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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/28533680/preparation-characterization-and-in-vitro-vivo-studies-of-oleanolic-acid-loaded-lactoferrin-nanoparticles
#1
Xiaojing Xia, Haowei Liu, Huixia Lv, Jing Zhang, Jianping Zhou, Zhiying Zhao
Oleanolic acid (OA), a pentacyclic triterpene, is used to safely and economically treat hepatopathy. However, OA, a Biopharmaceutics Classification System IV category drug, has low bioavailability owing to low solubility (<1 μg/mL) and biomembrane permeability. We developed a novel OA nanoparticle (OA-NP)-loaded lactoferrin (Lf) nanodelivery system with enhanced in vitro OA dissolution and improved oral absorption and bioavailability. The OA-NPs were prepared using NP albumin-bound technology and characterized using dynamic light scattering, scanning electron microscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro dissolution test...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28533679/effect-of-epigallocatechin-3-gallate-major-ingredient-of-green-tea-on-the-pharmacokinetics-of-rosuvastatin-in-healthy-volunteers
#2
Tae-Eun Kim, Na Ha, Yunjeong Kim, Hyunsook Kim, Jae Wook Lee, Ji-Young Jeon, Min-Gul Kim
Previous in vitro studies have demonstrated the inhibitory effect of green tea on drug transporters. Because rosuvastatin, a lipid-lowering drug widely used for the prevention of cardiovascular events, is a substrate for many drug transporters, there is a possibility that there is interaction between green tea and rosuvastatin. The aim of this study was to investigate the effect of green tea on the pharmacokinetics of rosuvastatin in healthy volunteers. An open-label, three-treatment, fixed-sequence study was conducted...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28507428/propranolol-therapy-for-infantile-hemangioma-our-experience
#3
Ling Zhang, Hai-Wei Wu, Weien Yuan, Jia-Wei Zheng
OBJECTIVE: Hemangiomas are the most common benign vascular tumors of infancy. Although most infantile hemangiomas (IHs) have the ability to involute spontaneously after initial proliferation and resolve without consequence, intervention is required in a subset of IHs, which develop complications resulting in ulceration, bleeding, or aesthetic deformity. The primary treatment for this subset of IHs is pharmacological intervention, and propranolol has become the new first-line treatment for complicated hemangiomas...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28496309/effect-of-electromagnetic-fields-and-antioxidants-on-the-trace-element-content-of-rat-teeth
#4
Mehmet Sinan Dogan, Mehmet Cihan Yavas, Yasemin Yavuz, Sait Erdogan, İsmail Yener, İbrahim Simsek, Zeki Akkus, Veysel Eratilla, Abdulsamet Tanik, Mehmet Zulkuf Akdag
The purpose of this study was to examine the possible effect of extremely low-frequency electromagnetic fields (ELF-EMFs), from a high-voltage source, on rat teeth in terms of changes in trace elements (TEs) and the effect of antioxidants (melatonin [MLT] and Ganoderma lucidum [GL]) in counteracting these effects. We used adult male Wistar albino rats with a mean weight of 250-300 g and divided the rats into eight groups. The groups were subjected to an ELF-EMF that was applied with a high-voltage line for 8 hours/day for 26 days (Groups I, II, and III) or 52 days (Groups V, VI, and VII)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28496308/atorvastatin-a-double-weapon-in-osteoporosis-treatment-an-experimental-and-clinical-study
#5
Naglaa El-Nabarawi, Mohamed El-Wakd, Mostafa Salem
OBJECTIVE: The aim of this study was to evaluate the effect of atorvastatin on the bone formation and resorption markers in ovariectomized rats (experimental study), and to study its effect on the bone mineral density (BMD) in postmenopausal osteoporotic women (clinical study). MATERIALS AND METHODS: The study involved experimental and clinical aspects. In the experimental aspect, 42 female Wistar rats were divided into five groups: Group I (n=6; sham-operated), Group II (n=6; 1 mL of carboxymethyl cellulose [CMC] was administered orally), Group III (n=6; 20 mg/kg orally of atorvastatin was administered), Group IV (n=12; untreated ovariectomized [OVX] rats and served as a model of osteoporosis [OP]) and Group V (n=12; 20 mg/kg orally of atorvastatin was administered to ovariectomized rats)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28496307/developing-selective-histone-deacetylases-hdacs-inhibitors-through-ebselen-and-analogs
#6
Yuren Wang, Jason Wallach, Stephanie Duane, Yuan Wang, Jianghong Wu, Jeffrey Wang, Adeboye Adejare, Haiching Ma
Histone deacetylases (HDACs) are key regulators of gene expression in cells and have been investigated as important therapeutic targets for cancer and other diseases. Different subtypes of HDACs appear to play disparate roles in the cells and are associated with specific diseases. Therefore, substantial effort has been made to develop subtype-selective HDAC inhibitors. In an effort to discover existing scaffolds with HDAC inhibitory activity, we screened a drug library approved by the US Food and Drug Administration and a National Institutes of Health Clinical Collection compound library in HDAC enzymatic assays...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28496306/erratum-combined-letrozole-and-clomiphene-versus-letrozole-and-clomiphene-alone-in-infertile-patients-with-polycystic-ovary-syndrome-erratum
#7
(no author information available yet)
[This corrects the article on p. 1427 in vol. 7.][This corrects the article on p. 1427 in vol. 7.].
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28496305/methanol-leaf-extract-of-actinodaphne-sesquipedalis-lauraceae-enhances-gastric-defense-against-ethanol-induced-ulcer-in-rats
#8
Hanita Omar, Noraziah Nordin, Pouya Hassandarvish, Maryam Hajrezaie, Ainnul Hamidah Syahadah Azizan, Mehran Fadaeinasab, Nazia Abdul Majid, Mahmood Ameen Abdulla, Najihah Mohd Hashim, Hapipah Mohd Ali
Actinodaphne sesquipedalis Hook. F. Var. Glabra (Kochummen), also known as "Medang payung" by the Malay people, belongs to the Lauraceae family. In this study, methanol leaf extract of A. sesquipedalis was investigated for their acute toxicity and gastroprotective effects to reduce ulcers in rat stomachs induced by ethanol. The rats were assigned to one of five groups: normal group (group 1), ulcer group (group 2), control positive drug group (group 3) and two experimental groups treated with 150 mg/kg (group 4) and 300 mg/kg (group 5) of leaf extract...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28496304/evaluation-of-the-antitumor-activity-of-nov202-a-novel-microtubule-targeting-and-vascular-disrupting-agent
#9
Linda Rickardson, Emma Kutvonen, Satu Orasniemi, Marita Högberg, Marko J Kallio, Stefan Rehnmark
PURPOSE: Overall, ~65% of patients diagnosed with advanced ovarian cancer (OC) will relapse after primary surgery and adjuvant first-line platinum- and taxane-based chemotherapy. Significant improvements in the treatment of OC are expected from the development of novel compounds having combined cytotoxic and antiangiogenic properties that make them effective on refractory tumors. METHODS: Permeability of NOV202 was determined with Caco-2 monolayer assay. The compound's pharmacokinetic profile and plasma:brain distribution were assessed in male C57Bl/6 mice...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28490863/development-and-evaluation-of-a-new-modular-nanotransporter-for-drug-delivery-into-nuclei-of-pathological-cells-expressing-folate-receptors
#10
Tatiana A Slastnikova, Andrey A Rosenkranz, Yuri V Khramtsov, Tatiana S Karyagina, Sergey A Ovechko, Alexander S Sobolev
PURPOSE: Modular nanotransporters (MNTs) are artificial multifunctional systems designed to facilitate receptor-specific transport from the cell surface into the cell nucleus through inclusion of polypeptide domains for accomplishing receptor binding and internalization, as well as sequential endosomal escape and nuclear translocation. The objective of this study was to develop a new MNT targeted at folate receptors (FRs) for precise delivery of therapeutic cargo to the nuclei of FR-positive cells and to evaluate its potential, particularly for delivery of therapeutic agents (eg, the Auger electron emitter (111)In) into the nuclei of target cancer cells...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28479852/a-first-in-human-double-blind-placebo-controlled-randomized-dose-escalation-study-of-dwp05195-a-novel-trpv1-antagonist-in-healthy-volunteers
#11
Jieon Lee, Bo-Hyung Kim, Kyung-Sang Yu, Hee Sun Kim, Ji Duck Kim, Joo-Youn Cho, SeungHwan Lee, Namyi Gu
OBJECTIVES: DWP05195 is a transient receptor potential vanilloid 1 (TRPV1) antagonist developed for managing pain. The purpose of this study was to evaluate the pharmacodynamics pharmacokinetics, safety, and tolerability of DWP05195 in healthy subjects. This was a first-in-human randomized, double-blinded, placebo-controlled, dose escalation study. SUBJECTS AND METHODS: DWP05195 or placebo was administered as a single dose of 10-600 mg in the single-dose study and as 100-400 mg once daily for 8 days in the multiple-dose studies...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28479851/proton-pump-inhibitors-use-and-risk-of-acute-kidney-injury-a-meta-analysis-of-observational-studies
#12
Yi Yang, Kaisha C George, Wei-Feng Shang, Rui Zeng, Shu-Wang Ge, Gang Xu
BACKGROUND: Recent studies have suggested a potential increased risk of acute kidney injury (AKI) among proton-pump inhibitor (PPI) users. However, the present results are conflicting. Thus, we performed a meta-analysis to investigate the association between PPI therapy and the risk of AKI. METHODS: EMBASE, PubMed, Web of Science, and Cochrane Library databases (up to September 23, 2016) were systematically searched for any studies assessing the relationship between PPI use and risk of AKI...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28461741/functional-characterization-of-wild-type-and-24-cyp2d6-allelic-variants-on-gefitinib-metabolism-in-vitro
#13
Ping Fang, Xiang Zheng, Jiayang He, Honglei Ge, Pengfei Tang, Jianping Cai, Guoxin Hu
BACKGROUND: Cytochrome P450 2D6 (CYP2D6), a member of the CYP450 enzyme super family, is a polymorphic enzyme that metabolizes ~25% of therapeutic drugs. CYP2D6 exhibits significant genetic polymorphisms which might cause adverse effects and therapeutic failures of some drugs. OBJECTIVE: The purpose of this study was to evaluate the catalytic activities of 22 novel CYP2D6 alleles (CYP2D6*87, *88, *89, *90, *91, *92, *93, *94, *95, *96, *97, *98, R25Q, F164L, E215K, F219S, V327M, D336N, V342M, R344Q, R440C, R497C) on the metabolism of gefitinib in vitro...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28461740/pharmacokinetic-interactions-between-glimepiride-and-rosuvastatin-in-healthy-korean-subjects-does-the-slco1b1-or-cyp2c9-genetic-polymorphism-affect-these-drug-interactions-observations-and-introspection-of-the-bioanalysis
#14
https://www.readbyqxmd.com/read/28458521/cerebrolysin-for-functional-recovery-in-patients-with-acute-ischemic-stroke-a-meta-analysis-of-randomized-controlled-trials
#15
Zefeng Wang, Ligen Shi, Shenbin Xu, Jianmin Zhang
Cerebrolysin has been shown to have an inconsistent efficacy on functional recovery in patients with acute ischemic stroke (AIS). The present meta-analysis aims to evaluate the value of cerebrolysin and to explore the potential influencing factors. The main electronic databases, including MEDLINE, EMBASE, and the Cochrane Library, were searched. The primary outcome was functional recovery at Day 90. The secondary outcomes included mortality and adverse events. A total of 1,649 patients with AIS were pooled from six randomized controlled trials (RCTs)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28458520/anti-platelet-effects-of-anti-glaucomatous-eye-drops-an-in-vitro-study-on-human-platelets
#16
Marilita M Moschos, Giannis A Moustafa, Vasiliki D Papakonstantinou, Michael Tsatsos, Konstantinos Laios, Smaragdi Antonopoulou
PURPOSE: Altered platelet aggregability has been implicated in the pathogenesis of glaucoma. This study aims to investigate the anti-platelet potential of intraocular pressure lowering drops, with the possibility of establishing it as an additional mechanism of anti-glaucomatous action. MATERIALS AND METHODS: The anti-aggregating effects of a series of anti-glaucomatous eye drops were determined on human platelets in the platelet aggregation model, using four known aggregating factors (platelet activating factor [PAF], adenosine diphosphate [ADP], thrombin receptor-activating peptide [TRAP], and arachidonic acid [AA])...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28458519/detection-approaches-for-multidrug-resistance-genes-of-leukemia
#17
REVIEW
Ying Du, Baoan Chen
Leukemia is a clonal malignant hematopoietic stem cell disease. It is the sixth most lethal cancer and accounts for 4% of all cancers. The main form of treatment for leukemia is chemotherapy. While some cancer types with a higher incidence than leukemia, such as lung and gastric cancer, have shown a sharp decline in mortality rates in recent years, leukemia has not followed this trend. Drug resistance is often regarded as the main clinical obstacle to effective chemotherapy in patients diagnosed with leukemia...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28458518/humanin-rescues-cultured-rat-cortical-neurons-from-nmda-induced-toxicity-through-the-alleviation-of-mitochondrial-dysfunction
#18
Ai-Ling Cui, Ying-Hua Zhang, Jian-Zhong Li, Tianbin Song, Xue-Min Liu, Hui Wang, Ce Zhang, Guo-Lin Ma, Hui Zhang, Kefeng Li
N-methyl-D-aspartate (NDMA) receptor-mediated excitotoxicity has been implicated in a variety of pathological situations such as Alzheimer's disease (AD) and Parkinson's disease. However, no effective treatments for the same have been developed so far. Humanin (HN) is a 24-amino acid peptide originally cloned from the brain of patients with AD and it prevents stress-induced cell death in many cells/tissues. In our previous study, HN was found to effectively rescue rat cortical neurons. It is still not clear whether HN protects the neurons through the attenuation of mitochondrial dysfunction...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28458517/a-comparative-study-on-endovascular-treatment-of-sub-acute-critical-limb-ischemia-mechanical-thrombectomy-vs-thrombolysis
#19
Mariya Kronlage, Ilka Printz, Britta Vogel, Erwin Blessing, Oliver J Müller, Hugo A Katus, Christian Erbel
OBJECTIVE: The aim of this study was to compare different interventional methods for treatment of (sub)acute limb ischemia upon thrombotic occlusions of the lower extremity in terms of their safety and efficacy in a tertiary hospital setting. DESIGN: This is a retrospective, single-center study of non-randomized data. METHODS: A total of 202 patients, including 26 critically ill patients, underwent rotational thrombectomy (Rotarex(®)), local thrombolysis (recombinant tissue plasminogen activator), or combination of both at the University Hospital Heidelberg (2006-2015)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28458516/profile-of-romosozumab-and-its-potential-in-the-management-of-osteoporosis
#20
REVIEW
Sian Yik Lim, Marcy B Bolster
Increased understanding of bone biology has led to the discovery of several unique signaling pathways that regulate bone formation and resorption. The Wnt signaling pathway plays a significant role in skeletal development, adult skeletal homeostasis, and bone remodeling. Sclerostin is an inhibitor of the Wnt signaling pathway. Romosozumab, a humanized monoclonal antibody that binds to sclerostin, prevents sclerostin from exerting this inhibitory effect. Therefore, in the presence of romosozumab, the Wnt signaling pathway is activated leading to bone formation and bone mineral density gain...
2017: Drug Design, Development and Therapy
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