Temperature stimuli-responsive nanoparticles from chitosan-graft-poly(N-vinylcaprolactam) as a drug delivery system

This work describes the preparation of thermosensitive chitosan-graft-poly(N-vinylcaprolactam) nanoparticles by ionic gelation and their potential use as a controlled drug delivery system, using doxorubicin as a model drug. A systematic study of the effect of the main processing parameters on both the size and thermoresponsive behavior of nanoparticles was investigated. The size of the particles is strongly dependent on the length of the poly(N-vinylcaprolactam) grafted chains and the concentration of the copolymer and crosslinking agent solutions. The molecular structure of the copolymer plays an essential role in the phase transition temperature of the particles, which decreases with the length of PVCL grafted chain. The system displayed proper drug-association parameters, and the drug-loaded nanoparticles exhibited dose-dependent cytotoxicity. A significant increase in the doxorubicin delivery rate was observed above the phase transition temperature (40 °C). These features indicate that these nanoparticles are suitable for the development of a new thermally controlled anti-cancer drug delivery system. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019 , 136, 47831.     

Structural and adhesion properties of poly(ethyl 2-cyanoacrylate) post-cured at different temperatures and times

The structure and properties of poly(ethyl 2-cyanoacrylate)s (pECNs) cured at 25?°C during 24?hours, and post-cured at different temperatures (45-90?°C) and times (2-6?hours) were studied. Irrespective of the post-cure conditions, pECN was not fully polymerized and two different structures of different molecular weights and topographies were obtained. The post-cure decreased the shear strength values in joints made with aluminum and ethyl cyanoacrylate due to the decrease in the percentage of higher molecular weight polymeric chains and the formation of new short polymeric chains by unzipping de-polymerization mechanism, both contributed to decrease the mechanical properties. On the other hand, the post-cure changed the morphology of pECN because of nano-spheres were produced by curing at 25?°C which were not present after post-cure at 90?°C.     

Anticoagulant, Antioxidant and Antitumor Activities of Heterofucans from the Seaweed Dictyopteris delicatula

In the present study, six families of sulfated polysaccharides were obtained from seaweed Dictyopteris delicatula by proteolytic digestion, followed by acetone fractionation and molecular sieving on Sephadex G-100. Chemical analyses demonstrated that all polysaccharides contain heterofucans composed mainly of fucose, xylose, glucose, galactose, uronic acid, and sulfate. The fucans F0.5v and F0.7v at 1.0 mg/mL showed high ferric chelating activity (～45%), whereas fucans F1.3v (0.5 mg/mL) showed considerable reducing power, about 53.2% of the activity of vitamin C. The fucan F1.5v presented the most prominent anticoagulant activity. The best antiproliferative activity was found with fucans F1.3v and F0.7v. However, F1.3v activity was much higher than F0.7v inhibiting almost 100% of HeLa cell proliferation. These fucans have been selected for further studies on structural characterization as well as in vivo experiments, which are already in progress.     

Evidence for the existence of a specific g protein-coupled receptor activated by guanosine

Guanosine, released extracellularly from neurons and glial cells, plays important roles in the central nervous system, including neuroprotection. The innovative DELFIA Eu‐GTP binding assay was optimized for characterization of the putative guanosine receptor binding site at rat brain membranes by using a series of novel and known guanosine derivatives. These nucleosides were prepared by modifying the purine and sugar moieties of guanosine at the 6‐ and 5′‐positions, respectively. Results of these experiments prove that guanosine, 6‐thioguanosine, and their derivatives activate a G protein‐coupled receptor that is different from the well‐characterized adenosine receptors.     

Neuropeptide S receptor: recent updates on nonpeptide antagonist discovery

Neuropeptide?S (NPS) is a 20-amino acid peptide of great interest due to its possible involvement in several biological processes, including food intake, locomotion, wakefulness, arousal, and anxiety. Structure-activity relationship studies of NPS have identified key points for structural modifications with the goal of modulating NPS receptor (NPSR) agonist activity or achieving antagonism at the same receptor. Only limited information is available for nonpeptide NPSR antagonists. In the last year, several studies have been reported in literature which present various series of small molecules as antagonists of this receptor. The results allow a comparison of the structures and activities of these molecules, leading to the design of new ligands with increased potency and improved pharmacological and pharmacokinetic profiles. This work presents a brief overview of the available information regarding structural features and pharmacological characterization of published nonpeptide NPSR antagonists.     

Biodegradable metals for cardiovascular stent application: interests and new opportunities

During the last decade, biodegradable metallic stents have been developed and investigated as alternatives for the currently-used permanent cardiovascular stents. Degradable metallic materials could potentially replace corrosion-resistant metals currently used for stent application as it has been shown that the role of stenting is temporary and limited to a period of 6-12 months after implantation during which arterial remodeling and healing occur. Although corrosion is generally considered as a failure in metallurgy, the corrodibility of certain metals can be an advantage for their application as degradable implants. The candidate materials for such application should have mechanical properties ideally close to those of 316L stainless steel which is the gold standard material for stent application in order to provide mechanical support to diseased arteries. Non-toxicity of the metal itself and its degradation products is another requirement as the material is absorbed by blood and cells. Based on the mentioned requirements, iron-based and magnesium-based alloys have been the investigated candidates for biodegradable stents. This article reviews the recent developments in the design and evaluation of metallic materials for biodegradable stents. It also introduces the new metallurgical processes which could be applied for the production of metallic biodegradable stents and their effect on the properties of the produced metals.     

Application of empirical modelling in multi-layers membrane manufacturing

Multistructured membranes based on ultrafine fibers of polymethylmethacrylate-co-methacrylic acid (PMMA-co-MAA) and TiO₂ nanoparticles have been obtained by electrohydrodynamic (EHD) technologies, for active filter media manufacturing. Process optimization of the nanofibers based layers has been investigated by response surface methodology (RSM) in order to predict the domain of the parameters where the smallest fiber diameter can be achieved. A quantitative relationship between electrospinning parameters and the responses (mean diameter and standard deviation) was established and then the final multi-layers structure of nanofibers and nanoparticles has been achieved for a controlled and robust process. The nanostructured membranes have been characterized by SEM imaging, EDAX, TGA analysis and water vapour permeability and their photocatalytic activity has been tested on VOCs degradation.