RESUMEN
Total starch granule-associated proteins (tGAP), including granule-channel (GCP) and granule-surface proteins (GSP), alter the physicochemical properties of starches. Quinoa starch (QS) acts as an effective emulsifier in Pickering emulsion. However, the correlation between the tGAP and the emulsifying capacity of QS at different scales remains unclear. Herein, GCP and tGAP were selectively removed from QS, namely QS-C and QS-A. Results indicated that the loss of tGAP increased the water permeability and hydrophilicity of the starch particles. Mesoscopically, removing tGAP decreased the diffusion rate and interfacial viscous modulus. Particularly, GSP had a more profound impact on the interfacial modulus than GCP. Microscopically and macroscopically, the loss of tGAP endowed QS with weakened emulsifying ability in terms of emulsions with larger droplet size and diminished rheological properties. Collectively, this work demonstrated that tGAP played an important role in the structural and interfacial properties of QS molecules and the stability of QS-stabilized emulsions.
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Chenopodium quinoa , Emulsionantes , Emulsiones , Interacciones Hidrofóbicas e Hidrofílicas , Proteínas de Plantas , Almidón , Chenopodium quinoa/química , Almidón/química , Emulsiones/química , Emulsionantes/química , Proteínas de Plantas/química , Tamaño de la Partícula , ReologíaRESUMEN
This study aimed to assess the suitability of Chachafruto flour (CHF) as a stabilizing agent for an oil-in-water emulsion and its impact on the physicochemical properties of the emulsion after spray drying. Emulsions with varying CHF concentrations (2 %, 3 %, and 4 %) were prepared and compared to a control. The results from the creaming index and particle size (emulsion) analyses indicated that the highest emulsion stability was achieved with 4 %CHF, attributed to its protein content (20.5 %). The encapsulates exhibited spherical and rough surface morphologies but without holes on the surface. Low moisture content (MC < 5 %) and water activity (aw < 0.2) were associated with powder stability. The encapsulates added with CHF showed good reconstitution properties. FTIR confirmed the absence of chemical interactions during the encapsulation process, contributing to the stability. Furthermore, the addition of CHF improved the thermal stability of the encapsulates. This study represents the first investigation on the emulsifying potential of Chachafruto flour.
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Cápsulas , Emulsiones , Harina , Tamaño de la Partícula , Agua , Emulsiones/química , Harina/análisis , Cápsulas/química , Agua/química , Secado por Pulverización , Aceites/químicaRESUMEN
This study assessed the effect of konjac glucomannan (KGM) on the aggregation of soy protein isolate (SPI) and its gel-related structure and properties. Raman results showed that KGM promoted the rearrangement of SPI to form more ß-sheets, contributing to the formation of an ordered structure. Atomic force microscopy, confocal laser scanning microscopy, and small-angle X-ray scattering results indicated that KGM reduced the size of SPI particles, narrowed their size distribution, and loosened the large aggregates formed by the stacking of SPI particles, improving the uniformity of gel system. As the hydrogen bonding between the KGM and SPI molecules enhanced, a well-developed network structure was obtained, further reducing the immobilized water's content (T22) and increasing the water-holding capacity (WHC) of SPI gel. Furthermore, this gel structure showed improved gel hardness and resistance to both small and large deformations. These findings facilitate the design and production of SPI-based gels with desired performance.
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Geles , Mananos , Proteínas de Soja , Proteínas de Soja/química , Mananos/química , Geles/química , Tamaño de la Partícula , Agregado de ProteínasRESUMEN
Hydrophobic bioactive compounds like astaxanthin (AST) exhibit poor water solubility and low bioavailability. Liposomes, which serve as nanocarriers, are known for their excellent biocompatibility and minimal immunogenicity. Traditionally, liposomes have been primarily constructed using phospholipids and cholesterol. However, the intake of cholesterol may pose a risk to human health. Phytosterol ester was reported to reduce level of cholesterol and improve properties of liposomes. In this study, phytosterol oleate was used to prepare liposomes instead of cholesterol to deliver AST (AST-P-Lip). The size range of AST-P-Lip was 100-220 nm, and the morphology was complete and uniform. In vitro studies showed that AST-P-Lip significantly enhanced the antioxidant activity and oral bioavailability of AST. During simulated digestion, AST-P-Lip protected AST from damage by gastric and intestinal digestive fluid. Additionally, AST-P-Lip had a good storage stability and safety. These results provide references for the preparation of novel liposomes and the delivery of bioactive compounds.
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Colesterol , Liposomas , Fitosteroles , Xantófilas , Liposomas/química , Xantófilas/química , Xantófilas/farmacología , Xantófilas/administración & dosificación , Humanos , Fitosteroles/química , Fitosteroles/farmacología , Fitosteroles/administración & dosificación , Colesterol/química , Tamaño de la Partícula , Disponibilidad Biológica , Ácido Oléico/química , Composición de Medicamentos , Animales , Antioxidantes/química , Antioxidantes/farmacologíaRESUMEN
This study comprehensively investigated the effects of high-temperature cooking (HT), complex enzyme hydrolysis (CE), and high-temperature cooking combined enzymatic hydrolysis (HE) on the chemical composition, microstructure, and functional attributes of soluble dietary fiber (SDF) extracted from corn bran. The results demonstrated that HE-SDF yielded the highest output at 13.80 ± 0.20 g/100 g, with enhancements in thermal stability, viscosity, hydration properties, adsorption capacity, and antioxidant activity. Cluster analysis revealed three distinct categories of SDF's physicochemical properties. Principal component analysis (PCA) confirmed the superior functional properties of HE-SDF. Correlation analysis showed positive relationships between the monosaccharide composition, purity, and viscosity of SDF and most of its functional attributes, whereas particle size and zeta potential were inversely correlated. Furthermore, a highly significant positive correlation was observed between crystallinity and thermal properties. These findings suggest that the HE method constitutes a viable strategy for enhancing the quality of SDF sourced from corn bran.
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Fibras de la Dieta , Zea mays , Zea mays/química , Fibras de la Dieta/análisis , Hidrólisis , Viscosidad , Análisis Multivariante , Calor , Tamaño de la Partícula , Antioxidantes/química , Culinaria , SolubilidadRESUMEN
Pro-fibrotic M2-like macrophages are widely implicated in the pathogenesis and progression of lung fibrosis due to their production of pro-fibrotic growth factors and cytokines. Yeast beta-glucan (YBG) microparticles have shown potential as immunomodulators that can convert macrophage polarization from a pro-fibrotic phenotype to an anti-fibrotic phenotype through the engagement of the Dectin-1 receptor. However, the processing conditions used to fabricate YBG microparticles can lead to unpredictable immunomodulatory effects. Herein, we report the use of Pressurized Gas eXpanded liquids (PGX) Technology® to fabricate YBG (PGX-YBG) microparticles with higher surface areas, lower densities, and smaller and more uniform size distributions compared to commercially available spray-dried YBGs. PGX-YBG is shown to activate Dectin-1 more efficiently in vitro while avoiding significant TLR 2/4 activation. Furthermore, PGX-YBG microparticles effectively modulate M2-like fibrosis-inducing murine and human macrophages into fibrosis-suppressing macrophages both in vitro as well as in ex vivo precision-cut murine lung slices, suggesting their potential utility as a therapeutic for addressing a broad spectrum of fibrotic end-point lung diseases.
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Macrófagos , beta-Glucanos , Animales , beta-Glucanos/química , beta-Glucanos/farmacología , Macrófagos/metabolismo , Macrófagos/efectos de los fármacos , Ratones , Humanos , Ratones Endogámicos C57BL , Lectinas Tipo C/metabolismo , Células RAW 264.7 , Fibrosis Pulmonar/patología , Fibrosis Pulmonar/tratamiento farmacológico , Saccharomyces cerevisiae , Tamaño de la PartículaRESUMEN
To investigate the seasonal characteristics in air pollution in Chengdu, a single particle aerosol mass spectrometry was used to continuously observe atmospheric fine particulate matter during one-month periods in summer and winter, respectively. The results showed that, apart from O3, the concentrations of other pollutants (CO, NO2, SO2, PM2.5 and PM10) were significantly higher in winter than in summer. All single particle aerosols were divided into seven categories: biomass burning (BB), coal combustion (CC), Dust, vehicle emission (VE), K mixed with nitrate (K-NO3), K mixed with sulfate and nitrate (K-SN), and K mixed with sulfate (K-SO4) particles. The highest contributions in both seasons were VE particles (24%). The higher contributions of K-SO4 (16%) and K-NO3 (10%) particles occurred in summer and winter, respectively, as a result of their different formation mechanisms. S-containing (K-SO4 and K-SN), VE, and BB particles caused the evolution of pollution in both seasons, and they can be considered as targets for future pollution reduction. The mixing of primary sources particles (VE, Dust, CC, and BB) with secondary components was stronger in winter than in summer. In summer, as pollution worsens, the mixing of primary sources particles with 62 [NO3]- weakened, but the mixing with 97 [HSO4]- increased. However, in winter, the mixing state of particles did not exhibit an obvious evolution rules. The potential source areas in summer were mainly distributed in the southern region of Sichuan, while in winter, besides the southern region, the contribution of the western region cannot be ignored.
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Aerosoles , Contaminantes Atmosféricos , Contaminación del Aire , Monitoreo del Ambiente , Material Particulado , Estaciones del Año , Aerosoles/análisis , Contaminantes Atmosféricos/análisis , Material Particulado/análisis , China , Contaminación del Aire/estadística & datos numéricos , Espectrometría de Masas , Tamaño de la PartículaRESUMEN
Thermodynamic modeling is still the most widely used method to characterize aerosol acidity, a critical physicochemical property of atmospheric aerosols. However, it remains unclear whether gas-aerosol partitioning should be incorporated when thermodynamic models are employed to estimate the acidity of coarse particles. In this work, field measurements were conducted at a coastal city in northern China across three seasons, and covered wide ranges of temperature, relative humidity and NH3 concentrations. We examined the performance of different modes of ISORROPIA-II (a widely used aerosol thermodynamic model) in estimating aerosol acidity of coarse and fine particles. The M0 mode, which incorporates gas-phase data and runs the model in the forward mode, provided reasonable estimation of aerosol acidity for coarse and fine particles. Compared to M0, the M1 mode, which runs the model in the forward mode but does not include gas-phase data, may capture the general trend of aerosol acidity but underestimates pH for both coarse and fine particles; M2, which runs the model in the reverse mode, results in large errors in estimated aerosol pH for both coarse and fine particles and should not be used for aerosol acidity calculations. However, M1 significantly underestimates liquid water contents for both fine and coarse particles, while M2 provides reliable estimation of liquid water contents. In summary, our work highlights the importance of incorporating gas-aerosol partitioning when estimating coarse particle acidity, and thus may help improve our understanding of acidity of coarse particles.
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Aerosoles , Contaminantes Atmosféricos , Modelos Químicos , Termodinámica , Aerosoles/análisis , Aerosoles/química , Contaminantes Atmosféricos/química , Contaminantes Atmosféricos/análisis , China , Monitoreo del Ambiente/métodos , Material Particulado/química , Material Particulado/análisis , Concentración de Iones de Hidrógeno , Tamaño de la PartículaRESUMEN
To explore air contamination resulting from special biomass combustion and suspended dust in Lhasa, the present study focused on the size distribution and chemical characteristics of particulate matter (PM) emission resulting from 7 types of non-fossil pollution sources. We investigated the concentration and size distribution of trace elements from 7 pollution sources collected in Lhasa. Combining Lhasa's atmospheric particulate matter data, enrichment factors (EFs) have been calculated to examine the potential impact of those pollution sources on the atmosphere quality of Lhasa. The highest mass concentration of total elements of biomass combustion appeared at PM0.4, and the second highest concentration existed in the size fraction 0.4-1 µm; the higher proportion (12 %) of toxic metals was produced by biomass combustion. The elemental composition of suspended dust and atmospheric particulate matter was close (except for As and Cd); the highest concentration of elements was all noted in PM2.5-10 (PM3-10). Potassium was found to be one of the main biomass markers. The proportion of Cu in suspended dust is significantly lower than that of atmospheric particulate matter (0.53 % and 3.75 %), which indicates that there are other anthropogenic sources. The EFs analysis showed that the Cr, Cu, Zn, and Pb produced by biomass combustion were highly enriched (EFs > 100) in all particle sizes. The EFs of most trace elements increased with decreasing particle size, indicating the greater influence of humanfactors on smaller particles.
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Aerosoles , Contaminantes Atmosféricos , Polvo , Monitoreo del Ambiente , Tamaño de la Partícula , Material Particulado , Contaminantes Atmosféricos/análisis , Aerosoles/análisis , Material Particulado/análisis , Polvo/análisis , Oligoelementos/análisis , Contaminación del Aire/estadística & datos numéricos , Contaminación del Aire/análisis , China , Atmósfera/químicaRESUMEN
Airborne microplastics (MPs) are important pollutants that have been present in the environment for many years and are characterized by their universality, persistence, and potential toxicity. This study investigated the effects of terrestrial and marine transport of MPs in the atmosphere of a coastal city and compared the difference between daytime and nighttime. Laser direct infrared imaging (LDIR) and polarized light microscopy were used to characterize the physical and chemical properties of MPs, including number concentration, chemical types, shape, and size. Backward trajectories were used to distinguish the air masses from marine and terrestrial transport. Twenty chemical types were detected by LDIR, with rubber (16.7%) and phenol-formaldehyde resin (PFR; 14.8%) being major components. Three main morphological types of MPs were identified, and fragments (78.1%) are the dominant type. MPs in the atmosphere were concentrated in the small particle size segment (20-50 µm). The concentration of MPs in the air mass from marine transport was 14.7 items/m3 - lower than that from terrestrial transport (32.0 items/m3). The number concentration of airborne MPs was negatively correlated with relative humidity. MPs from terrestrial transport were mainly rubber (20.2%), while those from marine transport were mainly PFR (18%). MPs in the marine transport air mass were more aged and had a lower number concentration than those in the terrestrial transport air mass. The number concentration of airborne MPs is higher during the day than at night. These findings could contribute to the development of targeted control measures and methods to reduce MP pollution.
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Contaminantes Atmosféricos , Monitoreo del Ambiente , Microplásticos , China , Microplásticos/análisis , Contaminantes Atmosféricos/análisis , Ciudades , Atmósfera/química , Tamaño de la PartículaRESUMEN
Control of N-nitrosodimethylamine (NDMA) in drinking water could be achieved by removing its precursors as one practical way. Herein, superfine powdered activated carbons with a diameter of about 1 µm (SPACs) were successfully prepared by grinding powdered activated carbon (PAC, D50=24.3 µm) and applied to remove model NDMA precursors, i.e. ranitidine (RAN) and nizatidine (NIZ). Results from grain diameter experiments demonstrated that the absorption velocity increased dramatically with decreasing particle size, and the maximum increase in k2 was 26.8-folds for RAN and 33.4-folds for NIZ. Moreover, kinetic experiments explained that rapid absorption could be attributed to the acceleration of intraparticle diffusion due to the shortening of the diffusion path. Furthermore, performance comparison experiments suggested that the removal of RAN and NIZ (C0=0.5 mg/L) could reach 61.3% and 60%, respectively, within 5 min, when the dosage of SAPC-1.1 (D50=1.1 µm) was merely 5 mg/L, while PAC-24.3 could only eliminate 17.5% and 18.6%. The adsorption isotherm was well defined by Langmuir isotherm model, indicating that the adsorption of RAN/NIZ was a monolayer coverage process. The adsorption of RAN or NIZ by SAPC-1.1 and PAC-24.3 was strongly pH dependent, and high adsorption capacity could be observed under the condition of pH > pka+1. The coexistence of humic acid (HA) had no significant effect on the adsorption performance because RAN/NIZ may be coupled with HA and removed simultaneously. The coexistence of anions had little effect on the adsorption also. This study is expected to provide an alternative strategy for drinking water safety triggered by NDMA.
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Carbón Orgánico , Dimetilnitrosamina , Tamaño de la Partícula , Contaminantes Químicos del Agua , Purificación del Agua , Adsorción , Carbón Orgánico/química , Contaminantes Químicos del Agua/química , Purificación del Agua/métodos , Dimetilnitrosamina/química , Cinética , Modelos QuímicosRESUMEN
This study embarks on an explorative investigation into the effects of typical concentrations and varying particle sizes of fine grits (FG, the involatile portion of suspended solids) and fine debris (FD, the volatile yet unbiodegradable fraction of suspended solids) within the influent on the mixed liquor volatile suspended solids (MLVSS)/mixed liquor suspended solids (MLSS) ratio of an activated sludge system. Through meticulous experimentation, it was discerned that the addition of FG or FD, the particle size of FG, and the concentration of FD bore no substantial impact on the pollutant removal efficiency (denoted by the removal rate of COD and ammonia nitrogen) under constant operational conditions. However, a notable decrease in the MLVSS/MLSS ratio was observed with a typical FG concentration of 20 mg/L, with smaller FG particle sizes exacerbating this reduction. Additionally, variations in FD concentrations influenced both MLSS and MLVSS/MLSS ratios; a higher FD concentration led to an increased MLSS and a reduced MLVSS/MLSS ratio, indicating FD accumulation in the system. A predictive model for MLVSS/MLSS was constructed based on quality balance calculations, offering a tool for foreseeing the MLVSS/MLSS ratio under stable long-term influent conditions of FG and FD. This model, validated using data from the BXH wastewater treatment plant (WWTP), showcased remarkable accuracy.
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Aguas del Alcantarillado , Eliminación de Residuos Líquidos , Eliminación de Residuos Líquidos/métodos , Tamaño de la Partícula , Contaminantes Químicos del Agua/análisisRESUMEN
The study investigates the potential of Rhizoclonium hieroglyphicum as a novel source for synthesizing nickel oxide nanoparticles (RH-NiONPs) and evaluates its biological applications. Phytochemicals in the algal extract serve as capping, reducing and stabilizing agent for nickel oxide nanoparticles. The process variables were optimized using BBD based RSM to obtain maximum RH-NiONPs. Characterization of RH-NiONPs using UV-Vis and FT-IR spectroscopy reveals the plasmon resonance peak at 340 nm and the functional groups responsible for reduction and stabilization. XRD confirmed the crystalline nature while the stability and size of the RH-NiONPs were determined by DLS and zeta potential. Toxicity assessments demonstrated the effect of RH-NiONPs against Vigna radiata, Allium cepa and Artemia salina was low. RH-NiONPs revealed significant zone of inhibition against the selected bacteria and fungi. The results of larvicidal activity showed that RH-NiONPs are toxic to 4th instar larvae of Daphnis nerii. Also, RH-NiONPs efficiently decolorized Reactive Violet 13 (92%) under sunlight irradiation and the experimental data well fits to Langmuir isotherm along with pseudo second order kinetic model. The thermodynamic studies enunciate the exothermic and non-spontaneous photocatalytic decolorization of reactive violet 13. Thus, the current study assesses the eco-friendly and cost-effective nature of RH-NiONPs along with its biological applications.
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Artemia , Nanopartículas del Metal , Níquel , Extractos Vegetales , Níquel/química , Níquel/farmacología , Animales , Extractos Vegetales/química , Extractos Vegetales/farmacología , Nanopartículas del Metal/química , Artemia/efectos de los fármacos , Cebollas/química , Cebollas/efectos de los fármacos , Daphnia/efectos de los fármacos , Vigna/química , Propiedades de Superficie , Larva/efectos de los fármacos , Tamaño de la Partícula , Pruebas de Sensibilidad Microbiana , Antibacterianos/farmacología , Antibacterianos/química , Antibacterianos/síntesis químicaRESUMEN
Perilla essential oil (PLEO) offers benefits for food preservation and healthcare, yet its instability restricts its applications. In this study, chitosan (CS) and TiO2 used to prepare composite particles. TiO2, after being modified with sodium laurate (SL), was successfully introduced at 0.1 %-3 % into the CS matrix. The resulting CS-SL-TiO2 composite particles can be formed by intertwining and rearranging through intramolecular and intermolecular interactions, and form an O/W interface with stability and viscoelasticity. The Pickering emulsions stabilized by these particles exhibit non-Newtonian pseudoplastic behavior, shear-thinning properties, and slow-release characteristics, along with antibacterial activity. Emulsions with 0.5 % and 1 % CS-SL-TiO2 composites demonstrated superior antibacterial effects against Escherichia coli and Staphylococcus aureus. The study revealed that all emulsions undergo Fickian diffusion and a sustained release of PLEO, with the Ritger-Peppas model best describing this release mechanism. The slow-release behaviors positively correlates with interfacial pressure, composite particle size, composite particle potential, composite contact angle, emulsion particle size and emulsion potential, but negatively correlates with diffusion rate, penetration rate, release kinetics and release rate. The findings lay groundwork for developing slow-release antimicrobial emulsions within polysaccharide matrices, showcasing promise for antimicrobial packaging solutions and enhanced food preservation techniques.
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Antibacterianos , Quitosano , Emulsiones , Escherichia coli , Staphylococcus aureus , Titanio , Agua , Quitosano/química , Quitosano/farmacología , Titanio/química , Antibacterianos/química , Antibacterianos/farmacología , Staphylococcus aureus/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Agua/química , Aceites Volátiles/química , Aceites Volátiles/farmacología , Tamaño de la Partícula , Preparaciones de Acción Retardada/química , Aceites de Plantas/química , Aceites de Plantas/farmacología , Pruebas de Sensibilidad Microbiana , Liberación de FármacosRESUMEN
Starch is one of the natural encapsulant materials widely used in food, pharmaceutical and cosmetic industries. Starch with high amylose content (above 40 %, w/w) is prone to form single helices V-type allomorph with a hydrophilic outer surface and a hydrophobic inner cavity making them suitable for encapsulation of hydrophobic compounds such as essential oils, fatty acids, and vitamins. Pea starch obtained from pea protein processing industries have a high amylose content (40 %, w/w) rendering them unsuitable for direct food applications as ingredients. Therefore, in this study, an in-house spraying procedure was used to synthesize nanoparticles using pea starch, to encapsulate neem oil, a natural antimicrobial compound obtained from neem plant (Azadirachta indica) seed. The synthesis of the oil-encapsulated starch nanoparticles (OESNP) was optimized using a Box-Behnken experimental design to study the influence of the processing parameters such as the initial starch concentration, homogenization speed, duration of homogenization, sample injection rate, and quantity of antisolvent (ethanol). The optimized sample showed an 80-90 % encapsulation efficiency and particle size of <500 nm. The spherical OESNPs also demonstrated sustained release of the oil compared to free oil when dispersed in water. X-ray diffraction analysis revealed the coexistence of C-type and V-type polymorphs in the loaded and unloaded nanoparticles. It is concluded that the synthesized OESNPs with controlled release hold the potential to utilize industrial pea starch waste for the delivery of natural pesticides in agriculture.
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Glicéridos , Nanopartículas , Pisum sativum , Almidón , Pisum sativum/química , Nanopartículas/química , Almidón/química , Glicéridos/química , Tamaño de la Partícula , Terpenos/química , Aceites de Plantas/química , Agricultura/métodos , Azadirachta/química , Amilosa/químicaRESUMEN
Oral Topiramate therapy is associated with systemic adverse effects including paresthesia,abdominal pain, and fluctuations in plasma levels. The purpose of this research was to develop an intranasal in situ gel based system comprising Topiramate polymeric nanoparticles and evaluate its potential both in vitro and in vivo. Poly (lactic-co-glycolic acid) (PLGA)nanoparticles prepared by nanoprecipitation method were added into the in situ gelling system of Poloxamer 407 and HPMC K4M. Selected formulation (TG5) was evaluated for physicochemical properties, nasal permeation and in vivo pharmacokinetics in rats. PLGAnanoparticles (O1) exhibited low particle size (~ 144.4 nm), good polydispersity index (0.202), negative zeta potential (-12.7 mV), and adequate entrapment efficiency (64.7%). Developed in situ gel showed ideal pH (6.5), good gelling time (35 s), gelling temperature(37â), suitable viscosity (1335 cP)and drug content of 96.2%. In vitro drug release conformedto Higuchi release kinetics, exhibiting a biphasic pattern of initial burst release and sustained release for 24 h. Oral administration of the drug to Sprague-Dawley rats (G3) showed higher plasma Cmax(504 ng/ml, p < 0.0001) when compared to nasal delivery of in situ gel (G4) or solution (G5). Additionally, AUC0-α of G3 (8786.82 ng/ml*h) was considerably higher than othergroups. Brain uptake data indicates a higher drug level with G4 (112.47 ng /ml) at 12 h when compared to G3. Histopathological examination of groups; G1 (intranasal saline), G2(intranasal placebo), G3, G4, and G5 did not show any lesions of pathological significance. Overall, the experimental results observed were promising and substantiated the potential of developed in situ gel for intranasal delivery.
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Administración Intranasal , Encéfalo , Geles , Nanopartículas , Mucosa Nasal , Copolímero de Ácido Poliláctico-Ácido Poliglicólico , Ratas Sprague-Dawley , Topiramato , Animales , Topiramato/administración & dosificación , Topiramato/farmacocinética , Nanopartículas/química , Ratas , Administración Intranasal/métodos , Copolímero de Ácido Poliláctico-Ácido Poliglicólico/química , Encéfalo/metabolismo , Encéfalo/efectos de los fármacos , Mucosa Nasal/metabolismo , Mucosa Nasal/efectos de los fármacos , Masculino , Tamaño de la Partícula , Fructosa/administración & dosificación , Fructosa/farmacocinética , Fructosa/química , Portadores de Fármacos/química , Liberación de Fármacos , Sistemas de Liberación de Medicamentos/métodos , Ácido Láctico/química , Ácido Láctico/administración & dosificación , Ácido Poliglicólico/química , Administración OralRESUMEN
Intestinal lymphatic transport offers an alternative and effective way to deliver drugs, such as avoiding first-pass metabolism, enhancing oral bioavailability, and facilitating the treatment of targeted lymphoid-related diseases. However, the clinical use of luteolin (LUT) is limited by its poor water solubility and low bioavailability, and enhancing lymphatic transport by nanoemulsion may be an efficient way to enhance its oral bioavailability. The objective of this work is to prepare the luteolin nanoemulsions (LUT NEs), optimized its preparation parameters by using Box-Behnken design optimization (BBD) and evaluated it in vitro and in vivo. An Caco-2 / Raji B cell co-incubation monolayer model was established to simulate the M-cell pathway, and the differences in the transmembrane transport of LUT and NEs were compared. Cycloheximide (CHX) was utilized to establish rat chylomicron (CM) blocking model, and for investigating the influence of pharmacokinetic parameters in rats thereafter. The results showed that LUT NEs have good stability, the particle sizes were about 23.87 ± 0.57 nm. Compared with LUT suspension, The Papp of LUT NEs was enhanced for 3.5-folds, the oral bioavailability was increased by about 2.97-folds. In addition, after binding with chylomicron, the oral bioavailability of LUT NEs was decreased for about 30% (AUC 0-∞ (µg/L*h): 5.356 ± 1.144 vs 3.753 ± 0.188). These results demonstrated that NEs could enhance the oral absorption of luteolin via lymphatic transport routes.
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Disponibilidad Biológica , Emulsiones , Luteolina , Nanopartículas , Tamaño de la Partícula , Ratas Sprague-Dawley , Luteolina/farmacocinética , Luteolina/administración & dosificación , Luteolina/química , Animales , Ratas , Humanos , Células CACO-2 , Administración Oral , Masculino , Nanopartículas/química , Solubilidad , Absorción Intestinal/fisiología , Quilomicrones/metabolismo , Transporte Biológico/fisiología , Sistema Linfático/metabolismoRESUMEN
The present study aimed to develop and optimize solidified supersaturated self-nanoemulsifying drug delivery systems (SNEDDS) for the combined administration of antihypertensive, antihyperglycemic, and antihyperlipidemic drugs to enhance their solubility and dissolution during the treatment of metabolic syndrome. Various SNEDDS formulations were prepared and subjected to pharmaceutical assessment. The solubility of candesartan (CC), glibenclamide (GB), and rosuvastatin (RC) in SNEDDS and supersaturated SNEDDS formulations was evaluated. The optimized formulation was solidified using Syloid adsorbent at different ratios. Pharmaceutical characterization of the formulations included particle size, zeta potential, in-vitro dissolution, PXRD, FTIR, and SEM analysis. The prepared optimized formulation (F6) was able to form homogeneous nanoemulsion droplets without phase separation, which is composed of Tween 20: PEG-400: Capmul MCM (4: 3: 3). It was mixed with 5% PVP-K30 to prepare a supersaturated liquid SNEDDS formulation (F9). In addition, it was found that the addition of PVP-K30 significantly increased solubility CC and GB from 20.46 ± 0.48 and 6.73 ± 0.05 to 27.67 ± 1.72 and 9.45 ± 0.32 mg/g, respectively. In-vitro dissolution study revealed that liquid and solid SNEDD formulations remarkably improved the dissolution rates of CC, GB, and RC compared to pure drugs. XRPD and FTIR analysis revealed that all drugs present in an amorphous state within prepared solidified supersaturated SNEDDS formulation. SEM images showed that liquid SNEDDS formulation was successfully adsorbed on the surface of Syloid. Overall, optimized F9 and solidified supersaturated SNEDDS formulations showed superior performance in enhancing drug solubility and dissolution rate. The present study revealed that the proposed triple combination therapy of metabolic syndrome holds a promising strategy during the treatment of metabolic syndrome. Further in-vivo studies are required to evaluate the therapeutic efficacy of prepared solidified supersaturated SNEDDS formulation.
Asunto(s)
Sistemas de Liberación de Medicamentos , Emulsiones , Hipoglucemiantes , Síndrome Metabólico , Tamaño de la Partícula , Solubilidad , Síndrome Metabólico/tratamiento farmacológico , Hipoglucemiantes/administración & dosificación , Hipoglucemiantes/química , Emulsiones/química , Sistemas de Liberación de Medicamentos/métodos , Química Farmacéutica/métodos , Antihipertensivos/química , Antihipertensivos/administración & dosificación , Hipolipemiantes/química , Hipolipemiantes/administración & dosificación , Nanopartículas/química , Polietilenglicoles/química , Composición de Medicamentos/métodosRESUMEN
Normal skin is the first line of defense in the human body. A burn injury makes the skin susceptible to bacterial infection, thereby delaying wound healing and ultimately leading to sepsis. The chances of biofilm formation are high in burn wounds due to the presence of avascular necrotic tissue. The most common pathogen to cause burn infection and biofilm is Pseudomonas aeruginosa. The purpose of this study was to create a microemulsion (ME) formulation for topical application to treat bacterial burn infection. In the present study, tea tree oil was used as the oil phase, Tween 80 and transcutol were used as surfactants, and water served as the aqueous phase. Pseudo ternary phase diagrams were used to determine the design space. The ranges of components as suggested by the design were chosen, optimization of the microemulsion was performed, and in vitro drug release was assessed. Based on the characterization studies performed, it was found that the microemulsion were formulated properly, and the particle size obtained was within the desired microemulsion range of 10 to 300 nm. The I release study showed that the microemulsion followed an immediate release profile. The formulation was further tested based on its ability to inhibit biofilm formation and bacterial growth. The prepared microemulsion was capable of inhibiting biofilm formation.