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https://www.readbyqxmd.com/read/29458210/preparation-of-a-solid-self-microemulsifying-drug-delivery-system-by-hot-melt-extrusion
#1
Luis Antonio D Silva, Susana L Almeida, Ellen C P Alonso, Priscila B R Rocha, Felipe T Martins, Luís A P Freitas, Stephania F Taveira, Marcilio S S Cunha-Filho, Ricardo N Marreto
Hot-melt extrusion (HME) has gained increasing attention in the pharmaceutical industry; however, its potential in the preparation of solid self-emulsifying drug delivery systems (S-SMEDDS) is still unexplored. This study sought to prepare enteric S-SMEDDS by HME and evaluate the effects of the process and formulation variables on S-SMEDDS properties via Box-Behnken design. Liquid SMEDDS were developed, and carvedilol was used as a class II model drug. Mean size, polydispersity index (PdI) and zeta potential of the resulting microemulsions were determined...
February 16, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29458209/dermal-anti-oxidant-anti-inflammatory-and-anti-aging-effects-of-compritol-ato-based-resveratrol-colloidal-carriers-prepared-using-mixed-surfactants
#2
Haidy Abbas, Rabab Kamel, Nesrine El-Sayed
In this study, Compritol ATO-based Resveratrol colloidal carriers (CCCs) were prepared. In most formulae, the use of a binary-mixture of surfactants improved the physicochemical properties. CCC6 (containing P407/P188 as bi-surfactants) attained the highest drug loading, release efficiency during 24 hr and occlusive effect for 48 hr; in addition to, a uniform particle size distribution within the desired range. In-vivo studies were done based on the analysis of anti-oxidant markers [catalase (CAT), reduced glutathione (GSH) and superoxide dismutase (SOD)], anti-inflammatory markers [interleukin 6 (IL-6), interleukin 8 (IL-8) and rat Nuclear factor-kappa B (NF-κB)] and anti-wrinkling markers [matrix metalloproteinase (MMP-1) and Granulocyte-macrophage colony-stimulating factor (GM-CSF)], after UVB-irradiation...
February 16, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29458204/a-review-of-implantable-biosensors-for-closed-loop-glucose-control-and-other-drug-delivery-applications
#3
Kee Scholten, Ellis Meng
Closed-loop drug delivery promises autonomous control of pharmacotherapy through the continuous monitoring of biomarker levels. For decades, researchers have strived for portable closed-loop systems, capable of treating ambulatory patients with chronic conditions such as diabetes mellitus. After years of development, the first of these systems have left the laboratory and entered commercial use. This long-awaited advance reflects recent development of chronically stable implantable biosensors, able to accurately measure biomarker levels in vivo...
February 16, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29458110/investigation-of-adhesive-interactions-in-the-specific-targeting-of-triptorelin-conjugated-peg-coated-magnetite-nanoparticles-to-breast-cancer-cells
#4
Jingjie Hu, Sina Youssefian, John Obayemi, Karen Malatesta, Nima Rahbar, Winston Soboyejo
The understanding of adhesive interaction at the nanoscale between functionalized nanoparticles and biological cells is of great importance to develop effective theranostic nanocarriers for targeted cancer therapy. Here, we report a combination of experimental and computational approaches to evaluate the adhesion between Triptorelin (a Luteinizing Hormone-Releasing Hormone (LHRH) agonist)-conjugated poly-(ethylene glycol) (PEG)-coated magnetite nanoparticles (Triptorelin-MNPs) and breast cells. The adhesion forces between Triptorelin-MNPs and normal/cancerous breast cells are obtained using atomic force microscopy...
February 16, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29458023/structural-characterization-of-the-hcov-229e-fusion-core
#5
Wei Zhang, Qianqian Zheng, Mengrong Yan, Xiaobo Chen, Haitao Yang, Weihong Zhou, Zihe Rao
HCoV-229E spike (S) protein mediates virion attachment to cells and subsequent fusion of the viral and cellular membranes. This protein is composed of an N-terminal receptor-binding domain (S1) and a C-terminal trans-membrane fusion domain (S2). S2 contains a highly conserved heptad repeat 1 and 2 (HR1 and HR2). In this study, the HRs sequences were designed and connected with a flexible linker. The recombinant fusion core protein was crystallized and its structure was solved at a resolution of 2.45 Å. Then we characterized the binding of HR1s and HR2s via both sequence alignment and structural analysis...
February 16, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29457894/small-molecule-allosteric-modulators-of-g-protein-coupled-receptors-drug-target-interactions
#6
Shaoyong Lu, Jian Zhang
G-protein-coupled receptors (GPCRs) are the largest class of signaling receptors that are most frequently targeted by therapeutic drugs. Allosteric modulators bound to GPCRs at allosteric sites provide the potential for differential selectivity and improved safety compared with traditional orthosteric ligands. The recent breakthroughs in GPCR structural biology have made structures of GPCRs from classes A, B, C, and F complexed with small-molecule allosteric modulators available. Knowledge on the detailed receptor-modulator interactions at the allosteric sites is useful for structure-based GPCR drug design of novel therapeutics...
February 19, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29457719/fabrication-of-bsa-auncs-based-nanostructures-for-cell-fluoresce-imaging-and-target-drug-delivery
#7
Caifeng Ding, Yujuan Xu, Yanan Zhao, Hua Zhong, Xiliang Luo
Drug delivery which can offer efficient and localized drug transportation together with imaging capabilities is highly demanded in the development of cancer theranostic approaches. Herein, we report the construction of bovine serum albumin (BSA) gold nanoclusters (BSA@AuNCs) for cell fluoresce imaging and target drug delivery. BSA@AuNCs were modified with cyclic arginine-glycine-aspartate (cRGD) with the product RGD-BSA@AuNCs to enhance the cell internalization of the nanoclusters. Furthermore, doxorubicin (DOX), a widely used a chemotherapy drug, was also used to modify RGD-BSA@AuNCs...
February 19, 2018: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29457713/probing-structural-changes-among-analogous-inhibitor-bound-forms-of-hiv-1-protease-and-a-drug-resistant-mutant-in-solution-by-nuclear-magnetic-resonance
#8
Shahid N Khan, John D Persons, Janet L Paulsen, Michel Guerrero, Celia A Schiffer, Nese Kurt-Yilmaz, Rieko Ishima
In the era of state-of-the-art inhibitor design and high-resolution structural studies, detection of significant but small protein structural differences in the inhibitor-bound forms is critical to further developing the inhibitor. Here, we probed differences in HIV-1 protease (PR) conformation among darunavir and four analogous inhibitor-bound forms and compared them with a drug-resistant mutant using nuclear magnetic resonance chemical shifts. Changes in amide chemical shifts of wild-type (WT) PR among these inhibitor-bound forms, ΔCSP, were subtle but detectable and extended >10 Å from the inhibitor-binding site, asymmetrically between the two subunits of PR...
February 19, 2018: Biochemistry
https://www.readbyqxmd.com/read/29457674/a-review-of-brain-stimulation-methods-to-treat-substance-use-disorders
#9
REVIEW
Alexandria S Coles, Karolina Kozak, Tony P George
BACKGROUND: Substance use disorders (SUDs) are a leading cause of disability worldwide. While several pharmacological and behavioral treatments for SUDs are available, these may not be effective for all patients. Recent studies using non-invasive neuromodulation techniques including Repetitive Transcranial Magnetic Stimulation (rTMS), Transcranial Direct Current Stimulation (tDCS), and Deep Brain Stimulation (DBS) have shown promise for SUD treatment. OBJECTIVE: Multiple studies were evaluated investigating the therapeutic potential of non-invasive brain stimulation techniques in treatment of SUDs...
February 19, 2018: American Journal on Addictions
https://www.readbyqxmd.com/read/29456815/crispr-cas9-a-new-approach-to-successful-knockdown-of-abcb1-p-glycoprotein-and-reversal-of-chemosensitivity-in-human-epithelial-ovarian-cancer-cell-line
#10
Leyla Norouzi-Barough, Mohammadreza Sarookhani, Rasoul Salehi, Mohammadreza Sharifi, Sahar Moghbelinejad
Objectives: Multidrug resistance (MDR) is a major obstacle in the successful chemotherapy of ovarian cancer. Inhibition of P-glycoprotein (P-gp), a member of ATP-binding cassette (ABC) transporters, is a well-known strategy to overcome MDR in cancer. The aim of this study was to investigate the efficiency and ability of CRISPR/Cas9 genome editing technology to knockdown ABCB1 gene expression in adriamycin resistant (A2780/ADR) ovarian cancer cell line and evaluate the sensitivity changes to doxorubicin...
February 2018: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/29456508/the-molecular-determinants-of-small-molecule-ligand-binding-at-p2x-receptors
#11
Gaia Pasqualetto, Andrea Brancale, Mark T Young
P2X receptors are trimeric eukaryotic ATP-gated cation channels. Extracellular ATP-their physiological ligand-is released as a neurotransmitter and in conditions of cell damage such as inflammation, and substantial evidence implicates P2X receptors in diseases including neuropathic pain, cancer, and arthritis. In 2009, the first P2X crystal structure, Danio rerio P2X4 in the apo - state, was published, and this was followed in 2012 by the ATP-bound structure. These structures transformed our understanding of the conformational changes induced by ATP binding and the mechanism of ligand specificity, and enabled homology modeling of mammalian P2X receptors for ligand docking and rational design of receptor modulators...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29456449/international-comparison-of-five-herbal-medicine-registration-systems-to-inform-regulation-development-united-kingdom-germany-united-states-of-america-united-arab-emirates-and-kingdom-of-bahrain
#12
Azhar H Alostad, Douglas T Steinke, Ellen I Schafheutle
Background: Herbal medicine (HM) regulation is less developed than that of allopathic medicines, with some countries lacking specific regulations. Objective: For the purpose of informing a registration system for HMs in Kuwait, which does not manufacture but imports all HMs, this study compared the similarities and differences between the current HM registration systems of five countries. Methods: The five countries were selected as major source countries of HM in Kuwait (United Kingdom (UK), Germany and United States of America (USA)) or because of geographical proximity or size and approach (United Arab Emirates (UAE) and Kingdom of Bahrain)...
2018: Pharmaceutical Medicine
https://www.readbyqxmd.com/read/29456387/clinico-epidemiological-profile-of-pediatric-rheumatology-disorders-in-eastern-india
#13
Pratap Kumar Patra, Manish Kumar
Background: Data on rheumatological disorders in children from developing countries like India are scarce. Hence, this study aimed to understand the clinical and epidemiological profile of rheumatological disorders in children as this can help organize comprehensive evidence-based health care services. Methodology: A retrospective hospital-based study was designed in pediatric rheumatology clinic of the All India Institute of Medical Sciences, Patna, India, from January 2015 to December 2016...
January 2018: Journal of Natural Science, Biology, and Medicine
https://www.readbyqxmd.com/read/29456273/the-effects-of-acute-cannabis-use-on-nontraffic-injury-risk-reviewing-the-available-literature-and-identifying-ways-forward
#14
Gabriel Andreuccetti, Yu Ye, Jaewook Kang, Rachael Korcha, Jane A Witbrodt, Heraclito B Carvalho, Cheryl J Cherpitel
Recent evidence has indicated that cannabis use before driving is associated with a modest but increased risk for traffic-related injuries. However, the question of whether recent cannabis use is associated with a greater risk for other types of injuries remains unanswered. Aiming to understand better how acute cannabis use might affect the risk for all causes of injury, we have summarized the limited data available in the literature on the risk of non-traffic injuries associated with recent cannabis use. Very few studies were able to provide estimate risks for all injuries or injuries other than those related to road traffic injuries, with the limited evidence available showing mixed findings...
June 2017: Contemporary Drug Problems
https://www.readbyqxmd.com/read/29456107/design-synthesis-and-discovery-of-5-1-3-diphenyl-1h-pyrazol-4-yl-methylene-pyrimidine-2-4-6-1h-3h-5h-triones-and-related-derivatives-as-novel-inhibitors-of-mpges-1
#15
Kai Ding, Ziyuan Zhou, Shuo Zhou, Yaxia Yuan, Kyungbo Kim, Ting Zhang, Xirong Zheng, Fang Zheng, Chang-Guo Zhan
Human mPGES-1 has emerged as a promising target in exploring a next generation of anti-inflammatory drugs, as selective mPGES-1 inhibitors are expected to discriminatively suppress the production of induced PGE2 without blocking the normal biosynthesis of other prostanoids including homeostatic PGE2 . Therefore, this therapeutic approach is believed to reduce the adverse effects associated with the application of traditional non-steroidal anti-inflammatory drugs (tNSAIDs) and selective COX-2 inhibitors (coxibs)...
February 8, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29455987/design-and-biological-response-of-doxycycline-loaded-chitosan-microparticles-for-periodontal-disease-treatment
#16
Silvana Gjoseva, Nikola Geskovski, Simona Dimchevska Sazdovska, Riste Popeski-Dimovski, Gjorgji Petruševski, Kristina Mladenovska, Katerina Goracinova
The aim of this study was to develop chitosan (CS) microparticulated mucoadhesive drug delivery system (DDS) with improved therapeutic performance and biological responce. Ionotropic gelation/spray drying process was used for preparation of doxycycline hyclate (DOXY) loaded low and medium molecular weight (LMw and MMw) CS/sodium tripolyphosphate microparticles (CS/TPP MPs), further coated with ethyl cellulose (EC) using coacervation/solvent displacement technique. The relevant physico-chemical and biopharmaceutical properties were optimized using experimental design approach...
April 15, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29455936/engineering-a-clinically-translatable-bioartificial-pancreas-to-treat-type-i-diabetes
#17
REVIEW
Gorka Orive, Dwaine Emerich, Ali Khademhosseini, Shinichi Matsumoto, R M Hernández, J L Pedraz, Tejal Desai, Riccardo Calafiore, Paul de Vos
Encapsulating, or immunoisolating, insulin-secreting cells within implantable, semipermeable membranes is an emerging treatment for type 1 diabetes. This approach can eliminate the need for immunosuppressive drug treatments to prevent transplant rejection and overcome the shortage of donor tissues by utilizing cells derived from allogeneic or xenogeneic sources. Encapsulation device designs are being optimized alongside the development of clinically viable, replenishable, insulin-producing stem cells, for the first time creating the possibility of widespread therapeutic use of this technology...
February 15, 2018: Trends in Biotechnology
https://www.readbyqxmd.com/read/29455637/molecular-dynamics-of-interaction-of-sesamin-and-related-compounds-with-the-cancer-marker-%C3%AE-catenin-an-in-silico-study
#18
Bindu Madhuri Cavuturu, Vishwambar Vishnu Bhandare, Amutha Ramaswamy, Neelakantan Arumugam
By virtue of their regulatory role in the biological process, certain protein-protein complexes form potential targets for designing and discovery of drugs. Alteration set in the controlled formation of such complexes results in dysregulation of several metabolic processes, leading to diseased condition. β-catenin/Tcf4 complex is one such protein-protein complex found altered in colorectal epithelial cells resulting in activation of target genes leading to cancer. Recently certain lignans from seeds of the oil crop sesame were found inhibiting initiation and progression of this type of cancer...
February 18, 2018: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29455526/structure-based-optimization-strategies-for-g-protein-coupled-receptor-gpcr-allosteric-modulators-a-case-study-from-analyses-of-new-metabotropic-glutamate-receptor-5-mglu-5-x-ray-structures
#19
John Christopher, Zoltán Orgován, Miles Congreve, Andrew S Dore, James C Errey, Fiona H Marshall, Jonathan S Mason, Krzysztof Okrasa, Prakash Rucktooa, Maria J Serrano-Vega, György G Ferenczy, Gyorgy M Keseru
Two interesting new X-ray structures of negative allosteric modulator (NAM) ligands for the mGlu5 receptor, M-MPEP (3) and fenobam (4), are reported. The new structures show how the binding of the ligands induces different receptor water channel conformations to previously published structures. The structure of fenobam, where a urea replaces the acetylenic linker in M-MPEP and mavoglurant, reveals a binding mode where the ligand is rotated by 180º compared to a previously proposed docking model. The need for multiple ligand structures for accurate GPCR structure-based drug design is demonstrated by the different growing vectors identified for the head groups of M-MPEP and mavoglurant and by the unexpected water mediated receptor interactions of a new chemotype represented by fenobam...
February 18, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29455521/self-assembly-of-binuclear-cu-ii-histidine-complex-for-absolute-configuration-and-enantiomeric-excess-determination-of-naproxen-by-tandem-mass-spectrometry
#20
Xiangying Yu, Man-Chu Chau, Wai Kit Tang, Chi-Kit Siu, Zhong-Ping Yao
Naproxen is one of the most consumed non-steroidal anti-inflammatory drugs and marketed as S-naproxen since R-naproxen is hepatotoxic. In this study, chiral recognition of naproxen has been investigated by tandem mass spectrometry (MS/MS). Among all diastereomeric complexes formed between naproxen and the examined chiral selectors, including cyclodextrins (α/β/γ-CD), modified phenylalanines (N-acetyl-phenylalanine, N-t-butoxycarbonyl-phenylalanine, N-9-fluorenylmethyloxycarbonyl-phenylalanine), amino acids (Trp, Phe, Tyr, His), glucose, tartaric acid and vancomycin, a novel binuclear metal bound diastereomeric complexes [(M(II))2 (S/R-Naproxen)(L-His)2 -3H]+ (M = Cu, Ni or Co with Cu being the best) could allow effective identification of the absolute configuration of naproxen and determination of its enantiomeric excess (ee) through MS/MS analysis...
February 17, 2018: Analytical Chemistry
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