804 results match your criteria Pharmaceuticals [Journal]


Inflammation and Depression: A Nervous Plea for Psychiatry to Not Become Immune to Interpretation.

Pharmaceuticals (Basel) 2019 Feb 14;12(1). Epub 2019 Feb 14.

Aquitaine Institute for Integrative and Cognitive Neuroscience (INCIA) UMR CNRS 5287, University of Bordeaux, 146 rue Léo Saignat, 33076 Bordeaux, France.

The possibility that inflammation plays a causal role in major depression is an important claim in the emerging field of immunopsychiatry and has generated hope for new treatments. The aims of the present review are first to provide some historical background and to consider the evidence in favor of the claim that inflammation is causally involved in major depression. The second part discusses some of the possibilities allowed for by the use of broad 'umbrella' concepts, such as inflammation and stress, in terms of proposing new working hypotheses and potential mechanisms. Read More

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http://dx.doi.org/10.3390/ph12010029DOI Listing
February 2019

Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson's Disease.

Pharmaceuticals (Basel) 2019 Feb 5;12(1). Epub 2019 Feb 5.

Department of Physiological Sciences, School of Medical Sciences, Santa Casa de Sao Paulo, Rua Cesario Mota Junior 61, Sao Paulo 01221-020, Brazil.

Parkinson's disease (PD) is a neurodegenerative disease characterized by the loss of dopaminergic neurons in the , leading to alteration of the integrity of dopaminergic transporters (DATs). In recent years, some radiopharmaceuticals have been used in the clinic to evaluate the integrity of DATs. These include tropane derivatives such as radiolabeled β-CIT and FP-CIT with iodine-123 (I), and TRODAT-1 with metastable technetium-99 (Tc). Read More

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http://dx.doi.org/10.3390/ph12010025DOI Listing
February 2019

Neurodegeneration with Brain Iron Accumulation Disorders: Valuable Models Aimed at Understanding the Pathogenesis of Iron Deposition.

Pharmaceuticals (Basel) 2019 Feb 9;12(1). Epub 2019 Feb 9.

Fondazione IRCCS Istituto Neurologico Carlo Besta, 20126 Milano, Italy.

Neurodegeneration with brain iron accumulation (NBIA) is a set of neurodegenerative disorders, which includes very rare monogenetic diseases. They are heterogeneous in regard to the onset and the clinical symptoms, while the have in common a specific brain iron deposition in the region of the basal ganglia that can be visualized by radiological and histopathological examinations. Nowadays, 15 genes have been identified as causative for NBIA, of which only two code for iron-proteins, while all the other causative genes codify for proteins not involved in iron management. Read More

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http://dx.doi.org/10.3390/ph12010027DOI Listing
February 2019

Curcumin and (-)- Epigallocatechin-3-Gallate Protect Murine MIN6 Pancreatic Beta-Cells Against Iron Toxicity and Erastin-Induced Ferroptosis.

Pharmaceuticals (Basel) 2019 Feb 6;12(1). Epub 2019 Feb 6.

Department of Nutritional Sciences, School of Life Course Sciences, King's College London. Franklin-Wilkins-Building, 150 Stamford Street, London, SE1 9NH, UK.

Ferroptosis is a form of programmed cell death that is characterized by lipid peroxidation and is inducible by iron and the accumulation of reactive oxygen species (ROS). It is triggered by erastin but inhibited by antioxidants such as -tocopherol, -carotene, polyphenols, and iron chelators such as deferoxamine (DFO), nitrilotriacetic acid (NTA), and ethylenediaminetetraacetic acid (EDTA). This study investigated the protective effects of two polyphenols, curcumin and (-)- epigallocatechin-3-gallate (EGCG), against iron loading and erastin-mediated ferroptosis in MIN6 cells. Read More

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http://dx.doi.org/10.3390/ph12010026DOI Listing
February 2019
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Camphor, Applied Epidermally to the Back, Causes Snout- and Chest-Grooming in Rats: A Response Mediated by Cutaneous TRP Channels.

Pharmaceuticals (Basel) 2019 Feb 2;12(1). Epub 2019 Feb 2.

Graduate Program in Neuroscience and Cognition, Federal University of ABC, São Bernardo do Campo 09606-070, SP, Brazil.

Thermoregulatory grooming, a behavioral defense against heat, is known to be driven by skin-temperature signals. Because at least some thermal cutaneous signals that drive heat defenses are likely to be generated by transient receptor potential (TRP) channels, we hypothesized that warmth-sensitive TRPs drive thermoregulatory grooming. Adult male Wistar rats were used. Read More

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http://dx.doi.org/10.3390/ph12010024DOI Listing
February 2019
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Modulators of Transient Receptor Potential (TRP) Channels as Therapeutic Options in Lung Disease.

Pharmaceuticals (Basel) 2019 Feb 1;12(1). Epub 2019 Feb 1.

Walther-Straub-Institute of Pharmacology and Toxicology, Member of the German Center for Lung Research(DZL), LMU Munich, Nussbaumstr. 26, D-80336 Munich, Germany.

The lungs are essential for gas exchange and serve as the gateways of our body to the external environment. They are easily accessible for drugs from both sides, the airways and the vasculature. Recent literature provides evidence for a role of Transient Receptor Potential (TRP) channels as chemosensors and essential members of signal transduction cascades in stress-induced cellular responses. Read More

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http://dx.doi.org/10.3390/ph12010023DOI Listing
February 2019
1 Read

Correction: Mateusz, S., et al. Iron Supplementation in Suckling Piglets: An Ostensibly Easy Therapy of Neonatal Iron Deficiency Anemia. Pharmaceuticals 2018, 11, 128.

Pharmaceuticals (Basel) 2019 Jan 29;12(1). Epub 2019 Jan 29.

Department of Molecular Biology, Institute of Genetics and Animal Breeding, Polish Academy of Sciences, Jastrzębiec, 05-552 Magdalenka, Poland.

The authors wish to make the following corrections to this paper [¹]: the term "liposomal" should be replaced with the term "sucrosomial" in the following places [... Read More

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http://dx.doi.org/10.3390/ph12010022DOI Listing
January 2019

On the Absolute Stereochemistry of Tolterodine: A Circular Dichroism Study.

Pharmaceuticals (Basel) 2019 Jan 26;12(1). Epub 2019 Jan 26.

Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Via Moruzzi 13, 56124 Pisa, Italy.

Tolterodine () is a potent muscarinic receptor antagonist used in the treatment of overactive urinary bladder (OAB) syndrome. Tolterodine is chiral and it was patented, and is currently marketed, as the l-tartrate salt of the ()-enantiomer. However, the existing literature does not offer an ultimate proof of a stereoselective mode of action of . Read More

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http://dx.doi.org/10.3390/ph12010021DOI Listing
January 2019

Identification of Potential Inhibitors from Pyriproxyfen with Insecticidal Activity by Virtual Screening.

Pharmaceuticals (Basel) 2019 Jan 25;12(1). Epub 2019 Jan 25.

Postgraduate Program in Biotechnology and Biodiversity-Network BIONORTE, Federal University of Amapá, Macapá, Amapá 68903-419, Brazil.

is the main vector of dengue fever transmission, yellow fever, Zika, and chikungunya in tropical and subtropical regions and it is considered to cause health risks to millions of people in the world. In this study, we search to obtain new molecules with insecticidal potential against via virtual screening. Pyriproxyfen was chosen as a template compound to search molecules in the database Zinc_Natural_Stock (ZNSt) with structural similarity using ROCS (rapid overlay of chemical structures) and EON (electrostatic similarity) software, and in the final search, the top 100 were selected. Read More

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http://dx.doi.org/10.3390/ph12010020DOI Listing
January 2019
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TRPV1 Inhibits the Ventilatory Response to Hypoxia in Adult Rats, but Not the CO₂-Drive to Breathe.

Pharmaceuticals (Basel) 2019 Jan 24;12(1). Epub 2019 Jan 24.

Department of Animal Morphology and Physiology, Faculty of Agricultural and Veterinarian Sciences, UNESP at Jaboticabal, Rod. Prof. Paulo Donato Castellane s/n, Jaboticabal SP 14870-000, Brazil.

Receptors of the transient receptor potential (TRP) channels superfamily are expressed in many tissues and have different physiological functions. However, there are few studies investigating the role of these channels in cardiorespiratory control in mammals. We assessed the role of central and peripheral TRPV1 receptors in the cardiorespiratory responses to hypoxia (10% O₂) and hypercapnia (7% CO₂) by measuring pulmonary ventilation ( V ˙ E ), heart rate (HR), mean arterial pressure (MAP) and body temperature (Tb) of male Wistar rats before and after intraperitoneal (AMG9810 [2. Read More

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http://dx.doi.org/10.3390/ph12010019DOI Listing
January 2019
2 Reads

[Lu]Lu-PSMA-617 Salivary Gland Uptake Characterized by Quantitative Autoradiography.

Pharmaceuticals (Basel) 2019 Jan 24;12(1). Epub 2019 Jan 24.

Department of Nuclear Medicine, University Medical Center Freiburg, Faculty of Medicine, University of Freiburg, 79106 Freiburg, Germany.

Irradiation of salivary glands remains the main dose-limiting side effect of therapeutic PSMA-inhibitors, especially when using alpha emitters. Thus, further advances in radiopharmaceutical design and therapy strategies are needed to reduce salivary gland uptake, thereby allowing the administration of higher doses and potentially resulting in improved response rates and better tumor control. As the uptake mechanism remains unknown, this work investigates the salivary gland uptake of [Lu]Lu-PSMA-617 by autoradiography studies on pig salivary gland tissue and on PSMA-overexpressing LNCaP cell membrane pellets. Read More

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http://dx.doi.org/10.3390/ph12010018DOI Listing
January 2019
4 Reads

L-Ferritin: One Gene, Five Diseases; from Hereditary Hyperferritinemia to Hypoferritinemia-Report of New Cases.

Pharmaceuticals (Basel) 2019 Jan 23;12(1). Epub 2019 Jan 23.

BloodGenetics SL, Esplugues de Llobregat, 08950 Barcelona, Spain.

Ferritin is a multimeric protein composed of light (L-ferritin) and heavy (H-ferritin) subunits that binds and stores iron inside the cell. A variety of mutations have been reported in the L-ferritin subunit gene ( gene) that cause the following five diseases: (1) hereditary hyperferritinemia with cataract syndrome (HHCS), (2) neuroferritinopathy, a subtype of neurodegeneration with brain iron accumulation (NBIA), (3) benign hyperferritinemia, (4) L-ferritin deficiency with autosomal dominant inheritance, and (5) L-ferritin deficiency with autosomal recessive inheritance. Defects in the gene lead to abnormally high levels of serum ferritin (hyperferritinemia) in HHCS and benign hyperferritinemia, while low levels (hypoferritinemia) are present in neuroferritinopathy and in autosomal dominant and recessive L-ferritin deficiency. Read More

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http://www.mdpi.com/1424-8247/12/1/17
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http://dx.doi.org/10.3390/ph12010017DOI Listing
January 2019
3 Reads

Can the Efficacy of [F]FDG-PET/CT in Clinical Oncology Be Enhanced by Screening Biomolecular Profiles?

Pharmaceuticals (Basel) 2019 Jan 23;12(1). Epub 2019 Jan 23.

Trinity Translational Medicine Institute, Department of Surgery, Trinity College Dublin, D08W9RT Dublin, Ireland.

Positron Emission Tomography (PET) is a functional imaging modality widely used in clinical oncology. Over the years the sensitivity and specificity of PET has improved with the advent of specific radiotracers, increased technical accuracy of PET scanners and incremental experience of Radiologists. However, significant limitations exist-most notably false positives and false negatives. Read More

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http://dx.doi.org/10.3390/ph12010016DOI Listing
January 2019
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Micellisation Mechanism and Behaviour of Soluplus®⁻Furosemide Micelles: Preformulation Studies of an Oral Nanocarrier-Based System.

Pharmaceuticals (Basel) 2019 Jan 19;12(1). Epub 2019 Jan 19.

Department of Pharmacy, University of Oslo, 0316 Oslo, Norway.

In this study, self-assembling Soluplus® micelles were examined for inherent properties. Through calorimetric analysis, the critical micelle concentration (CMC) could be determined at 25 and 37 °C, and the influence of three media (Milli-Q water, phosphate-buffered saline (PBS) with a pH of 7.4 and 0. Read More

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http://dx.doi.org/10.3390/ph12010015DOI Listing
January 2019
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Structural and In Vitro Functional Comparability Analysis of Altebrel™, a Proposed Etanercept Biosimilar: Focus on Primary Sequence and Glycosylation.

Pharmaceuticals (Basel) 2019 Jan 17;12(1). Epub 2019 Jan 17.

Mass Spectrometric Proteomics, Institute of Clinical Chemistry and Laboratory Medicine, Campus Forschung, N27 Raum 00.008, Universitätsklinikum Hamburg-Eppendorf, Martinistr. 52, 20246 Hamburg, Germany.

The demand for reliable comparability studies of biosimilars grows with their increased market share. These studies focus on physicochemical, structural, functional and clinical properties to ensure that a biosimilar has no significant differences to the originator product and can be released into the market without extensive clinical trials. In the current study, Enbrel (etanercept, the originator) and Altebrel™ (the proposed biosimilar) underwent direct comparison. Read More

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http://dx.doi.org/10.3390/ph12010014DOI Listing
January 2019
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Cholecystokinin-2 Receptor Targeting with Novel C-terminally Stabilized HYNIC-Minigastrin Analogs Radiolabeled with Technetium-99m.

Pharmaceuticals (Basel) 2019 Jan 15;12(1). Epub 2019 Jan 15.

Department of Nuclear Medicine, Medical University of Innsbruck, Anichstrasse 35, A-6020 Innsbruck, Austria.

The high overexpression of cholecystokinin-2 receptors (CCK2R) in tumors, such as medullary thyroid carcinoma, allows for highly specific diagnostic and therapeutic targeting with radiolabeled peptide probes derived from natural ligands for the receptor. Based on the ideal imaging characteristics, high availability and low cost of technetium-99m (Tc)-labeled radiopharmaceuticals we have developed two hydrazinonicotinic acid (HYNIC) conjugated minigastrin analogs allowing labeling at high specific activity. The CCK2R targeting peptide conjugates show specific amino acid substitutions in the C-terminal receptor-specific sequence with the aim to increase stability and tumor targeting. Read More

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http://www.mdpi.com/1424-8247/12/1/13
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http://dx.doi.org/10.3390/ph12010013DOI Listing
January 2019
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Optimization of the Automated Synthesis of [11C]mHED-Administered and Apparent Molar Activities.

Pharmaceuticals (Basel) 2019 Jan 14;12(1). Epub 2019 Jan 14.

Division of Nuclear Medicine, Department of Biomedical Imaging and Image-guided Therapy, Medical University of Vienna, 1090Vienna, Austria.

The tracer -Hydroxyephedrine ([[11C]HED) is one of the most applied PET tracers for cardiac imaging, whose radiosynthesis was already reported in 1990. While not stated in the literature, separation difficulties and an adequate formulation of the product are well known challenges in its production. Furthermore, the precursor (metaraminol) is also a substrate for the norepinephrine transporter, and can therefore affect the image quality. Read More

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http://dx.doi.org/10.3390/ph12010012DOI Listing
January 2019
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The Therapeutic Potential of Naringenin: A Review of Clinical Trials.

Pharmaceuticals (Basel) 2019 Jan 10;12(1). Epub 2019 Jan 10.

Zabol Medicinal Plants Research Center, Zabol University of Medical Sciences, Zabol 61615585, Iran.

Naringenin is a flavonoid belonging to flavanones subclass. It is widely distributed in several fruits, bergamot, tomatoes and other fruits, being also found in its glycosides form (mainly naringin). Several biological activities have been ascribed to this phytochemical, among them antioxidant, antitumor, antiviral, antibacterial, anti-inflammatory, antiadipogenic and cardioprotective effects. Read More

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http://www.mdpi.com/1424-8247/12/1/11
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http://dx.doi.org/10.3390/ph12010011DOI Listing
January 2019
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Juvenile Arthritis Patients Suffering from Chronic Inflammation Have Increased Activity of Both IDO and GTP-CH1 Pathways But Decreased BH4 Efficacy: Implications for Well-Being, Including Fatigue, Cognitive Impairment, Anxiety, and Depression.

Pharmaceuticals (Basel) 2019 Jan 8;12(1). Epub 2019 Jan 8.

Division of Pharmacology, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, Faculty of Science, Universities 99, 3584 CG Utrecht, The Netherlands.

Juvenile idiopathic arthritis (JIA) represents joint inflammation with an unknown cause that starts before the age of 16, resulting in stiff and painful joints. In addition, JIA patients often report symptoms of sickness behavior. Recent animal studies suggest that proinflammatory cytokines produce sickness behavior by increasing the activity of indoleamine-2,3-dioxygenase (IDO) and guanosinetriphosphate⁻cyclohydrolase-1 (GTP⁻CH1). Read More

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http://dx.doi.org/10.3390/ph12010009DOI Listing
January 2019
2 Reads

The Multi-Functional Calcium/Calmodulin Stimulated Protein Kinase (CaMK) Family: Emerging Targets for Anti-Cancer Therapeutic Intervention.

Pharmaceuticals (Basel) 2019 Jan 7;12(1). Epub 2019 Jan 7.

Priority Research Centre for Cancer Research, Innovation and Translation, School of Biomedical Sciences and Pharmacy, Hunter Medical Research Institute (HMRI) and University of Newcastle, Callaghan, NSW 2308, Australia.

The importance of Ca signalling in key events of cancer cell function and tumour progression, such as proliferation, migration, invasion and survival, has recently begun to be appreciated. Many cellular Ca-stimulated signalling cascades utilise the intermediate, calmodulin (CaM). The Ca/CaM complex binds and activates a variety of enzymes, including members of the multifunctional Ca/calmodulin-stimulated protein kinase (CaMK) family. Read More

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http://dx.doi.org/10.3390/ph12010008DOI Listing
January 2019
1 Read

Radioligands for Tropomyosin Receptor Kinase (Trk) Positron Emission Tomography Imaging.

Pharmaceuticals (Basel) 2019 Jan 3;12(1). Epub 2019 Jan 3.

Azrieli Centre for Neuro-Radiochemistry, Research Imaging Centre, Centre for Addiction and Mental Health, Toronto, ON M5T 1L8, Canada.

The tropomyosin receptor kinases family (TrkA, TrkB, and TrkC) supports neuronal growth, survival, and differentiation during development, adult life, and aging. TrkA/B/C downregulation is a prominent hallmark of various neurological disorders including Alzheimer's disease (AD). Abnormally expressed or overexpressed full-length or oncogenic fusion TrkA/B/C proteins were shown to drive tumorigenesis in a variety of neurogenic and non-neurogenic human cancers and are currently the focus of intensive clinical research. Read More

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http://www.mdpi.com/1424-8247/12/1/7
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http://dx.doi.org/10.3390/ph12010007DOI Listing
January 2019
6 Reads

Aptamer-Based Diagnostics and Therapeutics.

Authors:
Sarah Shigdar

Pharmaceuticals (Basel) 2019 Jan 2;12(1). Epub 2019 Jan 2.

School of Medicine Deakin University, Geelong, Victoria 3128, Australia.

Aptamers were first described almost 30 years ago, with the publication of three separate research papers describing how a randomized library of RNA sequences could be incubated with a target to find a sequence that specifically binds via van der Waals forces, covalent and hydrogen bonding, and not Watson Crick base pairing [... Read More

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http://dx.doi.org/10.3390/ph12010006DOI Listing
January 2019
2 Reads

Natural Compounds and Derivatives as Ser/Thr Protein Kinase Modulators and Inhibitors.

Pharmaceuticals (Basel) 2019 Jan 1;12(1). Epub 2019 Jan 1.

Department of Biochemistry and Molecular Biology, University of Southern Denmark, 5230 Odense M, Denmark.

The need for new drugs is compelling, irrespective of the disease. Focusing on medical problems in the Western countries, heart disease and cancer are at the moment predominant illnesses. Owing to the fact that ~90% of all 21,000 cellular proteins in humans are regulated by phosphorylation/dephosphorylation it is not surprising that the enzymes catalysing these reactions (i. Read More

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http://www.mdpi.com/1424-8247/12/1/4
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http://dx.doi.org/10.3390/ph12010004DOI Listing
January 2019
9 Reads

Iron Homeostasis in the Lungs-A Balance between Health and Disease.

Pharmaceuticals (Basel) 2019 Jan 1;12(1). Epub 2019 Jan 1.

Department of Pediatric Oncology, Hematology and Immunology, University of Heidelberg, 69120 Heidelberg, Germany.

A strong mechanistic link between the regulation of iron homeostasis and oxygen sensing is evident in the lung, where both systems must be properly controlled to maintain lung function. Imbalances in pulmonary iron homeostasis are frequently associated with respiratory diseases, such as chronic obstructive pulmonary disease and with lung cancer. However, the underlying mechanisms causing alterations in iron levels and the involvement of iron in the development of lung disorders are incompletely understood. Read More

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http://www.mdpi.com/1424-8247/12/1/5
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http://dx.doi.org/10.3390/ph12010005DOI Listing
January 2019
10 Reads

Development of [I]I-EOE-TPZ and [I]I-EOE-TPZMO: Novel Tirapazamine (TPZ)-Based Radioiodinated Pharmaceuticals for Application in Theranostic Management of Hypoxia.

Pharmaceuticals (Basel) 2019 Jan 1;12(1). Epub 2019 Jan 1.

Department of Oncology, Cross Cancer Institute, Faculty of Medicine and Dentistry, University of Alberta, 11560 University Avenue, Edmonton, AB T6G 1Z2, Canada.

: Benzotriazine-1,4-dioxides (BTDOs) such as tirapazamine (TPZ) and its derivatives act as radiosensitizers of hypoxic tissues. The benzotriazine-1-monoxide (BTMO) metabolite (SR 4317, TPZMO) of TPZ also has radiosensitizing properties, and via unknown mechanisms, is a potent enhancer of the radiosensitizing effects of TPZ. Unlike their 2-nitroimidazole radiosensitizer counterparts, radiolabeled benzotriazine oxides have not been used as radiopharmaceuticals for diagnostic imaging or molecular radiotherapy (MRT) of hypoxia. Read More

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http://www.mdpi.com/1424-8247/12/1/3
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http://dx.doi.org/10.3390/ph12010003DOI Listing
January 2019
5 Reads

Radiolabelled Aptamers for Theranostic Treatment of Cancer.

Pharmaceuticals (Basel) 2018 Dec 24;12(1). Epub 2018 Dec 24.

School of Medicine Deakin University, Geelong, Victoria 3128, Australia.

Cancer has a high incidence and mortality rate worldwide, which continues to grow as millions of people are diagnosed annually. Metastatic disease caused by cancer is largely responsible for the mortality rates, thus early detection of metastatic tumours can improve prognosis. However, a large number of patients will also present with micrometastasis tumours which are often missed, as conventional medical imaging modalities are unable to detect micrometastases due to the lack of specificity and sensitivity. Read More

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http://dx.doi.org/10.3390/ph12010002DOI Listing
December 2018
1 Read

Decrease of Antimicrobial Resistance through Polyelectrolyte-Coated Nanoliposomes Loaded with β-Lactam Drug.

Pharmaceuticals (Basel) 2018 Dec 23;12(1). Epub 2018 Dec 23.

Maestría en Formulación de Productos Químicos y Derivados, Facultad de Ciencias Naturales, Universidad Icesi, Calle 18 No. 122⁻135, Cali 760031, Colombia.

Currently, one of the greatest health challenges worldwide is the resistance to antibiotic drugs, which has led to the pursuit of new alternatives for the recovery of biological activity, where the use of different types of nano-systems has shown an interesting potential. In this study, we evaluated the antibiotic activity of a model drug (ampicillin) encapsulated within coated-nanoliposomes on strains of with different antibiotic-resistance degrees. Hence, liposomes were elaborated by the ethanol injection method and were coated with a cationic polymer (Eudragit E-100) through the layer-by-layer process. Read More

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http://dx.doi.org/10.3390/ph12010001DOI Listing
December 2018
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Dissipative Particle Dynamics Investigation of the Transport of Salicylic Acid through a Simulated In Vitro Skin Permeation Model.

Pharmaceuticals (Basel) 2018 Dec 5;11(4). Epub 2018 Dec 5.

School of Pharmacy, University of Wisconsin⁻Madison, 777 Highland Avenue, Madison, WI 53705, USA.

Permeation models are often used to determine diffusion properties of a drug through a membrane as it is released from a delivery system. In order to circumvent problematic in vivo studies, diffusion studies can be performed in vitro, using (semi-)synthetic membranes. In this study salicylic acid permeation was studied, employing a nitrocellulose membrane. Read More

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http://dx.doi.org/10.3390/ph11040134DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316323PMC
December 2018
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Differential Scanning Calorimetry Analyses of Idebenone-Loaded Solid Lipid Nanoparticles Interactions with a Model of Bio-Membrane: A Comparison with In Vitro Skin Permeation Data.

Pharmaceuticals (Basel) 2018 Dec 16;11(4). Epub 2018 Dec 16.

Department of Drug Sciences, University of Catania, V.le A. Doria 6, 95125 Catania, Italy.

Differential scanning calorimetry (DSC) has emerged as a helpful technique both to characterize drug delivery systems and to study their interactions with bio-membranes. In this work, we compared idebenone (IDE)-loaded solid lipid nanoparticle (SLN) interactions with bio-membranes assessed by DSC with previous in vitro skin penetration data to evaluate the feasibility of predicting IDE skin penetration using DSC analyses. In vitro interactions experiments were performed using multi-lamellar liposomes as a model of bio-membrane. Read More

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http://dx.doi.org/10.3390/ph11040138DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316718PMC
December 2018
2 Reads

Iron Regulation: Macrophages in Control.

Pharmaceuticals (Basel) 2018 Dec 14;11(4). Epub 2018 Dec 14.

Medical University of Vienna, Center for Pathobiochemistry and Genetics, Vienna 1090, Austria.

Macrophages are sentinel cells of the innate immune system and have important functions in development, tissue homeostasis, and immunity. These phylogenetically ancient cells also developed a variety of mechanisms to control erythropoiesis and the handling of iron. Red pulp macrophages in the spleen, Kupffer cells in the liver, and central nurse macrophages in the bone marrow ensure a coordinated metabolism of iron to support erythropoiesis. Read More

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http://dx.doi.org/10.3390/ph11040137DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316009PMC
December 2018
1 Read

Synthesis and Initial In Vivo Evaluation of [C]AZ683-A Novel PET Radiotracer for Colony Stimulating Factor 1 Receptor (CSF1R).

Pharmaceuticals (Basel) 2018 Dec 13;11(4). Epub 2018 Dec 13.

Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA.

Positron emission tomography (PET) imaging of Colony Stimulating Factor 1 Receptor (CSF1R) is a new strategy for quantifying both neuroinflammation and inflammation in the periphery since CSF1R is expressed on microglia and macrophages. AZ683 has high affinity for CSF1R (K = 8 nM; IC = 6 nM) and >250-fold selectivity over 95 other kinases. In this paper, we report the radiosynthesis of [C]AZ683 and initial evaluation of its use in CSF1R PET. Read More

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http://dx.doi.org/10.3390/ph11040136DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316681PMC
December 2018
1 Read

Established and Emerging Concepts to Treat Imbalances of Iron Homeostasis in Inflammatory Diseases.

Pharmaceuticals (Basel) 2018 Dec 11;11(4). Epub 2018 Dec 11.

Department of Internal Medicine II, Medical University of Innsbruck, 6020 Innsbruck, Austria.

Inflammation, being a hallmark of many chronic diseases, including cancer, inflammatory bowel disease, rheumatoid arthritis, and chronic kidney disease, negatively affects iron homeostasis, leading to iron retention in macrophages of the mononuclear phagocyte system. Functional iron deficiency is the consequence, leading to anemia of inflammation (AI). Iron deficiency, regardless of anemia, has a detrimental impact on quality of life so that treatment is warranted. Read More

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http://www.mdpi.com/1424-8247/11/4/135
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http://dx.doi.org/10.3390/ph11040135DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6315795PMC
December 2018
10 Reads

Functional Polymer Nanocarriers for Photodynamic Therapy.

Pharmaceuticals (Basel) 2018 Nov 30;11(4). Epub 2018 Nov 30.

CAS Key Laboratory of Soft Matter Chemistry, iChEM, and Department of Chemical Physics, University of Science and Technology of China, Hefei 230026, China.

Photodynamic therapy (PDT) is an appealing therapeutic modality in management of some solid tumors and other diseases for its minimal invasion and non-systemic toxicity. However, the hydrophobicity and non-selectivity of the photosensitizers, inherent serious hypoxia of tumor tissues and limited penetration depth of light restrict PDT further applications in clinic. Functional polymer nanoparticles can be used as a nanocarrier for accurate PDT. Read More

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http://dx.doi.org/10.3390/ph11040133DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6315651PMC
November 2018
1 Read

Evaluation of Radiolabeled Girentuximab In Vitro and In Vivo.

Pharmaceuticals (Basel) 2018 Nov 28;11(4). Epub 2018 Nov 28.

Clinic for Nuclear Medicine, University Medical Center Mainz, 55131 Mainz, Germany.

Girentuximab (cG250) targets carbonic anhydrase IX (CAIX), a protein which is expressed on the surface of most renal cancer cells (RCCs). cG250 labeled with Lu has been used in clinical trials for radioimmunotherapy (RIT) of RCCs. In this work, an extensive characterization of the immunoconjugates allowed optimization of the labeling conditions with Lu while maintaining immunoreactivity of cG250, which was then investigated in in vitro and in vivo experiments. Read More

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http://dx.doi.org/10.3390/ph11040132DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316122PMC
November 2018
12 Reads

Iron as a Therapeutic Target in -Related Hemochromatosis: Usual and Novel Aspects.

Pharmaceuticals (Basel) 2018 Nov 26;11(4). Epub 2018 Nov 26.

INSERM, Univ Rennes, INRA, CHU Rennes, Institut NUMECAN (Nutrition Metabolisms and Cancer), F-35033 Rennes, France.

Genetic hemochromatosis is an iron overload disease that is mainly related to the mutation in the gene. This gene controls the expression of hepcidin, a peptide secreted in plasma by the liver and regulates systemic iron distribution. Homozygous mutation induces hepcidin deficiency, leading to increased circulating transferrin saturation, and ultimately, iron accumulation in organs such as the liver, pancreas, heart, and bone. Read More

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http://www.mdpi.com/1424-8247/11/4/131
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http://dx.doi.org/10.3390/ph11040131DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6315470PMC
November 2018
8 Reads

D.C. Hydroalcoholic Extract Promotes Anti-Cytotoxic and Antitumor Activity.

Pharmaceuticals (Basel) 2018 Nov 23;11(4). Epub 2018 Nov 23.

Laboratório de Genética Vegetal e Toxicológica, Departamento de Ciências Biológicas, Universidade Federal do Espírito Santo, Vitória 29075-910, Brazil.

D.C. (mandacaru) is a cactus used as food and in the traditional medicine. Read More

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http://www.mdpi.com/1424-8247/11/4/130
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http://dx.doi.org/10.3390/ph11040130DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316405PMC
November 2018
10 Reads

Brain Iron Homeostasis: A Focus on Microglial Iron.

Pharmaceuticals (Basel) 2018 Nov 23;11(4). Epub 2018 Nov 23.

Department of Genetics and Complex Diseases, Harvard TH Chan School of Public Health, Boston, MA 02115, USA.

Iron is an essential trace element required for important brain functions including oxidative metabolism, synaptic plasticity, myelination, and the synthesis of neurotransmitters. Disruptions in brain iron homeostasis underlie many neurodegenerative diseases. Increasing evidence suggests that accumulation of brain iron and chronic neuroinflammation, characterized by microglia activation and secretion of proinflammatory cytokines, are hallmarks of neurodegenerative disorders including Alzheimer' s disease. Read More

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http://www.mdpi.com/1424-8247/11/4/129
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http://dx.doi.org/10.3390/ph11040129DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316365PMC
November 2018
10 Reads

Hepcidin Therapeutics.

Pharmaceuticals (Basel) 2018 Nov 21;11(4). Epub 2018 Nov 21.

Lady Davis Institute for Medical Research, Jewish General Hospital, Department of Medicine, McGill University, Montreal, QC H3T 1E2, Canada.

Hepcidin is a key hormonal regulator of systemic iron homeostasis and its expression is induced by iron or inflammatory stimuli. Genetic defects in iron signaling to hepcidin lead to "hepcidinopathies" ranging from hereditary hemochromatosis to iron-refractory iron deficiency anemia, which are disorders caused by hepcidin deficiency or excess, respectively. Moreover, dysregulation of hepcidin is a pathogenic cofactor in iron-loading anemias with ineffective erythropoiesis and in anemia of inflammation. Read More

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http://dx.doi.org/10.3390/ph11040127DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316648PMC
November 2018
6 Reads

Iron Supplementation in Suckling Piglets: An Ostensibly Easy Therapy of Neonatal Iron Deficiency Anemia.

Pharmaceuticals (Basel) 2018 Nov 22;11(4). Epub 2018 Nov 22.

Department of Molecular Biology, Institute of Genetics and Animal Breeding, Polish Academy of Sciences, Jastrzębiec, 05-552 Magdalenka, Poland.

In pigs, iron deficiency anemia (IDA) is the most prevalent deficiency disorder during the early postnatal period, frequently developing into a serious illness. On the other hand, in humans, only low-birth-weight infants, including premature infants, are especially susceptible to developing IDA. In both human and pig neonates, the initial cause of IDA is low birth iron stores. Read More

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http://dx.doi.org/10.3390/ph11040128DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6315738PMC
November 2018
2 Reads

Effects of Roxb. and L. in an In Vitro Intestinal Inflammation Model Using Immune Cells and Caco-2.

Pharmaceuticals (Basel) 2018 Nov 20;11(4). Epub 2018 Nov 20.

Department of Physical Sciences, Hearth and Environment, University of Siena, Via Laterina 8, 53100 Siena, Italy.

Inflammatory bowel diseases, which consist of chronic inflammatory conditions of the colon and the small intestine, are considered a global disease of our modern society. Recently, the interest toward the use of herbal therapies for the management of inflammatory bowel diseases has increased because of their effectiveness and favourable safety profile, compared to conventional drugs. Roxb. Read More

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http://dx.doi.org/10.3390/ph11040126DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316569PMC
November 2018
9 Reads

TRPM8 Channels and Dry Eye.

Pharmaceuticals (Basel) 2018 Nov 15;11(4). Epub 2018 Nov 15.

Department of Ophthalmology, Chonnam National University Medical School and Hospital, Gwangju 61469, Korea.

Transient receptor potential (TRP) channels transduce signals of chemical irritation and temperature change from the ocular surface to the brain. Dry eye disease (DED) is a multifactorial disorder wherein the eyes react to trivial stimuli with abnormal sensations, such as dryness, blurring, presence of foreign body, discomfort, irritation, and pain. There is increasing evidence of TRP channel dysfunction (i. Read More

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http://www.mdpi.com/1424-8247/11/4/125
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http://dx.doi.org/10.3390/ph11040125DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316058PMC
November 2018
8 Reads

Emerging and Dynamic Biomedical Uses of Ferritin.

Pharmaceuticals (Basel) 2018 Nov 13;11(4). Epub 2018 Nov 13.

Department of Neurosurgery, Penn State College of Medicine, Hershey, PA 17033, USA.

Ferritin, a ubiquitously expressed protein, has classically been considered the main iron cellular storage molecule in the body. Owing to the ferroxidase activity of the H-subunit and the nucleation ability of the L-subunit, ferritin can store a large amount of iron within its mineral core. However, recent evidence has demonstrated a range of abilities of ferritin that extends well beyond the scope of iron storage. Read More

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http://dx.doi.org/10.3390/ph11040124DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316788PMC
November 2018
1 Read

TNBC Challenge: Oligonucleotide Aptamers for New Imaging and Therapy Modalities.

Pharmaceuticals (Basel) 2018 Nov 13;11(4). Epub 2018 Nov 13.

Istituto per l'Endocrinologia e l'Oncologia Sperimentale G. Salvatore (IEOS), CNR, 80145 Naples, Italy.

Compared to other breast cancers, triple-negative breast cancer (TNBC) usually affects younger patients, is larger in size, of higher grade and is biologically more aggressive. To date, conventional cytotoxic chemotherapy remains the only available treatment for TNBC because it lacks expression of the estrogen receptor (ER), progesterone receptor (PR) and epidermal growth factor receptor 2 (HER2), and no alternative targetable molecules have been identified so far. The high biological and clinical heterogeneity adds a further challenge to TNBC management and requires the identification of new biomarkers to improve detection by imaging, thus allowing the specific treatment of each individual TNBC subtype. Read More

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http://dx.doi.org/10.3390/ph11040123DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316260PMC
November 2018
4 Reads

Single-Blind Placebo-Controlled Response Test with Phenytoin 10% Cream in Neuropathic Pain Patients.

Pharmaceuticals (Basel) 2018 Nov 12;11(4). Epub 2018 Nov 12.

Institute for Neuropathic Pain, Spoorlaan 2a, 3735 MV Bosch en Duin, The Netherlands.

Background: Phenytoin cream applied topically has been explored in neuropathic pain conditions. In several case series, phenytoin 5% and 10% cream could reduce pain in a clinically relevant way with a fast onset of action within 30 min, and with positive effects on sleep.

Objective: To evaluate a single-blind placebo-controlled response test (SIBRET) for use in clinical practice. Read More

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http://www.mdpi.com/1424-8247/11/4/122
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http://dx.doi.org/10.3390/ph11040122DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316219PMC
November 2018
11 Reads

Antidiabetic Drugs in NAFLD: The Accomplishment of Two Goals at Once?

Pharmaceuticals (Basel) 2018 Nov 8;11(4). Epub 2018 Nov 8.

Sezione di Gastroenterologia e Epatologia, DiBiMIS, University of Palermo, 90127 Palermo, Italy.

Non-Alcoholic Fatty Liver Disease (NAFLD) is the most common cause of chronic liver disease in Western countries, accounting for 20⁻30% of general population and reaching a prevalence of 55% in patients with type 2 diabetes mellitus (T2DM). Insulin resistance plays a key role in pathogenic mechanisms of NAFLD. Many drugs have been tested but no medications have yet been approved. Read More

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http://www.mdpi.com/1424-8247/11/4/121
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http://dx.doi.org/10.3390/ph11040121DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316860PMC
November 2018
14 Reads

Reductive Mobilization of Iron from Intact Ferritin: Mechanisms and Physiological Implication.

Pharmaceuticals (Basel) 2018 Nov 5;11(4). Epub 2018 Nov 5.

Department of Chemistry & Biomolecular Science, Clarkson University, Potsdam, NY 13699, USA.

Ferritins are highly conserved supramolecular protein nanostructures composed of two different subunit types, H (heavy) and L (light). The two subunits co-assemble into a 24-subunit heteropolymer, with tissue specific distributions, to form shell-like protein structures within which thousands of iron atoms are stored as a soluble inorganic ferric iron core. In-vitro (or in cell free systems), the mechanisms of iron(II) oxidation and formation of the mineral core have been extensively investigated, although it is still unclear how iron is loaded into the protein in-vivo. Read More

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http://www.mdpi.com/1424-8247/11/4/120
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http://dx.doi.org/10.3390/ph11040120DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6315955PMC
November 2018
7 Reads

Design, Synthesis, Experimental and Theoretical Characterization of a New Multitarget 2-Thienyl--Acylhydrazone Derivative.

Pharmaceuticals (Basel) 2018 Nov 1;11(4). Epub 2018 Nov 1.

Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio), Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, P.O. Box 68023, Rio de Janeiro 21941-902, RJ, Brazil.

Pulmonary arterial hypertension (PAH) is a chronic cardiovascular disease that displays inflammatory components, which contributes to the difficulty of adequate treatment with the available therapeutic arsenal. In this context, the -acylhydrazone derivative LASSBio-1359 was previously described as a multitarget drug candidate able to revert the events associated with the progression of PAH in animal models. However, in spite of having a dual profile as PDE4 inhibitor and adenosine A receptor agonist, LASSBio-1359 does not present balanced potencies in the modulation of these two targets, which difficult its therapeutic use. Read More

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http://www.mdpi.com/1424-8247/11/4/119
Publisher Site
http://dx.doi.org/10.3390/ph11040119DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316713PMC
November 2018
13 Reads

Lipid Nanoparticles and Their Hydrogel Composites for Drug Delivery: A Review.

Pharmaceuticals (Basel) 2018 Nov 1;11(4). Epub 2018 Nov 1.

CEA LETI MlNATEC Campus, University Grenoble Alpes, F-38000 Grenoble, France.

Several drug delivery systems already exist for the encapsulation and subsequent release of lipophilic drugs that are well described in the scientific literature. Among these, lipid nanoparticles (LNP) have specifically come up for dermal, transdermal, mucosal, intramuscular and ocular drug administration routes in the last twenty years. However, for some of them (especially dermal, transdermal, mucosal), the LNP aqueous dispersions display unsuitable rheological properties. Read More

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http://dx.doi.org/10.3390/ph11040118DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6315535PMC
November 2018
2 Reads

Variation in Prescription Opioid Dispensing across Neighborhoods of Diverse Socioeconomic Disadvantages in Victoria, Australia.

Pharmaceuticals (Basel) 2018 Nov 1;11(4). Epub 2018 Nov 1.

Health Information Management, School of Psychology and Public Health, La Trobe University, Melbourne, Victoria 3086, Australia.

The study examined the relationship between dispensing patterns of prescription opioids, neighborhood-disadvantage-index, and standardized doses dispensed. Three-year's dispensing data drawn from 80 local government areas (LGAs) within Victoria, Australia's second most populous state, was analyzed. Quantities dispensed in defined daily dose (DDD)/1000-people/day were computed for LGAs of low, moderate, high, and very high socio-economic disadvantage. Read More

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http://dx.doi.org/10.3390/ph11040116DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6315505PMC
November 2018
1 Read

TRPA1 Antagonists for Pain Relief.

Pharmaceuticals (Basel) 2018 Nov 1;11(4). Epub 2018 Nov 1.

Department of Physiology, Faculty of Medicine, (Haartmaninkatu 8) POB 63, University of Helsinki, 00014 Helsinki, Finland.

Here, we review the literature assessing the role of transient receptor potential ankyrin 1 (TRPA1), a calcium-permeable non-selective cation channel, in various types of pain conditions. In the nervous system, TRPA1 is expressed in a subpopulation of nociceptive primary sensory neurons, astroglia, oligodendrocytes and Schwann cells. In peripheral terminals of nociceptive primary sensory neurons, it is involved in the transduction of potentially harmful stimuli and in their central terminals it is involved in amplification of nociceptive transmission. Read More

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https://www.mdpi.com/1424-8247/11/4/117/pdf
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http://www.mdpi.com/1424-8247/11/4/117
Publisher Site
http://dx.doi.org/10.3390/ph11040117DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316422PMC
November 2018
20 Reads