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https://www.readbyqxmd.com/read/28219253/in-vitro-and-in-vivo-evaluation-of-macromolecular-prodrug-gc-fua-based-nanoparticle-for-hepatocellular-carcinoma-chemotherapy
#1
Can Huang, Na-Mei Li, Pei Gao, Sa Yang, Qian Ning, Wen Huang, Zhi-Ping Li, Peng-Ju Ye, Li Xiang, Dong-Xiu He, Xiang-Wen Tan, Cui-Yun Yu
A novel type of macromolecular prodrug delivery system is reported in this research. The N-galactosylated-chitosan-5-fluorouracil acetic acid conjugate (GC-FUA) based nanoparticle delivery system was evaluated in vitro and in vivo. Biocompatibility of GC-FUA-NPs was screened by BSA adsorption test and hemolysis activity examination in vitro. Cytotoxicity and cellular uptake study in HepG2 and A549 cells demonstrated that compared to free 5-Fu, the GC-FUA-NPs play great function in killing cancer cells for the cell endocytosis mediated by asialoglycoprotein receptor (ASGPR), which overexpresses on the cell surface...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28157445/creatinine-based-non-phospholipid-vesicular-carrier-for-improved-oral-bioavailability-of-azithromycin
#2
Shafi Ullah, Muhammad Raza Shah, Mohammad Shoaib, Muhammad Imran, Syed Wadood Ali Shah, Imdad Ali, Farid Ahmed
CONTEXT: Novel, safe, efficient and cost effective nano-carriers from renewable resources have got greater interest for enhancing solubility and bioavailability of hydrophobic dugs. OBJECTIVES: This study reports the synthesis of a novel biocompatible non-phospholipid human metabolite "Creatinine" based niosomal delivery system for Azithromycin improved oral bioavailability. METHODS: Synthesized surfactant was characterized through spectroscopic and spectrometric techniques and then evaluated for niosomal vesicles formation potential using Azithromycin as model drug...
February 3, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28155565/oral-administration-of-amphotericin-b-nanoparticles-antifungal-activity-bioavailability-and-toxicity-in-rats
#3
Mahasen A Radwan, Bushra T AlQuadeib, Lidija Šiller, Matthew C Wright, Benjamin Horrocks
Amphotericin B (AMB) is used most commonly in severe systemic life-threatening fungal infections. There is currently an unmet need for an efficacious (AMB) formulation amenable to oral administration with better bioavailability and lower nephrotoxicity. Novel PEGylated polylactic-polyglycolic acid copolymer (PLGA-PEG) nanoparticles (NPs) formulations of AMB were therefore studied for their ability to kill Candida albicans (C. albicans). The antifungal activity of AMB formulations was assessed in C. albicans...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28130039/polymer-conjugate-of-a-microtubule-destabilizer-inhibits-lung-metastatic-melanoma
#4
Ruinan Yang, Goutam Mondal, Rachel A Ness, Kinsie Arnst, Vaibhav Mundra, Duane D Miller, Wei Li, Ram I Mahato
Melanoma is the most aggressive type of skin cancer. It is highly metastatic, migrating through lymph nodes to distant sites of the body, especially to lungs, liver and brain. Systemic chemotherapy remains the mainstay of treatment; however, the development of multidrug resistance (MDR) restricts the efficacy of current chemotherapeutic drugs. We synthesized a series of microtubule destabilizers, substituted methoxybenzoyl-ary-thiazole (SMART) compounds, which inhibited tubulin polymerization and effectively circumvented MDR...
January 24, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28117787/use-of-a-monocyte-monolayer-assay-to-evaluate-fc%C3%AE-receptor-mediated-phagocytosis
#5
Tik Nga Tong, Donald R Branch
Although originally developed for predicting transfusion outcomes of serologically incompatible blood, the monocyte monolayer assay (MMA) is a highly versatile in vitro assay that can be modified to examine different aspects of antibody and Fcγ receptor (FcγR)-mediated phagocytosis in both research and clinical settings. The assay utilizes adherent monocytes from peripheral blood mononuclear cells isolated from mammalian whole blood. MMA has been described for use in both human and murine investigations. These monocytes express FcγRs (e...
January 2, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28097508/preparation-and-evaluation-of-biopolymeric-nanoparticles-as-drug-delivery-system-in-effective-treatment-of-rheumatoid-arthritis
#6
Vijay Kumar, Ankita Leekha, Aakriti Tyagi, Ankur Kaul, Anil Kumar Mishra, Anita Kamra Verma
PURPOSE: The study purposes to evaluate nanocrystalline biopolymeric nanoparticles encapsulating methotrexate and dexamethasone with high biocompatibility, enhanced therapeutic efficacy and reduced toxicity. METHODS: Chitosan nanoparticles were prepared by ionic gelation, and Methotrexate (MTX) and Dexamethasone (DEX) were loaded during the preparation and screened for their in vitro efficacy in HEK and RAW264.7 cells, ex vivo and in vivo efficacy. RESULTS: FTIR confirmed the involvement of phosphoric group of sTPP with amine groups of chitosan and also role of hydrogen bonding involved in the preparation of MTXCHNP and DEXCHNP...
January 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28092273/in-vivo-testing-of-extracorporeal-membrane-ventilators-ila-activve%C3%A2-vs-prototype-i-lung%C3%A2
#7
Sabine Kischkel, Stefan Bergt, Beate Brock, Johan von Grönheim, Anne Herbst, Marc-Jonas Epping, Georg Matheis, Esther Novosel, Joerg Schneider, Philipp Warnke, Andreas Podbielski, Jan P Roesner, Peter I Lelkes, Brigitte Vollmar
A side-by-side comparison of the decarboxylation efficacy of two pump-driven veno-venous extracorporeal lung assist devices, i.e. a first prototype of the new miniaturized ambulatory extracorporeal membrane ventilator, I-lung® versus the commercial system iLA-activve® over a period of 72 hours in a large animal model.Fifteen German Landrace pigs were anesthetized and underwent mechanical hypoventilation to induce severe hypercapnia. Decarboxylation was accomplished by either the I-lung® or the iLA-activve® via a double lumen catheter in the jugular vein...
January 4, 2017: ASAIO Journal: a Peer-reviewed Journal of the American Society for Artificial Internal Organs
https://www.readbyqxmd.com/read/28051909/in-vitro-heterogeneous-degradation-of-alginate-and-its-validation-of-different-molecular-weight-on-blood-bio-compatibility
#8
Mengxue Xu, Chao Feng, Juan Wang, Xuqian Lang, Guixue Xia, Xiaoping Yu, Qiuxia Ji, Xiaojie Cheng, Ming Kong, Ya Liu, Xiguang Chen
In the present work, sodium alginate (ALG) was degraded by heterogeneous phase acid degradation. The molecular weight distribution of ALG after degradation was close to homogenization. Then the blood bio-compatibility of ALG with different molecular weights (ALG-0h 50,075, ALG-0.5h 20,680, ALG-2h 13,170 and ALG-96h 1170 kDa) was evaluated in vitro and vivo. The human umbilical vein endothelial cells were used to assess the cytotoxicity of ALGs, ALG-0.5h and ALG-2h exhibited greater increment in percentage of cell viability comparing with ALG-0h and ALG-96h...
January 18, 2017: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/28045484/development-of-autologous-c5-vaccine-nanoparticles-to-reduce-intravascular-hemolysis-in-vivo
#9
Lingjun Zhang, Wen Qiu, Stephen Crooke, Yan Li, Areeba Abid, Bin Xu, M G Finn, Feng Lin
The complement system is emerging as a new target for treating many diseases. For example, Eculizumab, a humanized monoclonal antibody against complement component 5 (C5), has been approved for paroxysmal nocturnal hemoglobinuria (PNH) in which patient erythrocytes are lysed by complement. In this study, we developed vaccines to elicit autologous anti-C5 antibody production in mice for complement inhibition. Immunization of mice with a conservative C5 xenoprotein raised high titers of IgG's against the xenogenous C5, but these antibodies did not reduce C5 activity in the blood...
January 12, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28029254/pegylated-and-functionalized-aliphatic-polycarbonate-polyplex-nanoparticles-for-intravenous-administration-of-hdac5-sirna-in-cancer-therapy
#10
Antoine Frère, Alexandra Baroni, Elodie Hendrick, Anne-Sophie Delvigne, François Orange, Olivier Peulen, George R Dakwar, Jérôme Diricq, Philippe Dubois, Brigitte Evrard, Katrien Remaut, Kevin Braeckmans, Stefaan C De Smedt, Julie Laloy, Jean-Michel Dogné, Georges Feller, Laetitia Mespouille, Denis Mottet, Géraldine Piel
Guanidine and morpholine functionalized aliphatic polycarbonate polymers are able to deliver efficiently histone deacetylase 5 (HDAC5) siRNA into the cytoplasm of cancer cells in vitro leading to a decrease of cell proliferation were previously developed. To allow these biodegradable and biocompatible polyplex nanoparticles to overcome the extracellular barriers and be effective in vivo after an intravenous injection, polyethylene glycol chains (PEG750 or PEG2000) were grafted on the polymer structure. These nanoparticles showed an average size of about 150 nm and a slightly positive ζ-potential with complete siRNA complexation...
January 11, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28028023/incomplete-inhibition-by-eculizumab-mechanistic-evidence-for-residual-c5-activity-during-strong-complement-activation
#11
Markus J Harder, Nadine Kuhn, Hubert Schrezenmeier, Britta Höchsmann, Inge von Zabern, Christof Weinstock, Thomas Simmet, Daniel Ricklin, John D Lambris, Arne Skerra, Markus Anliker, Christoph Q Schmidt
Eculizumab inhibits the terminal, lytic pathway of complement by blocking the activation of the complement protein C5 and shows remarkable clinical benefits in certain complement-mediated diseases. However, several reports suggest that activation of C5 is not always completely suppressed in patients even under excess of eculizumab over C5 indicating that residual C5 activity may derogate the drug's therapeutic benefit under certain conditions. By using eculizumab and the tick-derived C5 inhibitor coversin we determine conditions ex vivo in which C5-inhibition is incomplete...
December 27, 2016: Blood
https://www.readbyqxmd.com/read/28007632/new-perspectives-in-the-topical-delivery-of-optimized-amphotericin-b-loaded-nanoemulsions-using-excipients-with-innate-anti-fungal-activities-a-mechanistic-and-histopathological-investigation
#12
Afzal Hussain, Sima Singh, Thomas J Webster, Farhan Jalees Ahmad
This study aimed to develop nanoemulsions (NEs) for the topical delivery of Amphotericin B using lipids and surfactants with innate antifungal activity. NEs were formulated by a slow spontaneous titration method and characterized for particle size, polydispersity index, zeta potential, zone of inhibition (ZOI), in vitro release, enhanced ex vivo rat skin permeation-deposition, hemolysis followed by interaction with the skin using scanning electron microscopy, and histopathology. The ZOI values of the optimized NEs (ANE3) were 21...
December 20, 2016: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/28007073/closing-in-on-the-pumpkin-trial-of-the-jarvik-2015-ventricular-assist-device
#13
REVIEW
J Timothy Baldwin, Iki Adachi, John Teal, Christopher A Almond, Robert D Jaquiss, M Patricia Massicotte, Kurt Dasse, Flora S Siami, Victor Zak, Jonathan R Kaltman, William T Mahle, Robert Jarvik
The Infant Jarvik ventricular assist device (VAD; Jarvik Heart, Inc., New York, NY) has been developed to support the circulation of infants and children with advanced heart failure. The first version of the device was determined to have elevated hemolysis under certain conditions. The objective of this work was to determine appropriate modifications to the Infant Jarvik VAD that would result in acceptably low hemolysis levels. In vitro hemolysis testing revealed that hemolysis was related to the shape of the pump blade tips and a critical speed over which hemolysis would occur...
January 2017: Seminars in Thoracic and Cardiovascular Surgery. Pediatric Cardiac Surgery Annual
https://www.readbyqxmd.com/read/28005445/preparation-and-in-vivo-safety-evaluations-of-antileukemic-homoharringtonine-loaded-pegylated-liposomes
#14
Dong Liu, Jing Xing, Fei Xiong, Fang Yang, Ning Gu
In order to improve the in vivo safety and specific delivery efficiency of the antileukemic homoharringtonine (HHT) at the targets, the long-circulating PEGylated liposomes loaded with HHT (LCLipo-HHT) were prepared. Their physical characteristics, in vitro drug release, in vivo pharmacokinetic properties and elementary toxicity were evaluated. The mean diameter of the prepared LCLipo-HHT is 75.6 ± 3.2 nm and the zeta potential is -16.9 ± 2.5 mV. The entrapment efficiency of HHT in the liposomes is 69...
April 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/27991616/atb-0-transporter-mediated-targeting-delivery-to-human-lung-cancer-cells-via-aspartate-modified-docetaxel-loading-stealth-liposomes
#15
Qiuhua Luo, Bin Yang, Wenhui Tao, Jia Li, Longfa Kou, He Lian, Xin Che, Zhonggui He, Jin Sun
Tumor cells have an increased demand for amino acids to support their rapid growth and malignant metastasis. Transfer of amino acids across plasma membranes depends on several amino acid transporters that are highly upregulated in tumor cells and are promising targets for tumor cell-selective therapy. In this study, stealth liposomal systems functionalized with aspartate-polyoxyethylene stearate conjugate (APS) were developed for transporter-mediated targeted delivery to ATB(0,+), which is overexpressed human lung cells...
December 19, 2016: Biomaterials Science
https://www.readbyqxmd.com/read/27983794/enhanced-corrosion-resistance-and-biocompatibility-of-magnesium-alloy-by-mg-al-layered-double-hydroxide
#16
Feng Peng, Hua Li, Donghui Wang, Peng Tian, Yaxin Tian, Guangyin Yuan, Demin Xu, Xuanyong Liu
Magnesium (Mg) and its alloys have been suggested as revolutionary biodegradable materials. However, fast degradation hinders its clinic application. To improve the corrosion resistance and biocompatibility of Mg-Nd-Zn-Zr alloy (JDBM), magnesium-aluminum-layered double hydroxide (Mg-Al LDH) was successfully introduced into Mg(OH)2 coating by hydrothermal treatment. The anions in the interlayer of Mg-Al LDH can be replaced by chloride ions, resulting in a relatively low chloride ion concentration near the surface of the coating...
December 28, 2016: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/27974282/aqueous-fraction-of-alstonia-boonei-de-wild-leaves-suppressed-inflammatory-responses-in-carrageenan-and-formaldehyde-induced-arthritic-rats
#17
Omowumi O Akinnawo, God'swill N Anyasor, Odutola Osilesi
Alstonia boonie de Wild is an ethnomedical plant used as therapy against inflammatory disorders. This study evaluated the most active anti-inflammatory and anti-oxidant fraction of A. boonei leaves using in vitro and in vivo models. Quantitative phytochemical analysis, anti-protein denaturation and hypotonicity-induced hemolysis of human red blood cell membrane (HRBC), radical scavenging activity assays, carrageenan and formaldehyde-induced inflammation models were carried out. Results showed that aqueous and ethyl acetate fractions of 70% methanol extract of A...
February 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27939571/ex-vivo-encapsulation-of-dexamethasone-sodium-phosphate-into-human-autologous-erythrocytes-using-fully-automated-biomedical-equipment
#18
Giovanni Mambrini, Marco Mandolini, Luigia Rossi, Francesca Pierigè, Giovanni Capogrossi, Patricia Salvati, Sonja Serafini, Luca Benatti, Mauro Magnani
Erythrocyte-based drug delivery systems are emerging as potential new solutions for the release of drugs into the bloodstream. The aim of the present work was to assess the performance of a fully automated process (EDS) for the ex-vivo encapsulation of the pro-drug dexamethasone sodium phosphate (DSP) into autologous erythrocytes in compliance with regulatory requirements. The loading method was based on reversible hypotonic hemolysis, which allows the opening of transient pores in the cell membrane to be crossed by DSP...
December 7, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27928710/synthesis-characterization-and-bioactivity-studies-of-novel-1-3-4-oxadiazole-small-molecule-that-targets-basic-phospholipase-a2-from-vipera-russelli
#19
Vivek Hamse Kameshwar, Kumar J R, Babu S Priya, S Nanjunda Swamy
Secretory phospholipase A2 (sPLA2) is a key enzyme participating in the inflammatory cascade followed by the action of cyclooxygenase-2 and lipoxygenases. Therefore, inhibitors of sPLA2 could be used as potent anti-inflammatory agents to treat the early phase of inflammation. In this study, we have prepared the fenoprofen and ibuprofen analogs containing 1,3,4-oxadiazole nucleus and tested against Vipera russelli venom's basic sPLA2 (VRV-PL-VIIIa). Among the tested ligands 5(a-t),2-(2-chlorophenyl)-5-(1-(4-phenoxyphenyl) ethyl)-1,3,4-oxadiazole (5m) inhibited the catalytic activity of VRV-PL-VIIIa with an IC50 value of 11...
February 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27888371/protective-effect-of-the-sulfated-agaran-isolated-from-the-red-seaweed-laurencia-aldingensis-against-toxic-effects-of-the-venom-of-the-snake-lachesis-muta
#20
Ana Cláudia Rodrigues da Silva, Luciana Garcia Ferreira, Maria Eugênia Rabello Duarte, Mutue Toyota Fujii, Eladio Flores Sanchez, Miguel Daniel Noseda, André Lopes Fuly
Snakebite is a serious occupational hazard affecting mainly rural populations of tropical and subtropical developing countries. Lachesis muta (Bushmaster) bites are extremely serious but are rarely reported in the literature. Bushmaster envenomings are characterized by intense local pain, edema, neurotoxicity, hypotension, local hemorrhage, and dramatic systemic alterations. Antivenom treatment has regularly been used for more than a century; however, it fails to neutralize local tissue damage and hemorrhage, leading to morbidity or disabilities in victims...
November 25, 2016: Marine Biotechnology
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