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https://www.readbyqxmd.com/read/28742140/short-16-mer-locked-nucleic-acid-splice-switching-oligonucleotides-restore-dystrophin-production-in-duchenne-muscular-dystrophy-myotubes
#1
Vanessa Borges Pires, Ricardo Simões, Kamel Mamchaoui, Célia Carvalho, Maria Carmo-Fonseca
Splice-switching antisense oligonucleotides (SSOs) offer great potential for RNA-targeting therapies, and two SSO drugs have been recently approved for treating Duchenne Muscular Dystrophy (DMD) and Spinal Muscular Atrophy (SMA). Despite promising results, new developments are still needed for more efficient chemistries and delivery systems. Locked nucleic acid (LNA) is a chemically modified nucleic acid that presents several attractive properties, such as high melting temperature when bound to RNA, potent biological activity, high stability and low toxicity in vivo...
2017: PloS One
https://www.readbyqxmd.com/read/28741876/discovery-of-novel-potent-muscarinic-m3-receptor-antagonists-with-proper-plasma-stability-by-structural-recombination-of-marketed-m3-antagonists
#2
Zuojuan Xiang, Jun Liu, Hongbin Sun, Xiaoan Wen
The marketed long-acting M3 antagonists for treatment of chronic obstructive pulmonary disease have inappropriate plasma stability (either overstable or excessively unstable), which causes substantial systemic exposure or poor patient compliance. To discover novel M3 antagonists with proper plasma stability, we synthesized and biologically evaluated a series of chiral quaternary ammonium salts of pyrrolidinol esters, which were designed by structural recombination of the marketed M3 antagonists. As a result, two novel potent M3 antagonists, (R/S)-3-[2-hydroxy-2,2-di(thiophen-2-yl)acetoxy]-1,1-dimethylpyrrolidinium bromides (1 a: Ki =0...
July 25, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28741242/the-weakening-effect-of-soluble-epoxide-hydrolase-inhibitor-auda-on-febrile-response-to-lipopolysaccharide-and-turpentine-in-rat
#3
Jakub Piotrowski, Tomasz Jędrzejewski, Małgorzata Pawlikowska, Agata Joanna Pacuła, Jacek Ścianowski, Wiesław Kozak
A still growing body of evidence suggests the importance of epoxyeicosatrienoic acids (EETs) in the regulation of inflammatory response; therefore, drugs that stabilize their levels by targeting the soluble epoxide hydrolase (sEH), an enzyme responsible for their metabolism, are currently under investigation. The effect of sEH inhibitors on molecular components of fever mechanism, i.e., on synthesis of pro-inflammatory cytokines or prostaglandins, has been repeatedly proven; however, the hypothesis that sEH inhibitors affect febrile response has never been tested...
July 24, 2017: Journal of Physiology and Biochemistry
https://www.readbyqxmd.com/read/28740614/new-class-of-antitrypanosomal-agents-based-on-imidazopyridines
#4
Daniel G Silva, J Robert Gillespie, Ranae M Ranade, Zackary M Herbst, Uyen T T Nguyen, Frederick S Buckner, Carlos A Montanari, Michael H Gelb
The present work describes the synthesis of 22 new imidazopyridine analogues arising from medicinal chemistry optimization at different sites on the molecule. Seven and 12 compounds exhibited an in vitro EC50 ≤ 1 μM against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei (T. brucei) parasites, respectively. Based on promising results of in vitro activity (EC50 < 100 nM), cytotoxicity, metabolic stability, protein binding, and pharmacokinetics (PK) properties, compound 20 was selected as a candidate for in vivo efficacy studies...
July 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28740601/synthesis-and-evaluation-of-a-linkable-functional-group-equipped-analogue-of-the-epothilones
#5
Corinne N Foley, Liang-An Chen, Dan L Sackett, James L Leighton
An approach to the validation of a linker strategy for the epothilone family of microtubule-stabilizing agents is reported. An analogue of epothilone B in which the C(6) methyl group has been replaced with a 4-azidobutyl group has been prepared by total chemical synthesis, and amides derived from the azido group have been shown to retain the activity of the parent compound. These results set the stage for an evaluation of the potential of the epothilones to serve as the drug component of antibody-drug conjugates and other selective tumor cell-targeting conjugates...
July 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28740381/chitosan-coated-diacerein-nanosuspensions-as-a-platform-for-enhancing-bioavailability-and-lowering-side-effects-preparation-characterization-and-ex-vivo-in-vivo-evaluation
#6
Ahmed N Allam, Sherif I Hamdallah, Ossama Y Abdallah
Nanodrug delivery systems have been widely reviewed for their use in several drug formulations to improve bioavailability, sustain effect, and decrease side effects of many candidate drugs. The objective of this study was to evaluate the potential of chitosan (CS)-coated nanosuspensions to enhance bioavailability and reduce the diarrheal side effect of diacerein (DCN) after oral administration. DCN nanosuspensions (DNS) were prepared by sonoprecipitation technique using different stabilizers at three different concentrations...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28739792/transfersomal-phage-cocktail-an-effective-treatment-against-methicillin-resistant-s-aureus-mrsa-mediated-skin-and-soft-tissue-infections-sstis
#7
Sanjay Chhibber, Ashu Shukla, Sandeep Kaur
Emergence of drug resistance has rekindled the interest in phage therapy as an alternative treatment option. Its potency, safety and proven efficacy is worth noting. However, phage therapy still suffers from issues of poor stability, narrow spectrum and poor pharmacokinetic profile. It therefore becomes essential to look into the use of Drug Delivery Systems (DDS) for efficient delivery of lytic phages in vivo For the first time, the present study has evaluated the use of nano-structured lipid based carriers i...
July 24, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28739504/improved-metabolic-stability-and-therapeutic-efficacy-of-a-novel-molecular-gemcitabine-phospholipid-complex
#8
Chander Parkash Dora, Varun Kushwah, Sameer S Katiyar, Pradeep Kumar, Viness Pillay, Sarasija Suresh, Sanyog Jain
The aim of the present research is to increase lipid solubility, metabolic stability and therapeutic efficacy of water soluble gemcitabine (GEM) via phospholipid complex (PC) formation. A novel phospholipid complex of GEM was successfully prepared and optimized. Physical interaction of GEM with phospholipid was evaluated by DSC, FT-IR, (1)H NMR, (31)P-NMR and P-XRD. SEM images of GEM-PC showed rough structure and TEM images of diluted aqueous dispersion of GEM-PC showed micellar structure. In silico study also revealed the significant interaction between drug and phospholipid...
July 21, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28739502/development-of-biomedical-5-fluorouracil-nanoplatforms-for-colon-cancer-chemotherapy-influence-of-process-and-formulation-parameters
#9
Elena Pretel, José L Arias, Laura Cabeza, Consolación Melguizo, José C Prados, Mireia Mallandrich, Joaquim Suñer, Beatriz Clares
In the present investigation solvent displacement or nanoprecipitation, and double emulsion/solvent evaporation methods were utilized to optimize poly(D,L-lactide-co-glycolide) nanoparticles for the vehiculization of the 5-fluorouracil. Formulation components from both the aqueous and organic phases, as well as, operating conditions were varied. Particles were characterized in terms of particle size and morphology, electrical properties, rheology, drug loading, stability, and drug release. Furthermore, in vitro cytotoxicity on human colon cells and different colon carcinoma cells was evaluated...
July 21, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28739375/oxidative-stress-and-inhibition-of-nitric-oxide-generation-underlie-methotrexate-induced-senescence-in-human-colon-cancer-cells
#10
Magdalena Dabrowska, Lukasz Uram, Zbigniew Zielinski, Wojciech Rode, Ewa Sikora
The response of human colon cancer C85 cells to methotrexate takes the form of reversible growth arrest of the type of stress-induced senescence. In the present study it is shown that during C85 cell progression into methotrexate-induced senescence, dihydrofolate reductase, the primary intracellular target for the drug, is stabilized at the protein level and its enzymatic activity, assayed in crude cellular extracts, decreases by 2-fold. Dihydrofolate reductase inhibition results in an increase in dihydrobiopterin level and an ultimate decrease in the tetrahydrobiopterin: dihydrobiopterin ratio in senescent cells...
July 21, 2017: Mechanisms of Ageing and Development
https://www.readbyqxmd.com/read/28738766/molecular-dynamics-and-biological-evaluation-of-2-chloro-7-cyclopentyl-7h-pyrrolo-2-3-d-pyrimidine-derivatives-against-breast-cancer
#11
Kulathooran Singaram, Dhamodaran Marimuthu, Selvakumar Baskaran, Suresh Kumar Chinaga, Dhivya Shanmugarajan, Thangavel Vadivel
In the present study, three series of 2-chloro-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidine derivatives 6(a-f), 7(a-c) and 8(a-c) have been synthesized and studied for their in vitro anti-cancer, antioxidant and receptor ligand interaction. Significant inhibition of MCF-7 cell line was observed for compounds 6e and 6f has compared with standard doxorubicin. However, these derivatives show good scavenging activities, perhaps compounds 7a, 8a, 6c and 6e show better antioxidant activities than ascorbic acid. Furthermore, molecular dynamics and simulation was conducted for best pose interacted compound 6e with active site of protein to study its stability and behaviour in nanoscale and in future this lead can serve as drug candidate to therapy ER-alpha for breast cancer...
July 24, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28738444/protein-coating-of-dna-nanostructures-for-enhanced-stability-and-immunocompatibility
#12
Henni Auvinen, Hongbo Zhang, Nonappa, Alisa Kopilow, Elina H Niemelä, Sami Nummelin, Alexandra Correia, Hélder A Santos, Veikko Linko, Mauri A Kostiainen
Fully addressable DNA nanostructures, especially DNA origami, possess huge potential to serve as inherently biocompatible and versatile molecular platforms. However, their use as delivery vehicles in therapeutics is compromised by their low stability and poor transfection rates. This study shows that DNA origami can be coated by precisely defined one-to-one protein-dendron conjugates to tackle the aforementioned issues. The dendron part of the conjugate serves as a cationic binding domain that attaches to the negatively charged DNA origami surface via electrostatic interactions...
July 24, 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/28738427/nanoemulsion-an-advanced-vehicle-for-efficient-drug-delivery
#13
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/28738425/preparation-and-characterization-of-pegylated-iron-oxide-gold-nanoparticles-for-delivery-of-sulforaphane-and-curcumin
#14
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/28738391/updated-palate-surgery-for-obstructive-sleep-apnea
#15
Hsueh-Yu Li
Initially described in 1981, uvulopalatopharyngoplasty was the first surgical procedure specially designed at the palatal level for snoring and obstructive sleep apnea (OSA). To date, palatal surgery remains the most commonly used surgery for OSA. The advancement of this surgery over the past 30 years has been a process of evolution in concepts, examination, and technique to increase safety and effectiveness in the treatment of OSA. Concept changes have emerged in the disease etiology, purpose of surgery, treatment priorities, staging of operations, integration therapy, and surgical endpoints...
2017: Advances in Oto-rhino-laryngology
https://www.readbyqxmd.com/read/28738270/chemical-structure-and-correlation-analysis-of-hiv-1-nnrt-and-nrt-inhibitors-and-database-curated-published-inhibition-constants-with-chemical-structure-in-diverse-datasets
#16
Birgit Viira, Alfonso T García-Sosa, Uko Maran
Human immunodeficiency virus (HIV-1) reverse transcriptase is a major target for designing anti-HIV drugs. Developed inhibitors are divided into non-nucleoside analog reverse-transcriptase inhibitors (NNRTIs) and nucleoside analog reverse-transcriptase inhibitors (NRTIs) depending on their mechanism. Given that many inhibitors have been studied and for many of them binding affinity constants have been calculated, it is beneficial to analyze the chemical landscape of these families of inhibitors and correlate these inhibition constants with molecular structure descriptors...
June 24, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28738158/efficient-interfacially-driven-vehiculization-of-corticosteroids-by-pulmonary-surfactant
#17
Alberto Hidalgo, Fabrizio Salomone, Nieves Fresno, Guillermo Orellana, Antonio Cruz, Jesus Perez-Gil
Pulmonary surfactant is a crucial system to stabilize the respiratory air-liquid interface. Furthermore, pulmonary surfactant has been proposed as an effective method for targeting drugs to the lungs. However, few studies have examined in detail the mechanisms of incorporation of drugs into surfactant, the impact of the presence of drugs on pulmonary surfactant performance at the interface under physiologically-meaningful conditions, or the ability of pulmonary surfactant to use the air-liquid interface to vehiculise drugs to long distances...
July 24, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28737673/magnetic-nanoemulsions-comparison-between-nanoemulsions-formed-by-ultrasonication-and-by-spontaneous-emulsification
#18
Nathalia Rodríguez-Burneo, Maria Antònia Busquets, Joan Estelrich
Nanoemulsions are particularly suitable as a platform in the development of delivery systems. The type of nanoemulsion with a higher stability will offer an advantage in the preparation of a delivery system for lipophilic drugs. Nanoemulsions can be fabricated by different processing methods, which are usually categorized as either high- or low-energy methods. In this study, a comparison between two methods of preparing magnetic oil-in-water (O/W) nanoemulsions is described. The nanoemulsions were formed by sonication (the high-energy method) or by spontaneous emulsification (the low-energy method)...
July 22, 2017: Nanomaterials
https://www.readbyqxmd.com/read/28736844/newly-designed-silica-containing-redox-nanoparticles-for-oral-delivery-of-novel-top2-catalytic-inhibitor-for-treating-colon-cancer
#19
Long Binh Vong, Shinya Kimura, Yukio Nagasaki
Although oral drug delivery is the most common route of drug administration, the conventional polymeric nanocarriers exhibit a low drug loading capacity and low stability in the gastrointestinal (GI) environments. In this study, a newly designed silica-containing redox nanoparticle (siRNP) with reactive oxygen species (ROS) scavenging capacity is developed as an ideal oral nanocarrier for a novel hydrophobic anticancer compound BNS-22 to treat colitis-associated colon cancer in vivo. Crosslinking of silica moieties significantly enhances the stability under acidic conditions and improves BNS-22 loading capacity of siRNP compared to the conventional redox nanoparticle...
July 24, 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/28736723/synthesis-and-characterization-of-bacterial-cellulose-and-gelatin-based-hydrogel-composites-for-drug-delivery-systems
#20
W Treesuppharat, P Rojanapanthu, C Siangsanoh, H Manuspiya, S Ummartyotin
Bacterial cellulose and gelatin were successfully used to develop a hydrogel composite material. Hydrogel was synthesized by copolymerization between bacterial cellulose and gelatin. Scanning electron microscopy (SEM) images showed that the bacterial cellulose chain was uniform in size and shape. Glutaraldehyde was employed as a crosslinking agent. H-bonds were formed via the reaction between the amine and hydroxyl groups, which were the functional groups of the gelatin and bacterial cellulose, respectively...
September 2017: Biotechnology Reports
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