Metabolomic Profile, Plasmatic Levels of Losartan and EXP3174, Blood Pressure Control in Hypertensive Patients and Their Correlation with COVID-19.

Systemic arterial hypertension (SAH) is one of the most prevalent chronic diseases worldwide and is related to serious health complications. It has been pointed out as a major risk factor for COVID-19. This study aimed to determine the impact of COVID-19 on the metabolomic profile, the correlation with the plasmatic levels of losartan and its active metabolite (EXP3174), biochemical markers, and blood pressure (BP) control in hypertensive patients.

J-filter: An experiment to simplify and isolate specific signals in H NMR spectra of complex mixtures based on scalar coupling constants.

One-dimensional selective NMR experiments relying on a J-filter element are proposed to isolate specific signals in crowded H spectral regions. The J-filter allows the edition or filtering of signals in a region of interest of the spectrum by exploiting the specific values of their H- H coupling constants and certain parameters of protons coupled to them that appear in less congested parts of the spectrum (chemical shifts and coupling constants). The new experiments permitted the isolation of specific peaks of phytosterol components in a sample obtained from a liquid nutraceutical recommended for lowering blood cholesterol levels in regions with complete overlap in the H spectrum.

Metabolomic Profile and Its Correlation with the Plasmatic Levels of Losartan, EXP3174 and Blood Pressure Control in Hypertensive and Chronic Kidney Disease Patients.

Systemic arterial hypertension (SAH) is one of the most prevalent chronic diseases worldwide and, when dysregulated, may cause serious complications. Losartan (LOS) blocks relevant physiological aspects of hypertension, acting mainly on the reduction of peripheral vascular resistance. Complications of hypertension include nephropathy, in which diagnosis is based on the observation of functional or structural renal dysfunction.

Zein Nanoparticles Containing Arginine-Based Surfactants: Physicochemical Characterization and Effect on the Biological Properties.

Cationic surfactants carry antimicrobial activity, based on their interaction and disruption of cell membranes. Nonetheless, their intrinsic toxicity limits their applicability. To overcome this issue, a feasible strategy consists of using solid nanoparticles to improve their delivery.

Antifungal Combination Eye Drops for Fungal Keratitis Treatment.

Fungal keratitis (FK) is a corneal mycotic infection that can lead to vision loss. Furthermore, the severity of FK is aggravated by the emergence of resistant fungal species. There is currently only one FDA-approved formulation for FK treatment forcing hospital pharmacy departments to reformulate intravenous drug preparations with unknown ocular bioavailability and toxicity.

Zein Nanoparticles Containing Arginine-Phenylalanine-Based Surfactants: Stability, Antimicrobial and Hemolytic Activity.

Although cationic surfactants have a remarkable antimicrobial activity, they present an intrinsic toxicity that discourages their usage. In this work novel zein nanoparticles loaded with arginine-phenylalanine-based surfactants are presented. The nanoparticles were loaded with two single polar head (LAM and PNHC) and two with double amino acid polar head surfactants, arginine-phenylalanine (CPAM, PANHC).

Silk fibroin/cholinium gallate-based architectures as therapeutic tools.

The combination of natural resources with biologically active biocompatible ionic liquids (Bio-IL) is presented as a combinatorial approach for developing tools to manage inflammatory diseases. Innovative biomedical solutions were constructed combining silk fibroin (SF) and Ch[Gallate], a Bio-IL with antioxidant and anti-inflammatory features, as freeze-dried 3D-based sponges. An evaluation of the effect of the Ch[Gallate] concentration (≤3% w/v) on the SF/Ch[Gallate] sponges was studied.

Unveiling an NMR-Invisible Fraction of Polymers in Solution by Saturation Transfer Difference.

The observation of signals in solution NMR requires nuclei with sufficiently large transverse relaxation times (). Otherwise, broad signals embedded in the baseline afford an invisible fraction of nuclei (IF). Based on the STD (saturation transfer difference) sequence, IF-STD is presented as a quick tool to unveil IF in the H NMR spectra of polymers.

Design, optimization, and in vitro characterization of idebenone-loaded PLGA microspheres for LHON treatment.

Biodegradable poly(lactic-co-glycolic acid) microspheres (PLGA MSs) are attractive delivery systems for site-specific maintained release of therapeutic active substances into the intravitreal chamber. The design, development, and characterization of idebenone-loaded PLGA microspheres by means of an oil-in-water emulsion/solvent evaporation method enabled the obtention of appropriate production yield, encapsulation efficiency and loading values. MSs revealed spherical shape, with a size range of 10-25 μm and a smooth and non-porous surface.

Targeted H NMR metabolomics and immunological phenotyping of human fresh blood and serum samples discriminate between healthy individuals and inflammatory bowel disease patients treated with anti-TNF.

Inflammatory bowel disease is a multifactorial etiology, associated with environmental factors that can trigger both debut and relapses. A high level of tumor necrosis factor-α in the gut is the main consequence of immune system imbalance. The aim of treatment is to restore gut homeostasis.

In situ forming and mucoadhesive ophthalmic voriconazole/HPβCD hydrogels for the treatment of fungal keratitis.

Fungal keratitis is a severe infectious corneal disease. At present, no voriconazole ophthalmic formulations are approved by the FDA or EMA. This lack of therapeutic options leads to the reformulation of intravenous voriconazole preparations (VFEND®) by the hospital pharmacy departments to prepare the appropriate ophthalmic formulations (pharmacy compounding).

Development and Characterization of a Tacrolimus/Hydroxypropyl-β-Cyclodextrin Eye Drop.

Uveitis is a vision inflammatory disorder with a high prevalence in developing countries. Currently, marketed treatments remain limited and reformulation is usually performed to obtain a tacrolimus eye drop as a therapeutic alternative in corticosteroid-refractory eye disease. The aim of this work was to develop a mucoadhesive, non-toxic and stable topical ophthalmic formulation that can be safely prepared in hospital pharmacy departments.

Toxicological and genotoxic evaluation of anacardic acid loaded-zein nanoparticles in mice.

Anacardic acid extracted from cashew nut shells of L has demonstrated important biological activities, such as antibacterial activity against the cariogenic specie . Zein nanoparticles containing anacardic acid (9.375 μg/mL) were evaluated in terms of toxicity and genotoxicity .

Hot melt-extrusion improves the properties of cyclodextrin-based poly(pseudo)rotaxanes for transdermal formulation.

This study aimed to investigate whether hot-melt extrusion (HME) processing can modify the interactions between drugs, cyclodextrins and polymers, and in turn alter the microstructure and properties of supramolecular gels. Mixtures composed of amphiphilic polymer (Soluplus), cyclodextrin (HPβCD or αCD), plasticizer (PEG400 or PEG6000) and colloidal silicon dioxide were processed by HME. Carvedilol (CAR) was added to the formulation aiming its transdermal delivery.

- Modeling Approach to Rationally Designed Simple and Versatile Drug Delivery Systems.

Rational design and development of a nanosystem usually relies on empirical approaches as well as a fair degree of serendipity. Understanding how nanosystems behave at the molecular level is of great importance for potential biomedical applications. In this work, we describe a nanosystem composed of two natural compounds, vitamin E and sphingomyelin, prepared by spontaneous emulsification (vitamin E-sphingomyelin nanosystems (VSNs)).

An experimental and computational NMR study of organometallic nine-membered rings: Trinuclear silver(I) complexes of pyrazolate ligands.

This work reports the calculation of the nuclear magnetic resonance (NMR) chemical shifts of eight trinuclear Ag(I) complexes of pyrazolate ligands using the relativistic program ZORA. The data from the literature concern exclusively H, C, and F nuclei. For this reason, one of the complexes that is derived from 3,5-bis-trifluoromethyl-1H-pyrazole has been studied anew, and the N and Ag chemical shifts determined for the first time in solution.

Both chemical and crystalline phase configuration influence the molecular features of humic acids in humic-calcium-phosphates fertilizers.

Phosphate-metal-humic complexes are very relevant in nature due to their crucial role in phosphate availability for plants and microorganisms. Synthetic phosphate-calcium-humic acid (HA) complexes have proven to be efficient sources of available phosphorus for crops. However, the current knowledge about their structure and molecular features is very poor.

The subdivision behavior of polymeric tablets.

The subdivision behavior of polymeric tablets produced with the well-known polymers Soluplus® (SOL), polyvinyl pyrrolidone co-vinyl acetate (PVPVA) and hydroxypropyl methylcellulose (HPMC) was evaluated in this study. The polymeric tablets were submitted to different post-treatments (aging, thermal and exposure to compressed gaseous carbon dioxide) and its mechanical, spectroscopic and microstructure properties were assessed. SOL tablets showed the best results for tablet subdivision, particularly, the mean mass variation (3.

Structure, rheology, and copper-complexation of a hyaluronan-like exopolysaccharide from Vibrio.

MO245 exopolysaccharide (EPS) was produced in laboratory conditions from Vibrio genus microorganism isolated from bacterial mats found in Moorea Island. Its structure consists of a linear tetrasaccharide repeating unit →4)-β-D-GlcpA-(1→4)-α-D-GalpNAc-(1→3)-β-D-GlcpNAc-(1→4)-β-D-GlcpA-(1→ containing covalently-linked 5% of glucose, galactose, and rhamnose, determined by methylation analyses and NMR spectroscopy. The molecular weight, radius of gyration (R) and intrinsic viscosity, [η], determined by gel permeation chromatography with light scattering and viscosity detection, were 513 ± 4 kDa (PDI, 1.

Lipopolysaccharide (LPS)-induced septic shock causes profound changes in myocardial energy metabolites in pigs.

Introduction: Energy deficiency is a cause for myocardial dysfunction during septic shock. In rodents, septic shock decreases the oxidation of long-chain fatty acids and glucose in the myocardium causing energy deficiency. However, the effect of septic shock on myocardial energy metabolites in large animals and human is unknown.

Biopharmaceutical Activities Related to Ellagic Acid, Chitosan, and Zein and Their Improvement by Association.

Ellagic acid (EA) has demonstrated several biological properties, such as antioxidant, antimicrobial, and enzymatic inhibition. Zein and chitosan (CHI) are natural polymers whose biological potential has also gained attention. Therefore, this paper aimed to evaluate the antimicrobial, antioxidant, anticollagenase, and antielastase properties of EA, zein, and chitosan isolated or in combination.

Cyclodextrin-based poly(pseudo)rotaxanes for transdermal delivery of carvedilol.

This work aimed to design supramolecular gels combining Soluplus or Solutol and alfa- and hydroxypropyl-β-cyclodextrin (α-CD, HPβ-CD) for carvedilol (CAR) transdermal delivery. Poly(pseudo)rotaxane formation (appearance, SEM, H NMR), drug solubilization, rheological properties and in vitro release were investigated. CAR-CD complexes were prepared in situ or by spray drying.

Sorbitan ester nanoparticles (SENS) as a novel topical ocular drug delivery system: Design, optimization, and in vitro/ex vivo evaluation.

We explored the potential of two types of sorbitan ester nanoparticles (SENS) as novel tools for topical ocular drug delivery. The optimized SENS formulation (SENS-OPT) consisted of nanoparticles (NPs) of 170.5 nm, zeta potential +33.

New Amphiphilic Composite for Preparing Efficient Coated Potassium-Fertilizers for Top-Dressing Fertilization of Annual Crops.

This study describes the efficiency of a new coating material for preparing granulated potassium-fertilizers with a potassium release to the soil solution sensitive to rainfall intensity. The composite is prepared by reaction of an alkyd-resin with cement in the absence of water. The complementary use of diverse analytical techniques showed that the presence of the cement fraction induced alkyd resin reticulation and gradual cement-resin hardening.

Mobility of Water and Polymer Species and Rheological Properties of Supramolecular Polypseudorotaxane Gels Suitable for Bone Regeneration.

The aim of this work was to prepare polypseudorotaxane-based supramolecular gels combining αCD with two temperature-responsive copolymers of different architecture (i.e., linear poloxamer P and X-shaped poloxamine T), at the lowest concentration as possible to form syringeable depots, and to shed light on the self-diffusion and spatial closeness of all components (including water) which in turn may determine the cooperative self-assembly phenomena and the performance of the gels at the macroscopic level.