Search results for "RELEASE"
showing 10 items of 602 documents
Famotidine inhibits toll-like receptor 3-mediated inflammatory signaling in SARS-CoV-2 infection
2021
Apart from prevention using vaccinations, the management options for COVID-19 remain limited. In retrospective cohort studies, use of famotidine, a specific oral H2 receptor antagonist (antihistamine), has been associated with reduced risk of intubation and death in patients hospitalized with COVID-19. In a case series, nonhospitalized patients with COVID-19 experienced rapid symptom resolution after taking famotidine, but the molecular basis of these observations remains elusive. Here we show using biochemical, cellular, and functional assays that famotidine has no effect on viral replication or viral protease activity. However, famotidine can affect histamine-induced signaling processes i…
More than a pore: How voltage-gated calcium channels act on different levels of neuronal communication regulation.
2021
ABSTRACT Voltage-gated calcium channels (VGCCs) represent key regulators of the calcium influx through the plasma membrane of excitable cells, like neurons. Activated by the depolarization of the membrane, the opening of VGCCs induces very transient and local changes in the intracellular calcium concentration, known as calcium nanodomains, that in turn trigger calcium-dependent signaling cascades and the release of chemical neurotransmitters. Based on their central importance as concierges of excitation-secretion coupling and therefore neuronal communication, VGCCs have been studied in multiple aspects of neuronal function and malfunction. However, studies on molecular interaction partners …
Role of aroma–matrix interactions on perception of structured emulsions
2011
The impact of the composition of spreads on in vivo aroma release and aroma perception was investigated using online proton transfer reaction mass spectrometry (PTR-MS) and sensory methodologies. Consumption of model products spread on bread induced a significant increase in aroma release and better discrimination in aroma perception, compared to when the product was tasted pure from a spoon. Dynamic release of a series of 10 aroma compounds was slower with the increase in solid fat content, and the quantity decreased when proteins were added. Sensory ranking of model products mostly confirmed the release results.
Salt and Aroma Compound Distributions Influence Flavour Release and Temporal Perception While Eating Hot-Served Flans.
2021
International audience; To counteract the negative effect of salt overconsumption on health, strategies have been developed to reduce the salt content in food products. Among them, two promising strategies based on odour-induced saltiness enhancement and the heterogeneous distribution of flavour compounds were combined and assessed in four-layer cream-based snacks. To investigate the relationship between saltiness enhancement, temporal release and perception of flavour compounds in hot snacks with heterogeneous distribution of salt and aroma compounds, complementary techniques were used: nose space PTR-Tof-MS (Proton Transfer Reaction-Time of Flight–Mass Spectrometry) to assess the release …
PHEA-PLA biocompatible nanoparticles by technique of solvent evaporation from multiple emulsions
2015
Nanocarriers of amphiphilic polymeric materials represent versatile delivery systems for poorly water soluble drugs. In this work the technique of solvent evaporation from multiple emulsions was applied to produce nanovectors based on new amphiphilic copolymer, the α,β-poly(N-2-hydroxyethyl)-DL-aspartamide-polylactic acid (PHEA-PLA), purposely synthesized to be used in the controlled release of active molecules poorly soluble in water. To this aim an amphiphilic derivative of PHEA, a hydrophilic polymer, was synthesized by derivatization of the polymeric backbone with hydrophobic grafts of polylactic acid (PLA). The achieved copolymer was thus used to produce nanoparticles loaded with α toc…
Stabilization of unilamellar catanionic vesicles induced by β-cyclodextrins: A strategy for a tunable drug delivery depot.
2018
The limited stability of catanionic vesicles has discouraged their wide use for encapsulation and controlled release of active substances. Their structure can easily break down to form lamellar phases, micelles or rearrange into multilamellar vesicles, as a consequence of small changes in their composition. However, despite the limited stability, catanionic vesicles possess an attractive architecture, which is able to efficiently encapsulate both hydrophobic and hydrophilic molecules. Therefore, improving the stability of the vesicles, as well as the control on unilamellar structures, are prerequisites for their wider application range. This study focuses on the impact of β-cyclodextrins fo…
Synchronizing the release rates of salicylate and indomethacin from degradable chitosan hydrogel and its optimization by definitive screening design.
2018
Abstract Three types of ionically crosslinked (with citric acid) chitosan discs were loaded with the highly water- soluble drug, sodium salicylate (SS) and the poorly water-soluble drug, indomethacin (Ind). In separate experiments the hydrated discs were immersed in a de-crosslinking solution comprising of different concentrations of calcium chloride, which induced a controlled erosion of the discs, a process which was optimized to synchronize the release rates of the two drugs over a predetermined period of time. The optimization was accomplished by manipulating six factors: chitosan MW, its amount in the formulation, the concentration of the crosslinker agent, the concentration of the de-…
Acid‐Cleavable Poly(ethylene glycol) Hydrogels Displaying Protein Release at pH 5
2020
Abstract PEG is the gold standard polymer for pharmaceutical applications, however it lacks degradability. Degradation under physiologically relevant pH as present in endolysosomes, cancerous and inflammatory tissues is crucial for many areas. The authors present anionic ring‐opening copolymerization of ethylene oxide with 3,4‐epoxy‐1‐butene (EPB) and subsequent modification to introduce acid‐degradable vinyl ether groups as well as methacrylate (MA) units, enabling radical cross‐linking. Copolymers with different molar ratios of EPB, molecular weights (M n) up to 10 000 g mol−1 and narrow dispersities (Đ<1.05) were prepared. Both the P(EG‐co‐isoEPB)MA copolymer and the hydrogels showed pH‐…
Quantitative analysis of the effect of controlled-release formulation on nonlinear gastrointestinal absorption of P-glycoprotein substrate talinolol …
2020
Abstract Oral absorption of talinolol, a substrate of P-glycoprotein (P-gp), from a sustained-release (SR) formulation was reportedly decreased compared to that from an immediate-release (IR) formulation. The aim of this study was to predict and understand the effect of controlled-release formulation on the oral absorption of P-gp substrates by developing a physiologically based pharmacokinetic (PBPK) absorption model incorporating multiple kinetic parameters obtained from in vitro studies, using talinolol as a model substrate. Simulation analysis using the developed PBPK absorption model indicated that the clinically observed marked decrease in the plasma concentration of talinolol adminis…
Acute effects of different foam rolling volumes in the interset rest period on maximum repetition performance
2017
Background - Foam rolling (FR) is a ubiquitous intervention utilised for the purpose of acutely increasing the range of motion without subsequent decreases in performance. Thus, it is commonly used during the periworkout period—that is, prior to, during, or after an athlete's workout.\ud \ud Objective - This study investigated how different FR durations applied to the quadriceps during the interset rest periods affects the numbers of repetitions in the knee extension exercise.\ud \ud Methods - Twenty-five females completed four sets of knee extensions with 10 repetitions of maximum load to concentric failure on four occasions. Between each set, a 4-minute rest interval was implemented in wh…