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https://www.readbyqxmd.com/read/28350438/an-acyl-linked-dimer-of-daptomycin-is-strongly-inhibited-by-the-bacterial-cell-wall
#1
Robert M Taylor, Bradley Scott, Scott Taylor, Michael Palmer
The lipopeptide antibiotic daptomycin is active against Gram-positive pathogens. It permeabilizes bacterial cell membranes, which involves the formation of membrane-associated oligomers. We here studied a dimer of daptomycin whose two subunits were linked through a bivalent aliphatic acyl chain. Unexpectedly, the dimer had very low activity on vegetative Staphylococcus aureus and Bacillus subtilis cells. However, activity resembled that of monomeric daptomycin on liposomes and on B. subtilis L-forms. These findings underscore the importance of the bacterial cell wall in daptomycin resistance...
March 28, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28346375/liposomal-formulations-in-clinical-use-an-updated-review
#2
REVIEW
Upendra Bulbake, Sindhu Doppalapudi, Nagavendra Kommineni, Wahid Khan
Liposomes are the first nano drug delivery systems that have been successfully translated into real-time clinical applications. These closed bilayer phospholipid vesicles have witnessed many technical advances in recent years since their first development in 1965. Delivery of therapeutics by liposomes alters their biodistribution profile, which further enhances the therapeutic index of various drugs. Extensive research is being carried out using these nano drug delivery systems in diverse areas including the delivery of anti-cancer, anti-fungal, anti-inflammatory drugs and therapeutic genes...
March 27, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28345887/from-detection-to-resection-photoacoustic-tomography-and-surgery-guidance-with-au-liposome-icg-nanoparticles-in-liver-cancer
#3
Tianpei Guan, Wenting Shang, Hui Li, Xin Yang, Chihua Fang, Jie Tian, Kun Wang
Conventional imaging methods encounter challenges in diagnosing liver cancer that is less than 10 mm and/or without typical hypervascular features. With deep penetration and high spatial resolution imaging capability, the emerging photoacoustic tomography may offer better diagnostic efficacy for non-invasive liver cancer detection. Moreover, near-infrared fluorescence imaging guided hepatectomy was proven to be able to identify nodules at millimeter level. Thus, suitable photoacoustic and fluorescence dual-modality imaging probe may benefit patients in early diagnosis and complete resection...
March 27, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28345623/liposomes-loaded-with-bioactive-lipids-enhance-antibacterial-innate-immunity-irrespective-of-drug-resistance
#4
Noemi Poerio, Francesca Bugli, Francesco Taus, Marilina B Santucci, Carlo Rodolfo, Francesco Cecconi, Riccardo Torelli, Francesco Varone, Riccardo Inchingolo, Fabio Majo, Vincenzina Lucidi, Sabrina Mariotti, Roberto Nisini, Maurizio Sanguinetti, Maurizio Fraziano
Phagocytosis is a key mechanism of innate immunity, and promotion of phagosome maturation may represent a therapeutic target to enhance antibacterial host response. Phagosome maturation is favored by the timely and coordinated intervention of lipids and may be altered in infections. Here we used apoptotic body-like liposomes (ABL) to selectively deliver bioactive lipids to innate cells, and then tested their function in models of pathogen-inhibited and host-impaired phagosome maturation. Stimulation of macrophages with ABLs carrying phosphatidic acid (PA), phosphatidylinositol 3-phosphate (PI3P) or PI5P increased intracellular killing of BCG, by inducing phagosome acidification and ROS generation...
March 27, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28344661/liposomal-irinotecan-in-gemcitabine-refractory-metastatic-pancreatic-cancer-efficacy-safety-and-place-in-therapy
#5
REVIEW
Emma Kipps, Kate Young, Naureen Starling
Pancreatic ductal adenocarcinoma (PDAC) is a lethal disease. The majority of patients are diagnosed with locally advanced or metastatic disease with a prognosis of short months. Therapeutic options are limited and until recently, there was no standard second-line chemotherapy option. Liposomal constructs have been engineered to encapsulate chemotherapy thereby preventing premature metabolism, improving distribution and minimizing toxicity. Favourable preclinical data on liposomal irinotecan and early phase trials, led to a recently published phase III trial of liposomal irinotecan in combination with fluorouracil and folinic acid in patients with metastatic PDAC, who progressed after gemcitabine-based chemotherapy...
March 2017: Therapeutic Advances in Medical Oncology
https://www.readbyqxmd.com/read/28344496/the-impact-of-formulation-attributes-and-process-parameters-on-black-seed-oil-loaded-liposomes-and-their-performance-in-animal-models-of-analgesia
#6
Zerin T Rushmi, Nasrin Akter, Rabeya J Mow, Merina Afroz, Mohsin Kazi, Marcel de Matas, Mahbubur Rahman, Mohammad H Shariare
This study aimed to formulate black seed oil (Nigella sativa) loaded liposomes using the ethanol injection method to enhance oral bioavailability and improve therapeutic activity in small animal studies of analgesia. The impact of formulation attributes and process parameters on the liposomal system was evaluated with key quality attributes being particle size, morphology, and entrapment efficiency. The particle size and entrapment efficiency of the liposome preparation were found to be between the range of 50-900 nm and 34-87% respectively...
March 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28344488/direct-and-enhanced-delivery-of-nanoliposomes-of-anti-schizophrenic-agent-to-the-brain-through-nasal-route
#7
Pratik Upadhyay, Jatin Trivedi, Kilambi Pundarikakshudu, Navin Sheth
The problem of inadequate oral bioavailability of Quetiapine Fumarate, a lipophilic drug used for schizophrenia, due to hepatic metabolism and repulsion by brain barrier was attempted in this study. Combination of two approaches, viz. Quetiapine inclusion into the liposomal carrier for better diffusion and administration through nasal route to avoid hepatic metabolism and barrier elimination was applied. Thin film hydration followed by sonication method was employed in liposome preparation and the formulation was optimized using 3(2) full factorial design...
March 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28343627/invited-review-milk-phospholipid-vesicles-their-colloidal-properties-and-potential-as-delivery-vehicles-for-bioactive-molecules
#8
E Arranz, M Corredig
The milk fat globule membrane (MFGM) is a unique colloidal assembly of phospholipids and proteins, with numerous potential applications as functional ingredient. The phospholipid components of the MFGM are gaining interest as they are a useful matrix for use as a constituent of delivery systems such as liposomes. Liposomes formulated with milk phospholipids are becoming an alternative to other sources of phospholipids such as soybean or egg yolk. However, incorporation of phospholipids fractionated from the milk fat globule membrane in dairy products requires an in-depth understanding of the functional properties of phospholipids...
March 23, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/28343016/evaluation-of-antitumor-activity-and-cardiac-toxicity-of-a-bone-targeted-ph-sensitive-liposomal-formulation-in-a-bone-metastasis-tumor-model-in-mice
#9
Diego Dos Santos Ferreira, Bruno Luís Jesus de Oliveira Pinto, Vidhya Kumar, Valbert Nascimento Cardoso, Simone Odília Fernandes, Cristina Maria Souza, Geovanni Dantas Cassali, Anna Moore, David Sosnovik, Christian Farrar, Elaine Amaral Leite, Ricardo José Alves, Mônica Cristina de Oliveira, Alexander Ramos Guimarães, Peter Caravan
Chemotherapy for bone tumors is a major challenge because of the inability of therapeutics to penetrate dense bone mineral. We hypothesize that a nanostructured formulation with high affinity for bone could deliver drug to the tumor while minimizing off-target toxicity. Here, we evaluated the efficacy and toxicity of a novel bone-targeted, pH-sensitive liposomal formulation containing doxorubicin in an animal model of bone metastasis. Biodistribution studies with the liposome showed good uptake in tumor, but low accumulation of doxorubicin in the heart...
March 22, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/28342847/na-k-atpase-interaction-with-methylglyoxal-as-reactive-metabolic-side-product
#10
Marika Svrckova, Martina Zatloukalova, Petra Dvorakova, Dominika Coufalova, David Novak, Lenka Hernychova, Jan Vacek
Proteins are subject to oxidative modification and the formation of adducts with a broad spectrum of reactive species via enzymatic and non-enzymatic mechanisms. Here we report that in vitro non-enzymatic methylglyoxal (MGO) binding causes the inhibition and formation of MGO advanced glycation end-products (MAGEs) in Na(+)/K(+)-ATPase (NKA). Concretely, MGO adducts with NKA amino acid residues (mainly Arg) and N(ε)-(carboxymethyl)lysine (CML) formation were found. MGO is not only an inhibitor for solubilized NKA (IC50 = 91±16 μM), but also for reconstituted NKA in the lipid bilayer environment, which was clearly demonstrated using a DPPC/DPPE liposome model in the presence or absence of the NKA-selective inhibitor ouabain...
March 22, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28342788/analytical-ultracentrifugation-for-analysis-of-doxorubicin-loaded-liposomes
#11
Dora Mehn, Patrizia Iavicoli, Noelia Cabaleiro, Sven Even Borgos, Fanny Caputo, Otmar Geiss, Luigi Calzolai, François Rossi, Douglas Gilliland
Analytical ultracentrifugation (AUC) is a powerful tool for the study of particle size distributions and interactions with high accuracy and resolution. In this work, we show how the analysis of sedimentation velocity data from the AUC can be used to characterize nanocarrier drug delivery systems used in nanomedicine. Nanocarrier size distribution and the ratio of free versus nanoparticle-encapsulated drug in a commercially available liposomal doxorubicin formulation are determined using interference and absorbance based AUC measurements and compared with results generated with conventional techniques...
March 22, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28342757/role-of-enzymatic-free-radical-scavengers-in-management-of-oxidative-stress-and-autoimmune-disorders
#12
REVIEW
Shikha Srivastava, Deependra Singh, Satish Patel, Manju R Singh
Autoimmune disorders are distinct with over production and accumulation of free radicals due to its undisclosed genesis. The cause of numerous disorders as cancer, arthritis, psoriasis, diabetes, alzheimer's, cardiovascular disease, Parkinson's, respiratory distress syndrome, colitis, crohn's, pulmonary fibrosis, obesity and ageing have been associated with immune dysfunction and oxidative stress. In an oxidative stress, reactive oxygen species generally provoke the series of oxidation at cellular level. The buildup of free radicals in turn triggers various inflammatory cells causing release of various inflammatory interleukins, cytokines, chemokines, and tumor necrosis factors which mediate signal transduction and transcription pathways as nuclear factor- kappa B (NF-κB), signal transducer and activator of transcription 3 (STAT3), hypoxia-inducible factor-1 (HIF-1α) and nuclear factor-erythroid 2-related factor (Nrf2)...
March 22, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28342238/a-peel-off-facial-mask-comprising-myoinositol-and-trehalose-loaded-liposomes-improves-adult-female-acne-by-reducing-local-hyperandrogenism-and-activating-autophagy
#13
Gabriella Fabbrocini, Claudia Capasso, Marianna Donnarumma, Mariateresa Cantelli, Michel Le Maître, Giuseppe Monfrecola, Enzo Emanuele
BACKGROUND: Hyperandrogenism and reduced skin autophagy have been implicated in the pathogenesis of adult female acne (AFA). Here, we tested whether a ready-to-use peel-off facial mask containing myoinositol (an androgen inhibitor) and trehalose-loaded liposomes (as activators of cutaneous autophagy) applied overnight every other day for 60 days can improve AFA. We also sought to investigate the molecular mechanisms underlying the clinical effects. OBJECTIVES: We conducted an uncontrolled, open-label clinical study in 40 cases of AFA to investigate the effect of the facial mask on lesion count, sebum production (measured with the Sebutape® technique), and Global Acne Grading System (GAGS) scale...
March 25, 2017: Journal of Cosmetic Dermatology
https://www.readbyqxmd.com/read/28341957/phase-ib-dose-finding-trial-of-lapatinib-plus-pegylated-liposomal-doxorubicin-in-advanced-her2-positive-breast-cancer
#14
Andrea Rocca, Lorenzo Cecconetto, Alessandro Passardi, Elisabetta Melegari, Daniele Andreis, Manuela Monti, Roberta Maltoni, Samanta Sarti, Elisabetta Pietri, Alessio Schirone, Francesco Fabbri, Caterina Donati, Oriana Nanni, Anna Fedeli, Marina Faedi, Dino Amadori
PURPOSE: Combination of anthracyclines with trastuzumab is hampered by cardiotoxicity. Pegylated liposomal doxorubicin and lapatinib could represent a safer alternative to combination therapy. METHODS: In this phase Ib study with 3 + 3 dose escalation design, patients with HER2-positive advanced breast cancer received pegylated liposomal doxorubicin 30 mg/m(2) intravenously on day 1 plus lapatinib 1250 (level 1) or 1500 (level 2) mg/day orally on days 1-21 of each 21-day cycle...
March 24, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28341149/docetaxel-loaded-ripl-peptide-iplvvplrrrrrrrrc-conjugated-liposomes-drug-release-cytotoxicity-and-antitumor-efficacy
#15
Ho Yub Yoon, Seong Shin Kwak, Moon Ho Jang, Min Hyung Kang, Si Woo Sung, Chang Hyun Kim, Sung Rae Kim, Dong Woo Yeom, Myung Joo Kang, Young Wook Choi
We previously synthesized the RIPL peptide (IPLVVPLRRRRRRRRC) to facilitate selective delivery into hepsin-expressing cancer cells and showed that RIPL peptide-conjugated liposomes (RIPL-L) enhanced the intracellular delivery of fluorescent probes in vitro. In this study, docetaxel-loaded RIPL-L (DTX-RIPL-L) were prepared and evaluated for in vitro drug release, cytotoxicity, and in vivo antitumor efficacy. DTX was successfully encapsulated by pre-loading, with an average encapsulation efficiency and drug loading capacity of 32...
March 21, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28340485/an-approach-for-liposome-immobilization-using-sterically-stabilized-micelles-ssms-as-a-precursor-for-bio-layer-interferometry-based-interaction-studies
#16
Jakob Wallner, Gabriele Lhota, Markus Schosserer, Karola Vorauer-Uhl
Non-fluidic bio-layer interferometry (BLI) has rapidly become a standard tool for monitoring almost all biomolecular interactions in a label-free, real-time and high-throughput manner. High-efficiency screening methods which measure the kinetics of liposomes with a variety of compounds require the immobilization of liposomes. In this work, a method is described for immobilizing liposomes for interaction studies, based on the biophysical principles of this biosensor platform. The immobilization approach includes the loading of DSPE-PEG(2000)-biotin containing sterically stabilized micelles (SSMs) which are restructured in a buffer change step, resulting in an accessible substrate for liposome immobilization...
March 12, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28339742/topiramate-modulates-post-infarction-inflammation-primarily-by-targeting-monocytes-or-macrophages
#17
Zhaohui Wang, Shiyuan Huang, Yuling Sheng, Xu Peng, Hui Liu, Nan Jin, Jun Cai, Yanwen Shu, Ting Li, Ping Li, Cheng Fan, Xiaofan Hu, Wenyong Zhang, Rui Long, Ya You, Caihong Huang, Yi Song, Chunhua Xiang, Jue Wang, Yong Yang, Kun Liu
Aims: Monocytes/macrophages response plays a key role in post-infarction inflammation that contributes greatly to post-infarction ventricular remodeling and cardiac rupture. Therapeutic targeting of the GABAA receptor, which is enriched in monocytes/macrophages but not expressed in the myocardium, may be possible after myocardial infarction. Methods and results: After MI was induced by ligation of the coronary artery, C57BL/6 mice were intraperitoneally administered with one specific agonist or antagonist of the GABAA receptor (topiramate or bicuculline), in the setting of presence or depletion of monocytes/macrophages...
February 17, 2017: Cardiovascular Research
https://www.readbyqxmd.com/read/28339539/unique-aggregation-of-conjugated-amphotericin-b-and-its-interaction-with-lipid-membranes
#18
Sarah Kagan, Diana E Ickowicz, Abraham J Domb, Arie Dagan, Itzhack Polacheck
The purpose of this paper was to investigate the aggregation of amphotericin B (AMB) and AMB-arabinogalactan conjugate (AMB-AGC), and the interactions of these drugs with free and membrane-embedded sterols. Aggregation of AMB and AMB-AGC was studied by circular dichroic (CD) and UV absorbance spectroscopic techniques. The effect of liposomes on the spectra was utilized to investigate the interactions of aggregates with membrane-embedded sterols. Interaction with free sterols was studied by measuring sterols' effect on AMB/AMB-AGC susceptibility test...
October 7, 2016: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
https://www.readbyqxmd.com/read/28339206/utilizing-electron-spin-echo-envelope-modulation-to-distinguish-between-the-local-secondary-structures-of-an-%C3%AE-helix-and-an-amphipathic-310-helical-peptide
#19
Lauren Bottorf, Sophia Rafferty, Indra Dev Sahu, Robert M McCarrick, Gary A Lorigan
Electron Spin Echo Envelope Modulation (ESEEM) spectroscopy was used to distinguish between the local secondary structures of an α-helix and a 310-helix. Previously, we have shown that ESEEM spectroscopy in combination with site-directed spin labeling (SDSL) and 2H-labeled amino acids (i) can probe the local secondary structure of α-helices, resulting in an obvious deuterium modulation pattern, where i+4 positions generally show larger 2H ESEEM peak intensities than i+3 positions. Here, we have hypothesized that due to the unique turn periodicities of an α-helix (3...
March 24, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28338414/targeted-therapy-of-octreotide-modified-oleanolic-acid-liposomes-to-somatostatin-receptor-overexpressing-tumor-cells
#20
Qianqian Wang, Ruiyan Zhu, Meili Wang, Shanshan Xing, Lei Li, Yuchu He, Weiwei Cao, Dawei Gao
AIM: To prepare and validate the efficacy of a novel targeted drug delivery system - octreotide (Oct)-modified oleanolic acid (OA) liposomes. MATERIALS & METHODS: OA liposomes (OA-L) were prepared by an ethanol injection method. The Oct-modified OA liposomes (O-OA-L) were synthesized and their properties were evaluated. Cellular uptake and competition inhibition studies were performed. RESULTS: The OA vesicles presented satisfactory particles size (100-200 nm), stability and drug release characteristics; their ζ potential was -1...
March 24, 2017: Nanomedicine
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