were also performed to support the binding mode of the compounds with G-quadruplex DNA. Read More

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http://dx.doi.org/10.1016/j.jinorgbio.2019.03.021DOI Listing

Cobalt(II) complexes with the non-steroidal anti-inflammatory drug diclofenac and nitrogen-donor ligands.

J Inorg Biochem 2019 Apr 5;196:110688. Epub 2019 Apr 5.

Laboratory of Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece. Electronic address:

The interaction of the non-steroidal anti-inflammatory drug sodium diclofenac with CoCl in the absence or presence of the nitrogen-donor ligands 2,2'-bipyridine, 1,10-phenanthroline, 2,2'-bipyridylamine, pyridine or imidazole resulted in the formation of six mononuclear Co(II) complexes. The complexes were characterized by diverse physicochemical and spectroscopic techniques and single-crystal X-ray crystallography revealing a monodentate or a bidentate chelating binding mode of the diclofenac ligands. The scavenging activity of the complexes was evaluated in vitro against the free radicals of 1,1-diphenyl-2-picrylhydrazyl, 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and hydroxyl; the complexes present significant scavenging activity of ABTS and hydroxyl radicals. Read More

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http://dx.doi.org/10.1016/j.jinorgbio.2019.04.002DOI Listing

Inactivation of NikR from Helicobacter pylori by a bismuth drug.

J Inorg Biochem 2019 Apr 8;196:110685. Epub 2019 Apr 8.

MOE Key Laboratory of Bioinorganic and Synthetic Chemistry, School of Chemistry, Sun Yat-sen University, Guangzhou, China, 510275. Electronic address:

The NikR protein is an essential DNA regulator of Helicobacter pylori, a human pathogen, which infects almost half of the world's population. Herein, we comprehensively characterized the interaction of a bismuth drug with Helicobacter pylori NikR. We show that Bi(III) can occupy the high-affinity Ni(II) site of NikR. Read More

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http://dx.doi.org/10.1016/j.jinorgbio.2019.03.025DOI Listing

Interaction of neurotransmitters and neurochemicals with lymphocytes.

J Neuroimmunol 2019 Apr 11;332:99-111. Epub 2019 Apr 11.

The University of Queensland Centre for Clinical Research, Royal Brisbane and Women's Hospital, Brisbane, Australia; Royal Brisbane and Women's Hospital, Herston, Brisbane, Australia. Electronic address:

Neurotransmitters and neurochemicals can act on lymphocytes by binding to receptors expressed by lymphocytes. This review describes lymphocyte expression of receptors for a selection of neurotransmitters and neurochemicals, the anatomical locations where lymphocytes can interact with neurotransmitters, and the effects of the neurotransmitters on lymphocyte function. Implications for health and disease are also discussed. Read More

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http://dx.doi.org/10.1016/j.jneuroim.2019.04.006DOI Listing

EEG changes in patients on antipsychotic therapy: A systematic review.

Epilepsy Behav 2019 Apr 15;95:1-9. Epub 2019 Apr 15.

Department of Neuroscience, Monash Medical Centre, Clayton, Victoria, Australia; School of Clinical Sciences at Monash Health, Department of Medicine, Monash University, Melbourne, Victoria, Australia; Department of Medicine, St. Vincent's Hospital, University of Melbourne, Melbourne, Australia. Electronic address:

Objectives: The objective of the study was to characterize the electroencephalogram (EEG) changes associated with different antipsychotic medications based on the evidence from the literature.

Methods: A systematic search of the databases Medline, PsycINFO, and PubMed was conducted. The Preferred Items Reporting for Systematic Reviews and Meta-Analyses (PRISMA) guidelines were followed in the construction of this systematic review. Read More

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http://dx.doi.org/10.1016/j.yebeh.2019.02.005DOI Listing

Current status of nanomaterial-based treatment for hepatocellular carcinoma.

Biomed Pharmacother 2019 Apr 15;116:108852. Epub 2019 Apr 15.

Departments of Biology, UAE University, Al Ain, United Arab Emirates. Electronic address:

Cancer continues to be the leading cause of death worldwide. Hepatocellular carcinoma (HCC), a prominent form of liver cancer, is the second leading cause of cancer-related deaths, thanks to the lack of efficient diagnostic tools and consequently late diagnosis and to the scarce of available suitable treatments. Thus, novel approaches to treat HCC are in demand. Read More

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http://dx.doi.org/10.1016/j.biopha.2019.108852DOI Listing

Synthesis and biological evaluation of purine-pyrazole hybrids incorporating thiazole, thiazolidinone or rhodanine moiety as 15-LOX inhibitors endowed with anticancer and antioxidant potential.

Bioorg Chem 2019 Apr 1;87:821-837. Epub 2019 Apr 1.

Genetic Engineering and Biotechnology Research Institute (GEBRI), City for Scientific Research and Technology, Alexandria, Egypt.

Novel purine-pyrazole hybrids combining thiazoles, thiazolidinones and rhodanines, were designed and tested as 15-LOX inhibitors, potential anticancer and antioxidant agents. All tested compounds were found to be potent 15-LOX inhibitors with IC ranging from 1.76 to 6. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.03.076DOI Listing

Akebia Saponin D inhibits the formation of atherosclerosis in ApoE mice by attenuating oxidative stress-induced apoptosis in endothelial cells.

Atherosclerosis 2019 Apr 10;285:23-30. Epub 2019 Apr 10.

Beijing Chao-Yang Hospital, Capital Medical University, Beijing, 100020, China. Electronic address:

Background And Aims: Akebia Saponin D (ASD) is a major bioactive triterpenoid saponin compound isolated from the Chinese herb Dipsacus asper wall (DSW). DSW has been long used as an anti-Alzheimer disease and anti-osteoporosis agent in clinics. However, anti-atherosclerotic effects of ASD have not been fully investigated. Read More

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http://dx.doi.org/10.1016/j.atherosclerosis.2019.04.202DOI Listing

Quantification of drugs encapsulated in liposomes by H NMR.

Colloids Surf B Biointerfaces 2019 Mar 31;179:414-420. Epub 2019 Mar 31.

Centre of Biological Engineering, University of Minho, Braga, Portugal. Electronic address:

Liposomes are one of the most important and extensively studied drug delivery system due to their ability to encapsulate different kinds of drugs. Exploiting the advantages of H Nuclear Magnetic Resonance (NMR) spectrometry, we established a rapid and easy method for quantification of drugs encapsulated in liposomes. An internal standard, pyridine, was used for quantitative determination of drug concentration. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09277765193018
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http://dx.doi.org/10.1016/j.colsurfb.2019.03.039DOI Listing
March 2019
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In-vitro blood and vascular compatibility of sirolimus-eluting organic/inorganic hybrid stent coatings.

Colloids Surf B Biointerfaces 2019 Apr 9;179:405-413. Epub 2019 Apr 9.

Research Institute of Advanced Manufacturing Technology, Korea Institute of Industrial Technology, Incheon, 21999, Republic of Korea. Electronic address:

The surface characteristics of coronary stents play a pivotal role in inhibiting in-stent restenosis and late-stent thrombosis. In this study, a sol-gel-derived silica xerogel-chitosan hybrid coating was applied to Co-Cr stent and was reported, for the first time, as a biocompatible drug delivery tool in vascular stent application. A dense and uniform chitosan-silica xerogel hybrid coating (<1-μm thick) was applied on bare Co-Cr material. Read More

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http://dx.doi.org/10.1016/j.colsurfb.2019.04.018DOI Listing

A novel oil-based suspension of a micro-environmental, pH-modifying solid dispersion for parenteral delivery: Formulation and stability evaluation.

Colloids Surf B Biointerfaces 2019 Apr 3;179:382-392. Epub 2019 Apr 3.

The Department of Veterinary Parasitology, College of Veterinary Medicine, China Agricultural University, Hai Dian District, Beijing, 100193, China. Electronic address:

The objective of this study was to evaluate a novel oil-based suspension as a potential parenteral drug delivery system for drugs with poor water solubility. Most of the new active pharmaceutical ingredients are weak acid or basic drugs with pH-dependent solubility. To limit this dependence, use of micro-environmental pH-modifying solid dispersions (micro pHm SD) has been proved to increase the bioavailability of these drugs. Read More

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http://dx.doi.org/10.1016/j.colsurfb.2019.04.001DOI Listing

MiR-219a-5p enhances cisplatin sensitivity of human non-small cell lung cancer by targeting FGF9.

Biomed Pharmacother 2019 Apr 15;114:108662. Epub 2019 Apr 15.

Department of Cardiothoracic Surgery, Hwamei Hospital, University of Chinese Academy Of Science , Ningbo, Zhejiang, China.

Cisplatin (DDP) resistance is a major obstacle in the treatment of non-small cell lung cancer (NSCLC). MicroRNA-219a-5p (miR-219a-5p) has been reported to be a tumor suppressor in several cancers, but whether it regulates chemosensitivity in NSCLC remains unclear. Here, using quantitative real time PCR analysis, we observed that miR-219a-5p was down-regulated in responding tumor tissues compared with that in non-responding tumor tissues from NSCLC patients received DDP-based chemotherapy. Read More

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http://dx.doi.org/10.1016/j.biopha.2019.108662DOI Listing

The impact of topical phenytoin loaded nanostructured lipid carriers in diabetic foot ulceration.

Foot (Edinb) 2019 Mar 14;40:14-21. Epub 2019 Mar 14.

Department of Diabetes and Endocrinology, Faculty of Medicine, Mansoura University, Mansoura 35516, Egypt. Electronic address:

Objective: The aim of this study is to develop, and characterize nanostructured lipid carriers (NLCs) of phenytoin (PHT) in order to improve its entrapment efficiency and sustained release to improve the healing process.

Methods: Twenty-seven patients with neuropathic diabetic foot ulceration (DFU) were enrolled in this study. Patients were comparable regarding size, grading of ulcer and control of diabetes with no major deformity. Read More

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http://dx.doi.org/10.1016/j.foot.2019.03.007DOI Listing

Repeated ketamine infusions for antidepressant-resistant PTSD: Methods of a multicenter, randomized, placebo-controlled clinical trial.

Contemp Clin Trials 2019 Apr 15. Epub 2019 Apr 15.

National Center for PTSD, Clinical Neurosciences Division, US Department of Veterans Affairs, West Haven, CT, USA; Department of Psychiatry, Yale University School of Medicine, New Haven, CT, USA. Electronic address:

Posttraumatic stress disorder (PTSD) is a debilitating disorder with limited medication treatment options. Recent reports have described the dearth of research on new drug development as a crisis in the pharmacotherapy of PTSD. There are only two PTSD medications approved by the U. Read More

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http://dx.doi.org/10.1016/j.cct.2019.04.009DOI Listing

Simultaneous assessment of compound activity on cardiac Nav1.5 peak and late currents in an automated patch clamp platform.

J Pharmacol Toxicol Methods 2019 Apr 15. Epub 2019 Apr 15.

Drug Safety Research and Development, Pfizer Inc., La Jolla, CA 92121, United States of America.

Introduction: High throughput in vitro profiling of the cardiac Nav1.5 peak sodium current (I) is widely used in cardiac safety screening. However, there is no standardized high throughput method to measure late I. Read More

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http://dx.doi.org/10.1016/j.vascn.2019.04.001DOI Listing

Inhalable co-amorphous budesonide-arginine dry powders prepared by spray drying.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Department of Pharmacy, University of Copenhagen, Universitetsparken 2, DK-2100, Copenhagen, Denmark; Wuya College of Innovation, Shenyang Pharmaceutical University, Wenhua Road 103, 110016, Shenyang, China. Electronic address:

Spray drying is a well-established technology to produce inhalable dry powders. However, the amorphous nature of the particles typically obtained from the process can lead to physically and chemically unstable products. The purpose of this study was to investigate whether spray-drying could be used as a manufacturing method to produce co-amorphous drug amino acid powders with high physical stability and inhalable particulate properties. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03785173193029
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http://dx.doi.org/10.1016/j.ijpharm.2019.04.036DOI Listing
April 2019
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Development and pharmacokinetics of a combination vaginal ring for sustained release of dapivirine and the protein microbicide 5P12-RANTES.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

School of Pharmacy, Queen's University Belfast, Belfast BT9 7BL, UK. Electronic address:

The past fifteen years have witnessed a resurgence of interest in vaginal ring technologies for drug delivery applications, mostly driven by the impetus for development of vaginally-administered antiretroviral microbicides to help reduce the high acquisition rates for human immunodeficiency virus (HIV) among Sub-Saharan African women. Currently, the lead candidate microbicide is a 28-day silicone elastomer vaginal ring releasing dapivirine (Ring-004), an experimental non-nucleoside reverse transcriptase inhibitor. The ring was tested in two pivotal Phase III clinical studies in 2016 and is currently undergoing review by the European Medicines Agency. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.040DOI Listing

Gold nanoparticles loaded with Cullin-5 DNA increase sensitivity to 17-AAG in Cullin-5 Deficient Breast Cancer Cells.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Department of Biological Sciences, Towson University, Towson, MD, United States. Electronic address:

HSP90 inhibitors have the potential to treat many types of cancer due to the dependence of tumor cells on HSP90 for cell growth and proliferation. The Cullin-5 (Cul5) E3 ubiquitin ligase is required for HSP90 inhibitors to induce client protein degradation and subsequent cell death. Cul5 is expressed at low levels in breast cancer cells compared to patient matched controls. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.022DOI Listing

Egg white coated alginate nanoparticles with electron sprayer for potential anticancer application.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Research Institute of Sun Yat-Sen University in Shenzhen, Shenzhen, 518057, PR China; Key Laboratory of Sensing Technology and Biomedical Instrument of Guangdong Province, School of Biomedical Engineering, Sun Yat-sen University, Guangzhou 510006, PR China. Electronic address:

To development biomimetic strategy for enhanced cancer therapy, the paclitaxel loaded egg white/sodium alginate nanoparticles were prepared by electronic spray method. Their appearance and particle size were observed by transmission electron microscope and particle size analyzer. The drug release behavior of nanoparticles was determined by high performance liquid chromatography (HPLC). Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.045DOI Listing

Formulation and processability screening for the rational design of ethylene-vinyl acetate based intra-vaginal rings.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Research Center Pharmaceutical Engineering GmbH, Inffeldgasse 13, 8010 Graz, Austria; Institute of Pharmaceutical Sciences, Department Pharmaceutical Technology and Biopharmacy, University of Graz, Universitaetsplatz 1, 8010 Graz, Austria. Electronic address:

The application of ethylene-vinyl acetate (EVA) copolymers in reservoir-type intra-vaginal rings (IVRs) offers advantages over silicones including i) versatile properties, ii) absence of curing chemistry, and iii) continuous and flexible processing via co-extrusion. Thus, we investigated the capability of EVA based IVRs to deliver broad ranges of estradiol (E2) thereby, fulfilling the requirements of local and systemic hormone replacement therapy (HRT) and contraception. To circumvent the high material needs associated with co-extrusion, we implemented a small-scale screening procedure that accurately predicts the E2 release from IVRs comprising E2 below its solubility concentration in the core. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.041DOI Listing

Post-irradiation recovery time strongly influences fractional laser-facilitated skin absorption.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Research Center for Food and Cosmetic Safety and Research Center for Chinese Herbal Medicine, Chang Gung University of Science and Technology, Kweishan, Taoyuan, Taiwan; Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan; Department of Anesthesiology, Chang Gung Memorial Hospital, Kweishan, Taoyuan, Taiwan. Electronic address:

Fractional CO laser treatment has been used in some clinical trials to promote topical drug delivery. Currently, there is no standard for laser settings to achieve a feasible therapy. The cutaneous recovery following laser treatment and its influence on drug absorption have not been well explored. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.043DOI Listing

Conjugal transfer of PMQR from uropathogenic E.coli under high ciprofloxacin selection pressure generates gyrA mutation.

Microb Pathog 2019 Apr 15. Epub 2019 Apr 15.

Department of Biochemistry and Medical Biotechnology, Calcutta School of Tropical Medicine, Kolkata, India. Electronic address:

Incidence of high fluoroquinolone resistance has been rising rapidly worldwide. Resistance against fluoroquinolones can be either chromosomal or plasmid mediated. Plasmid mediated quinolone resistant(PMQR) genes impart low level of resistance against fluoroquinolones but provides favorable background for selection of additional chromosomally encoded resistance mechanisms. Read More

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http://dx.doi.org/10.1016/j.micpath.2019.04.021DOI Listing

The historical development of pharmacopoeias and the inclusion of exotic herbal drugs with a focus on Europe and Brazil.

J Ethnopharmacol 2019 Apr 15:111891. Epub 2019 Apr 15.

Department of Biomedical Sciences, University of Cagliari, Via Ospedale 72, 09124, Cagliari, Italy. Electronic address:

Ethnopharmacological Relevance: In spite of the rich bio-cultural diversity found in the Neotropics relatively few herbal drugs native to South-America are included in the global pharmacopoeia.

Material And Methods: In the attempt to historically explain the inclusion of herbal drugs into official pharmacopoeias we consider the disparate epidemiology and cultural evolution of the New and the Old World. We then trace the development of pharmacopoeias and review forces that worked towards and against the synchronization of pharmacopoeias and highlight the role of early chemical and pharmacological studies in Europe. Read More

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http://dx.doi.org/10.1016/j.jep.2019.111891DOI Listing

Evaluation of the schistosomicidal, antioxidant and anti-inflammatory activities of the ethyl acetate fraction from Ozoroa pulcherrima Schweinf. Roots on Schistosoma mansoni-induced liver pathology in mice and its phytochemical characterization.

J Ethnopharmacol 2019 Apr 15:111883. Epub 2019 Apr 15.

Laboratory of Biology, Department of Animal Biology and Physiology, Faculty of Science, University of Yaoundé I, P.O. Box 812, Yaoundé, Cameroon; Centre for Schistosomiasis and Parasitology, P.O. Box 7244, Yaoundé, Cameroon. Electronic address:

Ethnopharmacological Relevance: Ozoroa pulcherrima Schweinf. (syn.: Heeria pulcherrrima Schweinf. Read More

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http://dx.doi.org/10.1016/j.jep.2019.111883DOI Listing

Anti-obesity effect of argel (Solenostemma argel) on obese rats fed a high fat diet.

J Ethnopharmacol 2019 Apr 15:111893. Epub 2019 Apr 15.

Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Egypt. Electronic address:

Ethnopharmacological Relevance: Solenostemma argel (Argel) is a desert plant commonly used in Egyptian and Sudanese traditional medicine to suppress appetite, for treatment of diabetes, and as antispasmodic and anti-inflammatory agents. Previously the anti-diabetic, hypolipidemic and lipase inhibitory activities of Argel were reported in animal studies and in-vitro assays. However, its specific mechanism of action as an anti-obesity agent has not been studied before. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03788741183492
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http://dx.doi.org/10.1016/j.jep.2019.111893DOI Listing
April 2019
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MPL nano-liposomal vaccine containing P5 HER2/neu-derived peptide pulsed PADRE as an effective vaccine in a mice TUBO model of breast cancer.

J Control Release 2019 Apr 15. Epub 2019 Apr 15.

Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Pharmaceutical Nanotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran. Electronic address:

Liposomal peptide-based vaccines can potentially suppress cancer cells proliferation in the host. To enhance the effectiveness of vaccination against cancer, additional strategies should also be employed. One strategy to promote peptide-based vaccine efficacy and induce powerful immune responses, is simultaneous activation of CD4 and CD8 T cells. Read More

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http://dx.doi.org/10.1016/j.jconrel.2019.04.019DOI Listing

Reconciliation of Recent Helicobacter pylori Treatment Guidelines in a Time of Increasing Resistance to Antibiotics.

Gastroenterology 2019 Apr 15. Epub 2019 Apr 15.

Department of Gastroenterology, Hepatology and infectious diseases, Otto-von-Guericke University, Magdeburg, Germany, and Ludwig Maximilian University Clinic, Med. Clinic II, Muenchen, Germany.

Increasing resistance to antibiotics, worldwide, has adverse effects on the effectiveness of standard therapies to eradicate Helicobacter pylori infection. We reviewed guidelines developed by expert groups in Europe, Canada, and the United States for the treatment of Helicobacter pylori infection. We compared the recommendations of these guidelines, reconciled them, and addressed the increasing resistance of H pylori to antibiotic therapy regimens. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00165085193570
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http://dx.doi.org/10.1053/j.gastro.2019.04.011DOI Listing
April 2019
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Dysregulation of Akt-FOXO1 pathway leads to dysfunction of regulatory T cells in psoriasis patients.

J Invest Dermatol 2019 Apr 15. Epub 2019 Apr 15.

Department of Dermatology, Xijing Hospital, Fourth Military Medical University, Xi'an, China. Electronic address:

Psoriasis is a T lymphocyte-driven systemic inflammatory disease. Regulatory T (Treg) cells are essential for establishing and maintaining immune tolerance. In this study, we found that the psoriatic patients and healthy controls had comparable percentages of circulating CD4CD25FOXP3 Treg cells, but psoriatic Treg cells had reduced suppressive function. Read More

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http://dx.doi.org/10.1016/j.jid.2018.12.035DOI Listing

Activation of the PP2A catalytic subunit by ivabradine attenuates the development of diabetic cardiomyopathy.

J Mol Cell Cardiol 2019 Apr 15. Epub 2019 Apr 15.

Department of Cardiology, Nanjing First Hospital, Nanjing Medical University, Nanjing, China. Electronic address:

Hyperglycemia-induced apoptosis plays a critical role in the pathogenesis of diabetic cardiomyopathy (DCM). Our previous study demonstrated that ivabradine, a selective I current antagonist, significantly attenuated myocardial apoptosis in diabetic mice, but the underlying mechanisms remained unknown. This study investigated the underlying mechanisms by which ivabradine exerts anti-apoptotic effects in experimental DCM. Read More

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http://dx.doi.org/10.1016/j.yjmcc.2019.04.011DOI Listing

The nanoscopic molecular pathway through human skin.

Biochim Biophys Acta Gen Subj 2019 Apr 15. Epub 2019 Apr 15.

Department of Biochemistry and Molecular Biology, University of Southern Denmark, Denmark. Electronic address:

Background: Knowledge regarding the barrier properties of human skin is important for understanding skin pathology, developing of transdermal drug delivery systems and computational skin absorption models; however, the molecular pathways through human skin remains to be fully investigated on a nanoscopic level. In particular the nanoscopic pathway of molecules passing the intercellular lipid bilayers separating the corneocytes in the stratum corneum (SC) is not fully elucidated.

Methods: Using stimulated emission depletion microscopy (STED) and Förster resonance energy transfer (FRET) the molecular pathways through the SC, the main barrier of the skin, are determined for lipophilic and water-soluble molecules at a nanoscopic resolution. Read More

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http://dx.doi.org/10.1016/j.bbagen.2019.04.012DOI Listing
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