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Drug Research

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https://www.readbyqxmd.com/read/28738427/nanoemulsion-an-advanced-vehicle-for-efficient-drug-delivery
#1
Asad Ali, Vaseem Ahamad Ansari, Usama Ahmad, Juber Akhtar, Afroz Jahan
Advanced drug delivery system has now gained preference over the conventional drug delivery system. One such research is nanoemulsion which is famous among the researchers because of ease of formation, stability, clarity, increased absorption rate leading to increasing in bioavailability and potential to form a formulation with both lipophilic as well as the hydrophilic drug. Long lasting stability (up to years) and ability to encapsulate both lipophilic and hydrophilic drug has given this colloidal system a valuable position in drug delivery...
July 24, 2017: Drug Research
https://www.readbyqxmd.com/read/28738426/long-term-effects-of-liraglutide-in-japanese-patients-with-type-2-diabetes-among-the-subgroups-with-different-renal-functions-results-of-2-year-prospective-study
#2
Takeyuki Hiramatsu, Akiko Ozeki, Hideaki Ishikawa, Shinji Furuta
Aims Very few studies have ever examined the effects of long-term (>1 year) administration of liraglutide in patients with type 2 diabetes mellitus (T2DM) and renal impairment. Therefore, we conducted a 2-year study to prospectively examine the effects of liraglutide in those patients. Methods A total of 148 patients with T2DM were enrolled and treated with liraglutide (0.6 or 0.9 mg/day). 97 patients completed the 2-year study without protocol deviations. These patients were divided into 3 groups according to the baseline estimated glomerular filtration ratio (eGFR) (in mL/min/1...
July 24, 2017: Drug Research
https://www.readbyqxmd.com/read/28738425/preparation-and-characterization-of-pegylated-iron-oxide-gold-nanoparticles-for-delivery-of-sulforaphane-and-curcumin
#3
Hossein Danafar, Ali Sharafi, Sonia Askarlou, Hamidreza Kheiri Manjili
Natural products have been used for the treatment of various diseases such as cancer. Curcumin (CUR) and sulforaphane (SF) have anti-cancer effects, but their application is restricted because of their low water solubility and poor oral bioavailability. To improve the bioavailability and solubility of SF and CUR, we performed an advanced delivery of SF and CUR with PEGylated gold coated Fe3O4 magnetic nanoparticles (PEGylated Fe3O4@Au NPs) to endorse SF and CUR maintenance as an effective and promising antitumor drugs...
July 24, 2017: Drug Research
https://www.readbyqxmd.com/read/28724167/in-vitro-controlled-release-of-two-new-tuberculocidal-adamantane-aminoethers-from-solid-pharmaceutical-formulations-ii
#4
Marilena Vlachou, Angeliki Siamidi, Dimitrios Spaneas, Dimitrios Lentzos, Polixeni Ladia, Konstantina Anastasiou, Ioannis Papanastasiou, Angeliki-Sofia Foscolos, Markos-Orestis Georgiadis, Vangelis Karalis, Tahsin Kellici, Thomas Mavromoustakos
The aim of the present investigation was to develop matrix tablet formulations for the in vitro controlled release of two new tuberculocidal adamantane aminoethers (compounds III and IV), congeneric to the adamantane derivative SQ109, which is in final clinical trials, and aminoethers (I) and (II), using carefully selected excipients, such as polyvinylpyrrolidone, sodium alginate and lactose. The tablets were prepared using the direct compression method and dissolution experiments were conducted using the US Pharmacopoeia type II apparatus (paddle method) in gastric and intestinal fluids...
July 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28724166/iron-pharmacokinetics-in-women-with-iron-deficiency-anaemia-following-a-single-oral-dose-of-a-novel-formulation-of-tardyferon-prolonged-release-ferrous-sulphate
#5
Andrew Leary, Laurence Barthe, Thierry Clavel, Claudie Sanchez, Zahida Issiakhem, Bruno Paillard, Jean-Marc Edmond
Numerous iron-containing preparations are available on the market; these vary in dosage, salt, chemical state of iron (ferric or ferrous) and in the iron delivery process (immediate or prolonged-release). Tardyferon® is a prolonged-release tablet containing 80 mg ferrous sulphate. The formulation has recently been modified; changes to the excipients which constitute the inert formulation matrix have allowed a decrease in tablet size for easier swallowing. The aim of this multicenter open-label study was to characterize the serum pharmacokinetics of iron in non-pregnant women aged 23-45 years with iron deficiency anaemia (IDA) following single oral administration of 160 mg Tardyferon® under fasting conditions...
July 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28724165/cytogenotoxicity-of-inclusion-complexes-of-diazepam-with-2-hydroxypropyl-%C3%AE-cyclodextrin
#6
Jasmina Hadžiabdić, Nevenka Kopjar, Davor Želježić, Selma Špirtović-Halilović, Davorka Završnik
Background Diazepam, as one of the most frequent prescribed drug from 1,4-benzodiazepine group, has certain limitations in pharmaceutical technology due to its poor solubility in water. By forming inclusion complexes with 2-hydroxypropyl-β-cyclodextrin, diazepam's biopharmaceutical properties can be greatly improved. Aim Aim of this research was to in vitro evaluate genotoxicity of prepared novel complexes of diazepam and their influence on proliferation of human peripheral blood lymphocytes. Methods For identification of possible genotoxicity of diazepam inclusion complexes, cytokinesis-block micronucleus assay has been chosen...
July 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28701011/action-plan-for-prolongation-of-nephrogenesis-in-preterm-and-growth-restricted-babies-explore-ultrastructure-of-the-nephrogenic-zone-identify-a-molecular-target-select-a-viable-drug-and-find-a-path-for-administration
#7
Will W Minuth
A large amount of investigations informs about primary steps of mammalian kidney development such as anlage of the organ and initial nephron formation, while only few data exists about the late phase of human kidney development. In particular, little attention was up to date addressed to the decrease of morphogenic activity in the nephrogenic zone short before birth and the vanishing of all stem cell niches aligned beyond the organ capsule. There is evidence that molecular controlling of this normal but degenerative developmental process also plays a decisive role in the kidneys of preterm and growth restricted babies...
July 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28672409/jack-bean-urease-inhibitors-and-antioxidant-activity-based-on-palmitic-acid-derived-1-acyl-3-arylthioureas-synthesis-kinetic-mechanism-and-molecular-docking-studies
#8
Aamer Saeed, Sajid Ur-Rehman, Pervaiz Ali Channar, Fayaz Ali Larik, Qamar Abbas, Mubashir Hassan, Hussain Raza, Sung-Yum Seo
A series of acylthioureas was synthesized and their inhibitory effects on the DPPH and jack bean urease were evaluated. The results showed that all of the synthesized compounds exhibited significant jack bean urease inhibitory activities. Especially, 1-(4-chlorophenyl)-3 palmitoylthiourea 5a bearing 4-chloro substituted phenyl ring exhibited the most potent tyrosinase inhibitory activity with an IC50 value 0.0170 μM compared to the IC50 value of 4.720 μM of thiourea used as standard. The inhibition mechanism analyzed by Lineweaver-Burk plots revealed that the type of inhibition of compound 5a on tyrosinase was noncompetitive...
July 3, 2017: Drug Research
https://www.readbyqxmd.com/read/28672408/ginger-extract-modulates-the-expression-of-chemokines-ccl20-and-ccl22-and-their-receptors-ccr6-and-ccr4-in-the-central-nervous-system-of-mice-with-experimental-autoimmune-encephalomyelitis
#9
Abdollah Jafarzadeh, Zahra Arabi, Rayhaneh Ahangar-Parvin, Marziyeh Mohammadi-Kordkhayli, Maryam Nemati
Background Chemokines facilitate the leukocytes infiltration into the central nervous system (CNS) which is an essential step in the pathogenesis of multiple sclerosis. Ginger has also a broad anti-inflammatory properties. The aim was to evaluate the effects of ginger extract on the expression of CCL20 and CCL22 and their receptors (CCR6 and CCR4, respectively) in experimental autoimmune encephalomyelitis (EAE). Material and Methods Female C57BL/6 mice used for EAE induction by immunization with myelin oligodendroglial glycoprotein...
July 3, 2017: Drug Research
https://www.readbyqxmd.com/read/28658699/extra-pulmonary-toxicity-assessment-of-gold-and-silver-nanorods-following-intra-tracheal-instillation-in-rats
#10
Harikiran Lingabathula, Narsimhareddy Yellu
The gold nanorods (GNRs) and silver nanorods (SNRs) are utilized in various types of industrial and commercial applications. But, there is limited availability of extra pulmonary toxicity data regarding these nanorods. The present investigation evaluated the extra pulmonary toxicity induced by 10 and 25 nm GNRs and SNRs in rats following intra tracheal instillation. The serum biochemical analysis results have shown elevated levels of serum alanine transaminase (ALT) and serum creatinine following 1 day and 1 week post instillation...
June 28, 2017: Drug Research
https://www.readbyqxmd.com/read/28651259/new-biguanides-as-anti-diabetic-agents-part-i-synthesis-and-evaluation-of-1-substituted-biguanide-derivatives-as-anti-diabetic-agents-of-type-ii-diabetes-insulin-resistant
#11
Samir Y Abbas, Wahid M Basyouni, Khairy A M El-Bayouk, Wael M Tohamy, Hanan F Aly, Azza Arafa, Mahmoud S Soliman
New 1-substituted-biguanide hydrochloride salts were synthesized via reacting benzo[1,3-d]dioxol-5-amine, phenylhydrazine, N,N-dimethylhydrazinecarboxamide, benzohydrazide and 2-phenyl acetohydrazide with dicyandiamide in acidic medium. Structures of the obtained biguanide salts were characterized by spectroscopic tools. The synthesized compounds were screened for their anti-diabetic activity with standard metformin drug. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives significantly decreased the elevated blood glucose level...
June 26, 2017: Drug Research
https://www.readbyqxmd.com/read/28628926/synthesis-characterisation-molecular-docking-anti-microbial-and-anti-diabetic-screening-of-substituted-4-indolylphenyl-6-arylpyrimidine-2-imine-derivatives
#12
Veerasamy Ramya, Santhirakasu Vembu, Ganesan Ariharasivakumar, Manathusamy Gopalakrishnan
The purpose of the research is to synthesise a novel series of (E)-2-(4-(1H-indol-3-yl)-6-p-substituted phenylpyrimidin-2-yl)dimethylguanidine derivatives since 3-(1H-indol-3-yl)-1-p-substituted phenylprop-2-en-1-one and evaluate their molecular docking studies, antimicrobial, and anti-diabetic activities. Among all the synthesized compounds (11a-g), compound 11a exhibits excellent CDOCKER energy (-11.36 kcal/mol). The entire compounds (11a-g) confirm very good antimicrobial activity towards the tested microorganisms...
June 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28628925/apoptosis-and-caspase-3-pathway-role-on-anti-proliferative-effects-of-scrophulariaoxy-sepala-methanolic-extract-on-caco-2-cells
#13
Ali Namvaran, Mehdi Fazeli, Safar Farajnia, Gholamreza Hamidian, Hassan Rezazadeh
Colorectal cancer is one the most important malignancies worldwide and finding new treatment option for this cancer is of high priority. Natural compounds are common source of drugs for treatment of various diseases including cancers. The aim of this study was to investigate the effects of Scrophularia oxysepala extract on Caco-2 cells and explore the possible role of caspase 3 pathway in inducing cell death in this cancer cells in compare with chemotherapy agents of cisplatin and capecitabine. The methanolic extract of Scrophularia oxysepala (SO) was prepared by drench method...
June 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28628924/chrysin-alters-micrornas-expression-levels-in-gastric-cancer-cells-possible-molecular-mechanism
#14
Farideh Mohammadian, Younes Pilehvar-Soltanahmadi, Shahriar Alipour, Mehdi Dadashpour, Nosratollah Zarghami
Background Gastric carcinoma still remains the second most common cause of cancer mortality in the world. Chrysin, as a flavone, has showed cancer chemopreventive activity. The cellular and molecular mechanisms of chrysin in cancer cells have not been fully understood. Objective In this study, we investigate expression levels of let-7a, miR-9, mir-18a, miR-21, miR-22, miR-34a, miR-126 and mir-221 to describe the anti-cancer effects of chrysin. Materials and Methods The cytotoxic effects of chrysin were assessed using MTT assay...
June 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28628923/cremophor-el-alters-the-plasma-protein-binding-and-pharmacokinetic-profile-of-valspodar-in-rats
#15
Ziyad Binkhathlan
Cremophor EL is a nonionic surfactant widely used in pharmaceutical formulations. Nonetheless, there are several reports on the influence of this excipient on the protein binding, pharmacokinetics, and pharmacodynamics of drugs. Valspodar is an investigational non-immunosuppressive derivative of cyclosporine A, used in clinical trials for treatment of multidrug resistant tumors. The formulation of valspodar (Amdray(®)) contains cremophor EL and ethanol as solubilizing agents. The main aim of the current study was to assess the plasma protein binding (in vitro) and the pharmacokinetic profile of valspodar in the cremophor EL-based formulation in comparison to a cremophor EL-free formulation following intravenous (i...
June 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28586926/cytoprotective-effects-of-pumpkin-cucurbita-moschata-fruit-extract-against-oxidative-stress-and-carbonyl-stress
#16
Reyhaneh Shayesteh, Mohammad Kamalinejad, Hasan Adiban, Azin Kardan, Fariborz Keyhanfar, Mohammad Reza Eskandari
Background Diabetes mellitus is a chronic endocrine disorder that is associated with significant mortality and morbidity due to microvascular and macrovascular complications. Diabetes complications accompanied with oxidative stress and carbonyl stress in different organs of human body because of the increased generation of free radicals and impaired antioxidant defense systems. In the meantime, reactive oxygen species (ROS) and reactive carbonyl species (RCS) have key mediatory roles in the development and progression of diabetes complications...
June 6, 2017: Drug Research
https://www.readbyqxmd.com/read/28586925/inhibitory-effect-of-abitylguanide-on-adenovirus-replication
#17
Angel S Galabov, Vesselina Vassileva, Vera Karabasheva
N'N'-anhydro-bis(β-hydroxy-ethyl)biguanide.HCl (abitylguanide) demonstrated a marked inhibitory effect on replication in cell cultures of a broad spectrum of human adenoviruses both standard laboratory strains and strains isolated from epidemic keratoconjunctivitis patients. The strongest inhibitory activity was found in viruses belonging to subgroup C (Rosen's subgroup III). The compound susceptible period of human adenovirus 5 replication in primary cell cultures of human embryo kidney cells included the total replication cycle and was especially pronounced during the exponential phase of the virus growth curve...
June 6, 2017: Drug Research
https://www.readbyqxmd.com/read/28561241/in-vitro-controlled-release-from-solid-pharmaceutical-formulations-of-two-new-adamantane-aminoethers-with-antitubercular-activity-i
#18
Marilena Vlachou, Angeliki Siamidi, Evanthia Diamantidi, Alexandra Iliopoulou, Ioannis Papanastasiou, V Ioannidou, Violeta Kourbeli, Angeliki-Sofia Foscolos, Anthony Vocat, Stewart T Cole, Vangelis Karalis, Tahsin Kellici, Thomas Mavromoustakos
The aim of the present investigation was to develop matrix tablet formulations for the in vitro controlled release of 2 new tuberculocidal adamantane aminoethers (compounds I and II), congeneric to the adamantane derivative SQ109, which is in final clinical trials, using carefully selected excipients, such as polyvinylpyrrolidone, sodium alginate and lactose. The tablets were prepared using the direct compression method and dissolution experiments were conducted using the US Pharmacopoeia type II apparatus (paddle method) in gastric and intestinal fluids...
May 30, 2017: Drug Research
https://www.readbyqxmd.com/read/28561240/preparation-and-characterization-of-copolymeric-polymersomes-for-protein-delivery
#19
Alireza Nomani, Hamed Nosrati, Hamidreza Kheiri Manjili, Leila Khesalpour, Hossein Danafar
Biodegradable copolymeric polymersomes have been used for controlled drug delivery of proteins. These polymersomes important areas to overcome formulation associated problems of the proteins. The aim of this study was to develop polymersomes using biodegradable copolymers for delivery of bovine serum albumin (BSA) as a model protein. Encapsulated BSA by mPEG-PCL polymersomes led to formation of BSA-loaded mPEG-PCL polymersomes. The polymersomes synthesized with the protein-polymer ratio of 1:4 at 15 000 rpm gave maximum loading, minimum polydispersion with maximally sustained protein release pattern, among the prepared polymersomes...
May 30, 2017: Drug Research
https://www.readbyqxmd.com/read/28561239/determination-of-fenofibric-acid-in-rat-plasma-and-its-application-to-a-comparative-pharmacokinetic-study-of-jw322-and-fenofibrate
#20
Tae Kon Kim
In this study, a sensitive and reliable method for the quantitation of fenofibric acid in rat plasma was developed and validated using high performance liquid chromatography (HPLC). The plasma samples were prepared by deproteinization, and sildenafil was used as an internal standard. Chromatographic separation was achieved using a reversed-phase (C18) column. The mobile phase, 0.02 M ammonium acetate buffer:acetonitrile (35:65, v/v), was run at a flow rate of 1.0 mL/min, and the column eluent was monitored using an ultraviolet detector at 280 nm at room temperature...
May 30, 2017: Drug Research
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