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1.
Food Chem ; 352: 129398, 2021 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-33652197

RESUMEN

We investigated the effects of ultrasonic treatment (400 W, 20 kHz, 45.52 W/L) and storage time (0 d, 3 d, 7 d and 10 d) on functional properties, structural changes and in vitro digestion of actomyosin complex isolated from vacuum-packed pork. As storage time increased, turbidity, surface hydrophobicity, active sulfhydryl and total sulfhydryl of actomyosin complex increased, while protein solubility decreased. Ultrasonic treatment increased surface hydrophobicity, protein solubility and active sulfhydryl content but decreased turbidity and total sulfhydryl content compared with the control. Ultrasonic treatment caused a reduction in α-helix content on 0 day and the fluorescence intensity of tryptophan and tyrosine residues. It increased pancreatin digestibility of actomyosin complex and the number of peptides of smaller than 1 kDa. However, it decreased the number of peptides. The findings provide a new insight into the application of appropriate ultrasonic treatment to promote meat digestibility.


Asunto(s)
Actomiosina/química , Digestión , Almacenamiento de Alimentos , Carne/análisis , Ondas Ultrasónicas , Actomiosina/metabolismo , Animales , Interacciones Hidrofóbicas e Hidrofílicas , Solubilidad , Compuestos de Sulfhidrilo/química , Porcinos
2.
Molecules ; 26(5)2021 Feb 24.
Artículo en Inglés | MEDLINE | ID: mdl-33668137

RESUMEN

Flow batteries can play an important role as energy storage media in future electricity grids. Organic compounds, based on abundant elements, are appealing alternatives as redox couples for redox flow batteries. The straightforward scalability, the independence of material sources, and the potentially attractive price motivate researchers to investigate this technological area. Four different benzyl-morpholino hydroquinone derivatives were synthesized as potential redox active species. Compounds bearing central symmetry were shown to be about an order of magnitude less soluble in water than isomers without central symmetry. Counter ions also affected solubility. Perchlorate, chlorate, sulfate and phosphate anions were investigated as counter ions. The formations of different polymorphs was observed, showing that their solubility is not a function of their structure. The kinetics of the transformation can give misleading solubility values according to Ostwald's rule. The unpredictability of both the kinetics and the thermodynamics of the formation of polymorphs is a danger for new organic compounds designed for flow battery applications.


Asunto(s)
Suministros de Energía Eléctrica , Hidroquinonas/química , Cristalografía por Rayos X , Hidroquinonas/síntesis química , Iones/química , Modelos Moleculares , Estructura Molecular , Solubilidad , Termodinámica , Agua/química
3.
AAPS PharmSciTech ; 22(3): 84, 2021 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-33649887

RESUMEN

Prediction of performance of traditional, reformulated, and novel oral formulations in adults and pediatrics is of great importance. This study was conducted to assess solubility of celecoxib in age-appropriate fasted- and fed-state gastric and intestinal biorelevant media, classify celecoxib into biopharmaceutical classification system (BCS), and assess the effects of age-related developmental changes in the composition and volume of gastrointestinal fluids on the solubility and performance of oral formulations containing celecoxib. Solubility of celecoxib was assessed at 37°C in the pH range specified by the BCS-based criteria in 13 age-appropriate biorelevant media reflective of the gastric and proximal small intestinal environment in both fasted and fed states in adults and different pediatric subpopulations. A validated HPLC-UV method was used to quantify celecoxib. Experimental and computational molecular descriptors and in vivo pharmacokinetic data were used to assign the permeability class of celecoxib. Celecoxib belonged to BCS class 2. The pediatric to adult solubility ratios were outside the 80-125% boundaries in 3 and borderline in 1 biorelevant media. Significant age-related variability could be predicted for oral formulations containing celecoxib intended for pediatric use. Findings of this study indicated that the criteria used in the adult BCS might not be directly applied to pediatric subpopulations.


Asunto(s)
Productos Biológicos/clasificación , Productos Biológicos/farmacocinética , Celecoxib/clasificación , Celecoxib/farmacocinética , Ayuno/metabolismo , Absorción Gastrointestinal/fisiología , Administración Oral , Adulto , Antiinflamatorios no Esteroideos/clasificación , Antiinflamatorios no Esteroideos/farmacocinética , Líquidos Corporales/química , Líquidos Corporales/metabolismo , Niño , Preescolar , Evaluación Preclínica de Medicamentos/métodos , Predicción , Absorción Gastrointestinal/efectos de los fármacos , Humanos , Lactante , Recién Nacido , Permeabilidad , Solubilidad
4.
Molecules ; 26(4)2021 Feb 20.
Artículo en Inglés | MEDLINE | ID: mdl-33672444

RESUMEN

Regioselective synthesis of novel 2H,3H-[1,4]thiazino[2,3,4-ij]quinolin-4-ium derivatives has been developed by annulation reactions of 8-quinolinesulfenyl halides with vinyl chalcogenides (vinyl ethers, divinyl sulfide, divinyl selenide and phenyl vinyl sulfide) and tetravinyl silane. The novel reagent 8-quinolinesulfenyl bromide was used in the annulation reactions. The influence of the substrate structure and the nature of heteroatoms on the direction of the reactions and on product yields has been studied. The opposite regiochemistry was observed in the reactions with vinyl chalcogenides and tetravinyl silane. The obtained condensed heterocycles are novel water-soluble functionalized compounds with promising biological activity.


Asunto(s)
Compuestos de Quinolinio/síntesis química , Estructura Molecular , Compuestos de Quinolinio/química , Solubilidad , Estereoisomerismo , Agua/química
5.
Food Chem ; 352: 129395, 2021 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-33677211

RESUMEN

Myofibrillar proteins (MPs), as a food-grade material, have the potential to improve the solubility and bioavailability of curcumin. However, the interaction mechanism between MPs and curcumin under charge regulation induced by alkaline pH and NaCl was unclear. In this study, the binding between curcumin and MPs at pH 12 was confirmed by the fluorescence quenching under different NaCl concentration (0, 0.3, 0.6 and 0.9 mol/L). Further kinetic experiments showed, MPs possessed a higher affinity to bind curcumin in the presence of NaCl, especially at 0.6 M NaCl. Followed pH shifting from 12 to 7 does not affect UV-Vis absorption spectra of protein-curcumin dispersions. The secondary structure of MPs was not affected by binding with curcumin. Formation of this stable complex can be explained by hydrophobic other than electrostatic interaction. Therefore, the presence of NaCl facilitated exposure of hydrophobic pocket to improve the binding affinity between curcumin and MPs due to the importance of hydrophobic interaction.


Asunto(s)
Curcumina/metabolismo , Proteínas Musculares/metabolismo , Curcumina/química , Interacciones Hidrofóbicas e Hidrofílicas , Cinética , Proteínas Musculares/química , Unión Proteica , Cloruro de Sodio/química , Solubilidad , Electricidad Estática
6.
Food Chem ; 351: 129315, 2021 Jul 30.
Artículo en Inglés | MEDLINE | ID: mdl-33647686

RESUMEN

Mangiferin-loaded nanobilosomes (MGF-NBSs) were developed using microfluidic-based techniques to improve aqueous solubility, digestive stability, and cellular antioxidant activity (CAA) of mangiferin. Preliminary experiments showed that optimal formation conditions were 5:1 aqueous (water) to solvent (ethanol) phase ratio and 85 mL/min total flow rate. Further optimization using response surface methodology provided the optimal formulation (200 mg encapsulant consisting of 90.91% phosphatidylcholine and 9.09% sodium glycocholate, and 25.89 mg mangiferin), achieving 9.25% mangiferin loading and 80.65% encapsulation efficiency. Mono-dispersed MGF-NBSs with an average size of around 48.14 nm and zeta potential of -30.1 mV were obtained. FTIR and DSC results confirmed the successful encapsulation of mangiferin into the nanobilosomes and revealed interactions among the components. MGF-NBSs showed a 7-fold increase in the aqueous solubility compared with non-encapsulated mangiferin. CAA of MGF-NBSs in Caco-2 cells was 2 times higher than that of mangiferin and the in vitro digestive stability was improved.


Asunto(s)
Antioxidantes/química , Antioxidantes/farmacología , Nanoestructuras/química , Agua/química , Xantonas/química , Xantonas/farmacología , Antioxidantes/metabolismo , Células CACO-2 , Digestión , Composición de Medicamentos , Humanos , Dispositivos Laboratorio en un Chip , Tamaño de la Partícula , Solubilidad , Xantonas/metabolismo
7.
Water Res ; 196: 117039, 2021 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-33761397

RESUMEN

Ozone (O3) has been widely used for the elimination of recalcitrant micropollutants in aqueous environments, due to its strong oxidation ability. However, the utilization efficiency of O3 is constrained by its low solubility and short half-life during the treatment process. Herein, an integrated approach, using nanobubble technology and micro-environmental chemistry within cyclodextrin inclusion cavities, was studied in order to enhance the reactivity of ozonisation. Compared with traditional macrobubble aeration with O3 in water, nanobubble aeration achieved 1.7 times higher solubility of O3, and increased the mass transfer coefficient 4.7 times. Moreover, the addition of hydroxypropyl-ß-cyclodextrin (HPßCD) further increased the stability of O3 through formation of an inclusion complex in its molecule-specific cavity. At a HPßCD:O3 molar ratio of 10:1, the lifespan of O3 reached 18 times longer than in a HPßCD-free O3 solution. Such approach accelerated the removal efficiency of the model micropollutant, 4-chlorophenol by 6.9 times, compared with conventional macrobubble ozonation. Examination of the HPßCD inclusion complex by UV-visible spectroscopy and Nuclear Magnetic Resonance analyses revealed that both O3 and 4-chlorophenol entered the HPßCD cavity, and Benesi-Hildebrand plots indicated a 1:1 stoichiometry of the host and guest compounds. Additionally, molecular docking simulations were conducted in order to confirm the formation of a ternary complex of HPßCD:4-chlorophenol:O3 and to determine the optimal inclusion mode. With these results, our study highlights the viability of the proposed integrated approach to enhance the ozonation of organic micropollutants.


Asunto(s)
Ciclodextrinas , Ozono , Contaminantes Químicos del Agua , 2-Hidroxipropil-beta-Ciclodextrina , Simulación del Acoplamiento Molecular , Solubilidad , Contaminantes Químicos del Agua/análisis
8.
AAPS PharmSciTech ; 22(3): 99, 2021 Mar 11.
Artículo en Inglés | MEDLINE | ID: mdl-33709248

RESUMEN

The objective of this work was to investigate the influence of tablet location along the bottom of a USP apparatus II vessel on polymer erosion and drug release of surface-erodible sustained-release tablets using computational simulation methods. Computational fluid dynamics (CFD) methods were performed to simulate the velocity distribution. A mathematical model was developed to describe polymer erosion and tablet deformation according to the mass transfer coefficient. Numerical analysis was used to simulate drug release controlled by drug diffusion and polymer erosion. The results indicated that tablets located at the off-center position deformed faster than the tablets located at the center position. However, tablet location had no profound impact on drug release rate since all drug release profiles were "similar" according to the f2 similarity values which were above 50. Hence, our simulation supported that the USP apparatus II was a reliable and robust device for the dissolution testing of surface-erodible sustained-release tablets.


Asunto(s)
Simulación por Computador , Liberación de Fármacos , Polímeros/química , Polímeros/farmacocinética , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Hidrodinámica , Solubilidad , Comprimidos
9.
AAPS PharmSciTech ; 22(3): 108, 2021 Mar 14.
Artículo en Inglés | MEDLINE | ID: mdl-33718989

RESUMEN

The combination of self-microemulsifying drug delivery system (SMEDDS) and mesoporous silica materials favors the oral delivery of poorly water-soluble drugs (PWSD). However, the influence of the surface property of the mesopores towards the drug release and in vivo pharmacokinetics is still unknown. In this study, SBA-15 with hydroxyl groups (SBA-15-H), methyl groups (SBA-15-M), amino groups (SBA-15-A), or carboxyl groups (SBA-15-C) was combined with SMEDDS containing sirolimus (SRL). The diffusion and self-emulsifying of SMEDDS greatly improved the drug release over the raw SRL and SRL-SBA-15-R (R referred to as the functional groups). Results of drug absorption and X-ray photoelectron spectroscopy (XPS) showed strong hydrogen binding between SRL and the amino groups of SBA-15-A, which hindered the drug release and oral bioavailability of SRL-SMEDDS-SBA-15-A. The favorable release of SRL-SMEDDS-SBA-15-C (91.31 ± 0.57%) and SRL-SMEDDS-SBA-15-M (91.76 ± 3.72%) contributed to enhancing the maximum blood concentration (Cmax) and the area under the concentration-time curve (AUC0→48). In conclusion, the release of SRL-SMEDDS-SBA-15-R was determined by the surface affinity of the SBA-15-R and the interaction between the SRL molecules and the surface of SBA-15-R. This study suggested that the SMEDDS-SBA-15 was a favorable carrier for PWSD, and the surface property of the mesopores should be considered for the optimization of the SMEDDS-SBA-15.


Asunto(s)
Sistemas de Liberación de Medicamentos/métodos , Liberación de Fármacos/fisiología , Absorción Intestinal/fisiología , Sirolimus/administración & dosificación , Sirolimus/farmacocinética , Administración Oral , Animales , Antibacterianos/administración & dosificación , Antibacterianos/química , Antibacterianos/farmacocinética , Disponibilidad Biológica , Perros , Emulsiones/administración & dosificación , Emulsiones/química , Emulsiones/farmacocinética , Absorción Intestinal/efectos de los fármacos , Masculino , Dióxido de Silicio/administración & dosificación , Dióxido de Silicio/química , Dióxido de Silicio/farmacocinética , Sirolimus/química , Solubilidad , Propiedades de Superficie
10.
Water Res ; 195: 116975, 2021 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-33677241

RESUMEN

At sites where aqueous film forming foams (AFFFs) are used for fire suppression or training activities, interactions between dissolved foam constituents and organic liquids could alter contaminant migration in the subsurface. In this study, batch reactor and column experiments were conducted to investigate the potential for AFFF solutions to enhance the solubility and mobility of three representative non-aqueous phase liquid (NAPLs), JP-4 jet fuel, trichloroethene (TCE), and tetrachloroethene (PCE). For AFFF concentrations up to 5% wt. (50,000 mg/L), aqueous solubilities of TCE and PCE increased by less than 50%, indicating the absence of micellar solubilization. However, NAPL-water interfacial tensions were reduced to less than 1.5 mN/m and resulted in accumulation of up to 2.25 mg/m2 of AFFF at the NAPL-water interface. To assess the potential for AFFF to mobilize residual (entrapped) NAPL at a field application rate of 3% wt. (30,000 mg/L), columns were packed with two size fractions of Ottawa sands (20-30 mesh and 60-80 mesh) that yielded residual NAPL saturations ranging from 11.7 to 17.6%. Following injection of 3 pore volumes of the 3% wt. AFFF solution, partial mobilization of residual NAPL was observed for PCE, TCE, and JP-4, with saturation reductions of 0.7 to 2% in 20-30 mesh and 0.3% to 1.3% in 60-80 mesh Ottawa sand. The columns were then flushed with an ultralow-IFT surfactant solution consisting of 4% wt. 1:1 Aerosol AY/OT, which resulted in nearly complete mobilization of the remaining residual NAPL. When NAPL desaturation curves were expressed in terms of the total trapping number (NT), the threshold value of NT required for NAPL mobilization by 3% wt. AFFF was approximately 2 × 10-5, consistent with previous studies. These findings demonstrate that AFFF solutions can lead to partial mobilization of residual NAPL, and that the total trapping number concept can be used to predict such behavior a priori. In addition, the observed IFT reductions are sufficient to alter NAPL accumulation and redistribution behavior in the subsurface through enhanced spreading above the water table (e.g., JP-4) or penetration into lower-permeability media (e.g., TCE, PCE).


Asunto(s)
Arena , Contaminantes Químicos del Agua , Aerosoles , Cuarzo , Solubilidad , Contaminantes Químicos del Agua/análisis
11.
AAPS PharmSciTech ; 22(3): 92, 2021 Mar 08.
Artículo en Inglés | MEDLINE | ID: mdl-33683477

RESUMEN

Venetoclax (VX) used in the treatment of chronic lymphocytic leukemia possesses low oral bioavailability (5.4%) and undergoes first-pass metabolism. Development of a formulation to overcome its bioavailability problem can be done by using nanocrystals which has many scientific applications. Nanocrystals of VX were formulated using amalgamation of precipitation and high-pressure homogenization method, in which polyvinyl alcohol (PVA) was selected as stabilizer. Process parameters like concentration of stabilizer, homogenization pressure, number of homogenization cycle, and concentration of lyoprotectant were optimized to obtain the desired particle size for the preparation of nanocrystal formulation. HPLC methods were developed and validated in-house for determination of in vitro dissolution data and in vivo bioavailability data. Physicochemical characterization was done to determine the particle size (zeta sizer), crystalline nature (DSC and XRPD), solubility (shaker bath), and dissolution (USP type 2 apparatus). Lyophilized VX nanocrystals of size less than 350 nm showed substantial increase in saturation solubility (~20 folds) and dissolution in comparison with free VX. In vitro release study revealed that 100% dissolution was achieved in 120 min as compared to VX free base which is having less than 43.5% dissolution in 120 min. Formulations of VX remain stable for 6 months under accelerated stability conditions. In vivo pharmacokinetic data in male Sprague-Dawley rats showed (~2.02 folds) significant increase in oral bioavailability of VX formulation as compared to free drug because of rapid dissolution and absorption which makes the nanocrystal formulation a better approach for oral administration of poorly soluble drugs.


Asunto(s)
Antineoplásicos/administración & dosificación , Compuestos Bicíclicos Heterocíclicos con Puentes/administración & dosificación , Sulfonamidas/administración & dosificación , Administración Oral , Animales , Antineoplásicos/química , Antineoplásicos/farmacocinética , Disponibilidad Biológica , Compuestos Bicíclicos Heterocíclicos con Puentes/química , Compuestos Bicíclicos Heterocíclicos con Puentes/farmacocinética , Cromatografía Líquida de Alta Presión , Liofilización , Masculino , Nanopartículas , Tamaño de la Partícula , Alcohol Polivinílico , Ratas , Ratas Sprague-Dawley , Solubilidad , Sulfonamidas/química , Sulfonamidas/farmacocinética
12.
AAPS PharmSciTech ; 22(3): 94, 2021 Mar 08.
Artículo en Inglés | MEDLINE | ID: mdl-33683493

RESUMEN

Hydrochlorothiazide (HTZ) is a first-line drug used in the treatment of hypertension suffered from low oral bioavailability due to poor aqueous solubility and permeability. Hence, lyophilized egg white protein-based solid dispersion (HTZ-EWP SD) was developed to explore its feasibility as a solid dispersion carrier for enhanced aqueous solubility and permeability of HTZ. The HTZ-EWP SD was prepared using the kneading method. HTZ-EWP SD was characterized using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FT-IR), powder X-ray diffractometer (PXRD), solubility, in vitro dissolution, and ex vivo permeation studies. The physico-chemical evaluation suggested the formation of the solid dispersion. Optimized HTZ-EWP SD4 drastically enhanced (~32-fold) aqueous solubility (~16.12 ± 0.08 mg/mL) over to pure HTZ (~ 0.51 ± 0.03 mg/mL). The dissolution study in phosphate buffer media (pH 6.8) revealed that HTZ-EWP SD4 significantly enhanced the release rate of HTZ (~ 87 %) over to HTZ (~ 25 %). The permeation rate of HTZ from optimized HTZ-EWP SD4 was enhanced significantly (~ 84 %) compared to pure HTZ (~ 24 %). Optimized HTZ-EWP-SD4 enhanced the rate of HTZ dissolution (~ 86 %) in FeSSIF (fed state simulated intestinal fluid), compared to a low dissolution rate (~ 72 %) in FaSSIF (fasted state simulated intestinal fluid) state after 2-h study. Obtained results conclude that lyophilized egg white protein can be utilized as an alternative solid dispersion carrier for enhancing the solubility and permeability of HTZ.


Asunto(s)
Diuréticos/administración & dosificación , Diuréticos/química , Portadores de Fármacos/química , Proteínas del Huevo/química , Hidroclorotiazida/administración & dosificación , Hidroclorotiazida/química , Disponibilidad Biológica , Tampones (Química) , Composición de Medicamentos , Liberación de Fármacos , Estabilidad de Medicamentos , Permeabilidad , Solubilidad , Agua
13.
Int J Nanomedicine ; 16: 1457-1472, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33654396

RESUMEN

Purpose: Rheumatoid arthritis is an autoimmune disorder that directly affects joints. However, other body organs including heart, eyes, skin, blood vessels and lungs may also be affected. The purpose of this study was to design and evaluate a nanoemulgel formulation of diflunisal (DIF) and solubility enhanced diflunisal (DIF-IC) for enhanced topical anti-inflammatory activity. Methodology: Nanoemulsion formulations of both DIF and DIF-IC were prepared and incorporated in three different gelling agents, namely carboxymethylcellulose sodium (CMC-Na), sodium alginate (Na-ALG) and xanthan gum (XG). All the formulations were evaluated in term of particle size, pH, conductivity, viscosity, zeta potential and in vitro drug release. The formulation 2 (NE2) of both DIF and DIF-IC which expressed optimum release and satisfactory physicochemical properties was incorporated with gelling agents to produce final nanoemulgel formulations. The optimized nanoemulgel formulation was subjected to three different in vivo anti-inflammatory models including carrageenan-induced paw edema model, histamine-induced paw edema model and formalin-induced paw edema model. Results: DIF-IC-loaded nanoemulgel formulations yielded significantly enhanced in vitro skin permeation than DIF-loaded nanoemulgel. The nanoemulgel formulation of DIF-IC formulated with XG produced improved in vivo anti-inflammatory activity. Conclusion: It was recommended that DIF-IC-based nanoemulgel formulation prepared with XG could be a better option for effective topical treatment of inflammatory conditions.


Asunto(s)
Diflunisal/administración & dosificación , Sistemas de Liberación de Medicamentos , Emulsiones/química , Nanogeles/química , Polietilenglicoles/química , Polietileneimina/química , Administración Tópica , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Carragenina , Diflunisal/química , Diflunisal/farmacología , Diflunisal/uso terapéutico , Modelos Animales de Enfermedad , Composición de Medicamentos , Liberación de Fármacos , Edema/tratamiento farmacológico , Edema/patología , Conductividad Eléctrica , Concentración de Iones de Hidrógeno , Masculino , Tamaño de la Partícula , Permeabilidad , Transición de Fase , Ratas , Piel/efectos de los fármacos , Absorción Cutánea/efectos de los fármacos , Solubilidad , Tensoactivos/química , Viscosidad
14.
Carbohydr Polym ; 260: 117835, 2021 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-33712172

RESUMEN

Bacterial breeding is the main cause of food perishability, which is harmful to human health. Silver nanoparticles (AgNPs) are one of the most widely used antimicrobial agents, but they are easy to release and cause cumulative toxicity. In this work, with corn stalk as green reductant and GO as template, a simple electrostatic self-assembled sandwich-like chitosan (CS) wrapped rGO@AgNPs nanocomposite film (CS/rGO@AgNPs) was synthesized to achieve stabilizing and controlled-release of AgNPs. The results showed that the the CS/rGO@AgNPs film continued releasing AgNPs for up to 14 days, and the final release amount of silver nanoparticles was only about 1.9 %. More importantly, the nanocomposite film showed durable antibacterial effect and good antibacterial activity against E. coli and S. aureus, and they showed no toxicity to cells. Hence, the nanocomposite film has potential application as an effective and safe packaging material to prolong the shelf life of food products.


Asunto(s)
Antibacterianos/química , Quitosano/química , Grafito/química , Nanopartículas del Metal/química , Nanocompuestos/química , Antibacterianos/farmacología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Materiales Biocompatibles Revestidos/química , Materiales Biocompatibles Revestidos/farmacología , Escherichia coli/efectos de los fármacos , Humanos , Nanocompuestos/toxicidad , Plata/química , Solubilidad , Staphylococcus aureus/efectos de los fármacos , Resistencia a la Tracción
15.
Food Chem ; 352: 129267, 2021 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-33691207

RESUMEN

In this study, a soluble complex formed between 0.5% (w/v) heated whey protein isolate (HWPI) and 5% (w/v) octenyl succinic anhydride (OSA)-modified starch at pH 4.5 was used to encapsulate ß-carotene for improving its solubility and stability. The apparent aqueous solubility of ß-carotene was increased markedly (264.05 ± 72.53 µg/mL) after encapsulation in the soluble complex. Transmission electron microscopy and scanning electron microscopy were used to evaluate the effect of the encapsulation of ß-carotene on the structure of the soluble complex. Fourier transform infrared spectroscopy showed that the characteristic peaks of ß-carotene disappeared in the soluble complex, suggesting that ß-carotene may have been encapsulated into the soluble complex via hydrophobic interactions. X-ray diffraction indicated that the ß-carotene was in an amorphous form within the soluble complex. An accelerated stability test showed that the soluble complex could effectively improve the chemical stability of ß-carotene during long-term storage under low pH conditions.


Asunto(s)
Almidón/análogos & derivados , Proteína de Suero de Leche/química , beta Caroteno/química , Cápsulas , Interacciones Hidrofóbicas e Hidrofílicas , Solubilidad , Almidón/química
16.
Carbohydr Polym ; 260: 117703, 2021 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-33712119

RESUMEN

Present research work was aimed at masking the bitter taste of anti- viral drug Oseltamivir phosphate (Ost) by complexing it with pea starch maltodextrin- Kleptose Linecaps® (Mld). The Ost groups involved in triggering the bitter sensation were identified by computationally assessing its interaction with human bitter taste receptor hTAS2R 38. A series of exhaustive molecular dynamics (MD) simulation was run using Schrodinger® suite to understand the type of interaction of Ost with Mld. Experimentally, complexes of Ost with Mld were realized by solution method. The complexes were characterized using differential scanning colorimetry (DSC), fourier transform-infrared spectroscopy (FT-IR), powder X-ray diffraction (PXRD), hot stage microscopy (HSM), scanning electron microscopy (SEM), proton NMR (1H-NMR) and Carbon-13 nuclear magnetic resonance (13C-NMR). Ost-oral dispersible mini tablets (ODMT) were prepared by direct compression and optimised using mixture designs. Finally, bitter taste perception of Ost-ODMT was evaluated in healthy human volunteers of either sex. Computational assessment, involving interaction of Ost with bitter receptor, predicted the involvement of free amino group of Ost in triggering the bitter response whereas, MD simulation predicted the formation of stable complex between Ost and double helical confirmation of Mld. Different characterization techniques confirmed the findings of MD simulation. Results from the taste assessment in human volunteers revealed a significant reduction in bitter taste of prepared Ost-ODMT.


Asunto(s)
Composición de Medicamentos , Oseltamivir/química , Polisacáridos/química , Agentes Aversivos/química , Agentes Aversivos/farmacología , Femenino , Humanos , Gripe Humana/tratamiento farmacológico , Masculino , Simulación de Dinámica Molecular , Oseltamivir/uso terapéutico , Solubilidad , Percepción del Gusto/efectos de los fármacos , Adulto Joven
17.
Carbohydr Polym ; 260: 117776, 2021 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-33712132

RESUMEN

Pearl millet (Pennisetum glaucum (L.) R.Br.) is a sustainable and underutilized starch source, constituting up to 70 % starch in its grain. Pearl millet could be used as a cheaper source of starch as compared to other cereals for developing functional foods. This review is mainly focused on isolation methods, and chemical composition of the pearl millet starch (PMS). Techno-functional characteristics such as; gelatinization, pasting properties, solubility, swelling power, and digestibility to infer wider application of the PMS critically highlighted in the review. Native starches have limited functionalitiesfor food applications due to the instability in developed pastes and gels. A number of modifications (physical, mechanical and enzymatic) have been developed to increase the functionality and to obtain desired characteristics of PMS thus improving its utilization in food applications. Further, the utilization of native as well as modified PMS is also discussed comprehensively. In addition, a number of recommendations to further improve its functionality and increase its application are also discussed.


Asunto(s)
Pennisetum/metabolismo , Almidón/química , Portadores de Fármacos/química , Embalaje de Alimentos , Geles/química , Peso Molecular , Nanopartículas/química , Solubilidad , Difracción de Rayos X
18.
Carbohydr Polym ; 260: 117778, 2021 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-33712134

RESUMEN

To deal with serious environmental damage resulting from plastic packaging materials, biodegradable films using natural products have gained considerable attention. Here, we provide a simple, fast, and environmentally-friendly route to construct a biodegradable film using chitosan (CS), bacterial cellulose (BC), and curcumin (Cur). Composite films (CSn-BC-Cur) using CS with different molecular weights were investigated, and their water moisture content (MC), water solubility (WS), contact angle (CA), mechanical properties, barrier properties, and antioxidant properties were compared. The obtained films were characterized by SEM, XRD, and TGA. The results showed that chitosan with a higher molecular weight presented higher contact angles and mechanical properties, along with a lower moisture content, water vapor transmission rate, and oxygen transmission rate. Furthermore, when the composite film was placed in 95 % ethanol, it released active substances. The results suggest that these composite films can be used as promising materials for food packaging.


Asunto(s)
Celulosa/química , Quitosano/química , Curcumina/química , Embalaje de Alimentos , Antioxidantes/química , Resistencia al Corte , Solubilidad , Temperatura , Agua/química
19.
Int J Mol Sci ; 22(4)2021 Feb 17.
Artículo en Inglés | MEDLINE | ID: mdl-33671465

RESUMEN

To change their behaviors, cells require actin proteins to assemble together into long polymers/filaments-and so a critical goal is to understand the factors that control this actin filament (F-actin) assembly and stability. We have identified a family of unusual actin regulators, the MICALs, which are flavoprotein monooxygenase/hydroxylase enzymes that associate with flavin adenine dinucleotide (FAD) and use the co-enzyme nicotinamide adenine dinucleotide phosphate (NADPH) in Redox reactions. F-actin is a specific substrate for these MICAL Redox enzymes, which oxidize specific amino acids within actin to destabilize actin filaments. Furthermore, this MICAL-catalyzed reaction is reversed by another family of Redox enzymes (SelR/MsrB enzymes)-thereby revealing a reversible Redox signaling process and biochemical mechanism regulating actin dynamics. Interestingly, in addition to the MICALs' Redox enzymatic portion through which MICALs covalently modify and affect actin, MICALs have multiple other domains. Less is known about the roles of these other MICAL domains. Here we provide approaches for obtaining high levels of recombinant protein for the Redox only portion of Mical and demonstrate its catalytic and F-actin disassembly activity. These results provide a ground state for future work aimed at defining the role of the other domains of Mical - including characterizing their effects on Mical's Redox enzymatic and F-actin disassembly activity.


Asunto(s)
Actinas/metabolismo , Drosophila melanogaster/enzimología , Pruebas de Enzimas , Oxigenasas de Función Mixta/química , Oxigenasas de Función Mixta/metabolismo , Animales , Biocatálisis , Chaperoninas/metabolismo , Frío , Oxidación-Reducción , Dominios Proteicos , Proteínas Recombinantes/aislamiento & purificación , Solubilidad
20.
AAPS PharmSciTech ; 22(3): 112, 2021 Mar 21.
Artículo en Inglés | MEDLINE | ID: mdl-33748914

RESUMEN

Telmisartan (TLM) is a potent antihypertensive drug with pH-dependent aqueous solubility. This work aimed to enhance the solubility and dissolution rate of TLM by the co-amorphous drug amino acid (AA) approach by combining TLM, with different types and ratios of AAs. The co-amorphous TLM-AA blends were prepared by freeze-drying and investigated for solid-state characteristics like the dissolution rate enhancement of TLM. Among the prepared co-amorphous formulations, TLM-arginine (ARG) exhibited the greatest enhancement in solubility with increasing the molar ratio of ARG. The TLM-ARG at 1:2 ratio showed about a 57-fold increase in solubility of TLM and the highest dissolution percentage in phosphate buffer (pH7.5) (100% in 20 minutes) compared to both crystalline TLM (20% in 60 min) and physical mixture. Powder XRD, DSC, FTIR analysis and SEM demonstrated the formation of amorphous form within the co-amorphous formulations. Only TLM:ARG (1:0.5) were stable at (40°C, 75% RH) for a minimum of 90 days. In conclusion, ARG was able to stabilize the amorphous form of TLM and enhances its aqueous solubility and dissolution. The 1:2 w/w ratio of TLM-ARG co-amorphous showed the best solubility and dissolution rate while the 1:0.5 w/w ratio showed the best stability.


Asunto(s)
Aminoácidos/química , Bloqueadores del Receptor Tipo 1 de Angiotensina II/administración & dosificación , Telmisartán/administración & dosificación , Bloqueadores del Receptor Tipo 1 de Angiotensina II/química , Tampones (Química) , Rastreo Diferencial de Calorimetría , Composición de Medicamentos , Liberación de Fármacos , Estabilidad de Medicamentos , Solubilidad , Telmisartán/química , Difracción de Rayos X
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