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https://www.readbyqxmd.com/read/28926423/a-noninterventional-multicenter-prospective-phase-iv-study-of-trabectedin-in-patients-with-advanced-soft-tissue-sarcoma
#1
Angela Buonadonna, Charlotte Benson, Jose Casanova, Bernd Kasper, Antonio López Pousa, Filomena Mazzeo, Thomas Brodowicz, Nicolas Penel
This prospective, noninterventional study is the first phase IV trial designed to evaluate trabectedin in patients with advanced soft tissue sarcoma in real-life clinical practice across Europe. To be included in the study, patients must have received more than or equal to one cycle of trabectedin and be currently on treatment. The primary endpoint was progression-free survival as defined by investigators. The secondary endpoints included objective response rate, disease control rate, time to progression and the growth modulation index (GMI), overall survival, and an assessment of the cancer-related symptoms and safety...
September 18, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28926061/network-based-modelling-and-percolation-analysis-of-conformational-dynamics-and-activation-in-the-cdk2-and-cdk4-proteins-dynamic-and-energetic-polarization-of-the-kinase-lobes-may-determine-divergence-of-the-regulatory-mechanisms
#2
G M Verkhivker
The overarching goal of delineating molecular principles underlying differentiation of the activation mechanisms in cyclin-dependent kinases (CDKs) is important for understanding regulatory divergences among closely related kinases which can be exploited in drug discovery of targeted and allosteric inhibitors. To systematically characterize dynamic, energetic and network signatures of the activation mechanisms, we combined atomistic simulations and elastic network modeling with the analysis of the residue interaction networks and rigidity decomposition of the CDK2-cyclin A and CDK4-cyclin D1/D3 complexes...
September 19, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28925888/a-self-nanoemulsifying-drug-delivery-system-for-poorly-water-soluble-tolbutamide-development-optimization-and-pharmacodynamic-studies
#3
Deepti Pandita, Neelam Kumari, Viney Lather
The current investigation involves the development of a thermodynamically stable and dilutable self-nanoemulsifying drug delivery system (SNEDDS) for tolbutamide, a poorly water soluble hypoglycemic drug, in order to achieve higher water solubility and enhanced dissolution rate which in turn improves its oral bioavailability. Pseudo-ternary phase diagrams suggested the suitability of oleic acid (lipid), Tween 20 (surfactant) and PEG 400 (co-surfactant) for developing the SNEEDS formulations. The optimal SNEDDS formulation having mean globule diameter, viscosity, polydispersity value of 58...
September 15, 2017: Pharmaceutical Nanotechnology
https://www.readbyqxmd.com/read/28925725/light-sensitive-drugs-in-topical-formulations-stability-indicating-methods-and-photostabilization-strategies
#4
Giuseppina Ioele, Lorena Tavano, Michele De Luca, Rita Muzzalupo, Annalisa Mancuso, Gaetano Ragno
Photostability tests applied on commercial specialties for topical use have demonstrated a greater vulnerability of several drugs, due to greater exposure to light than other pharmaceutical forms. Photodegradation of a drug can considerably modify its pharmacokinetic behavior by varying the therapeutic index. The evaluation of the degradation profile of a drug, according to the ICH rules, is of primary importance in developing an appropriate topical formulation. Advanced strategies have been proposed to increase the protection from the light of the photolabile drugs...
September 19, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28925709/effect-of-hydrophobic-chain-length-on-the-stability-and-guest-exchange-behavior-of-shell-sheddable-micelles-formed-by-disulfide-linked-diblock-copolymers
#5
Haiyan Fan, Yixia Li, Jinxian Yang, Xiaodong Ye
Reduction-responsive micelles hold enormous promise for the application as drug carriers due to the fast drug release triggered by reducing conditions and high anticancer activity. However, the effect of hydrophobic chain length on the stability and guest exchange of reduction-responsive micelles, especially for the micelles formed by diblock copolymers containing single disulfide group, are not fully understood. Here, shell-sheddable micelles formed by a series of disulfide-linked copolymer poly(ethylene glycol)-b-poly(-caprolactone) (PEG-SS-PCL) containing the same chain length of PEG but different chain lengths of hydrophobic block PCL were prepared and well characterized...
September 19, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28925395/small-molecules-targeted-to-the-microtubule-hec1-interaction-inhibit-cancer-cell-growth-through-microtubule-stabilization
#6
M Ferrara, G Sessa, M Fiore, F Bernard, I A Asteriti, E Cundari, G Colotti, S Ferla, M Desideri, S Buglioni, D Trisciuoglio, D Del Bufalo, A Brancale, F Degrassi
Highly expressed in cancer protein 1 (Hec1) is a subunit of the kinetochore (KT)-associated Ndc80 complex, which ensures proper segregation of sister chromatids at mitosis by mediating the interaction between KTs and microtubules (MTs). HEC1 mRNA and protein are highly expressed in many malignancies as part of a signature of chromosome instability. These properties render Hec1 a promising molecular target for developing therapeutic drugs that exert their anticancer activities by producing massive chromosome aneuploidy...
September 18, 2017: Oncogene
https://www.readbyqxmd.com/read/28925394/tissue-inhibitor-of-metalloproteinase-1-promotes-cell-proliferation-through-yap-taz-activation-in-cancer
#7
T Ando, D Charindra, M Shrestha, H Umehara, I Ogawa, M Miyauchi, T Takata
Tissue inhibitor of metalloproteinase-1 (TIMP-1), a member of the TIMP family (TIMP-1 to 4), is highly expressed in various types of cancer and forms a complex with its receptor CD63 and Integrin β1. However, the precise oncogenic mechanism of TIMP-1 remains unclear. Yes-associated protein (YAP) and transcriptional co-activator with PDZ binding motif (TAZ) are transcription co-activators enhancing the transcription of specific genes related to cell proliferation. But the mechanism of aberrant YAP/TAZ activation in cancer is not fully understood...
September 18, 2017: Oncogene
https://www.readbyqxmd.com/read/28925033/polyamine-mediated-stoichiometric-assembly-of-ribonucleoproteins-for-enhanced-mrna-delivery
#8
Jiahe Li, Yanpu He, Wade Wang, Connie Wu, Celestine Hong, Paula T Hammond
Messenger RNA (mRNA) represents a promising class of nucleic acid drugs. Although numerous carriers have been developed for mRNA delivery, the inefficient mRNA expression inside cells remains a major challenge. Inspired by the dependence of mRNA on 3'-terminal polyadenosine nucleotides (poly A) and poly A binding proteins (PABPs) for optimal expression, we complexed synthetic mRNA containing a poly A tail with PABPs in a stoichiometric manner and stabilized the ribonucleoproteins (RNPs) with a family of polypeptides bearing different arrangements of cationic side groups...
September 19, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28924948/magnetic-nanoparticles-for-the-delivery-of-dapagliflozin-to-hypoxic-tumors-physicochemical-characterization-and-cell-studies
#9
Athina Angelopoulou, Efstathia Voulgari, Argiris Kolokithas-Ntoukas, Aristides Bakandritsos, Konstantinos Avgoustakis
In solid tumors, hypoxia (lack of oxygen) is developed, which leads to the development of resistance of tumor cells to chemotherapy and radiotherapy through various mechanisms. Nevertheless, hypoxic cells are particularly vulnerable when glycolysis is inhibited. For this reason, in this study, the development of magnetically targetable nanocarriers of the sodium-glucose transporter protein (SGLT2) inhibitor dapagliflozin (DAPA) was developed for the selective delivery of DAPA in tumors. This nanomedicine in combination with radiotherapy or chemotherapy should be useful for effective treatment of hypoxic tumors...
September 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28924730/effects-of-the-preparation-process-on-the-properties-of-amorphous-solid-dispersions
#10
Siyuan Huang, Robert O Williams
The use of amorphous solid dispersions to improve the bioavailability of active ingredients from the BCS II and IV classifications continues to gain interest in the pharmaceutical industry. Over the last decade, methods for generating amorphous solid dispersions have been well established in commercially available products and in the literature. However, the amorphous solid dispersions manufactured by different technologies differ in many aspects, primarily chemical stability, physical stability, and performance, both in vitro and in vivo...
September 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28923924/near-atomic-structure-of-jasplakinolide-stabilized-malaria-parasite-f-actin-reveals-the-structural-basis-of-filament-instability
#11
Sabrina Pospich, Esa-Pekka Kumpula, Julian von der Ecken, Juha Vahokoski, Inari Kursula, Stefan Raunser
During their life cycle, apicomplexan parasites, such as the malaria parasite Plasmodium falciparum, use actomyosin-driven gliding motility to move and invade host cells. For this process, actin filament length and stability are temporally and spatially controlled. In contrast to canonical actin, P. falciparum actin 1 (PfAct1) does not readily polymerize into long, stable filaments. The structural basis of filament instability, which plays a pivotal role in host cell invasion, and thus infectivity, is poorly understood, largely because high-resolution structures of PfAct1 filaments were missing...
September 18, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28923766/development-of-stability-enhanced-ternary-solid-dispersions-via-combinations-of-hpmcp-and-soluplus-%C3%A2-processed-by-hot-melt-extrusion
#12
Ahmad B Albadarin, Catherine B Potter, Mark Davis, Javed Iqbal, Sachin Korde, Sudhir Pagire, Anant Paradkar, Gavin Walker
The aim of this study was to evaluate a novel combination of hydroxypropyl methylcellulose phthalate (HPMCP-HP-50) and Soluplus(®) polymers for enhanced physicochemical stability and solubility of the produced amorphous solid dispersions (ASDs). This was achieved using hot melt extrusion (HME) to convert the crystalline active pharmaceutical ingredient (API) into a more soluble amorphous form within the ternary systems. Itraconazole (ITZ), a Biopharmaceutics Classification System class II (BCS II) API, was utilized as the model drug...
September 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28922598/proteolytic-unlocking-of-ultra-stable-twin-acylhydrazone-linkers-for-lysosomal-acid-triggered-release-of-anticancer-drugs
#13
Yiwu Zheng, Jing Ren, Yaqi Wu, Xiaoting Meng, Yibing Zhao, Chuanliu Wu
Targeted prodrugs exploiting cleavable linkers capable of responding to endogenous stimuli have increasingly been explored for cancer therapy. Successful application of these prodrug designs relies on the manipulation of both stability and responsiveness of the cleavable linkers, which, however, are difficult to be finely regulated, particularly for acid-responsive acylhydrazone bonds. Here we developed a new class of peptide-bridged twin-acylhydrazone linkers (PTA linkers) displaying both an ultrahigh stability and a rapid responsiveness-highly stable in neutral and acidic conditions due to effect of cooperativity between the two acylhydrazone bonds, easily cleavable in acidic conditions after enzymatically-triggered unlocking of the two bonds...
September 18, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28921988/interaction-of-food-additives-with-intestinal-efflux-transporters
#14
Noora Sjöstedt, Feng Deng, Oskari Rauvala, Tuomas Tepponen, Heidi Kidron
Breast cancer resistance protein (BCRP), multidrug resistance associated protein 2 (MRP2) and P-glycoprotein (P-gp) are ABC transporters that are expressed in the intestine, where they are involved in the efflux of many drugs from enterocytes back into the intestinal lumen. The inhibition of BCRP, MRP2 and P-gp can result in the enhanced absorption and exposure of substrate drugs. Food additives are widely used by the food industry to improve the stability, flavor and consistency of food products. Although they are considered safe for consumption, their interactions with intestinal transporters are poorly characterized...
September 18, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28921691/quantitative-determination-and-validation-of-octreotide-acetate-using-1-h-nmr-spectroscopy-with-internal-standard-method
#15
Chen Yu, Qian Zhang, Peng-Yao Xu, Yin Bai, Wen-Bin Shen, Bin Di, Meng-Xiang Su
Quantitative nuclear magnetic resonance (qNMR) is a well-established technique in quantitative analysis. We presented a validated (1) H quantitative nuclear magnetic resonance ((1) H-qNMR) method for assay of octreotide acetate (OCT-Ac), a kind of cyclic octopeptide. Deuterium oxide was used to remove the undesired exchangeable peaks, which was referred to as proton exchange, in order to make the quantitative signals isolated in the crowded spectrum of the peptide and ensure precise quantitative analysis. Gemcitabine hydrochloride was chosen as the suitable internal standard (IS)...
September 15, 2017: Magnetic Resonance in Chemistry: MRC
https://www.readbyqxmd.com/read/28921497/quantitative-analysis-of-nucleic-acid-stability-with-ligands-under-high-pressure-to-design-novel-drugs-targeting-g-quadruplexes
#16
Shuntaro Takahashi, Naoki Sugimoto
Nucleic acids (DNA and RNA) can form various non-canonical structures. Because some serious diseases are caused by the conformational change of G-quadruplex DNA structures, the development of ligands that bind and stabilize G-quadruplex DNA is of interest to the field of nucleic acid chemistry. Volumetric changes (ΔV) in the biomolecular reaction include the structural change of biomolecules and hydration behaviors, which provide information about the tertiary interaction between G-quadruplex DNA and ligands...
September 18, 2017: Current Protocols in Nucleic Acid Chemistry
https://www.readbyqxmd.com/read/28921443/polyester-based-nanoparticles-for-the-encapsulation-of-monoclonal-antibodies
#17
Flávia Sousa, Pedro Fonte, Andreia Cruz, Patrick J Kennedy, Inês Mendes Pinto, Bruno Sarmento
Aliphatic polyesters have been widely explored for biomedical applications (e.g., drug delivery systems, biomedical devices, and tissue engineering). Recently, polyesters have been used in nanoparticle formulations for the controlled release of monoclonal antibodies (mAbs) for the enhanced efficacy of antibody-based therapy. Polyester-based nanoparticles for mAb delivery provide decreased antibody dosage, increased antibody stability and protection and longer therapeutic action, ultimately translating to an increased therapeutic index...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28920712/maximized-nanodrug-loaded-mesenchymal-stem-cells-by-a-dual-drug-loaded-mode-for-the-systemic-treatment-of-metastatic-lung-cancer
#18
Sen Yao, Xuqian Li, Jingxuan Liu, Yuqing Sun, Zhuanhe Wang, Yanyan Jiang
Mesenchymal stem cells (MSCs), exhibiting tumor-tropic and migratory potential, can serve as cellular carriers to improve the effectiveness of anticancer agents. However, several challenges, such as the safety issue, the limited drug loading, the conservation of stemness and migration of MSCs, still remain in the MSC-based delivery system. In the present study, a novel nano-engineered MSC delivery system was established by loading doxorubicin (DOX)-polymer conjugates for the systemic treatment of pulmonary metastasis of breast cancer...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28920684/stilbene-boronic-acids-form-a-covalent-bond-with-human-transthyretin-and-inhibit-its-aggregation
#19
Thomas P Smith, Ian W Windsor, Katrina T Forest, Ronald T Raines
Transthyretin (TTR) is a homotetrameric protein. Its dissociation into monomers leads to the formation of fibrils that underlie human amyloidogenic diseases. The binding of small molecules to the thyroxin-binding sites in TTR stabilizes the homotetramer and attenuates TTR amyloidosis. Herein, we report on boronic acid-substituted stilbenes that limit TTR amyloidosis in vitro. Assays of affinity for TTR and inhibition of its tendency to form fibrils were coupled with X-ray crystallographic analysis of nine TTR·ligand complexes...
September 18, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28920464/absorption-sites-of-orally-administered-drugs-in-the-small-intestine
#20
Teruo Murakami
In pharmacotherapy, drugs are mostly taken orally to be absorbed systemically from the small intestine, and some drugs are known to have preferential absorption sites in the small intestine. It would therefore be valuable to know the absorption sites of orally administered drugs and the influencing factors. Areas covered:In this review, the author summarizes the reported absorption sites of orally administered drugs, as well as, influencing factors and experimental techniques. Information on the main absorption sites and influencing factors can help to develop ideal drug delivery systems and more effective pharmacotherapies...
September 17, 2017: Expert Opinion on Drug Discovery
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