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https://www.readbyqxmd.com/read/29775717/temozolomide-loaded-nano-lipid-based-chitosan-hydrogel-for-nose-to-brain-delivery-characterization-nasal-absorption-histopathology-and-cell-line-study
#1
Anam Khan, Mohd Aqil, Syed Sarim Imam, Abdul Ahad, Yasmin Sultana, Asgar Ali, Khalid Khan
The present study was designed to develop and optimize Temozolomide nano lipid chitosan gel delivery (TMZNLCHG) to target the brain through nasal route. The formulation was developed using chitosan as a gelling agent and Vit E: gelucire 44/14 blend as lipid. The formulations were evaluated for particle size, drug loading, morphology, drug release, nasal diffusion, cell line study, and histopathology study. The average particle size, PDI, %EE, loading, drug release, and % permeation were found to be 134 nm, 0...
May 15, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29775690/molecular-subtyping-of-colorectal-cancer-recent-progress-new-challenges-and-emerging-opportunities
#2
REVIEW
Wei Wang, Raju Kandimalla, Hao Huang, Lina Zhu, Ying Li, Feng Gao, Ajay Goel, Xin Wang
Colorectal cancer (CRC) is one of the leading causes of cancer-related deaths worldwide. Similar to many other malignancies, CRC is a heterogeneous disease, making it a clinical challenge for optimization of treatment modalities in reducing the morbidity and mortality associated with this disease. A more precise understanding of the biological properties that distinguish patients with colorectal tumors, especially in terms of their clinical features, is a key requirement towards a more robust, targeted-drug design, and implementation of individualized therapies...
May 15, 2018: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/29775647/exposure-to-imipenem-cilastatin-causes-nephrotoxicity-and-even-urolithiasis-in-wistar-rats
#3
Amal Tahri, Amina Lahyani, Rim Kallel, Fatma Ayadi, Tahia Boudawara, Zouheir Sahnoun
Imipenem/cilastatin is a broad-spectrum β-lactam antibiotic used to treat several bacterial infections. The present study was designed to validate the nephrotoxic effect of this drug in rats and to explore its potentional urolithiatic effect. Thirty two Wistar rats were randomly divided into four groups: three experimental groups treated with different imipenem/cilastatin dosages (30, 50 and 80 mg/kg/day) and a control group.The experimental groups were given intraperitoneal imipenem/cilastatin injections twice daily for 7 days, and the control group was given intraperitoneal vehicle NaCl 0...
May 15, 2018: Toxicology
https://www.readbyqxmd.com/read/29775277/cid-9998128-compound-is-a-potential-multi-target-drug-for-alzheimer-s-disease
#4
Nguyen Quoc Thai, Zuzana Bednarikova, Miroslav Gancar, Huynh Quang Linh, Chin-Kun Hu, Mai Suan Li, Zuzana Gazova
We have probed capability of small CID 9998128 compound as a potential multi-target drug for the Alzheimer's disease (AD) using in silico and in vitro experiments. By all-atom simulation and MM-PBSA method we have demonstrated that this compound strongly binds to both amyloid beta 42 (Aβ42 ) fibrils and β-secretase and the van der Waals interaction is dominating over the electrostatic interaction in binding affinity. A detailed analysis at the atomic level revealed that indazole in CID 99998128 structure made a major contribution to instability of all studied complexes...
May 18, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29775190/phosphonium-carbosilane-dendrimers-interaction-with-a-simple-biological-membrane-model
#5
Dominika Wrobel, Radka Kubikova, Monika Müllerová, Tomas Strašák, Květoslav RůŽička, Michal Fulem, Jan Maly
The influence of three generations of five different phosphonium carbosilane dendrimers and one ammonium carbosilane dendrimer as a reference (PMe3, PBu3, P(Et2)2(CH2)3OH, PPh3, P(MeOPh)3 and NMe3, peripheral functional groups) on dimyristoylphosphatidylcholine (DMPC) or a lipid mixture dimyristoylphosphatidylcholine/dimyristoylphosphatidylglycerol (DMPC/DMPG) of liposomes was studied by fluorescence polarization measurements and differential scanning calorimetry. All types of dendrimers interacted with neutral as well as negatively charged liposomes, but the strength and observed influence were different...
May 18, 2018: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29774657/cheminformatics-in-drug-discovery-an-industrial-perspective
#6
REVIEW
Hongming Chen, Thierry Kogej, Ola Engkvist
Cheminformatics has established itself as a core discipline within large scale drug discovery operations. It would be impossible to handle the amount of data generated today in a small molecule drug discovery project without persons skilled in cheminformatics. In addition, due to increased emphasis on "Big Data", machine learning and artificial intelligence, not only in the society in general, but also in drug discovery, it is expected that the cheminformatics field will be even more important in the future...
May 18, 2018: Molecular Informatics
https://www.readbyqxmd.com/read/29774608/virion-like-membrane-breaking-nanoparticles-with-tumor-activated-cell-and-tissue-dual-penetration-conquer-impermeable-cancer
#7
Xiao Zhang, Xianghui Xu, Yachao Li, Cheng Hu, Zhijun Zhang, Zhongwei Gu
Poor drug penetration into tumor cells and tissues is a worldwide difficulty in cancer therapy. A strategy is developed for virion-like membrane-breaking nanoparticles (MBNs) to smoothly accomplish tumor-activated cell-and-tissue dual-penetration for surmounting impermeable drug-resistant cancer. Tailor-made dendritic arginine-rich peptide prodrugs are designed to mimic viral protein transduction domains and globular protein architectures. Attractively, these protein mimics self-assemble into virion-like nanoparticles in aqueous solution, having highly ordered secondary structure...
May 17, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29774603/programmed-nanoparticle-loaded-nanoparticles-for-deep-penetrating-3d-cancer-therapy
#8
Jinhwan Kim, Changshin Jo, Won-Gwang Lim, Sungjin Jung, Yeong Mi Lee, Jun Lim, Haeshin Lee, Jinwoo Lee, Won Jong Kim
Tumors are 3D, composed of cellular agglomerations and blood vessels. Therapies involving nanoparticles utilize specific accumulations due to the leaky vascular structures. However, systemically injected nanoparticles are mostly uptaken by cells located on the surfaces of cancer tissues, lacking deep penetration into the core cancer regions. Herein, an unprecedented strategy, described as injecting "nanoparticle-loaded nanoparticles" to address the long-lasting problem is reported for effective surface-to-core drug delivery in entire 3D tumors...
May 18, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29774442/integrated-models-of-care-for-individuals-with-opioid-use-disorder-how-do-we-prevent-hiv-and-hcv
#9
REVIEW
Katherine M Rich, Joshua Bia, Frederick L Altice, Judith Feinberg
PURPOSE OF REVIEW: To describe models of integrated and co-located care for opioid use disorder (OUD), hepatitis C (HCV), and HIV. RECENT FINDINGS: The design and scale-up of multidisciplinary care models that engage, retain, and treat individuals with HIV, HCV, and OUD are critical to preventing continued spread of HIV and HCV. We identified 17 models within primary care (N = 3), HIV specialty care (N = 5), opioid treatment programs (N = 6), transitional clinics (N = 2), and community-based harm reduction programs (N = 1), as well as two emerging models...
May 17, 2018: Current HIV/AIDS Reports
https://www.readbyqxmd.com/read/29774078/targeting-intracellular-mmps-efficiently-inhibits-tumor-metastasis-and-angiogenesis
#10
Yaqi Lv, Xiangmei Zhao, Lidan Zhu, Sijia Li, Qingqing Xiao, Wei He, Lifang Yin
Treatment for metastatic cancer is a great challenge throughout the world. Commonly, directed inhibition of extracellular matrix metalloproteinases (MMPs) secreted by cancer cells can reduce metastasis. Here, a novel nanoplatform (HPMC NPs) assembled from hyaluronic acid (HA)-paclitaxel (PTX) prodrug and marimastat (MATT)/β-casein (CN) complexes was established to cure a 4T1 metastatic cancer model via targeting CD44 and intracellular, rather than extracellular, MMPs. Methods: HPMC NPs were prepared by assembling the complexes and prodrug under ultrasonic treatment, which the interaction between them was evaluated by förster resonance energy transfer, circular dichroism and fluorescence spectra...
2018: Theranostics
https://www.readbyqxmd.com/read/29774057/ocrelizumab-a-new-milestone-in-multiple-sclerosis-therapy
#11
REVIEW
Patricia Mulero, Luciana Midaglia, Xavier Montalban
B cells play a central role in the pathogenesis of multiple sclerosis (MS): they are involved in the activation of pro-inflammatory T cells, secretion of pro-inflammatory cytokines and production of autoantibodies directed against myelin. Hence, the use of B cell-depleting monoclonal antibodies as therapy for autoimmune diseases, including MS, has increased in recent years. Previous results with rituximab, the first therapeutic B cell-depleting chimeric monoclonal antibody that showed efficacy in MS clinical trials, encouraged researchers to evaluate the efficacy of a humanized anti-CD20 antibody, ocrelizumab, in MS...
2018: Therapeutic Advances in Neurological Disorders
https://www.readbyqxmd.com/read/29773899/management-of-acute-hcv-infection-in-the-era-of-direct-acting-antiviral-therapy
#12
REVIEW
Marianne Martinello, Behzad Hajarizadeh, Jason Grebely, Gregory J Dore, Gail V Matthews
The management of acute HCV infection has not been standardized following the availability of direct-acting antiviral agents (DAAs) for chronic HCV infection, and substantial uncertainty exists regarding the optimal treatment regimen and duration. Despite the lack of direct evidence, the 2016 American Association for the Study of Liver Diseases (AASLD)-Infectious Diseases Society of America (IDSA) guidelines supported "the same regimens for acute HCV as recommended for chronic HCV infection … owing to high efficacy and safety", whereas the 2016 European Association for the Study of the Liver (EASL) guidelines recommended sofosbuvir-ledipasvir, sofosbuvir-velpatasvir or sofosbuvir plus daclatasvir for 8 weeks in acute HCV infection, with a longer duration of 12 weeks recommended for those infected with HIV and/or baseline HCV RNA levels >1,000,000 IU/ml...
May 17, 2018: Nature Reviews. Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/29773873/therapeutic-nanoparticles-penetrate-leaves-and-deliver-nutrients-to-agricultural-crops
#13
Avishai Karny, Assaf Zinger, Ashima Kajal, Janna Shainsky-Roitman, Avi Schroeder
As the world population grows, there is a need for efficient agricultural technologies to provide global food requirements and reduce environmental toll. In medicine, nanoscale drug delivery systems grant improved therapeutic precision by overcoming biological barriers and enhancing drug targeting to diseased tissues. Here, we loaded nanoscale drug-delivery systems with agricultural nutrients, and applied them to the leaves of tomato plants. We show that the nanoparticles - liposomes composed of plant-derived lipids, penetrate the leaf and translocate in a bidirectional manner, distributing to other leaves and to the roots...
May 17, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29773424/a-device-for-high-throughput-monitoring-of-degradation-in-soft-tissue-samples
#14
D S Tzeranis, I Panagiotopoulos, S Gkouma, G Kanakaris, N Georgiou, N Vaindirlis, G Vasileiou, M Neidlin, A Gkousioudi, V Spitas, G A Macheras, L G Alexopoulos
This work describes the design and validation of a novel device, the High-Throughput Degradation Monitoring Device (HDD), for monitoring the degradation of 24 soft tissue samples over incubation periods of several days inside a cell culture incubator. The device quantifies sample degradation by monitoring its deformation induced by a static gravity load. Initial instrument design and experimental protocol development focused on quantifying cartilage degeneration. Characterization of measurement errors, caused mainly by thermal transients and by translating the instrument sensor, demonstrated that HDD can quantify sample degradation with <6 μm precision and <10 μm temperature-induced errors...
May 3, 2018: Journal of Biomechanics
https://www.readbyqxmd.com/read/29773394/grafting-of-steroids-to-hyaluronan-towards-the-design-of-delivery-systems-for-antioxidants-the-role-of-hydrophobic-core
#15
Gloria Huerta-Ángeles, Martina Brandejsová, Jaroslav Novotný, Kateřina Kopecká, Jana Šógorková, Daniela Šmejkalová, Vladimír Velebný
In this work, amphiphilic hyaluronic acid (HA) was synthesized by the chemical bonding of steroids. Particularly, succinyl cholesterol (SCH), cholic acid (CA), deoxycholic acid (DOCA), and 18β-glycyrrhetinic acid (GA) were activated by benzoyl chloride towards the esterification reaction of HA in water. The degree of substitution can be controlled by varying the feed ratio of mixed anhydride to HA and up to 25% (mol/mol) can be obtained. Due to mild reaction conditions, no degradation of the polysaccharide was observed...
August 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29773319/advancements-in-nanomedicine-for-multiple-myeloma
#16
REVIEW
Alexandre Detappe, Mark Bustoros, Tarek H Mouhieddine, P Peter Ghoroghchian
In the past decades, considerable progress has been made in our understanding and treatment of multiple myeloma. Several challenges remain including our abilities to longitudinally image tumor responses to treatment, to combine various therapeutic agents with different mechanisms of action but with overlapping toxicities, and to efficiently harness the power of the immune system to augment remission and/or to induce permanent cures. Nanomedicine may help to address many of these outstanding issues, affording novel diagnostic capabilities and offering disruptive technologies that promise to revolutionize treatment...
May 14, 2018: Trends in Molecular Medicine
https://www.readbyqxmd.com/read/29773063/conversion-of-protein-active-regions-into-peptidomimetic-therapeutic-leads-using-backbone-cyclization-and-cycloscan-how-to-do-it-yourself
#17
Samuel J S Rubin, Yftah Tal-Gan, Chaim Gilon, Nir Qvit
Protein-protein interactions (PPIs) are particularly important for controlling both physiologic and pathologic biological processes but are difficult to target due to their large and/or shallow interaction surfaces unsuitable for small molecules. Linear peptides found in nature interact with some PPIs, and protein active regions can be used to design synthetic peptide compounds for inhibition of PPIs. However, linear peptides are limited therapeutically by poor metabolic and conformational stability, which can compromise their bioactivity and half-life...
May 17, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29773055/crystal-engineering-upcoming-paradigm-for-efficacious-pulmonary-drug-delivery
#18
Preshita P Desai, Sanyat S Mapara, Vandana B Patravale
BACKGROUND AND OBJECTIVE: Pulmonary drug delivery has transformed over a past few decades from being a platform for local pulmonary disease treatment to systemic drug delivery opportunities. In case of pulmonary delivery systems, particle properties are critical as they affect inhalation efficacy, pulmonary deposition, drug delivery and overall performance. With this in view, particle engineering has emerged as an advanced science that helps in designing of efficacious pulmonary delivery systems...
May 17, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29772772/multiplicative-effects-of-social-and-psychological-risk-factors-on-college-students-suicidal-behaviors
#19
Shervin Assari
Less is known about the multiplicative effects of social and psychological risk and protective factors of suicidality on college campuses. The current study aimed to investigate the multiplicative effects of social (identifying oneself as gay/lesbian, financial difficulty, violence victimization, and religiosity) and psychological (anxiety, depression, problem alcohol use, drug use) and risk/protective factors on suicidal behaviors among college students in the United States. Using a cross-sectional design, the Healthy Mind Study (HMS; 2016⁻2017), is a national online survey of college students in the United States...
May 17, 2018: Brain Sciences
https://www.readbyqxmd.com/read/29772746/design-synthesis-and-biological-evaluation-of-benzimidazole-derived-biocompatible-copper-ii-and-zinc-ii-complexes-as-anticancer-chemotherapeutics
#20
Mohamed F AlAjmi, Afzal Hussain, Md Tabish Rehman, Azmat Ali Khan, Perwez Alam Shaikh, Rais Ahmad Khan
Herein, we have synthesized and characterized a new benzimidazole-derived "BnI" ligand and its copper(II) complex, [Cu(BnI)₂], 1 , and zinc(II) complex, [Zn(BnI)₂], 2 , using elemental analysis and various spectroscopic techniques. Interaction of complexes 1 and 2 with the biomolecules viz. HSA (human serum albumin) and DNA were studied using absorption titration, fluorescence techniques, and in silico molecular docking studies. The results exhibited the significant binding propensity of both complexes 1 and 2 , but complex 1 showed more avid binding to HSA and DNA...
May 16, 2018: International Journal of Molecular Sciences
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