RESUMEN

Candida auris is a multidrug-resistant yeast that has seen a worrying increase during the COVID-19 pandemic. Give7/n this, new therapeutic options, such as controlled-release nanomaterials, may be promising in combating the infection. Therefore, this study aimed to develop amphotericin B (AmB) and micafungin (MICA)-loaded nanoemulsions (NEMA) and evaluated against biofilms of C. auris. Nanoemulsions (NEs) were characterized and determined minimum inhibitory concentration MIC90, checkerboard and anti-biofilm. NEMA presented a size of 53.7 and 81.4 nm for DLS and NTA, respectively, with good stability and spherical morphology. MICAmB incorporated efficiency was 88.4 and 99.3%, respectively. The release results show that AmB and MICA obtained a release of 100 and 63.4%, respectively. MICAmB and NEMA showed MIC90 values of 0.015 and 0.031 ug/mL, respectively and synergism. NEMA showed greater metabolic inhibition and morphological changes in mature biofilms. This drugs combination and co-encapsulation proved to be a promising therapy against C. auris biofilms.

Asunto(s)

Anfotericina B , Antifúngicos , Biopelículas , Candida auris , Emulsiones , Micafungina , Pruebas de Sensibilidad Microbiana , Biopelículas/efectos de los fármacos , Antifúngicos/farmacología , Antifúngicos/química , Antifúngicos/administración & dosificación , Anfotericina B/farmacología , Anfotericina B/administración & dosificación , Anfotericina B/química , Micafungina/farmacología , Micafungina/administración & dosificación , Emulsiones/farmacología , Emulsiones/química , Candida auris/efectos de los fármacos , Humanos , SARS-CoV-2/efectos de los fármacos , COVID-19 , Nanopartículas/química

RESUMEN

AIMS: Evaluate the in vitro efficacy of the essential oils derived from Aloysia citrodora (Verbenaceae), Cymbopogon winterianus (Poaceae), and Ocimum gratissimum (Lamiaceae) against Acanthamoeba polyphaga trophozoites. Additionally, microemulsions formulated with these essential oils, along with their major components, were analyzed. METHODS AND RESULTS: The prepared microemulsions were characterized using polarized light microscopy and rheological techniques. The amoebicidal activity was determined by measuring the inhibitory concentration (IC50). Flow cytometry was employed to detect membrane damage and alterations in trophozoites size. The results revealed transparent and thermodynamically stable microemulsions. The essential oil from O. gratissimum exhibited a lower IC50, with values of 280.66 and 47.28 µg ml-1 after 24 and 48 h, respectively. When microemulsions containing essential oils were tested, the IC50 values exhibited a reduction of over 80% after 24 h. Particularly, eugenol, a constituent of the O. gratissimum essential oil, displayed higher amoebicidal activity. The essential oils also caused damage to the cell membrane, resulting in the subsequent death of the trophozoites. CONCLUSIONS: The EOs of A. citrodora, C. winterianus, and O. gratissimum and their microemulsions showed antiparasitic effect against A. polyphaga trophozoites, representing promising alternatives for the treatment of diseases caused by this protozoan.

Asunto(s)

Acanthamoeba , Cymbopogon , Emulsiones , Ocimum , Aceites Volátiles , Trofozoítos , Verbenaceae , Aceites Volátiles/farmacología , Aceites Volátiles/química , Cymbopogon/química , Ocimum/química , Emulsiones/farmacología , Trofozoítos/efectos de los fármacos , Acanthamoeba/efectos de los fármacos , Verbenaceae/química , Amebicidas/farmacología , Aceites de Plantas/farmacología , Extractos Vegetales/farmacología

RESUMEN

BACKGROUND: The combination of photodynamic therapy (PDT) and LL-37 has never been tested in an animal study and our research team background suggests this strategy might be a promising alternative to intensify periodontitis resolution. This study aimed to assess the effects of multiple sessions of PDT with chlorin-e6 conjugated to the antimicrobial peptide LL-37 loaded nanoemulsion, as adjunctive therapy in experimental periodontitis in rats. METHODS: Experimental periodontitis was induced in 81 rats. After disease establishment, animals were assigned to three groups: SRP (scaling and root planning); SRP + 1PDT, SRP followed by a single PDT session; SRP + 4PDT (n = 27), SRP followed by four PDT sessions at 0, 24, 48 and 72 h after SRP. Animals were subjected to euthanasia at 7, 14 and 28 days, and samples were submitted to osteoclast quantification, immunological and microtomography analysis. RESULTS: All treatments resulted in significant periodontal improvements and there was no significant difference between the groups in both local inflammatory response and healing process. Minimal adjunctive effects could be found for the combined therapy in terms of cytokine levels (IL-1ß and IL-10), with no statistical significance. However, the number of TRAP-positive osteoclasts per mm of alveolar bone linear surface for the group treated with PDT sessions was significantly lower than those treated with SRP only. CONCLUSIONS: Multiple PDT sessions with chlorin-e6 and LL-37 nanoemulsion as an adjunct to scaling and root planning reduced the presence of osteoclast in the local site but did not contribute towards bone regeneration and IL-1ß and IL-10 levels.

Asunto(s)

Péptidos Catiónicos Antimicrobianos , Catelicidinas , Clorofilidas , Emulsiones , Periodontitis , Fotoquimioterapia , Fármacos Fotosensibilizantes , Porfirinas , Animales , Fotoquimioterapia/métodos , Periodontitis/tratamiento farmacológico , Ratas , Porfirinas/farmacología , Porfirinas/uso terapéutico , Fármacos Fotosensibilizantes/farmacología , Fármacos Fotosensibilizantes/uso terapéutico , Raspado Dental/métodos , Masculino , Ratas Wistar , Aplanamiento de la Raíz/métodos

RESUMEN

A nanoemulsion containing CdTe quantum dots (NE-CdTe-QD) was developed to shield cells from cadmium toxicity and shown to be a promising candidate for brain tumor diagnosis. CdTe-QD was characterized by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and Raman spectroscopy. CdTe-QD exhibited high luminescence emission at 700 nm, and their stability was maintained when encapsulated in lipidic/polymeric nanoemulsions (198 ± 2.0 nm; PDI = 0.174; - 49.0 mV). The biological effects of free and nanoemulsified CdTe-QD were tested in normal cells (NHF) and glioblastoma cell lines (U87-MG and T98G). Membrane colocalization of NE-CdTe-QD by T98G cells was observed. Instead, intracellular endoplasmic reticulum localization of NE-CdTe-QD was verified in U87-MG cells. Cell viability was reduced only when NE-CdTe-QD permeated the membrane of GBM cells, as observed in U87-MG cells, whereas no cytotoxic effects were observed in normal fibroblasts. Incorporating quantum dots directly into the brain cells is difficult. However, the nanoemulsions reduced the toxicity of CdTe-QD in zebrafish larvae and increased their circulation time, and direct injection into the zebrafish brain did not affect neural cell viability. This validates the potential application of these nanomaterials as diagnostic agents and satisfies the necessary criteria for their use as photosensitizers in photodynamic therapy.

Asunto(s)

Compuestos de Cadmio , Supervivencia Celular , Emulsiones , Puntos Cuánticos , Telurio , Pez Cebra , Puntos Cuánticos/química , Telurio/química , Animales , Compuestos de Cadmio/química , Emulsiones/química , Humanos , Supervivencia Celular/efectos de los fármacos , Línea Celular Tumoral , Neoplasias Encefálicas/tratamiento farmacológico , Neoplasias Encefálicas/patología

RESUMEN

This study aimed to develop microemulsions (MEs) containing α-bisabolol for the topical treatment of cutaneous leishmaniasis (CL). Initially, pseudoternary phase diagrams were developed using α-bisabolol as the oil phase, Eumulgin® CO 40 as the surfactant, Polymol® HE as the co-surfactant, and distilled water as the aqueous phase. Two transparent liquid systems (TLS) containing 5% of α-bisabolol were selected and characterized (F5E25 and F5EP25). Next, skin permeation and retention assays were performed using Franz cells. The interaction of the formulation with the stratum corneum (SC) was evaluated using the FTIR technique. The cytotoxicity was evaluated in murine peritoneal macrophages. Finally, the antileishmanial activity of microemulsions was determined in promastigotes and amastigotes of L. amazonensis (strain MHOM/BR/77/LTB 0016). As a result, the selected formulations showed isotropy, nanometric size (below 25 nm), Newtonian behavior and pH ranging from 6.5 to 6.9. The MEs achieved a 2.5-fold increase in the flux and skin-permeated amount of α-bisabolol. ATR-FTIR results showed that microemulsions promoted fluidization and extraction of lipids and proteins of the stratum corneum, increasing the diffusion coefficient and partition coefficient of the drug in the skin. Additionally, F5E25 and F5EP25 showed higher activity against promastigotes (IC50 13.27 and 18.29, respectively) compared to unencapsulated α-bisabolol (IC50 53.8). Furthermore, F5E25 and F5EP25 also showed antileishmanial activity against intracellular amastigotes of L. amazonensis, with IC50 50 times lower than free α-bisabolol and high selectivity index (up to 15). Therefore, the systems obtained are favorable to topical administration, with significant antileishmanial activity against L. amazonensis promastigotes and amastigotes, being a promising system for future in vivo trials.

Asunto(s)

Emulsiones , Macrófagos Peritoneales , Sesquiterpenos Monocíclicos , Sesquiterpenos , Piel , Animales , Sesquiterpenos Monocíclicos/farmacología , Sesquiterpenos Monocíclicos/química , Emulsiones/química , Ratones , Sesquiterpenos/farmacología , Sesquiterpenos/química , Piel/parasitología , Macrófagos Peritoneales/efectos de los fármacos , Macrófagos Peritoneales/parasitología , Leishmaniasis Cutánea/tratamiento farmacológico , Leishmaniasis Cutánea/parasitología , Espectroscopía Infrarroja por Transformada de Fourier , Absorción Cutánea/efectos de los fármacos , Ratones Endogámicos BALB C , Femenino , Leishmania/efectos de los fármacos , Tensoactivos/farmacología , Tensoactivos/química , Antiprotozoarios/farmacología , Antiprotozoarios/química

RESUMEN

Bacteria can synthesize a broad spectrum of multifunctional polysaccharides including extracellular polysaccharides (EPS). Bacterial EPS can be utilized in the food, pharmaceutical, and biomedical areas owing to their physical and rheological properties in addition to generally presenting low toxicity. From an ecological viewpoint, EPS are biodegradable and environment compatible, offering several advantages over synthetic compounds. This study investigated the EPS produced by Klebsiella oxytoca (KO-EPS) by chemically characterizing and evaluating its properties. The monosaccharide components of the KO-EPS were determined by HPLC coupled with a refractive index detector and GC-MS. The KO-EPS was then analyzed by methylation analysis, FT-IR and NMR spectroscopy to give a potential primary structure. KO-EPS demonstrated the ability to stabilize hydrophilic emulsions with various hydrophobic compounds, including hydrocarbons and vegetable and mineral oils. In terms of iron chelation capacity, the KO-EPS could sequester 41.9 % and 34.1 % of the most common iron states, Fe2+ and Fe3+, respectively. Moreover, KO-EPS exhibited an improvement in the viscosity of aqueous dispersion, being proportional to the increase in its concentration and presenting a non-Newtonian pseudoplastic flow behavior. KO-EPS also did not present a cytotoxic effect indicating that the KO-EPS could have potential applications as a natural thickener, bioemulsifier, and bioremediation agent.

Asunto(s)

Biodegradación Ambiental , Emulsiones , Klebsiella oxytoca , Polisacáridos Bacterianos , Reología , Klebsiella oxytoca/metabolismo , Polisacáridos Bacterianos/química , Polisacáridos Bacterianos/biosíntesis , Emulsionantes/química , Emulsionantes/metabolismo , Biotecnología/métodos , Viscosidad , Interacciones Hidrofóbicas e Hidrofílicas

RESUMEN

Microbial resistance to drugs continues to be a global public health issue that demands substantial investment in research and development of new antimicrobial agents. Essential oils (EO) have demonstrated satisfactory and safe antimicrobial action, being used in pharmaceutical, cosmetic, and food formulations. In order to improve solubility, availability, and biological action, EO have been converted into nanoemulsions (NE). This review identified scientific evidence corroborating the antimicrobial action of nanoemulsions of essential oils (NEEO) against antibiotic-resistant pathogens. Using integrative review methodology, eleven scientific articles evaluating the antibacterial or antifungal assessment of NEEO were selected. The synthesis of evidence indicates that NEEO are effective in combating multidrug-resistant microorganisms and in the formation of their biofilms. Factors such as NE droplet size, chemical composition of essential oils, and the association of NE with antibiotics are discussed. Furthermore, NEEO showed satisfactory results in vitro and in vivo evaluations against resistant clinical isolates, making them promising for the development of new antimicrobial and antivirulence drugs.

Asunto(s)

Bacterias , Biopelículas , Emulsiones , Aceites Volátiles , Aceites Volátiles/farmacología , Aceites Volátiles/química , Emulsiones/química , Emulsiones/farmacología , Biopelículas/efectos de los fármacos , Bacterias/efectos de los fármacos , Antibacterianos/farmacología , Pruebas de Sensibilidad Microbiana , Humanos , Antiinfecciosos/farmacología , Antifúngicos/farmacología , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Hongos/efectos de los fármacos , Nanopartículas/química , Animales

RESUMEN

This study aimed to evaluate the effect of applying oxidized cassava starch-based edible coatings with addition of lemongrass essential oil emulsion on 'Palmer' mangoes stored under refrigeration. A completely randomized design was used, arranged in a 5 × 3 factorial scheme, with five types of coatings and three evaluation times. The evaluated postharvest quality parameters consisted of weight loss, pulp and peel firmness, biochemical transformations related to pigments, and pulp and peel coloration of mango. The application of edible coatings with a 0.9 % EO concentration resulted in delayed fruit ripening, evidenced mainly by a 7.25 % reduction in weight loss, a 29.23 % increase in soluble solids content, and a 24.15 % decrease in total chlorophyll, when compared to uncoated fruits, which showed 19.8 %, 48.66 %, and 82.00 %, respectively, over the storage period. This effect was also evident in the angle Hue (°h) measurement, with uncoated fruits showing a decrease of 32.2 %. The antimicrobial effect and absence of anthracnose symptoms were observed in the fruits in which the coating with 0.9 % EO was applied. Therefore, biodegradable coating with the addition of 0.9 % emulsion EO, can be used as postharvest treatments for maintenance quality of 'Palmer' mangoes during refrigerated storage.

Asunto(s)

Emulsiones , Conservación de Alimentos , Frutas , Mangifera , Manihot , Aceites Volátiles , Almidón , Mangifera/química , Manihot/química , Aceites Volátiles/química , Aceites Volátiles/farmacología , Almidón/química , Conservación de Alimentos/métodos , Frutas/química , Almacenamiento de Alimentos/métodos , Películas Comestibles

RESUMEN

BACKGROUND: Implementing encapsulation techniques is pivotal in safeguarding bioactive molecules against environmental conditions for drug delivery systems. Moreover, the food-grade nanocarrier is a delivery system and food ingredient crucial in creating nutraceutical foods. Nano α-lactalbumin has been shown to be a promissory nanocarrier for hydrophobic molecules. Furthermore, the nanoprotein can enhance the tecno-functional properties of food such as foam and emulsion. The present study investigated the nanostructured α-lactalbumin protein (nano α-la) as a delivery and controlled release system for bioactive molecules in a gastric-intestinal in vitro mimic system. RESULTS: The nano α-la was synthesized by a low self-assembly technique, changing the solution ionic strength by NaCl and obtaining nano α-la 191.10 ± 21.33 nm and a spherical shape. The nano α-la showed higher encapsulation efficiency and loading capacity for quercetin than riboflavin, a potential carrier for hydrophobic compounds. Thermal analysis of nano α-la resulted in a ΔH of -1480 J g-1 for denaturation at 57.44 °C. The nanostructure formed by self-assembly modifies the foam volume increment and stability. Also, differences between nano and native proteins in emulsion activity and stability were noticed. The release profile in vitro showed that the nano α-la could not hold the molecules in gastric fluid. The Weibull and Korsmeyer-Peppas model better fits the release profile behavior in the studied fluids. CONCLUSION: The present study shows the possibility of nano α-la as an alternative to molecule delivery systems and nutraceutical foods' formulation because of the high capacity to encapsulate hydrophobic molecules and the improvement of techno-functional properties. However, the nanocarrier is not perfectly suitable for the sustainable delivery of molecules in the gastrointestinal fluid, demanding improvements in the nanocarrier. © 2024 Society of Chemical Industry.

Asunto(s)

Preparaciones de Acción Retardada , Lactalbúmina , Nanoestructuras , Lactalbúmina/química , Preparaciones de Acción Retardada/química , Nanoestructuras/química , Portadores de Fármacos/química , Interacciones Hidrofóbicas e Hidrofílicas , Tracto Gastrointestinal/metabolismo , Composición de Medicamentos , Quercetina/química , Humanos , Riboflavina/química , Modelos Biológicos , Sistemas de Liberación de Medicamentos , Liberación de Fármacos , Emulsiones/química , Tamaño de la Partícula

RESUMEN

Alternative protein sources have been required to meet the significant plant protein demand. Agro-industrial by-products such as leaves have considerable potential as a source of macromolecules once they are mostly discarded as waste. The current study evaluated dried cassava leaves as a protein source. First, alkaline extraction parameters (solid-liquid ratio, pH, and temperature) were optimized and the run that result in the highest protein yield were acidified at pH 2.5 or 4. The influence of carbohydrate solubilized on protein precipitation was also evaluated by removing it via alcoholic extraction prior to precipitation. The experimental design showed that high pH and temperature conditions associated with a low solid-liquid ratio led to increased protein yields. The presence of carbohydrates in the supernatant significantly influenced protein precipitation. The protein concentrate had around 17.51% protein when it was obtained from a supernatant with carbohydrates, while protein content increased to 26.88% when it was obtained from carbohydrate-free supernatant. The precipitation pH also influenced protein content, whereas protein content significantly decreased when pH increased from 2.5 to 4. The natural interaction between carbohydrates and proteins from cassava leaves positively influenced the emulsion stability index and the foaming capacity and stability. Thus, the presented results bring insights into challenges in extracting and precipitation proteins from agro-industrial by-products.

Asunto(s)

Precipitación Química , Manihot , Hojas de la Planta , Proteínas de Plantas , Temperatura , Manihot/química , Hojas de la Planta/química , Concentración de Iones de Hidrógeno , Proteínas de Plantas/aislamiento & purificación , Proteínas de Plantas/química , Emulsiones/química

RESUMEN

Using green techniques to convert native starches into nanoparticles is an interesting approach to producing stabilizers for Pickering emulsions, aiming at highly stable emulsions in clean label products. Nanoprecipitation was used to prepare the Pickering starch nanoparticles, while ultrasound technique has been used to modulate the size of these nanoparticles at the same time as the emulsion was developed. Thus, the main objective of this study was to evaluate the stabilizing effect of cassava starch nanoparticles (SNP) produced by the nanoprecipitation technique combined with ultrasound treatment carried out in the presence of water and oil (more hydrophobic physicochemical environment), different from previous studies that carry out the mechanical treatment only in the presence of water. The results showed that the increased ultrasound energy input could reduce particle size (117.58 to 55.75 nm) and polydispersity (0.958 to 0.547) in aqueous dispersions. Subsequently, Pickering emulsions stabilized by SNPs showed that increasing emulsification (ultrasonication) time led to smaller droplet sizes and monomodal size distribution. Despite flocculation, long-term ultrasonication (6 and 9 min) caused little variation in the droplet size after 7 days of storage. The cavitation effects favored the interaction between oil droplets through weak attraction forces and particle sharing, favoring the Pickering stabilization against droplet coalescence. Our results show the potential to use only physical modifications to obtain nanoparticles that can produce coalescence-stable emulsions that are environmentally friendly.

Asunto(s)

Emulsiones , Manihot , Nanopartículas , Tamaño de la Partícula , Almidón , Manihot/química , Almidón/química , Emulsiones/química , Nanopartículas/química , Agua/química , Sonicación/métodos , Floculación

RESUMEN

Bioemulsifiers are compounds produced by microorganisms that reduce the interfacial forces between hydrophobic substances and water. Due to their potential in the pharmaceutical and food industries and their efficiency in oil spill remediation, they have been the subject of study in the scientific community while being safe, biodegradable, and sustainable compared to synthetic options. These biomolecules have high molecular weight and polymeric structures, distinguishing them from traditional biosurfactants. Emulsan, a bioemulsifier exopolysaccharide, is produced by Acinetobacter strains and is highly efficient in forming stable emulsions. Its low toxicity and high potential as an emulsifying agent promote its application in pharmaceutical and food industries as a drug-delivery vehicle and emulsion stabilizer. Due to the high environmental impact of oil spills, bioemulsifiers have great potential for environmental applications, such as bioremediation. This unique feature gives them a distinct mechanism of action in forming emulsions, resulting in minimal environmental impact. A better understanding of these aspects can improve the use of bioemulsifiers and environmental remediation in various industries. This review will discuss the production and characterization of Emulsan, focusing on recent advancements in cultivation conditions, purification techniques, compound identification, and ecotoxicity.

Asunto(s)

Biodegradación Ambiental , Emulsionantes , Emulsionantes/química , Polisacáridos Bacterianos/química , Polisacáridos Bacterianos/biosíntesis , Polisacáridos Bacterianos/aislamiento & purificación , Emulsiones , Tensoactivos/química , Acinetobacter/metabolismo

RESUMEN

For many years, it has been speculated that elevated testosterone levels may be critically involved in the genesis and proliferation of prostate cancer. METHODS: The effect of testosterone on the metabolic activity of hormone-independent [PC-3] and hormone-dependent [LNCAP] cancer cells was investigated in vitro. Additionally, the impact of testosterone nanoemulsion [nanocare®] on cell viability was accessed by flow cytometry. RESULTS: Despite the dependency of the normal prostate and of most prostatic cancers upon androgens, the obtained results indicate that, contrary to prevailing opinion, the supplementation of testosterone with higher doses in nanoemulsion was able to lower the metabolic activity and viability of prostate cancer cells. CONCLUSIONS: We conclude that the growth of hormone-independent and hormone-dependent prostate cancer cells was reduced by the exposure of a nanoemulsion of bioidentical testostosterone in vitro. To the best of our knowledge, this is the first time that the potential effect of a testosterone nanoemulsion on the metabolic activity of prostate cancer cells has been shown. Such tests suggest that the growth of hormone-independent and hormone-dependent prostate cancer cells was reduced by the administration of bioidentical testostosterone, and this might be an interesting strategy for prostate cancer treatment in diagnosed patients.

Asunto(s)

Supervivencia Celular , Emulsiones , Neoplasias de la Próstata , Testosterona , Humanos , Masculino , Neoplasias de la Próstata/metabolismo , Neoplasias de la Próstata/patología , Neoplasias de la Próstata/tratamiento farmacológico , Testosterona/farmacología , Supervivencia Celular/efectos de los fármacos , Línea Celular Tumoral , Nanopartículas/química , Proliferación Celular/efectos de los fármacos , Células PC-3 , Andrógenos/farmacología

RESUMEN

α-Bisabolol (α-BIS) is a sesquiterpene alcohol present in chamomile essential oil [Chamomilla recutita (L.) Rauschert]. Despite its numerous pharmacological effects, its pharmacokinetics remain understudied. An analytical method capable of quantifying α-BIS in plasma is crucial to enable pharmacokinetic analysis. Presently, only one study has quantified it using mass spectrometry. Administering α-BIS requires a nanoemulsion for intravenous injection. This study aimed to develop and validate a bioanalytical method using high-performance liquid chromatography with an ultraviolet detector to quantify α-BIS in rat plasma. The method employed acetonitrile and ultrapure water (80:20, v/v) as the mobile phase, with a flow rate of 1 ml/min and concentrations ranging from 465 to 29.625 µg/ml. All US Food and Drug Administration-designated assays were successful, indicating the method's precision, accuracy, sensitivity and linearity in determining α-BIS in rat plasma. The developed nanoemulsion, assessed through dynamic light scattering analysis, the ensemble collection of particles and polydispersity index evaluation, proved safe and effective for intravenous administration. The pharmacokinetic parameters such as volume of distribution, clearance and half-life indicated that α-BIS tends to persist in the body. This study provides a foundation for further research to explore α-BIS's potential pharmaceutical applications in the future.

Asunto(s)

Emulsiones , Sesquiterpenos Monocíclicos , Animales , Cromatografía Líquida de Alta Presión/métodos , Ratas , Emulsiones/química , Reproducibilidad de los Resultados , Sesquiterpenos Monocíclicos/farmacocinética , Sesquiterpenos Monocíclicos/sangre , Sesquiterpenos Monocíclicos/química , Masculino , Proyectos Piloto , Modelos Lineales , Límite de Detección , Sesquiterpenos/farmacocinética , Sesquiterpenos/sangre , Sesquiterpenos/química , Ratas Sprague-Dawley , Espectrofotometría Ultravioleta/métodos

RESUMEN

Background and Purpose: Natural products are potential sources of anticancer components. Among various species, the lipophilic extract of the Viscum album subsp. austriacum (Wiesb.) Vollm. (VALE) has shown promising therapeutic potential. The present work aimed to qualify the plant source and characterize the extract's chemical profile. In addition, a self-nanoemulsifying drug delivery system (SNEDDS) containing VALE (SNEDDS-VALE) was developed. Methods: V. album subsp. austriacum histochemistry was performed, and the chemical profile of VALE was analyzed by GC-MS. After the SNEEDS-VALE development, its morphology was visualized by transmission electron microscopy (TEM), while its stability was evaluated by the average droplet size, polydispersity index (PdI) and pH. Lastly, SNEDDS-VALE chemical stability was evaluated by LC-DAD-MS. Results: The histochemical analysis showed the presence of lipophilic compounds in the leaves and stems. The major compound in the VALE was oleanolic acid, followed by lupeol acetate and ursolic acid. SNEDDS was composed of medium chain triglyceride and Kolliphor® RH 40 (PEG-40 hydrogenated castor oil). A homogeneous, isotropic and stable nanoemulsion was obtained, with an average size of 36.87 ± 1.04 nm and PdI of 0.14 ± 0.02, for 14 weeks. Conclusion: This is the first histochemistry analysis of V. album subsp. austriacum growing on Pinus sylvestris L. which provided detailed information regarding its lipophilic compounds. A homogeneous, isotropic and stable SNEDDS-VALE was obtained to improve the low water solubility of VALE. Further, in vitro and in vivo experiments should be performed, in order to evaluate the antitumoral potential of SNEDDS-VALE.

Asunto(s)

Emulsiones , Extractos Vegetales , Viscum album , Extractos Vegetales/química , Extractos Vegetales/administración & dosificación , Viscum album/química , Emulsiones/química , Hojas de la Planta/química , Sistemas de Liberación de Medicamentos/métodos , Tamaño de la Partícula , Sistema de Administración de Fármacos con Nanopartículas/química , Nanopartículas/química

RESUMEN

The effect of the substitution of emulsifying salt by the young bamboo flour (BF) (0, 25, 50, 75, 100 % w/w) on requeijão cremoso processed cheese [REQ, REQ 25, REQ 75 REQ 100]) processing was investigated. Gross composition, calcium and sodium values, functional properties (melting rate), color parameters (L, a*, b*, C*, and Whiteness Index, WI), texture profile, fatty acid profile, volatile organic compounds (VOCs), and sensory profiling were evaluated. No effect was observed on the gross composition; however, sodium and melting rate values were decreased, and calcium values presented the opposite behavior. BF could modify the optical parameters, observing an increase in WI values. Higher BF addition increased hardness and lowered elasticity, and regarding the fatty acid profile, there is no significant difference. Different volatile compounds were noted in a proportional form with the BF addition, which was reflected in similar sensory acceptance for REQ 25 and control samples. Although some aspects require further in-depth studies, using BF as a substitute for emulsifying salt in requeijão cremoso processed cheese appears to be a viable option, especially when considering partial replacements.

Asunto(s)

Queso , Harina , Manipulación de Alimentos , Compuestos Orgánicos Volátiles , Queso/análisis , Harina/análisis , Compuestos Orgánicos Volátiles/análisis , Manipulación de Alimentos/métodos , Humanos , Gusto , Ácidos Grasos/análisis , Color , Emulsiones/química , Dureza , Calcio/análisis , Calcio/química

RESUMEN

Carvacrol has demonstrated antioxidant activity; however, its high volatility and low water solubility limit its direct application in food matrices. Then, an effective encapsulation system is required to protect it. This study aimed to design and characterize a carvacrol-based additive encapsulated in a spray-dried multilayer emulsion based on chitosan/sodium alginate/maltodextrin. Spray-drying temperature of 120 °C and 3 %(w/w) maltodextrin content maximized both encapsulation efficiency (~97 %) and loading capacity (~53 %). The powder's antioxidant properties were evaluated in two food simulant media: water (SiW) and water-ethanol (SiD). The highest antioxidant activity was observed in SiW for both ABTS•+ (8.2 ± 0.3mgEAG/g) and FRAP (4.1 ± 0.2mgEAG/g) methods because of the reduced release of carvacrol in SiD vs. SiW, as supported by micro- and macrostructural observations by SAXS and microscopy, respectively. An increase from 143 to 157 °C attributable to carvacrol protection and Tg = 44.4 °C (> ambient) were obtained by TGA and DSC, respectively. FT-IR confirmed intermolecular interactions (e.g. -COO- and -NH3+) as well as H-bonding formation. High water solubility (81 ± 3 %), low hygroscopicity (8.8 ± 0.2 %(w/w), poor flowability (CI:45 ± 4), and high cohesiveness (HR:1.8 ± 0.1) between particles were achieved, leading to a powdered antioxidant additive with high potential for applications which required avoiding/reducing oxidation on hydrophilic and hydrophobic food products.

Asunto(s)

Alginatos , Antioxidantes , Quitosano , Cimenos , Emulsiones , Polisacáridos , Polvos , Quitosano/química , Antioxidantes/química , Antioxidantes/farmacología , Cimenos/química , Alginatos/química , Emulsiones/química , Polisacáridos/química , Ácido Glucurónico/química , Ácidos Hexurónicos/química

RESUMEN

Essential oils show several biological properties, such as antimicrobial activity, but have limitations regarding their availability and stability. To maximize their antimicrobial effect and protection against environmental conditions, Pickering-type emulsions were used to vehiculate oregano essential oil (OEO) using cellulose nanofibers (CNF) as emulsion stabilizer. Enzymatic hydrolysis was used to produce CNF from a food industry waste (cassava peel), obtaining an environmentally sustainable emulsion stabilizer. It was evaluated how the different properties of the nanofibers affected the stability of the emulsions. Furthermore, the composition of the dispersed phase was varied (different ratios of OEO and sunflower oil-SO) in view of the target application in biodegradable active coatings. Even at very low concentration (0.01 % w/w), CNF was able to form kinetically stable emulsions with small droplet sizes using oil mixtures (OEO + SO). The stabilization mechanism was not purely Pickering, as there was a reduction in interfacial tension. Excellent antimicrobial activity was observed against bacteria and the fungus Alternaria alternata, demonstrating the ability to apply these emulsions in active systems such as coatings and films. An improvement in the stability of emulsions was observed when using a mixture of oils, which is extremely advantageous considering costs and stability to heat treatments, since the desired antimicrobial activity is maintained for the final application.

Asunto(s)

Antiinfecciosos , Celulosa , Emulsiones , Nanofibras , Aceites Volátiles , Origanum , Nanofibras/química , Emulsiones/química , Aceites Volátiles/química , Aceites Volátiles/farmacología , Celulosa/química , Celulosa/farmacología , Antiinfecciosos/farmacología , Antiinfecciosos/química , Origanum/química , Alternaria/efectos de los fármacos

RESUMEN

Cholesterol-rich nanoemulsion (LDE) can carry chemotherapeutic agents in the circulation and can concentrate those agents in the neoplastic and inflammatory tissues. This method improves the biodistribution of the drug and reduces toxicity. However, the structural stability of LDE particles, without or with associated drugs, has not been extensively investigated. The aim of the present study is to investigate the structural stability of LDE and LDE associated to paclitaxel, etoposide or methotrexate in aqueous solution over time by small-angle X-ray scattering (SAXS and Ultra SAXS) and dynamic light scattering (DLS). The results show that LDE and LDE associated with those chemotherapeutic agents had reproducible and stable particle diameter, physical structure, and aggregation behavior over 3-month observation period. As estimated from both DLS and Ultra-SAXS methods, performed at pre-established intervals, the average particle diameter of LDE alone was approx. 32 nm, of LDE-paclitaxel was 31 nm, of LDE-methotrexate was 35 nm and of LDE-etoposide was 36 nm. Ultra-SAXS analysis showed that LDE nanoparticles were quasi-spherical, and SAXS showed that drug molecules inside the particles showed a layered-like organization. Formulations of LDE with associated PTX, ETO or MTX were successfully tested in animal experiments and in patients with cancer or with cardiovascular disease, showing markedly low toxicity, good tolerability and possible superior pharmacological action. Our results may be useful for ensuing clinical trials of this novel Nanomedicine tool, by strengthening the knowledge of the structural aspects of those LDE formulations.

Asunto(s)

Colesterol , Emulsiones , Metotrexato , Nanopartículas , Emulsiones/química , Colesterol/química , Nanopartículas/química , Metotrexato/química , Humanos , Animales , Tamaño de la Partícula , Paclitaxel/química , Paclitaxel/farmacología , Dispersión del Ángulo Pequeño , Etopósido/química , Antineoplásicos/química , Antineoplásicos/farmacología , Difracción de Rayos X , Estructura Molecular

RESUMEN

Although rare, amoebic keratitis (AK) is a disease caused by Acanthamoeba spp. that can lead to blindness. The drugs currently available for its treatment are very toxic, which has motivated the investigation for more effective and safe therapeutic options. In this study, the in vitro activity of ß-caryophyllene (BCP) was exploited taking into account its action against other protozoans as well as its well-known healing and anti-inflammatory properties (aspects relevant for the AK pathogenesis). On the other hand, high volatilization and oxidation phenomena are found for this compound, which led to its incorporation into nanoemulsions (NEs). Two emulsifying agents were tested, resulting in monodisperse systems with reduced droplet size (<265 nm) and high surface charge (positive and negative for NEs prepared with cetrimonium bromide -CTAB and Phosal® 50+, respectively). NEs prepared with CTAB were shown to be more stable after long-term storage at 4 and 25 °C than those prepared with Phosal®. Pure BCP, at the highest concentration (500 µM), resulted in a level of inhibition of Acanthamoeba trophozoites equivalent to that of reference drug (chlorhexidine). This activity was even greater after oil nanoencapsulation. The reduced droplet size could improve the interaction of the oil with the microorganism, justifying this finding. Changes in surface charge did not impact the activity. Positively charged NEs improved the interaction and retention of BCP in the cornea and thus should be prioritized for further studies.

Asunto(s)

Queratitis por Acanthamoeba , Emulsiones , Sesquiterpenos Policíclicos , Queratitis por Acanthamoeba/tratamiento farmacológico , Queratitis por Acanthamoeba/parasitología , Sesquiterpenos Policíclicos/química , Nanopartículas , Administración Oftálmica , Cetrimonio/química , Animales , Acanthamoeba/efectos de los fármacos , Estabilidad de Medicamentos , Tamaño de la Partícula , Soluciones Oftálmicas , Humanos