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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/27932866/effect-of-peritoneal-dialysis-fluid-containing-osmo-metabolic-agents-on-human-endothelial-cells
#1
Mario Bonomini, Sara Di Silvestre, Pamela Di Tomo, Natalia Di Pietro, Domitilla Mandatori, Lorenzo Di Liberato, Vittorio Sirolli, Francesco Chiarelli, Cesare Indiveri, Assunta Pandolfi, Arduino Arduini
BACKGROUND: The use of glucose as the only osmotic agent in peritoneal dialysis (PD) solutions (PDSs) is believed to exert local (peritoneal) and systemic detrimental actions, particularly in diabetic PD patients. To improve peritoneal biocompatibility, we have developed more biocompatible PDSs containing xylitol and carnitine along with significantly less amounts of glucose and have tested them in cultured Human Vein Endothelial Cells (HUVECs) obtained from the umbilical cords of healthy (C) and gestational diabetic (GD) mothers...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27932865/statistical-modeling-methods-to-analyze-the-impacts-of-multiunit-process-variability-on-critical-quality-attributes-of-chinese-herbal-medicine-tablets
#2
Fei Sun, Bing Xu, Yi Zhang, Shengyun Dai, Chan Yang, Xianglong Cui, Xinyuan Shi, Yanjiang Qiao
The quality of Chinese herbal medicine tablets suffers from batch-to-batch variability due to a lack of manufacturing process understanding. In this paper, the Panax notoginseng saponins (PNS) immediate release tablet was taken as the research subject. By defining the dissolution of five active pharmaceutical ingredients and the tablet tensile strength as critical quality attributes (CQAs), influences of both the manipulated process parameters introduced by an orthogonal experiment design and the intermediate granules' properties on the CQAs were fully investigated by different chemometric methods, such as the partial least squares, the orthogonal projection to latent structures, and the multiblock partial least squares (MBPLS)...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27932864/efficacy-and-tolerability-of-vilazodone-for-major-depressive-disorder-evidence-from-phase-iii-iv-randomized-controlled-trials
#3
Ligen Shi, Jingyi Wang, Shenbin Xu, Yunrong Lu
Vilazodone is a new molecule approved for major depressive disorder (MDD). This report focuses on the efficacy and tolerability of vilazodone for MDD. MEDLINE, EMBASE, and Cochrane Library were searched. A total of 1,930 patients from four trials were included. A significant improvement in the Montgomery-Asberg Depression Rating Scale (MADRS) total score was seen as early as week 2 (P<0.01) in vilazodone-treated patients. The results showed a higher rate of MADRS response with vilazodone compared with placebo (P<0...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27932863/non-imidazole-based-histamine-h3-receptor-antagonists-with-anticonvulsant-activity-in-different-seizure-models-in-male-adult-rats
#4
Bassem Sadek, Ali Saad, Gniewomir Latacz, Kamil Kuder, Agnieszka Olejarz, Tadeusz Karcz, Holger Stark, Katarzyna Kieć-Kononowicz
A series of twelve novel non-imidazole-based ligands (3-14) was developed and evaluated for its in vitro binding properties at the human histamine H3 receptor (hH3R). The novel ligands were investigated for their in vivo protective effects in different seizure models in male adult rats. Among the H3R ligands (3-14) tested, ligand 14 showed significant and dose-dependent reduction in the duration of tonic hind limb extension in maximal electroshock (MES)-induced seizure model subsequent to acute systemic administration (5, 10, and 20 mg/kg, intraperitoneally), whereas ligands 4, 6, and 7 without appreciable protection in MES model were most promising in pentylenetetrazole (PTZ) model...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27920502/physicochemical-stability-of-ternary-admixtures-of-butorphanol-ketamine-and-droperidol-in-polyolefin-bags-for-patient-controlled-analgesia-use
#5
Baoxia Fang, Linhai Wang, Junfeng Gu, Fuchao Chen, Xiao-Ya Shi
BACKGROUND: Delivery of drug admixtures by intravenous patient-controlled analgesia is a common practice for the management of postoperative pain; however, analytical confirmation of the compatibility and stability of butorphanol tartrate, ketamine hydrochloride, and droperidol combined in ternary admixtures is not available. METHODS: Butorphanol tartrate, ketamine hydrochloride, and droperidol have been examined for compatibility and stability when combined with 0...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27920501/three-generations-of-epidermal-growth-factor-receptor-tyrosine-kinase-inhibitors-developed-to-revolutionize-the-therapy-of-lung-cancer
#6
REVIEW
Haijun Zhang
Lung cancer, ~80%-85% of which is non-small-cell lung cancer (NSCLC), is the leading cause of cancer-related mortality worldwide. Sensitizing mutations in epidermal growth factor receptor (EGFR) gene (EGFRm(+)), such as exon 19 deletions and exon 21 L858R point mutations, are the most important drivers in NSCLC patients. In this respect, small-molecule EGFR tyrosine kinase inhibitors (TKIs) have been designed and developed, which launched the era of targeted, personalized and precise medicine for lung cancer...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27920500/design-synthesis-and-evaluation-of-vegf-sirna-crs-as-a-novel-vector-for-gene-delivery
#7
Wen Zhao, Yifan Zhang, Xueyun Jiang, Chunying Cui
Small interfering RNA (siRNA) delivery is a prospective method in gene therapy, but it has application limitations such as negative charge, water solubility and high molecular weight. In this study, a safe and efficient nano-vector, CRS, was designed and synthesized to facilitate siRNA delivery. Physical and chemical properties of VEGF-siRNA/CRS were characterized by methods including scanning electron microscopy (SEM), transmission electron microscopy, zeta potential (ζ) measurement, drug-releasing rate measurement, gel electrophoresis and confocal microscopy...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27920499/smart-nanocrystals-of-artemether-fabrication-characterization-and-comparative-in-vitro-and-in-vivo-antimalarial-evaluation
#8
Syed Muhammad Hassan Shah, Farhat Ullah, Shahzeb Khan, Syed Muhammad Mukarram Shah, Marcel de Matas, Zahid Hussain, Muhammad Usman Minhas, Naser M AbdEl-Salam, Khaled Hafez Assi, Mohammad Isreb
Artemether (ARTM) is a very effective antimalarial drug with poor solubility and consequently low bioavailability. Smart nanocrystals of ARTM with particle size of 161±1.5 nm and polydispersity index of 0.172±0.01 were produced in <1 hour using a wet milling technology, Dena(®) DM-100. The crystallinity of the processed ARTM was confirmed using differential scanning calorimetry and powder X-ray diffraction. The saturation solubility of the ARTM nanocrystals was substantially increased to 900 µg/mL compared to the raw ARTM in water (145...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27920498/feasibility-of-sequential-adjuvant-chemotherapy-with-a-3-month-oxaliplatin-based-regimen-followed-by-3-months-of-capecitabine-in-patients-with-stage-iii-and-high-risk-stage-ii-colorectal-cancer-jswog-c2-study
#9
Atsushi Tsuruta, Kazuki Yamashita, Hiroaki Tanioka, Akihito Tsuji, Michio Inukai, Toshiki Yamakawa, Tomoki Yamatsuji, Masanori Yoshimitsu, Kazuhiro Toyota, Taketoshi Yamano, Takeshi Nagasaka, Masazumi Okajima
BACKGROUND: Six months of oxaliplatin-based chemotherapy is the standard adjuvant chemotherapy for completely resected stage III colorectal cancer (CRC). Also, patients with stage II CRC who are considered to be at high risk of disease recurrence often receive the same adjuvant chemotherapy treatment. We prospectively investigated the extent and degree of neuropathy suffered by stage III and high-risk stage II resectable CRC patients who underwent sequential approach involving 3 months of an oxaliplatin-based regimen followed by 3 months of capecitabine...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27920497/efficacy-and-safety-of-two-fixed-dose-combinations-of-s-amlodipine-and-telmisartan-ckd-828-versus-s-amlodipine-monotherapy-in-patients-with-hypertension-inadequately-controlled-using-s-amlodipine-monotherapy-an-8-week-multicenter-randomized-double-blind-phase
#10
Sang-Hyun Ihm, Hui-Kyung Jeon, Tae-Joon Cha, Taek-Jong Hong, Sang-Hyun Kim, Nae-Hee Lee, Jung Han Yoon, Namsik Yoon, Kyung-Kuk Hwang, Sang-Ho Jo, Ho-Joong Youn
PURPOSE: To evaluate the blood pressure (BP) lowering efficacy and safety of CKD-828, a fixed-dose combination of S-amlodipine (the more active isomer of amlodipine besylate, which is calcium channel blocker) and telmisartan (long acting angiotensin receptor blocker), in patients with hypertension inadequately controlled with S-amlodipine monotherapy. PATIENTS AND METHODS: Eligible patients (N=187) who failed to respond after 4-week S-amlodipine 2.5 mg monotherapy (sitting diastolic blood pressure [sitDBP] ≥90 mmHg) to receive CKD-828 2...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27920496/fabrication-of-anti-vitiligo-ointment-containing-psoralea-corylifolia-in-vitro-and-in-vivo-characterization
#11
Irshad Hussain, Nisar Hussain, Abdul Manan, Abdur Rashid, Barkat Khan, Sattar Bakhsh
BACKGROUND: Vitiligo is a repugnant and odious dermatological malady of the time. It has an detrimental impact on the pigmentation of the human skin as a result of the destruction of cutaneous melanocytes. It affects 1%-2% of the population worldwide. Different therapeutic regimens have been deployed to treat vitiligo, but none of them could stand alone to be stated as a perfect cure. Recently, a change has been observed through novel experimental-designed optimization leading to the development of an anti-vitiligo ointment containing Psoralea corylifolia (PC) seed powder...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27920495/card9-as-a-potential-target-in-cardiovascular-disease
#12
REVIEW
Matthew R Peterson, Samantha E Haller, Jun Ren, Sreejayan Nair, Guanglong He
Systemic inflammation and localized macrophage infiltration have been implicated in cardiovascular pathologies, including coronary artery disease, carotid atherosclerosis, heart failure, obesity-associated heart dysfunction, and cardiac fibrosis. Inflammation induces macrophage infiltration and activation and release of cytokines and chemokines, causing tissue dysfunction by instigating a positive feedback loop that further propagates inflammation. Cytosolic adaptor caspase recruitment domain family, member 9 (CARD9) is a protein expressed primarily by dendritic cells, neutrophils, and macrophages, in which it mediates cytokine secretion...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895469/comparison-of-bile-salt-phosphatidylcholine-mixed-micelles-in-solubilization-to-sterols-and-stability
#13
Qin Guo, Jie Cai, Pengyu Li, Dongling Xu, Xiaomin Ni, Hui Wen, Dan Liu, Suizhen Lin, Haiyan Hu
Androst-3β,5α,6β-triol (Triol) is a promising neuroprotective agent, but its poor solubility restricts its development into parenteral preparations. In this study, Triol is significantly solubilized by bile salt/phosphatidylcholine mixed micelles (BS/PC-MM). All BS/PC-MM systems are tested to remarkably improve the drug solubility with various stabilities after drug loading. Among them, the sodium glycocholate (SGC)/egg phosphatidylcholine (EPC) system with 2:1 ratio in weight and the total concentration of SGC and EPC of 100 mg/mL is proved to produce stable mixed micelles with high drug loading...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895468/increased-localized-delivery-of-piroxicam-by-cationic-nanoparticles-after-intra-articular-injection
#14
Sung Rae Kim, Myoung Jin Ho, Sang Hyun Kim, Ha Ra Cho, Han Sol Kim, Yong Seok Choi, Young Wook Choi, Myung Joo Kang
Piroxicam (PRX), a potent nonsteroidal anti-inflammatory drug, is prescribed to relieve postoperative and/or chronic joint pain. However, its oral administration often results in serious gastrointestinal adverse effects including duodenal ulceration. Thus, a novel cationic nanoparticle (NP) was explored to minimize the systemic exposure and increase the retention time of PRX in the joint after intra-articular (IA) injection, by forming micrometer-sized electrostatic clusters with endogenous hyaluronic acid (HA) in the synovial cavity...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895467/dietary-arginine-silicate-inositol-complex-inhibits-periodontal-tissue-loss-in-rats-with-ligature-induced-periodontitis
#15
Serkan Dundar, Abubekir Eltas, Sema S Hakki, Sıddık Malkoc, M Ozay Uslu, Mehmet Tuzcu, James Komorowski, I Hanifi Ozercan, Fatih Akdemir, Kazim Sahin
The purpose of this study was to induce experimental periodontitis in rats previously fed diets containing arginine silicate inositol (ASI) complex and examine the biochemical, immunological, and radiological effects. Fifty two 8-week-old female Sprague Dawley rats were equally divided into four groups. The control group included those fed a standard rat diet with no operation performed during the experiment. The periodontitis, ASI I, and ASI II groups were subjected to experimental periodontitis induction for 11 days after being fed a standard rat diet alone, a diet containing 1...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895466/pharmacokinetics-pharmacodynamics-and-safety-of-ckd-519-a-cetp-inhibitor-in-healthy-subjects
#16
Choon Ok Kim, Eun Sil Oh, Chungam Choi, Yeonjoo Kim, Sera Lee, Semi Kim, Min Soo Park
CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor being developed for the treatment of dyslipidemia to raise high-density lipoprotein cholesterol. We investigated the safety, tolerability, pharmacokinetics, and pharmacodynamics of single doses of CKD-519 in healthy adult subjects. A randomized, double-blinded, placebo-controlled, single ascending dose study was performed. Eight healthy subjects were enrolled in each CKD-519 dose group (25, 50, 100, 200, or 400 mg) and randomized to CKD-519 (n=6) or matching placebo (n=2)...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895465/oncolytic-adenovirus-expressing-interleukin-18-improves-antitumor-activity-of-dacarbazine-for-malignant-melanoma
#17
Chunhua Yang, Hang Cao, Ning Liu, Kai Xu, Meng Ding, Li-Jun Mao
Conditionally replicating adenoviruses have emerged as novel therapeutic agents for cancer. This study aimed to evaluate synergistic antitumor activity of replication-competent adenovirus armed with interleukin (IL)-18 (ZD55-IL-18) and dacarbazine (DTIC) against melanoma. Melanoma A375 cells or nude mouse tumor xenografts were treated with ZD55-IL-18 alone or together with DTIC. The results showed that ZD55-IL-18 competently replicated in A375 cells and expressed IL-18, and these were not affected by DTIC. ZD55-IL-18 enhanced the cytotoxicity of DTIC accompanied by increased apoptosis...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895464/selexipag-in-the-treatment-of-pulmonary-arterial-hypertension-design-development-and-therapy
#18
REVIEW
Elizabeth Ashley Hardin, Kelly M Chin
Pulmonary arterial hypertension is characterized by abnormalities in the small pulmonary arteries including increased vasoconstriction, vascular remodeling, proliferation of smooth muscle cells, and in situ thrombosis. Selexipag, a novel, oral prostacyclin receptor agonist, has been shown to improve hemodynamics in a phase II clinical trial and reduce clinical worsening in a large phase III clinical trial involving patients with pulmonary arterial hypertension. In this paper, we describe the prostacyclin signaling pathway, currently available oral prostanoid medications, and the development and clinical use of selexipag...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895463/lentivirus-mediated-knockdown-of-nlk-inhibits-small-cell-lung-cancer-growth-and-metastasis
#19
Mutian Lv, Yaming Li, Xin Tian, Shundong Dai, Jing Sun, Guojiang Jin, Shenyi Jiang
Nemo-like kinase (NLK), an evolutionarily conserved serine/threonine kinase, has been recognized as a critical regulator of various cancers. In this study, we investigated the role of NLK in human small-cell lung cancer (SCLC), which is the most aggressive form of lung cancer. NLK expression was evaluated by quantitative real-time polymerase chain reaction in 20 paired fresh SCLC tissue samples and found to be noticeably elevated in tumor tissues. Lentivirus-mediated RNAi efficiently suppressed NLK expression in NCI-H446 cells, resulting in a significant reduction in cell viability and proliferation in vitro...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895462/effects-of-resveratrol-on-p-glycoprotein-and-cytochrome-p450-3a-in-vitro-and-on-pharmacokinetics-of-oral-saquinavir-in-rats
#20
Jiapeng Li, Yang Liu, Jingru Zhang, Xiaotong Yu, Xiaoling Wang, Libo Zhao
BACKGROUND: The intestinal cytochrome P450 3A (CYP 3A) and P-glycoprotein (P-gp) present a barrier to the oral absorption of saquinavir (SQV). Resveratrol (RESV) has been indicated to have modulatory effects on P-gp and CYP 3A. Therefore, this study was to investigate the effects of RESV on P-gp and CYP 3A activities in vitro and in vivo on oral SQV pharmacokinetics in rats. METHODS: In vitro, intestinal microsomes were used to evaluate RESV effect on CYP 3A-mediated metabolism of SQV; MDR1-expressing Madin-Darby canine kidney (MDCKII-MDR1) cells were employed to assess the impact of RESV on P-gp-mediated efflux of SQV...
2016: Drug Design, Development and Therapy
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