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Liposomes characterization

Robin Cloarec, Sylvian Bauer, Natacha Teissier, Fabienne Schaller, Hervé Luche, Sandra Courtens, Manal Salmi, Vanessa Pauly, Emilie Bois, Emilie Pallesi-Pocachard, Emmanuelle Buhler, François J Michel, Pierre Gressens, Marie Malissen, Thomas Stamminger, Daniel N Streblow, Nadine Bruneau, Pierre Szepetowski
Congenital cytomegalovirus (CMV) infections represent one leading cause of neurodevelopmental disorders. Recently, we reported on a rat model of CMV infection of the developing brain in utero , characterized by early and prominent infection and alteration of microglia-the brain-resident mononuclear phagocytes. Besides their canonical function against pathogens, microglia are also pivotal to brain development. Here we show that CMV infection of the rat fetal brain recapitulated key postnatal phenotypes of human congenital CMV including increased mortality, sensorimotor impairment reminiscent of cerebral palsy, hearing defects, and epileptic seizures...
2018: Frontiers in Cellular Neuroscience
Zheng Zheng, Julia Saar, Bo Zhi, Tian Autumn Qiu, Miranda J Gallagher, D Howard Fairbrother, Christy L Haynes, Karen Lienkamp, Zeev Rosenzweig
The paper describes the interactions between poly (oxonorbornenes) (PONs)-coated gold nanoparticles (AuNPs) with phospholipid vesicles, and shows that the strength of these interactions strongly depends on the molecular structure of PONs, specifically their amine/alkyl side chain ratio. PONs, which are a recently introduced class of cationic polyelectrolytes, can be systematically varied to control the amine/alkyl ratio and to explore how the chemical character of cationic polyelectrolytes affect their interactions and the interactions of their nanoparticle conjugates with model membranes...
March 21, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
Louise Wogelred, Fredrik Höök, Björn Agnarsson, Peter Sjövall
Accurate detection and quantification of individual molecules is important for the development of improved diagnostic methods as well as biochemical characterization of disease progression and treatments. Time-of-flight secondary ion mass spectrometry (ToF-SIMS) is a surface analysis technique capable of imaging the distribution of specific molecules on surfaces with a high spatial resolution (<1 μm) and high sensitivity. ToF-SIMS is particularly suitable for detection of molecules up to ∼2 kDa, including lipids, whereas larger molecules, such as peptides and proteins, are fragmented during analysis, which makes them difficult to identify...
March 15, 2018: Biointerphases
Hari R Desu, Laura A Thoma, George C Wood
PURPOSE: Acute lung injury (ALI) is a fatal syndrome in critically ill patients. It is characterized by lung edema and inflammation. Numerous pro-inflammatory mediators are released into alveoli. Among them, interleukin-1beta (IL-1β) causes an increase in solute permeability across the alveolar-capillary barrier leading to edema. It activates key effector cells (alveolar epithelial and endothelial cells) releasing inflammatory chemokines and cytokines. The purpose of the study was to demonstrate that nebulized liposomes inhibit ALI in vivo...
March 13, 2018: Pharmaceutical Research
Jahidur Rashid, Kamrun Nahar, Snehal Raut, Ali Keshavarz, Fakhrul Ahsan
We investigated the feasibility of a combination therapy comprising fasudil, a Rho-kinase inhibitor, and DETA NONOate (diethylenetriamine NONOate, DN), a long acting nitric oxide donorboth loaded in liposomes modified with a homing peptide, CAR (CARSKNKDC)in the treatment of pulmonary arterial hypertension (PAH). We first prepared and characterized unmodified- and CAR-modified-liposomes of fasudil and DN. Using individual drugs alone or a mixture of fasudil and DN as controls, we studied the efficacy of the two liposomal preparations in reducing mean pulmonary arterial pressure (mPAP) in monocrotaline (MCT) and SUGEN-hypoxia induced PAH rats...
March 12, 2018: Molecular Pharmaceutics
Zhilin Chen, James Moon, Wei Cheng
The number and spacing of B-cell epitopes on antigens have a profound impact on the activation of B cells and elicitation of antibody responses, the quantitative aspects of which may be utilized for rational design of vaccines. Ni-chelating liposomes have been widely used as protein carriers in experimental studies of vaccine delivery, owing to the convenience and versatility of this conjugation chemistry. However, the epitope number per particle as well as the stability of protein conjugation on liposomes remain far less characterized...
March 12, 2018: Bioconjugate Chemistry
Ewelina Wieczorek, Dariusz T Mlynarczyk, Malgorzata Kucinska, Jolanta Dlugaszewska, Jaroslaw Piskorz, Lukasz Popenda, Wojciech Szczolko, Stefan Jurga, Marek Murias, Jadwiga Mielcarek, Tomasz Goslinski
5,7-Diaryl-substituted symmetrical diazepinoporphyrazine and tribenzodiazepinoporphyrazine were synthesized and characterized using UV-Vis, MS MALDI, and various NMR techniques. The expected photosensitizing potentials of these porphyrazines were evaluated by measuring their abilities to generate singlet oxygen in organic solvents and by comparing them with that of the recently obtained dendrimeric G1-type diazepinoporhyrazine. Absorbance and fluorescence measurements were performed to study the aggregation properties of the novel macrocycles...
February 26, 2018: European Journal of Medicinal Chemistry
Zahraa S Al-Ahmady, Marilena Hadjidemetriou, James Gubbins, Kostas Kostarelos
Thermally triggered drug release from temperature-sensitive liposomes (TSL) holds great promise for cancer therapy. Different types of TSL have been designed recently for heat triggered drug release inside tumor blood vessels or after accumulation into the tumor interstitium. However, justification of drug release profiles was mainly based on in vitro release data. While these methods could be good enough to give early indication about the thermal sensitivity of TSL, they are still far from being optimum. This is because these methods do not take into consideration the actual adsorption of proteins onto the surface of TSL after their in vivo administration, also known as "protein corona" and the influence this could have on drug release...
March 6, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Jasmin Monpara, Chryso Kanthou, Gillian M Tozer, Pradeep R Vavia
PURPOSE: This work explores synthesis of novel cholesterol derivative for the preparation of cationic liposomes and its interaction with Paclitaxel (PTX) within liposome membrane using molecular dynamic (MD) simulation and in-vitro studies. METHODS: Cholesteryl Arginine Ethylester (CAE) was synthesized and characterized. Cationic liposomes were prepared using Soy PC (SPC) at a molar ratio of 77.5:15:7.5 of SPC/CAE/PTX. Conventional liposomes were composed of SPC/cholesterol/PTX (92:5:3 M ratio)...
March 8, 2018: Pharmaceutical Research
Shima Gholizadeh, Emmy M Dolman, Rebecca Wieriks, Rolf W Sparidans, Wim E Hennink, Robbert J Kok
PURPOSE: Sepantronium bromide (YM155) is a hydrophilic quaternary compound that cannot be administered orally due to its low oral bioavailability; it is furthermore rapidly eliminated via the kidneys. The current study aims at improving the pharmacokinetic profile of YM155 by its formulation in immunoliposomes that can achieve its enhanced delivery into tumor tissue and facilitate uptake in neuroblastoma cancer cells. METHODS: PEGylated YM155 loaded liposomes composed of DPPC, cholesterol and DSPE-PEG2000 were prepared via passive film-hydration and extrusion method...
March 7, 2018: Pharmaceutical Research
Jiulong Zhang, Chunrong Yang, Shuang Pan, Menghao Shi, Jie Li, Haiyang Hu, Mingxi Qiao, Dawei Chen, Xiuli Zhao
Mitochondrial-targeting therapy was considered to be a promising approach for the efficient treatment of cancer while positive charge induced nonspecific cytotoxicity severely limits its application. To overcome this drawback, a novel mitochondria targeted conjugate triphenylphosphine-docetaxel (TD) has been synthesized successfully and incorporated it into liposomes (EPSLP/TD), which possessed excellent pH-sensitive characteristic, EphA 10 mediated active targetability as well as mitochondria-targeting capability...
November 2018: Drug Delivery
Masayuki Miyagi, Kentaro Uchida, Shotaro Takano, Hisako Fujimaki, Jun Aikawa, Hiroyuki Sekiguchi, Naoshige Nagura, Seiji Ohtori, Gen Inoue, Masashi Takaso
Upregulation of inflammatory cytokines and various growth factors is a significant contributor to discogenic low back pain. The aim of this study was to investigate possible regulation of pain-related molecules by macrophages and the role of macrophage-derived molecules in injured intervertebral disc (IVD)s. C57BL/6J mice were used in this study. We characterized the expression profiles of genes for tumor necrosis factor (TNF)-alpha, interleukin (IL)-1beta, nerve growth factor (NGF), and vascular endothelial growth factor (VEGF) in both intact and injured IVDs...
March 6, 2018: Journal of Orthopaedic Research: Official Publication of the Orthopaedic Research Society
Daihyun Kim, Jinghui Luo, Edgar A Arriaga, Alexandra Ros
Resolving the heterogeneity of particle populations by size is important when the particle size is a signature of abnormal biological properties leading to disease. Accessing size heterogeneity in the sub-micrometer regime is particularly important to resolve populations of sub-cellular species or diagnostically relevant bioparticles. Here, we demonstrate a ratchet migration mechanism capable of separating sub-µm sized species by size and apply it to biological particles. The phenomenon is based on a deterministic ratchet effect, is realized in a microfluidic device and exhibits fast migration allowing separation in tens of seconds...
March 6, 2018: Analytical Chemistry
Daan Vorselen, Margherita Marchetti, Carmen López-Iglesias, Peter J Peters, Wouter H Roos, Gijs J L Wuite
Small multilamellar vesicles may have benefits over unilamellar vesicles for drug delivery, such as an increased volume for hydrophobic drugs. In addition, their altered mechanical properties might be beneficial for cellular uptake. Here, we show how atomic force microscopy (AFM) can be used to detect and characterize multilamellar vesicles. We quantify the size of each break event occurring during AFM nanoindentations, which shows good agreement with the thickness of supported lipid bilayers. Analyzing the size and number of these events for individual vesicles allows us to distinguish between vesicles consisting of 1 up to 5 bilayers...
March 5, 2018: Nanoscale
Marinalva Cardoso Dos Santos, Thais Kroetz, Cristiana Lima Dora, Fernando Carlos Giacomelli, Tiago Elias Allievi Frizon, Claus Tröger Pich, Luciano da Silva Pinto, Amanda Sigal Soares, Fabiano Severo Rodembusch, Vânia Rodrigues de Lima, Alexandre Gonçalves Dal-Bó
Investigations focused on the interactions of nanoparticles with lectins are relevant since it is well accepted that such proteins can be recognized by carbohydrates as parts of cell membranes. This can ultimately enhance the cellular uptake of the produced assemblies. In this framework, the physical interactions of phosphatidylcholine (PC) liposomes and the Bauhinia variegate lectin (BVL) are reported here. BVL-liposome interactions were characterized by a variety of techniques to understand the influence of BVL in the structural features, thermodynamic and spectroscopic properties of the hybrid material...
February 24, 2018: Journal of Colloid and Interface Science
Damodara N Reddy, Sukrit Singh, Chris M W Ho, Janki Patel, Paul Schlesinger, Stephen Rodgers, Allan Doctor, Garland R Marshall
Gramicidin A, a topical antibiotic made from alternating L and D amino acids, is characterized by its wide central pore; upon insertion into membranes, it forms channels that disrupts ion gradients. We present helical peptidomimetics with this characteristic wide central pore that have been designed to mimic gramicidin A channels. Mimetics were designed using molecular modeling focused on oligomers of heterochiral dipeptides of proline analogs, in particular azaproline (AzPro). Molecular Dynamics simulations in water confirmed the stability of the designed helices...
February 20, 2018: European Journal of Medicinal Chemistry
Syed Mahmood, Uttam Kumar Mandal, Bappaditya Chatterjee
Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method...
February 28, 2018: International Journal of Pharmaceutics
Lisa Belfiore, Darren N Saunders, Marie Ranson, Kristofer J Thurecht, Gert Storm, Kara L Vine
The development of therapeutic resistance to targeted anticancer therapies remains a significant clinical problem, with intratumoral heterogeneity playing a key role. In this context, improving the therapeutic outcome through simultaneous targeting of multiple tumor cell subtypes within a heterogeneous tumor is a promising approach. Liposomes have emerged as useful drug carriers that can reduce systemic toxicity and increase drug delivery to the tumor site. While clinically-used liposomal drug formulations show marked therapeutic advantages over free drug formulations, ligand-functionalized liposome drug formulations that can target multiple tumor cell subtypes may further improve the therapeutic efficacy by facilitating drug delivery to a broader population of tumor cells making up the heterogeneous tumor tissue...
March 1, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Wenshuang Wu, Ming-Hai Tang, Huan Tang, Kai Chen, Jie Fu, Lun Wang, Lin-Lin Xue, Aihua Peng, Haoyu Ye, Li-Juan Chen
Natural products and their derivatives have historically been invaluable as a source of therapeutic agents. Honokiol, as a well-known natural product in Chinese herbal medicine Houpu, is finally being studied in a Phase I clinical trial (CTR20170822) in patients with Advanced Non-Small Cell Lung Cancer (NSCLS) in China this year. During the honokiol liposome formulation process, five major impurities were present in the range of 0.05-0.1% based on the HPLC analysis. These five major impurities were obtained from the forced degradation product of honokiol through countercurrent chromatography and prep-HPLC...
February 21, 2018: Journal of Pharmaceutical and Biomedical Analysis
Bappa Maiti, Mohini Kamra, Anjali A Karande, Santanu Bhattacharya
Herein, five new α-tocopheryl cationic gemini lipids with hydroxyethyl bearing headgroups (THnS, n = 4, 5, 6, 8, 12) have been synthesized for efficient plasmid DNA (pDNA) delivery into cancer cells. Among these gemini lipid formulations, the lipid with an octamethylene [-(CH2 )8 ] spacer (TH8S) showed the highest transfection efficiency (TE) that was comparable to that of the commercial standard lipofectamine 2000 (L2K) in terms of luciferase expression in HepG2 (liver hepatocellular carcinoma) cells. The addition of the helper lipid DOPE (1,2-dioleoyl phosphatidyl ethanolamine) with cationic lipids in mixed liposomes further enhanced the TE and the optimized molar ratio was 2 : 1 (DOPE : cationic lipid)...
March 2, 2018: Organic & Biomolecular Chemistry
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