Background: The integration of positron emission tomography (PET) and magnetic resonance imaging (MRI) holds promise for advancing diagnostic imaging capabilities. The METRICS project aims to develop cyclotron-driven production of Mn for PET/MRI imaging.
Results: Using the Cr(p,n)Mn reaction, we designed chromium metal targets via Spark Plasma Sintering and developed a separation procedure for isolating Mn.
The data presented in this article are an update of the dataset provided by Musazzi et al. [1] and are related to the research article entitled "Equivalence assessment of creams with quali-quantitative differences in light of the EMA and FDA regulatory framework" [2]. In vitro permeation study (IVPT) is typically conducted using the method of Franz's diffusion cell for assessing the biopharmaceutical performance of topically applied products.
View Article and Find Full Text PDFLocal drug delivery to the esophagus is hampered by rapid transit time and poor permeability of the mucosa. If some strategies aimed to improve the residence time have been proposed, non-invasive approaches to increase the drug penetration in the mucosa have not been described so far. Herein, we designed mucosa-penetrating liposomes to favor the penetration and retention of curcumin (CURC) in the esophagus.
View Article and Find Full Text PDFSelf-immolative (SI) spacers are degradable chemical connectors widely used in prodrugs and drug conjugates to release pharmaceutical ingredients in response to specific stimuli. Amine-carbamate SI spacers are particularly versatile, as they have been used to release different hydroxy cargos, ranging from 2° and 3° alcohols to phenols and oximes. In this work, we describe the ability of three amine-carbamate SI spacers to release three structurally similar imidazoquinoline payloads, bearing either a 1°, a 2° or a 3° alcohol as the leaving group.
View Article and Find Full Text PDFHerein, we investigate the use of organic photocatalysts in the visible light-promoted β-functionalization of carbonyl compounds. In particular, we studied the addition of aliphatic aldehydes to α,β-unsaturated compounds (β-Michael addition), and the reaction of cyclic ketones with either ketones (β-aldol condensation) or imines (β-Mannich reaction). Among the dyes tested, donor-acceptor cyanoarenes gave the best results, promoting the transformations of interest in moderate to good yields.
View Article and Find Full Text PDFMaterials (Basel)
September 2023
Very few metals can be found in metallic form in nature; the vast majority have to be processed from their ores at a great cost in terms of energy and money [...
View Article and Find Full Text PDFFeasibility of electrospinning in the manufacturing of sildenafil-containing orodispersible films (ODFs) intended to enhance oxygenation and to reduce pulmonary arterial pressure in pediatric patients was evaluated. Given the targeted subjects, the simplest and safest formulation was chosen, using water as the only solvent and pullulan, a natural polymer, as the sole fiber-forming agent. A systematic characterization in terms of shear and extensional viscosity as well as surface tension of solutions containing different amounts of pullulan and sildenafil was carried out.
View Article and Find Full Text PDFThe deformation behavior of duplex stainless steel under tension and bending, accompanied by a pulsed current and when heated by an external source, is investigated. The stress-strain curves are compared at the same temperatures. The contribution to the decrease in flow stresses is greater when using a multi-pulse current at the same temperature, compared to external heating.
View Article and Find Full Text PDFThe realization of isotopically enriched Ti targets for nuclear cross-section measurements requires particular attention, from the starting material preparation up to the deposition technique. In this work, a cryomilling process was developed and optimized, aimed at reducing the size of Ti metal sponge as provided by the supplier (size up to 3 mm), to the optimal size of 10 µm, to fit the High Energy Vibrational Powder Plating technique used for target manufacturing. The optimization of the cryomilling protocol and the HIVIPP deposition using Ti material was thus performed.
View Article and Find Full Text PDFSalicylaldehyde (SA) derivatives are emerging as useful fragments to obtain reversible-covalent inhibitors interacting with the lysine residues of the target protein. Here the SA installation at the C terminus of an integrin-binding cyclopeptide, leading to enhanced ligand affinity for the receptor as well as stronger biological activity in cultured glioblastoma cells is reported.
View Article and Find Full Text PDFOver the past 20 years, the interest in Cannabis oily extracts for medicinal use compounded in pharmacy has consistently grown, along with the need to have preparations of adequate quality. Hot maceration (M) is the most frequently used method to compound oily solutions. In this work, we systematically studied the possibility of using an ultrasonic homogenizer and a sonotrode (US) as an alternative extraction method.
View Article and Find Full Text PDFIn this work, plasma electrolytic oxidation (PEO) process was applied on AlSi10Mg samples, produced with laser powder bed fusion (L-PBF), in the as printed condition and after different heat treatments, and, for comparison, on as-cast samples of AlSi10Mg. PEO process was performed in direct-current mode using high current densities and short time in a basic silicate electrolyte. For the first time, the effects of silicon morphology in L-PBF AlSi10Mg samples, in as printed condition and after different heat treatments, on the obtained PEO coating were investigated in terms of microstructure and corrosion properties.
View Article and Find Full Text PDFThe development of laser powder bed fusion (LPBF) additive manufacturing techniques for microfabrication raises the need for the employment of new process configurations and parameters. In this study, micro-LPBF of Ni-based superalloy Inconel 718 using a spot laser of 30 µm was examined. The response surface method with a central composite design was employed to determine the optimum process parameter.
View Article and Find Full Text PDFAmine-carbamate self-immolative (SI) spacers represent practical and versatile tools in targeted prodrugs, but their slow degradation mechanism limits drug activation at the site of disease. We engineered a pyrrolidine-carbamate SI spacer with a tertiary amine handle which strongly accelerates the spacer cyclization to give a bicyclic urea and the free hydroxy groups of either cytotoxic (Camptothecin) or immunostimulatory (Resiquimod) drugs. In silico conformational analysis and pK calculations suggest a plausible mechanism for the superior efficacy of the advanced SI spacer compared to state-of-art analogues.
View Article and Find Full Text PDFThe human gonadotropin releasing hormone (GnRH-I) and its sea lamprey analogue GnRH-III specifically bind to GnRH receptors on cancer cells and can be used as targeting moieties for targeted tumor therapy. Considering that the selective release of drugs in cancer cells is of high relevance, we were encouraged to develop cleavable, self-immolative GnRH-III-drug conjugates which consist of a -aminobenzyloxycarbonlyl (PABC) spacer between a cathepsin B-cleavable dipeptide (Val-Ala, Val-Cit) and the classical anticancer drugs daunorubicin (Dau) and paclitaxel (PTX). Alongside these compounds, non-cleavable GnRH-III-drug conjugates were also synthesized, and all compounds were analyzed for their antiproliferative activity.
View Article and Find Full Text PDFCyclative cleavage of an amine-carbamate self-immolative spacer to deliver a hydroxyl cargo was inhibited by spacer derivatisation with a phosphate monoester handle. This trifunctional spacer was installed in a model anticancer prodrug that showed fast drug release only when incubated with both a protease and a phosphatase enzyme.
View Article and Find Full Text PDFBackground: Functional exercise capacity assessment is recommended in children with cystic fibrosis (CF). The six-minute walk test (6MWT) is a valid evaluation of exercise capacity but can be technically complex. Inversely, the sit-to-stand test (STST) is a simple method to evaluate exercise capacity, and is validated in healthy children and adults with CF.
View Article and Find Full Text PDFA novel high silicon austempered (AHS) steel has been studied in this work. The effect of different austenitizing temperatures, in full austenitic and biphasic regime, on the final microstructure was investigated. Specimens were austenitized at 780 °C, 830 °C, 850 °C and 900 °C for 30 min and held isothermally at 350 °C for 30 min.
View Article and Find Full Text PDFThe recent increased interest in orodispersible films (ODF) stems from their ideal potential to circumvent several pharmacotherapy-related problems, such as improved medication compliance and adherence, especially in children, elderly and uncooperative patients. Their administration is well accepted by the majority of patients because ODF dissolve upon contact with the saliva in the oral cavity without the need for water intake. ODF application in personalized pharmacotherapy is currently being exploited.
View Article and Find Full Text PDFThe paper entitled "Mucoadhesive Budesonide Formulation for the Treatment of Eosinophilic Esophagitis 2020, , 211" discusses the physicochemical and technological characterization of a formulation to treat eosinophilic esophagitis [...
View Article and Find Full Text PDFThe COVID-19 outbreak is spreading worldwide pushing the national healthcare systems to find effective protocols to prevent contagion and to reduce the patients' mortality and the severity of long-term effects. In the absence of authorised pharmacological treatments, chloroquine, and hydroxychloroquine, which are known as anti-malaria drugs, had been widely used off-label until concerns about their efficacy/safety limited their use to hospitalized patients affected by severe COVID-19. Regardless of their clinical use, their manipulation is necessary since the pure drug substance is not always promptly available and most of the drug products available on the market are tablets designed to be ingested; no liquid dosage forms are available.
View Article and Find Full Text PDFThis work aimed to design low-melting pressure sensitive adhesives and to demonstrate the feasibility of the preparation of (trans)dermal patches by hot-melt ram extrusion printing. This approach allows defining both the geometry of (trans)dermal patch and the drug strength easily according to patient needs. The preparation steps are the mixing of a poly-ammonium methacrylate polymer (i.
View Article and Find Full Text PDFPrestrained at 5% and 15% duplex stainless steel UNS S32750 specimens have been subjected to electropulsing treatments with current density of 100 A/mm and 200 A/mm and 100 and 500 pulses for each current density value. Corrosion tests, X-ray diffraction, microhardness and residual stresses were collected before and after the electropulsing treatments. Tensile tests were performed after the electropulsing treatments in order to compare the mechanical response to reference tensile tests performed before pulsing treatments.
View Article and Find Full Text PDFThe use of multimeric ligands is considered as a promising strategy to improve tumor targeting for diagnosis and therapy. Herein, tetrameric RGD (Arg-Gly-Asp) peptidomimetics were designed to target α β integrin-expressing tumor cells. These compounds were prepared by an oxime chemoselective assembly of cyclo(DKP-RGD) ligands and a cyclodecapeptide scaffold, which allows a tetrameric presentation.
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