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https://www.readbyqxmd.com/read/28738502/formulation-and-optimization-of-lacidipine-loaded-niosomal-gel-for-transdermal-delivery-in-vitro-characterization-and-in-vivo-activity
#1
Mohd Qumbar, Ameeduzzafar, Syed Sarim Imam, Javed Ali, Javed Ahmad, Asgar Ali
The aim of the present research work is to formulate lacidipine (LAC) loaded niosomes formulation for the management of hypertension by thin film hydration technique. The developed formulations were statistically optimized by four factors, three levels Box-Behnken design and were evaluated for vesicle size, entrapment efficiency, and flux. The optimized LAC niosomes was further evaluated for permeation depth by confocal laser scanning microscopy (CLSM) and converted to gel formulation. Further, the optimized LAC niosomes gel was evaluated for ex-vivo permeation study, skin irritation study, stability study and pharmacodynamics study...
July 18, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28738158/efficient-interfacially-driven-vehiculization-of-corticosteroids-by-pulmonary-surfactant
#2
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/28736857/non-covalent-assembly-method-that-simultaneously-endows-a-liposome-surface-with-targeting-ligands-protective-peg-chains-and-deep-red-fluorescence-reporter-groups
#3
Scott K Shaw, Wenqi Liu, Seamus Brennan, Maria Betancourt-Mendiola, Bradley D Smith
A new self-assembly method is used to rapidly functionalize the surface of liposomes without perturbing the membrane integrity or causing leakage of the aqueous contents. The key molecule is a cholesterol-squaraine-PEG conjugate with three important structural elements: a cholesterol membrane anchor, a fluorescent squaraine docking station that allows rapid and high-affinity macrocycle threading, and a long PEG-2000 chain to provide steric shielding of the decorated liposome. The two-step method involves spontaneous insertion of the conjugate into the outer leaflet of pre-formed liposomes followed by squaraine threading with a tetralactam macrocycle that has appended targeting ligands...
July 23, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28736158/nanoliposomes-carrying-her2-neu-derived-peptide-ae36-with-cpg-odn-exhibit-therapeutic-and-prophylactic-activities-in-a-mice-tubo-model-of-breast-cancer
#4
Nastaran Barati, Amin Reza Nikpoor, Atefeh Razazan, Fatemeh Mosaffa, Ali Badiee, Atefeh Arab, Zahra Gholizadeh, Javad Behravan, Mahmoud Reza Jaafari
This study was designed to prepare and characterize nanoliposomal vaccine formulation encapsulating AE36 HER2/neu-derived peptide with or without CpG and evaluate the immunologic and therapeutic responses of that in BALB/c mice model of Her2 overexpressing breast cancer. AE36 was encapsulated in liposomes composed of DOTAP, DOPE and Cholesterol (DDC) or DD with. The formulations could induce both CD8+ and CD4+ responses and stimulate production of cytokines which was detected by Enzyme-linked immunospot assay (ELISpot) kits, cytotoxicity test and intracellular cytokine assay by flow cytometry...
July 20, 2017: Immunology Letters
https://www.readbyqxmd.com/read/28735341/the-effect-of-nanosecond-high-voltage-electric-pulses-on-the-shape-and-permeability-of-polymersome-guvs
#5
Tina Batista Napotnik, Gianluca Bello, Eva-Kathrin Sinner, Damijan Miklavčič
Polymersomes, vesicles composed of block copolymers, are promising candidates as membrane alternatives and functional containers, e.g., as potential carriers for functional molecules because of their stability and tunable membrane properties. In the scope of possible use for membrane protein delivery to cells by electrofusion, we investigated the cytotoxicity of such polymersomes as well as the effects of nanosecond electric pulses with variable repetition rate on the shape and permeability of polymersomes in buffers with different conductivities...
July 22, 2017: Journal of Membrane Biology
https://www.readbyqxmd.com/read/28735042/improved-selectivity-and-cytotoxic-effects-of-irinotecan-via-liposomal-delivery-a-comparative-study-on-hs68-and-hela-cells
#6
Ana Casadó, Margarita Mora, M Lluïsa Sagristá, Santi Rello-Varona, Pilar Acedo, Juan Carlos Stockert, Magdalena Cañete, Angeles Villanueva
Irinotecan (CPT-11) is an effective chemotherapeutic agent widely used to treat different cancers. Otherwise, the liposomal delivery of anti-tumor agents has been shown to be a promising strategy. The aim of this study has been to analyze the effect of liposomal CPT-11 (CPT-11lip) on two human cell lines (Hs68 and HeLa) to establish the suitability of this CPT-11 nanocarrier. We have demonstrated the highest uptake of CPT-11lip in comparison with that of CPT-11sol, in lactate buffer, and that CPT-11lip was internalized in the cells through an endocytic process whereas CPT-11sol does so by passive diffusion...
July 19, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28734877/enzymatic-and-free-radical-formation-of-cis-and-trans-epoxyeicosatrienoic-acids-in-vitro-and-in-vivo
#7
Theresa Aliwarga, Brianne S Raccor, Rozenn N Lemaitre, Nona Sotoodehnia, Sina A Gharib, Libin Xu, Rheem A Totah
Epoxyeicosatrienoic acids (EETs) are metabolites of arachidonic acid (AA) oxidation that have important cardioprotective and signaling properties. AA is an ω -6 polyunsaturated fatty acid (PUFA) that is prone to autoxidation. Although hydroperoxides and isoprostanes are major autoxidation products of AA, EETs are also formed from the largely overlooked peroxyl radical addition mechanism. While autoxidation yields both cis- and trans-EETs, cytochrome P450 (CYP) epoxygenases have been shown to exclusively catalyze the formation of all regioisomer cis-EETs, on each of the double bonds...
July 19, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28734478/ph-dependent-membrane-interactions-of-the-histidine-rich-cell-penetrating-peptide-lah4-l1
#8
Justine Wolf, Christopher Aisenbrey, Nicole Harmouche, Jesus Raya, Philippe Bertani, Natalia Voievoda, Regine Süss, Burkhard Bechinger
The histidine-rich designer peptide LAH4-L1 exhibits antimicrobial and potent cell-penetrating activities for a wide variety of cargo including nucleic acids, polypeptides, adeno-associated viruses, and nanodots. The non-covalent complexes formed between the peptide and cargo enter the cell via an endosomal pathway where the pH changes from neutral to acidic. Here, we investigated the membrane interactions of the peptide with phospholipid bilayers and its membrane topology using static solid-state NMR spectroscopy...
July 19, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28733701/copper-ii-complexes-of-bidentate-ligands-exhibit-potent-anti-cancer-activity-regardless-of-platinum-sensitivity-status
#9
Mohamed Wehbe, Cody Lo, Ada W Y Leung, Wieslawa H Dragowska, Gemma M Ryan, Marcel B Bally
Insensitivity to platinum, either through inherent or acquired resistance, is a major clinical problem in the treatment of many solid tumors. Here, we explored the therapeutic potential of diethyldithiocarbamate (DDC), pyrithione (Pyr), plumbagin (Plum), 8-hydroxyquinoline (8-HQ), clioquinol (CQ) copper complexes in a panel of cancer cell lines that differ in their sensitivity to platins (cisplatin/carboplatin) using a high-content imaging system. Our data suggest that the copper complexes were effective against both platinum sensitive (IC50 ~ 1 μM platinum) and insensitive (IC50 > 5 μM platinum) cell lines...
July 21, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28732901/multiple-polysaccharide-drug-complex-loaded-liposomes-a-unique-strategy-in-drug-loading-and-cancer-targeting
#10
Hima Bindu Ruttala, Thiruganesh Ramasamy, Biki Gupta, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
In the present study, a unique strategy was developed to develop nanocarriers containing multiple therapeutics with controlled release characteristics. In this study, we demonstrated the synthesis of dextran sulfate-doxorubicin (DS-DOX) and alginate-cisplatin (AL-CIS) polymer-drug complexes to produce a transferrin ligand-conjugated liposome. The targeted nanoparticles (TL-DDAC) were nano-sized and spherical. The targeted liposome exhibited a specific receptor-mediated endocytic uptake in cancer cells. The enhanced cellular uptake of TL-DDAC resulted in a significantly better anticancer effect in resistant and sensitive breast cancer cells compared to that of the free drugs...
October 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28732726/the-immunoregulatory-activities-of-astragalus-polysaccharide-liposome-on-macrophages-and-dendritic-cells
#11
Weimin Zhang, Wuren Ma, Jing Zhang, Xiaoping Song, Wenjing Sun, Yunpeng Fan
The objective of this study is to investigate the immunomodulatory activities of astragalus polysaccharide liposome (APSL) on murine peritoneal macrophages and bone marrow derived dendritic cells (DCs). The results showed that APSL not only significantly improved the phagocytosis of macrophages, the contents of IL-6 and IL-12, and the secretion of nitric oxide (NO) and inducible nitric oxide synthase (iNOS) in macrophages, but also promoted the proliferation of DCs precursor cells, enhanced the abilities of DCs on stimulating T-cell proliferation and presenting antigen, upregulated IFN-γ and IL-2 production of DCs, and improved the expression of CD80 and CD86 in DCs compared with astragalus polysaccharide (APS)...
July 18, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28731329/generation-and-characterization-of-anti-vglut-nanobodies-acting-as-inhibitors-of-transport
#12
Stephan Schenck, Laura Kunz, Daniela Sahlender, Els Pardon, Eric R Geertsma, Iaroslav Savtchouk, Toshiharu Suzuki, Yvonne Neldner, Saša Štefanić, Jan Steyaert, Andrea Volterra, Raimund Dutzler
The uptake of glutamate by synaptic vesicles is mediated by vesicular glutamate transporters (VGLUTs). The central role of these transporters in excitatory neurotransmission underpins their importance as pharmacological targets. Although several compounds inhibit VGLUTs, highly specific inhibitors were so far unavailable, thus limiting applications to in vitro experiments. Besides their potential in pharmacology, specific inhibitors would also be beneficial for the elucidation of transport mechanisms. To overcome this shortage, we generated nanobodies (Nbs) by immunization of a llama with purified rat VGLUT1 and subsequent selection of binders from a phage display library...
July 21, 2017: Biochemistry
https://www.readbyqxmd.com/read/28731323/analyzing-liposomal-drug-delivery-systems-in-three-dimensional-cell-culture-models-using-maldi-imaging-mass-spectrometry
#13
Jessica K Lukowski, Eric M Weaver, Amanda B Hummon
Cancer chemotherapeutics often fail to reach all diseased cells. To help solve this problem, researchers are investigating novel drug delivery systems. Liposomes are an attractive option due to their low toxicity, high biocompatibility, and potential to carry a large amount of a drug to the tumor site, all while avoiding being eliminated from the body. This study evaluates the penetration of doxorubicin-encased liposomes into three-dimensional cell cultures, or spheroids. Liposomes composed of lipids containing head groups of phosphatidylcholine (PC), phosphatidylethanolamine (PE), and cholesterol were created by extrusion...
July 21, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28731030/cryo-em-structure-and-biochemical-analysis-reveal-the-basis-of-the-functional-difference-between-human-pi3kc3-c1-and-c2
#14
Meisheng Ma, Jun-Jie Liu, Yan Li, Yuwei Huang, Na Ta, Yang Chen, Hua Fu, Ming-Da Ye, Yuehe Ding, Weijiao Huang, Jia Wang, Meng-Qiu Dong, Li Yu, Hong-Wei Wang
Phosphatidylinositol 3-phosphate (PI3P) plays essential roles in vesicular trafficking, organelle biogenesis and autophagy. Two class III phosphatidylinositol 3-kinase (PI3KC3) complexes have been identified in mammals, the ATG14L complex (PI3KC3-C1) and the UVRAG complex (PI3KC3-C2). PI3KC3-C1 is crucial for autophagosome biogenesis, and PI3KC3-C2 is involved in various membrane trafficking events. Here we report the cryo-EM structures of human PI3KC3-C1 and PI3KC3-C2 at sub-nanometer resolution. The two structures share a common L-shaped overall architecture with distinct features...
July 21, 2017: Cell Research
https://www.readbyqxmd.com/read/28730191/processing-structure-relationships-of-poly-ethylene-glycol-modified-liposomes
#15
Kenneth P Mineart, Elizabeth G Kelley, Michihiro Nagao, Vivek M Prabhu
Liposomes with PEG-modified surfaces are amenable to nanocarrier applications and can be prepared via two PEGylated lipid incorporation routes: before and after extrusion (i.e., co-extrusion and post-insertion, respectively). The current study quantifies the processing influence on PEG chain partitioning between the interior and exterior liposome surfaces for the first time using small angle neutron scattering.
July 21, 2017: Soft Matter
https://www.readbyqxmd.com/read/28729631/therapeutic-effects-of-long-circulating-mir-135a-containing-cationic-immunoliposomes-against-gallbladder-carcinoma
#16
Guanghua Yang, Baobing Yin
Gallbladder carcinoma (GBC) is the most common malignant tumour in the biliary tract, but effective therapeutics are lacking. Based on our previous studies, miR-135a is a potential tool to inhibit GBC proliferation. In this study, we constructed miR-135a-loaded DSPE-PEG2000 liposomes modified with Anti-EGFR antibodies (Anti-EGFR-CIL-miR-135a). The results of an analysis of their physicochemical properties indicated the particle size of it was 222.0 ± 2.1 nm in diameter with an uptake efficiency of 86...
July 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28729400/vessel-targeted-chemophototherapy-with-cationic-porphyrin-phospholipid-liposomes
#17
Dandan Luo, Jumin Geng, Nasi Li, Kevin A Carter, Shuai Shao, G Ekin Atilla-Gokcumen, Jonathan F Lovell
Cationic liposomes have been used for targeted drug delivery to tumor blood vessels, via mechanisms that are not fully elucidated. Doxorubicin (Dox)-loaded liposomes were prepared that incorporate a cationic lipid; 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), along with a small amount of porphyrin-phospholipid (PoP). Near infrared (NIR) light induced release of entrapped Dox via PoP-mediated DOTAP photo-oxidation. The formulation was optimized to enable extremely rapid NIR light-triggered Dox release (i...
July 20, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28728449/efficiency-and-cytotoxicity-analysis-of-cationic-lipids-mediated-gene-transfection-into-ags-gastric-cancer-cells
#18
Nasrin Gharaati-Far, Mohammad Reza Tohidkia, Alireza Dehnad, Yadollah Omidi
In this effort, we provided comparative study on optimization of transfection conditions for AGS human gastric cancer cell line using two commercial non-liposomal cationic lipids. Using reporter vector pEGFP-N1, transfection efficiency of Attractene™ and X-tremeGENE HP™ transfection reagents in terms of cell densities and DNA/reagent ratios was determined in AGS cells by flow cytometry and fluorescence microscopy. In addition, influence of transfection reagents on direct cytotoxicity and cell viability was respectively, measured using lactate dehydrogenase (LDH) leakage and MTT assays...
July 20, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28728446/hpma-copolymer-phospholipase-c-and-dextrin-phospholipase-a2-as-model-triggers-for-polymer-enzyme-liposome-therapy-pelt
#19
Elaine L Ferguson, Anna Scomparin, Hanna Hailu, Ronit Satchi-Fainaro
'Polymer Enzyme Liposome Therapy' (PELT) is a two-step anticancer approach in which a liposomal drug and polymer-phospholipase conjugate are administered sequentially to target the tumour interstitium by the enhanced permeability and retention effect, and trigger rapid, local, drug release. To date, however, the concept has only been described theoretically. We synthesised two polymer conjugates of phospholipase C (PLC) and A2 (PLA2) and evaluated their ability to trigger anthracycline release from the clinically-used liposomes, Caelyx® and DaunoXome(®)...
July 21, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/28727583/serum-bupivacaine-concentration-after-periarticular-injection-with-a-mixture-of-liposomal-bupivacaine-and-bupivacaine-hcl-during-total-knee-arthroplasty
#20
Michael J Buys, Marian F Murphy, Christine M Warrick, Nathan L Pace, Jeremy M Gililland, Christopher E Pelt, Byron R Bankhead, John L Patzkowsky, Ken B Johnson
BACKGROUND AND OBJECTIVES: A relatively new technique to reduce postoperative pain for total knee arthroplasty is to inject a mixture of 266 mg of liposomal bupivacaine and 125 mg of 0.25% bupivacaine HCl with epinephrine 1:300,000 around the knee joint at the time of surgery. Currently, no publications report serum bupivacaine concentrations over time after periarticular injection of liposomal mixed with free bupivacaine. This information is important to ensure safe serum bupivacaine concentrations are maintained especially when considering supplemental or rescue peripheral nerve blocks...
July 20, 2017: Regional Anesthesia and Pain Medicine
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