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•Stable nanoemulsion formulation containing 1,8-cineole was obtained.•TEM analysis showed non-aggregated nanosized droplets with irregular spherical shapes.•Cineole-containing ...nanoemulsion was successful used against Gram-positive strains.
1,8-cineole is a monoterpene commonly used by the food, cosmetic, and pharmaceutical industries owing to its flavor and fragrances properties. In addition, this bioactive monoterpene has demonstrated bactericidal and fungicidal activities. However, such activities are limited due to its low aqueous solubility and stability. This study aimed to develop nanoemulsion containing cineole and assess its stability and antibacterial activity in this context. The spontaneous emulsification method was used to prepare nanoemulsion (NE) formulations (F1, F2, F3, F4, and F5). Following the development of NE formulations, we chose the F1 formulation that presented an average droplet size (in diameter) of about 100 nm with narrow size distribution (PdI <0.2) and negative zeta potential (∼ – 35 mV). According to the analytical centrifugation method with photometric detection, F1 and F5 formulations were considered the most stable NE with lower droplet migration velocities. In addition, F1 formulation showed high incorporation efficiency (> 80 %) and TEM analyses demonstrated nanosized oil droplets with irregular spherical shapes and without any aggregation tendency. Antibacterial activity assessment showed that F1 NE was able to enhance the cineole action against Staphylococcus aureus, Enterococcus faecalis, and Streptococcus pyogenes. Therefore, using a simple and reproducible method of low energy emulsification we designed a stable nanoemulsion containing 1,8-cineole with improved antibacterial activity against Gram-positive strains.
mTOR is a signaling pathway involved in cell survival, cell stress response, and protein synthesis that may be a key point in sepsis-induced cardiac dysfunction. Curcumin has been reported in vitro ...as an mTOR inhibitor compound; however, there are no studies demonstrating this effect in experimental sepsis. Thus, this study aimed to evaluate the action of curcumin on the mTOR pathway in the heart of septic mice. Free curcumin (FC) and nanocurcumin (NC) were used, and samples were obtained at 24 and 120 h after sepsis. Histopathological and ultrastructural analysis showed that treatments with FC and NC reduced cardiac lesions caused by sepsis. Our main results demonstrated that curcumin reduced mTORC1 and Raptor mRNA at 24 and 120 h compared with the septic group; in contrast, mTORC2 mRNA increased at 24 h. Additionally, the total mTOR mRNA expression was reduced at 24 h compared with the septic group. Our results indicate that treatment with curcumin and nanocurcumin promoted a cardioprotective response that could be related to the modulation of the mTOR pathway.
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Hesperetin is a flavanone with recognized biological activities. However, such activities are limited due to its restricted aqueous solubility and stability. In this regard, the main ...aim of this study was to develop and characterize lipid nanocarriers containing hesperetin. Nanostructured lipid carriers (NLC) were prepared using phase inversion temperature method and characterized by size, polydispersity index (PdI), zeta potential, physical stability, TEM analysis, encapsulation efficiency, in vitro release, and in vitro cytotoxic effect in cell line. Lipid nanocarriers presented diameter below 80 nm, narrow PdI (<0.2), and negative zeta potential (–20 mV). Accelerated stability studies of NLC demonstrated good physical stability for a period of 12 months. According to TEM, NLC were almost spherical with particle size <100 nm and homogeneous size distribution. DSC curves showed that formulations presented lipid core with a higher degree of crystalline disorder. Lipid nanocarriers were able to entrap hesperitin with efficiency 72.7 % (±0.92). In vitro release studies confirmed that NLC could modulate hesperetin release during 72 h. In vitro cytotoxicity assay of hesperitin-loaded NLC on T98G glioblastoma grade IV cells presented significant cytotoxic effect. Therefore, NLC were able to encapsulate successfully hesperetin and demonstrated excellent in vitro cytotoxicity on glioblastoma cells.
We have prepared and characterized a cholesterol-rich nanoemulsion called LDE, a mimic of classic lipoprotein macromolecules, that can be applied as a new drug delivery system for aluminum ...phthalocyanine chloride (PcAlCl). The LDE containing PcAlCl system prepared herein had mean size and zeta potential of 127 nm and −29 mV, respectively, and encapsulation rate efficiency was 81%, and stability of 17 months. Compared to classical liposomes, LDE was more efficient, especially in brain diseases like glioblastoma (GBM), as revealed by tests on the U-87 MG cell line. The LDEPc formulation did not display dark cytotoxicity, as expected. The best light dose for LDEPc was 1.0 J·cm−2: its activity was 55% higher than PcAlCl in a compatible organic medium. In the U-87 MG cells, apoptosis was the preferential pathway activated by PDT. These results strongly support the use of LDE as a new theranostic system.
Abstract Fig. (1) and (2) Representation of blood brain barrier opening by the nanoparticles. This figure is partially a derivative of the “FUSF BBB illustration” by the Focused Ultrasound Foundation, used under CC. (3) PcAlCl chemical structure. Display omitted
•Cholesterol-rich nanoemulsion produced LDE as novel drug delivery system•Aluminum Chloride Phthalocyanine (PcAlCl) was successful loaded into the LDE.•LDE and LDE- PcAlCl were stable over 18 months.•PcAlCl delivered by LDE and photoactivated by PDT (Photodynamic Therapy) caused a photodamage in Glioblastoma (U87-MG).
The perineuronal net (PNN) is a well-described highly specialized extracellular matrix structure found in the central nervous system. Thus far, no reports of its presence or connection to ...pathological processes have been described in the peripheral nervous system. Our study demonstrates the presence of a PNN in the spinal afferent innervation of the distal colon of mice and characterizes structural and morphological alterations induced in an ulcerative colitis (UC) model. C57Bl/6 mice were given 3% dextran sulfate sodium (DSS) to induce acute or chronic UC. L6/S1 dorsal root ganglia (DRG) were collected. PNNs were labeled using fluorescein-conjugated Wisteria Floribunda (WFA) l lectin, and calcitonin gene-related peptide (CGRP) immunofluorescence was used to detect DRG neurons. Most DRG cell bodies and their extensions toward peripheral nerves were found surrounded by the PNN-like structure (WFA+), labeling neurons' cytoplasm and the pericellular surfaces. The amount of WFA+ neuronal cell bodies was increased in both acute and chronic UC, and the PNN-like structure around cell bodies was thicker in UC groups. In conclusion, a PNN-like structure around DRG neuronal cell bodies was described and found modulated by UC, as changes in quantity, morphology, and expression profile of the PNN were detected, suggesting a potential role in sensory neuron peripheral sensitization, possibly modulating the pain profile of ulcerative colitis.
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