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Drug Design, Development and Therapy

Heba A Abou-Taleb, Rasha A Khallaf, Jelan A Abdel-Aleem
Objective: One of the greatest challenges drug formulation is facing is poor bioavailability via oral route. In this regard, nasal drug delivery has been commonly used as an alternative route to improve drug bioavailability. Nefopam hydrochloride (NF) is an analgesic drug that suffers from poor bioavailability due to extensive metabolism in liver. Accordingly, the goal of the present study was to improve NF bioavailability via niosomal-based formulation designed for intranasal delivery...
2018: Drug Design, Development and Therapy
Silvia Bartollino, Flavia Chiosi, Silvio di Staso, Maurizio Uva, Arduino Pascotto, Michele Rinaldi, Jan M Keppel Hesselink, Ciro Costagliola
Phenytoin is a non-sedative barbiturate derivate and has been recently rediscovered as a neuroprotective and retinoprotective compound in patients affected by optic neuritis secondary to multiple sclerosis. However, currently there are still no neuroprotective compounds registered and available in the clinic. We reviewed the literature supporting the retinoprotective properties of phenytoin and analyzed the various approaches and definitions from the first research periods onwards. The retinoprotective role of phenytoin was already known in the 1970s, but only recently has this effect been rediscovered, confirming that it could indeed provide structural protection of the retinal cells...
2018: Drug Design, Development and Therapy
Siwei Cai, Qianhui Yang, Xiaorong Li, Yan Zhang
Diabetic macular edema (DME) has shown an increasing prevalence during the past years and is the leading cause of diabetic retinopathy blindness. Traditional treatment modalities include laser and corticosteroid therapy, which, however, either act through unclear mechanisms or cause cataracts and elevated intraocular pressure. In recent years, as the pathogenic role of VEGF in DME has been well-recognized, the intravitreal injection of anti-VEGF drugs has become the first-line treatment of DME due to their great efficacy in improving visual acuity and mitigating macular edema...
2018: Drug Design, Development and Therapy
Wencheng Ding, Teng Ji, Wei Xiong, Tian Li, Demin Pu, Rong Liu
Purpose: In this study, we investigated the effect of Realgar on the apoptosis of HPV16-positive cervical cells in vitro. Methods: The effect of Realgar on the apoptosis of HPV16-positive cervical cells was investigated by annexin V-fluorescein isothiocyanate/propidium iodide staining and growth inhibition assays using HPV16-positive cervical cancer cell line SiHa and HPV16-positive immortalized cervical epithelial cell line S12. The expression of genes was measured by real-time PCR, and the expression of corresponding proteins was detected by Western blotting...
2018: Drug Design, Development and Therapy
Kwang-Hee Shin, Ji-Young Jeon, Kyungho Jang, Tae-Eun Kim, Min-Gul Kim
Purpose: The aim of this study was to evaluate the dose-proportional pharmacokinetic characteristics of pregabalin following the administration of GLA5PR GLARS-NF1 tablets (150, 300, 450, and 600 mg) in the fed state. Subjects and methods: An open-label, randomized, single-dose, parallel study was conducted in 40 eligible subjects who were randomly assigned to receive a single 150, 300, 450, or 600 mg dose of GLA5PR GLARS-NF1. Serial blood samples were collected before and after dosing for 36 hours, and plasma concentrations were determined using liquid chromatography-tandem mass spectrometry...
2018: Drug Design, Development and Therapy
Jie Wu, Wenqiang Fan, Ling Ma, Xiuqin Geng
Aim: MicroRNAs (miRNA) are a class of small, highly conserved noncoding RNA molecules, which contain 18-28 nucleotides and are involved in the regulation of gene expression. It has been proved that microRNAs play a very important role in several key cellular processes, such as cell differentiation, cell cycle progression, and apoptosis, as well as in autoimmune disease. One recently identified miRNA, miR-708-5p, has been demonstrated to have profound roles in suppressing oncogenesis in different types of tumors...
2018: Drug Design, Development and Therapy
Victor Yu Glanz, Veronika A Myasoedova, Andrey V Grechko, Alexander N Orekhov
The demand for novel anti-influenza drugs persists, which is highlighted by the recent pandemics of influenza affecting thousands of people across the globe. One of the approaches to block the virus spreading is inhibiting viral sialidase (neuraminidase). This enzyme cleaves the sialic acid link between the newly formed virions and the host cell surface liberating the virions from the cell and maintaining the cycle of infection. Viral neuraminidases appear therefore as attractive therapeutic targets for preventing further spread of influenza infection...
2018: Drug Design, Development and Therapy
Yi Liu, Xiaoqing Ma, Jing Guo, Zhen Lin, Miao Zhou, Wenjuan Bi, Jinsong Liu, Jingxiao Wang, Haiping Lu, Gang Wu
Introduction: Alcoholism can lead to low mineral density, compromised regenerative bone capacity and delayed osteointegration of dental implants. This may be partially attributed to the inhibitive effect of all-trans retinoic acid (ATRA), a metabolite of alcohol, on osteoblastogenesis. Our previous studies demonstrated that heterodimeric bone morphogenetic protein 2/7 (BMP2/7) was a more potent BMP than homodimeric BMP2 or BMP7, and could antagonize the inhibitive effect of ATRA to rescue osteoblastogenesis...
2018: Drug Design, Development and Therapy
Jin Ma, Chunxia Yin, Shiyu Ma, Huiliang Qiu, Chaoyang Zheng, Qiuxiong Chen, Chunhua Ding, Weihui Lv
Purpose: Shensong Yangxin (SSYX) capsule is a traditional Chinese medicine that has been used widely to treat cardiac arrhythmia. This study aimed to assess whether SSYX prevents atrial fibrillation (AF) after chronic myocardial infarction (MI)-induced heart failure and to determine the underlying mechanisms. Materials and methods: The study included 45 male Sprague Dawley rats. The rats underwent MI induction or sham surgery. One week after MI induction surgery, we performed serial echocardiography and administered SSYX capsule to some rats that experienced MI...
2018: Drug Design, Development and Therapy
Cheng-Ting Zi, Liu Yang, Feng-Qing Xu, Fa-Wu Dong, Dan Yang, Yan Li, Zhong-Tao Ding, Jun Zhou, Zi-Hua Jiang, Jiang-Miao Hu
Background: Podophyllotoxin is a potent cytotoxic agent and serves as a useful lead compound for the development of antitumor drugs. Several podophyllotoxin-derived antitumor agents, including etoposide, are currently in clinical use; however, their therapeutic efficacy is often limited due to side effects and the development of resistance by cancer cells. Previous studies have shown that 4β-1,2,3-triazole derivatives of podophyllotoxin exhibit more potent anticancer activity and better binding to topoisomerase-II than etoposide...
2018: Drug Design, Development and Therapy
Seong Shin Kwak, Eun Seok Lee, Ho Yub Yoon, Chang Hyun Kim, Yoon Tae Goo, Myung Joo Kang, Sangkil Lee, Bong Sang Lee, Hong Ryeol Jeon, Chang Hyun Oh, Young Wook Choi
Purpose: To develop an immediate release-type tablet containing varenicline salicylate (VRC-S), a smoking cessation agent, formulation and stability studies were performed. The in vitro dissolution and in vivo pharmacokinetic (PK) behavior of the tablets were compared with those of the commercial product (Champix) as a reference. Materials and methods: The characteristics of the powder were investigated by particle morphology, size distribution, solubility, hygroscopicity, differential scanning calorimetry, and powder X-ray diffraction...
2018: Drug Design, Development and Therapy
Mitsuhiro Abe, Kenji Tsushima, Masashi Sakayori, Kenichi Suzuki, Jun Ikari, Jiro Terada, Koichiro Tatsumi
Introduction: The INPULSIS-ON trial demonstrated that nintedanib reduced decline in forced vital capacity (FVC) and low pulmonary function (%FVC < 50%) of patients with idiopathic pulmonary fibrosis (IPF). However, there is no sufficient evidence in real world. Objectives: Reveal the utility and adverse events of nintedanib for severe IPF patients. Methods: This was a single-center retrospective study. Patients who met the eligibility criteria of the INPULSIS trial (%FVC ≥ 50%; %DLCO [diffusing capacity of the lung carbon monoxide % predicted] ≥ 30%) were classified as Mild to Moderate Group (n = 34); patients who did not meet the criteria were classified as Severe Group (n=17)...
2018: Drug Design, Development and Therapy
Xuchun Che, Rong Lu, Zheng Fu, Yajun Sun, Zhi-Feng Zhu, Jin-Ping Li, Song Wang, Jing Jia, Qing Wang, Zhi Yao
Background: Tyroserleutide (YSL) inhibits the growth and metastasis of human hepatocellular carcinoma (HCC). This paper studied the effect of YSL on metastasis of human HCC and investigated its mechanisms. Methods: In vivo, experimental lung metastasis models of human HCC SK-HEP-1 cells in nude mice were established, and In vitro, the proliferation, adhesion and invasion of SK-HEP-1 cells were detected. Results: In vivo, YSL significantly inhibited the metastasis of human HCC...
2018: Drug Design, Development and Therapy
Wei Zhang, Kimberly R Jordan, Brian Schulte, Enkhtsetseg Purev
Background: Chimeric antigen receptor (CAR) T-cell therapy is highly effective for treating acute lymphoblastic leukemia and non-Hodgkin's lymphoma with high rate complete responses. However, the broad clinical application of CAR T-cell therapy has been challenging, largely due to the lack of widespread ability to produce and high cost of CAR T-cell products using traditional methods of production. Automated cell processing in a closed system has emerged as a potential method to increase the feasibility of producing CAR T cells locally at academic centers due to its minimal reliance on experienced labor, thereby making the process less expensive and more consistent than traditional methods of production...
2018: Drug Design, Development and Therapy
Lihong Chen, Jinhua Wang, Jianbo Wu, Qiaomei Zheng, Jifen Hu
Background: Indirubin is the active component of Danggui Longhui Wan, a traditional Chinese medicine formulation. Due to its anti-inflammation and anti-tumor effects, indirubin has been widely used for the treatment of inflammation, cancer, and other chronic disease. Herein, we aimed to investigate the role and mechanism of indirubin in human ovarian cancer cell proliferation. Materials and methods: The cell viability was determined by Cell Counting Kit-8 and colony formation assays by treatment with different dosages of indirubin over 72 hours...
2018: Drug Design, Development and Therapy
Feng Yang, Aimei Li, Han Liu, Hairong Zhang
Purpose: Gastric cancer is one of the most common human epithelial malignancies, and using nanoparticles (NPs) in the diagnosis and treatment of cancer has been extensively studied. The aim of this study was to develop hyaluronic acid (HA) containing lipid NPs coloaded with cisplatin (CDDP) and sorafenib (SRF) for the treatment of gastric cancer. Materials and methods: HA and CDDP containing lipid prodrug was synthesized using polyethylene glycol (PEG) as a linker (HA-PEG-CDDP)...
2018: Drug Design, Development and Therapy
Bingchen Lang, Lingli Zhang, Chunsong Yang, Yunzhu Lin, Wensheng Zhang, Fengshan Li
Objective: One conundrum that frequently occurs during clinical anesthesia is etomidate-induced myoclonus, which results in multiple risks. The aim of the study was to evaluate systematically the effect of pretreatment with lidocaine on preventing etomidate-induced myoclonus. Materials and methods: The literature search was performed from the inception to April 2018 in PubMed, Embase, Cochrane Library, and China National Knowledge Infrastructure. All randomized controlled trials that used lidocaine to prevent etomidate-induced myoclonus were enrolled...
2018: Drug Design, Development and Therapy
Dan Xu, Shu-Ting Lu, Yu-Shuang Li, Aju Baidya, Hao Mei, Yong He, Bo Wu
Background: Gliomas are one of the most common types of primary brain tumors. It is usually evaluated by gadolinium(III)-based contrast agents by magnetic resonance imaging (MRI) in the clinic. Methotrexate (MTX), as a type of folate analog that inhibits the enzyme dihydrofolate reductase, is widely used as a chemotherapeutic agent to treat gliomas in the experiment. Purpose: In this study, a novel theranostic agent MTX-DOTA-Gd (MTX-Gd) was synthesized, which integrates magnetic resonance imaging (MRI) with anticancer treatment...
2018: Drug Design, Development and Therapy
Yaguang Wang, Yafen Gao, Jun Ma
Background: Penehyclidine hydrochloride (PHC) is an anticholinergic drug manufactured in China. It is used widely in clinics as a reversal agent in cases of organic phosphorus poisoning and as a preanesthetic medication. Compared with other anticholinergic agents, PHC confers substantial advantages. Here, in this review, we focus on its important clinical effects for organic phosphorus poisoning, preanesthetic medication, and the protective effects on certain visceral organs. Materials and methods: Our bibliographic sources include the PubMed and China National Knowledge Infrastructure (CNKI) databases, updated in March 2018...
2018: Drug Design, Development and Therapy
Changshun Chen, Chen Zhu, Xiang Hu, Qiuli Yu, Qianjin Zheng, Shengxiang Tao, Lihong Fan
Purpose: The aims of this research were to combine α-hemihydrate calcium sulfate/octacalcium phosphate (α-CSH/OCP) with sodium hyaluronate (SH) or SH sulfate (SHS) to determine whether these composites can be used as a new type of bone repair material. This study may provide a theoretical basis and new ideas for the construction of active bone repair materials and their clinical application. Methods: In this study, we combined α-CSH/OCP with SH or SHS. Scanning electron microscopy (SEM), Fourier-transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), thermogravimetric analysis (TGA), and the wettability test were performed, and porosity, setting time, in vitro degradation, and the mechanical properties of these composite materials were analyzed to evaluate the ultrastructural and physicochemical properties...
2018: Drug Design, Development and Therapy
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