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1.
Ultrason Sonochem ; 109: 107012, 2024 Aug 02.
Artículo en Inglés | MEDLINE | ID: mdl-39098098

RESUMEN

Ultrasound-assisted extraction (UAE) was evaluated as a green procedure to produce faba beans protein isolates from faba beans. Magnetic stirring was performed as conventional extraction. A three-level five-factor Box-Behnken Design (BBD) was applied to obtain the optimal UAE conditions to concurrently maximize extraction yield and protein content. The response surface methodology (RSM) showed a quadratic curvature for extraction yield and protein. The optimal extraction conditions were determined as: Power of 123 W, solute/solvent ratio of 0.06 (1:15 g/mL), sonication time of 41 min, and total volume of 623 mL with a desirability value of 0.82. Under these conditions, the extraction yield of 19. 75 ± 0.87 % (Protein yield of 67.84 %) and protein content of 92.87 ± 0.53 % were obtained for optimum ultrasound extraction. Control samples using magnetic stirring under similar conditions without ultrasound treatment showed an extraction yield of 16.41 ± 0.02 % (Protein yield of 54.65 %) and a protein content of 89. 88 ± 0.40 %. This shows that BBD can effectively be used to optimize the extraction of proteins from faba beans using optimal extraction conditions, resulting in a higher extraction yield and protein purity.

2.
Artículo en Inglés | MEDLINE | ID: mdl-39099216

RESUMEN

BACKGROUND: Unpredictable situations such as clotting of blood, deep vein thrombosis, and pulmonary embolism arise in the body, which is the leading cause of mortality. Such conditions generally arise after surgery as well as after treatment with oral anticoagulant agents. Apixaban is a novel oral anticoagulant widely recommended for the prevention and treatment of strokes and blood clots suffering from nonvalvular atrial fibrillation by suppressing factor Xa. Apixaban has a log P of 2.71 with poor solubility and reported maximum bioavailability of approximately 50%. OBJECTIVE: Hence, the current research mainly focused on the improvement of solubility, bioavailability, and therapeutic efficacy of Apixaban via solid lipid nanoparticles (SLN). METHODS: The SLN was developed using the hot-homogenization method using a high-pressure homogenizer. The drug-lipid compatibility study was assessed by the FTIR, and the thermal analysis was performed using differential scanning calorimetry (DSC). During the scrutiny of lipids, the highest solubility of Apixaban was estimated in the glyceryl monostearate, hence selected for the formulation. Moreover, the colloidal solution was stabilized by the polyethylene glycol 200. The Design of Expert software (Version 13, Stat-Ease) was implemented for the optimization analysis by considering the 3-independent factors and 2-dependent parameters. The Patents on the SLN are Indian 202321053691, U.S. Patent, 10,973,798B2, U.S. Patent, U.S. Patent 2021/0069121A1, U.S. Patent 2022/0151945A1. RESULTS: Box-Behnken design was applied along with ANOVA, which showed a p-value less than 0.05 for the dependent parameters such as particle size and entrapment efficiency (p-value: 0.0476 and 0.0379). The optimized batch F10 showed a particle size of 167.1 nm, -19.5 mV zeta potential, and an entrapment efficiency of 87.32%. The optimized batch F10 was lyophilized and analyzed by Scanning electron microscopy (SEM), which showed a particle size of 130 nm. The solid powder was filled into the capsule for oral delivery. CONCLUSION: The marked improvement in solubility and bioavailability was achieved with F10- loaded Apixaban via Solid lipid nanoparticles. Moreover, the sustained released profile also minimizes the unseen complications that occur due to the clotting of blood.

3.
Int J Biol Macromol ; : 134348, 2024 Jul 30.
Artículo en Inglés | MEDLINE | ID: mdl-39089557

RESUMEN

In this study, four adsorbents were developed: layered silicate magadiite material (mag), Hexadecyltrimethylammonium intercalated magadiite (HDTMA@mag), a cross-linked composite of sodium alginate and magadiite (ALG@mag) and a cross-linked composite of sodium alginate and HDTMA@magadiite (ALG@HDTMA@mag). The adsorbents were evaluated for their effectiveness in removing of Methylene Blue (MB) and Eriochrome Black T (EBT) dyes. The prepared adsorbents were characterized using SEM, XRD, FTIR, and potential zeta measurements. Kinetic modeling results indicated that both film diffusion and intraparticle diffusion are useful as rate-determining processes in adsorption for all adsorbents. For both dyes, the Langmuir isotherm model provided a good correlation with the adsorption equilibrium data. ANOVA analysis for the best adsorbent (ALG@HDTMA@mag beads) revealed that MB removal was significantly influenced by the positive individual effects of contact time and ALG@HDTMA@mag dose. However, the individual effect of MB concentration exhibited an antagonistic effect throughout the adsorption process. The optimal parameters for achieving an adsorption capacity of 118.54 mg/g were a dye concentration of 60 ppm, a contact period of 1800 min, and an ALG@HDTMA@mag dose of 50 mg.

4.
Food Chem ; 460(Pt 2): 140700, 2024 Jul 30.
Artículo en Inglés | MEDLINE | ID: mdl-39094337

RESUMEN

Faba beans, rich in protein and ideal for Swedish cultivation, are limited in food industry use due to anti-nutritional factors (ANFs) that hinder nutrient absorption. An extraction method was developed in our study to mitigate ANFs in faba beans, using aqueous alkaline methods and isoelectric precipitation with differential salt concentration. This method yielded 15.8 g of protein per 100 g of flour, with a protein concentration exceeding 83% of the total extract. It reduced ANFs like phytic acid (28.0%), lectins (87.5%), vicine (98.5%), and convicine (99.7%). Extraction conditions were optimized using response surface methodology, identifying pH 6, 2 h, and 20 °C as the most effective parameters, achieving an 86% reduction in phytic acid, closely matched the model's predictions (R2 = 0.945). This method effectively reduced ANFs, offering a sustainable approach for producing proteins suitable for diverse food products, including plant-based alternatives.

5.
Int J Biol Macromol ; 275(Pt 1): 133513, 2024 Jun 30.
Artículo en Inglés | MEDLINE | ID: mdl-38955292

RESUMEN

This research uses a novel TiO2@CSC.Alg composite sponge was created by encasing TiO2 nanoparticles in the natural polymers alginate and chitosan, resulting in a nanocomposite that is both ecologically friendly and biocompatible. Using the generated nanocomposite as a new environmentally friendly adsorbent, As(V) heavy metal ions were effectively removed from aqueous media. The following techniques were used to analyse the physicochemical properties of the obtained materials: pHZPC, FTIR, XRD, BET, SEM, and XPS. Utilizing nitrogen adsorption/desorption isotherms, the TiO2@CSC.Alg composite sponge's textural properties were identified. This revealed a BET surface area of 168.42 m2/g and a total pore volume of 1.18 cc/g, indicating its porous nature and potential for high adsorption capacity. Examine the effects of temperature, pH, dose, and beginning concentration on adsorption. The adsorption characteristics were determined based on equilibrium and adsorption kinetics measurements. The adsorption process was both pseudo-second-order (PSOE) and Langmuir isothermally fit. Chemisorption was the adsorption method since the adsorption energy was 25.45 kJ·mol-1. An endothermic and spontaneous adsorption process was indicated by more metal being absorbed as the temperature increased. The optimal conditions for adsorption were optimized via Box-Behnken design software to be pH of 5 in the solution, a dosage of 0.02 g of the TiO2@CSC.Alg composite sponge per 25 mL, and an arsenate (As(V)) solution the adsorption capacity was 202.27 mg/g are ideal for efficient adsorption. These parameters are critical in achieving the maximum adsorption capacity of the composite sponge for arsenate, which could be beneficial for water purification applications. Utilizing Design-Expert software's response surface methodology (RSM) and Box-Behnken design (BBD), the adsorption process was optimized with the fewest planned tests. After six successive cycles of adsorption and desorption, the adsorbent stability was confirmed by the adsorbent reusability test without any noticeable decrease in removal efficacy. Additionally, it displayed good efficiency, the same XRD and XPS data before and after reuse, and no change in chemical composition.

6.
Polymers (Basel) ; 16(14)2024 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-39065337

RESUMEN

Additive manufacturing (AM), particularly fused filament fabrication (FFF), has gained significant attention for its design flexibility and cost-effectiveness. This study focuses on optimizing FFF parameters that employ response surface methodology (RSM) to enhance the flexural performance of polyethylene terephthalate glycol (PETG) parts. Three essential parameters-layer height, print speed, and nozzle temperature-were varied, and their effects on flexural strength, flexural modulus, flexural toughness for ultimate strength, flexural toughness at 5% strain, and strain at ultimate strength were evaluated. Based on a Box-Behnken design, the experiments revealed significant effects of these parameters on the mechanical responses. The analysis of variance (ANOVA) indicates that layer height predominantly affects flexural modulus and toughness, while nozzle temperature significantly impacts flexural strength. The RSM models exhibited high accuracy, with R2 values exceeding 99%. Optimal parameter combinations yield remarkable improvements: flexural strength reached 39.55 MPa, flexural modulus peaked at 1344.60 MPa, flexural toughness for ultimate strength reached 218.22 J/mm3, flexural toughness at 5% strain reached 381.47 J/mm3, and strain at ultimate strength reached 3.50%. Validation experiments confirm the effectiveness of the optimization, with errors below 3.17%.

7.
Pharmaceutics ; 16(7)2024 Jul 04.
Artículo en Inglés | MEDLINE | ID: mdl-39065595

RESUMEN

The article aimed to formulate an MLX binary ethosome hydrogel for topical delivery to escalate MLX solubility, facilitate dermal permeation, avoid systemic adverse events, and compare the permeation flux and efficacy with the classical type. MLX ethosomes were prepared using the hot method according to the Box-Behnken experimental design. The formulation was implemented according to 16 design formulas with four center points. Independent variables were (soya lecithin, ethanol, and propylene glycol concentrations) and dependent variables (vesicle size, dispersity index, encapsulation efficiency, and zeta potential). The design suggested the optimized formula (MLX-Ethos-OF) with the highest desirability to perform the best responses formulated and validated. It demonstrates a 169 nm vesicle size, 0.2 dispersity index, 83.1 EE%, and -42.76 mV good zeta potential. MLX-Ethos-OF shows an amorphous form in PXRD and a high in vitro drug release of >90% over 7 h by diffusion and erosion mechanism. MLX-Ethos-OF hyaluronic acid hydrogel was fabricated and assessed. It shows an elegant physical appearance, shear thinning system rheological behavior, good spreadability, and skin-applicable pH value. The ex vivo permeation profile shows a flux rate of 70.45 µg/cm2/h over 12 h. The in vivo anti-inflammatory effect was 53.2% ± 1.3 over 5 h. compared with a 10.42 flux rate and 43% inflammatory inhibition of the classical ethosomal type. The conclusion is that binary ethosome is highly efficient for MLX local delivery rather than classical type.

8.
Colloids Surf B Biointerfaces ; 242: 114098, 2024 Jul 16.
Artículo en Inglés | MEDLINE | ID: mdl-39067191

RESUMEN

Despite the promising potential of Solanum plant glycoalkaloids in combating skin cancer, their clinical trials have been halted due to dose-dependent toxicity and poor water solubility. In this study, we present a rational approach to address these limitations and ensure colloidal stability of the nanoformulation over time by designing solid lipid-polymer hybrid nanoparticles (SLPH). Leveraging the biocompatible and cationic properties of polyaspartamides, we employed a new polyaspartamide derivative (P1) as a raw material for this class of nanostructures. Subsequently, we prepared SLPH through a one-step process involving hot-melt emulsification followed by ultrasonication. The physicochemical properties of the SLPH were thoroughly characterized using dynamic light scattering (DLS), ζ-potential analysis, nanoparticle tracking analysis (NTA), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), and transmission electron microscopy (TEM). The optimized formulation exhibited long-term stability over six months under low temperatures, maintaining a particle size around 200 nm, a polydispersity index (PdI) lower than 0.2, and a ζ-potential between +35-40 mV. Furthermore, we evaluated the cytotoxic effect of the SLPH against human cutaneous melanoma cells (SK-MEL-28) compared to human foreskin fibroblast cells (HFF-1). Encapsulation of glycoalkaloids into the nanoparticles (SLPH-GE) resulted in a two-fold greater selective cytotoxic profile for melanoma cells than glycoalkaloids-free (GE). The nanoparticles disrupted the stratum corneum barrier with a penetration depth of approximately 77 µm. These findings underscore the potential of the developed nanosystem as an effective glycoalkaloid carrier with suitable colloidal and biological properties for further studies in topical treatment strategies for cutaneous melanoma.

9.
Sci Rep ; 14(1): 17193, 2024 Jul 26.
Artículo en Inglés | MEDLINE | ID: mdl-39060299

RESUMEN

The presence of heavy metals and pollutant dyes can have detrimental effects on aquatic ecosystems and compromise aquatic aesthetics. This study investigates the use of unprocessed waste gem meerschaum powder as a new adsorbent in the removal of both Cu(II) and methylene blue (MB) from aqueous solutions to reduce water pollution. The structure of the waste powder was characterized by FT-IR, XRD, SEM and BET methods. Optimization of Cu(II) and MB dye removal was carried out using design of experiment technique. Under optimum conditions, remarkable removal efficiencies of 95.5% (± 3.7) for Cu(II) and 97.8% (± 0.4) for MB were achieved. The removal of Cu(II) followed the Freundlich isotherm model, while the removal of MB dye adhered to the Langmuir isotherm model. Both adsorption processes obeyed the pseudo-second-order kinetic model and occurred spontaneously. This innovative approach offers a promising solution to water pollution by highlighting the importance of sustainable and cost-effective waste use.

10.
Pharm Dev Technol ; 29(6): 639-647, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38980085

RESUMEN

Doxepin, a Class-I Biopharmaceutics Drug Disposition Classification System (BDDCS) drug, exhibits poor bioavailability due to extensive first-pass metabolism. This research focuses on enhancing the delivery of doxepin by formulating nanostructured lipid carriers (NLCs) through the utilization of the Box-Behnken Design methodology. These optimized NLCs are intended for intranasal administration, with the ultimate goal of improving nose-to-brain drug delivery. NLCs were formulated using a high-speed homogenization technique. The optimized batch had a small particle size (75.80 ± 5.48 nm, PDI = 0.286), high entrapment efficiency (94.10 ± 0.16%), and sustained ex vivo release (82.25 ± 4.61% at 24 h). Characterization studies confirmed the conversion of doxepin from a crystalline to an amorphous state with uniform distribution in the lipid matrix. In vivo pharmacokinetic studies in rats showed significantly higher doxepin concentration in the brain tissue (Cmax = 16.77 µg/g, tmax = 30 min) after intranasal administration compared to intravenous administration (Cmax = 2.53 µg/g, tmax = 6 h). High-drug targeting efficiency (DTE = 284.3%) and direct transport percentage (DTP = 64.8%) suggested direct penetration of NLCs in the brain via olfactory and trigeminal pathways. In conclusion, the study highlights the potential of NLCs to improve the bioavailability of doxepin through nose-to-brain delivery and thereby potentially enable the treatment of neurological disorders.


Asunto(s)
Administración Intranasal , Disponibilidad Biológica , Encéfalo , Doxepina , Portadores de Fármacos , Lípidos , Nanoestructuras , Animales , Doxepina/farmacocinética , Doxepina/administración & dosificación , Encéfalo/metabolismo , Lípidos/química , Portadores de Fármacos/química , Ratas , Masculino , Nanoestructuras/química , Tamaño de la Partícula , Sistemas de Liberación de Medicamentos/métodos , Ratas Sprague-Dawley , Liberación de Fármacos , Biofarmacia/métodos , Mucosa Nasal/metabolismo
11.
J Biomech ; 172: 112227, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-39004042

RESUMEN

Considering the high strength and excellent biocompatibility of low-nickel stainless steel, this paper focused on optimizing the design of a vascular stent made from this material using finite element analysis (FEA) combined with the response surface methodology (RSM). The aim is to achieve the desired compressive resistance for the stent while maintaining a thin stent wall thickness. The parameters of the stent's support unit width (H), strut width (W), and thickness (T) were selected as input parameters, while the output parameters obtained from FEA included the compressive load, the equivalent plastic strain (PEEQ), axial shortening rate, radial recoil rate, and metal coverage rate. The mathematical models of input parameters and output parameters were established by using the Box Behnken design (BBD) of RSM. The model equations were solved under constrained conditions, and the optimal structural parameters, namely H, W, and T, were finally determined as 0.770 mm, 0.100 mm, and 0.075 mm respectively. In this situation, the compression load of the stent reached the target value of 0.38 N/mm; the PEEQ resulting from the stent expansion was small; the axial shortening, radial recoil, and metal coverage index were all minimized within the required range.


Asunto(s)
Fuerza Compresiva , Análisis de Elementos Finitos , Acero Inoxidable , Stents , Humanos , Níquel , Estrés Mecánico , Diseño de Prótesis , Modelos Cardiovasculares , Ensayo de Materiales
12.
J Environ Manage ; 365: 121683, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-38963968

RESUMEN

Ammonia recovery from wastewater has positive environmental benefits, avoiding eutrophication and reducing production energy consumption, which is one of the most effective ways to manage nutrients in wastewater. Specifically, ammonia recovery by membrane distillation has been gradually adopted due to its excellent separation properties for volatile substances. However, the global optimization of direct contact membrane distillation (DCMD) operating parameters to maximize ammonia recovery efficiency (ARE) has not been attempted. In this work, three key operating factors affecting ammonia recovery, i.e., feed ammonia concentration, feed pH, and DCMD running time, were identified from eight factors, by a two-level Plackett-Burman Design (PBD). Subsequently, Box-Behnken design (BBD) under the response surface methodology (RSM) was used to model and optimize the significant operating parameters affecting the recovery of ammonia though DCMD identified by PBD and statistically verified by analysis of variance (ANOVA). Results showed that the model had a high coefficient of determination value (R2 = 0.99), and the interaction between NH4Cl concentration and feed pH had a significant effect on ARE. The optimal operating parameters of DCMD as follows: NH4Cl concentration of 0.46 g/L, feed pH of 10.6, DCMD running time of 11.3 h, and the maximum value of ARE was 98.46%. Under the optimized conditions, ARE reached up to 98.72%, which matched the predicted value and verified the validity and reliability of the model for the optimization of ammonia recovery by DCMD process.


Asunto(s)
Amoníaco , Destilación , Aguas Residuales , Amoníaco/química , Destilación/métodos , Aguas Residuales/química , Eliminación de Residuos Líquidos/métodos , Modelos Teóricos , Concentración de Iones de Hidrógeno , Membranas Artificiales
13.
Int J Biol Macromol ; 276(Pt 2): 133750, 2024 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-39019375

RESUMEN

In this study, O-quaternary ammonium chitosan (O-HTCC) containing bicationic antibacterial active groups was synthesized to develop an O-HTCC/PVA porous nanofibrous film to enhance antibacterial activity, leveraging surface modification and nano-porous structure design. Uniform and smooth nanofibrous structures (average diameter: 72-294 nm) were successfully obtained using a simple and feasible electrospinning method. A response surface model via Box-Behnken design (BBD) was used to clarify the interaction relationship between O-HTCC fiber diameter and three critical electrospinning parameters (O-HTCC concentration, applied voltage, feed flow rate), predicting that the minimum O-HTCC fiber diameter (174 nm) could be achieved with 7 wt% of O-HTCC concentration, 14 kV of voltage, and 0.11 mL/h of feed flow rate. Linear regression (R2 = 0.9736, Radj2 = 0.9716) and the Anderson Darling test demonstrated the excellent fit of the RSM-BBD model. Compared to N-HTCC/PVA nanofibrous film, the O-HTCC/PVA version showed increased growth inhibition and more effective antibacterial efficacies against Escherichia coli (E. coli) (~;86.34 %) and Staphylococcus aureus (S. aureus) (~;99.99 %). DSC revealed improved thermal stability with an increased melting temperature (238 °C) and endothermic enthalpy (157.7 J/g). This study holds potential for further development of antibacterial packaging to extend food shelf-life to reduce bacterial infection.

14.
Int J Biol Macromol ; 276(Pt 2): 133909, 2024 Jul 17.
Artículo en Inglés | MEDLINE | ID: mdl-39025186

RESUMEN

In this research, aluminum metal-organic framework encapsulated with poly (itaconic acid) grafted crosslinked chitosan composite sponge (Al-MOF@PIC) was prepared. SEM, FTIR, XPS, XRD, and BET techniques were employed to thoroughly characterize the synthesized material and establish its structure and characteristics. The study discovered that the Al-MOF@PIC is an efficient way to remove dyes, which constitute a significant number of contaminants in industrial wastewater. Subsequently the adsorption of methyl violet 2B (MV-2B) dye, the surface area, pore size, and pore volume of the adsorbent decreased from 1860.68 m2/g, 1.62 nm, and 1.52 cc/g to 1426.45 m2/g, 1.11 nm, and 0.92 cc/g, individually. This modification suggested that a portion of the MV-2B dye had been removed by adsorption over the adsorbent's pores. The excellent adsorption capacity of the material was further confirmed by batch adsorption tests, which displayed a maximum adsorption capability of 646.76 mg/g for the elimination of MV-2B dye. The high adsorption energy of 26.8 kJ/mol designates that chemisorption is primarily responsible for MV-2B dye adsorption against the sponge adsorbent. The Al-MOF@PIC composite sponge demonstrated exceptional reusability over six cycles, demonstrating its strength and durability. The Al-MOF@PIC composite sponge successfully removes MV-2B from water by pore filling, π-π stacking, hydrogen bonding, and electrostatic interactions, which are the key mechanisms behind the adsorption of the dye pollutant. Its potential for practical applications is further demonstrated using Box Behnken-design (BBD) to optimize the adsorption consequences.

15.
Int J Pharm ; 661: 124459, 2024 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-38996822

RESUMEN

Resveratrol (RSV) has powerful antioxidant activities. However, the bioavailability is still limited due to low solubility and transport issues. Nanocrystal technology has been introduced to address these issues; however, the bulky formulation of the nanocrystal process through nanosuspension faces a big challenge in terms of stability and scale-up ability. This work aimed to enhance the bioavailability of RSV through nanocrystal formulation incorporated into soluble mesoporous carriers for superior solid-state stability and feasibility. This formulation was designed and developed rationally through scientific justification in the nanocrystal formulation along with quality by design paradigm. Box-Behnken design was applied to determine the optimized formulation based on the particle size and distribution, drug loading, zeta potential, and supersaturation parameters. The nanocrystal was formed through evaporation of drug, polymer, and surfactant in the solvent incorporated into mesoporous material. The nanocrystal was evaluated by vibrational spectroscopy, thermal analyses, and SEM and TEM photographs, followed by crystallinity evaluation. The results indicated that the factors only affected the particle size variation, zeta potential, drug loading, and the time to reach the supersaturation peak level. The optimized formulation was achieved by 68 % desirability value, producing 133.3 ± 1.2 nm particle size and -24.6 mV zeta potential. The physical and chemical evaluation characterization indicated no interaction between RSV and carrier. In addition, there was no difference in crystallinity between the RSV nanocrystal and native RSV. Moreover, the RSV nanocrystal improved the bioavailability nearly twice compared to the RSV suspension.


Asunto(s)
Disponibilidad Biológica , Nanopartículas , Tamaño de la Partícula , Resveratrol , Solubilidad , Resveratrol/farmacocinética , Resveratrol/química , Resveratrol/administración & dosificación , Nanopartículas/química , Porosidad , Animales , Prueba de Estudio Conceptual , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Masculino , Composición de Medicamentos/métodos , Antioxidantes/farmacocinética , Antioxidantes/química , Antioxidantes/administración & dosificación , Química Farmacéutica/métodos , Tensoactivos/química , Ratas
16.
Nanomedicine (Lond) ; : 1-15, 2024 Jul 16.
Artículo en Inglés | MEDLINE | ID: mdl-39012199

RESUMEN

Aim: The study explores the synergistic potential of atorvastatin (ATR) and quercetin (QUER)- loaded solid lipid nanoparticles (SLN) in combating breast cancer. Materials & methods: SLNs were synthesized using a high-shear homogenization method and optimized using Box-Behnken design. The SLNs were characterized and evaluated for their in vitro anticancer activity. Results: The optimized SLN exhibited narrow size distribution (PDI = 0.338 ± 0.034), a particle size of 72.5 ± 6.5 nm, higher entrapment efficiency (<90%), sustained release and spherical surface particles. The in vitro cytotoxicity studies showed a significant reduction in IC50 values on MDA-MB-231 cell lines. Conclusion: We report a novel strategy of repurposing well-known drugs and encapsulating them into SLNs as a promising drug-delivery system against breast cancer.


[Box: see text].

17.
Lipids Health Dis ; 23(1): 214, 2024 Jul 09.
Artículo en Inglés | MEDLINE | ID: mdl-38982376

RESUMEN

Omega-3 polyunsaturated fatty acids (n-3 PUFAs), mainly including α-linolenic acid (ALA), eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA), possess antioxidant properties and play a crucial role in growth and development. However, the combined effects of ALA, EPA, and DHA at different concentrations have rarely been reported. This work explored the effects of EPA, ALA, and DHA on the viability and antioxidant capacity of mouse hepatocytes, with the objective of enhancing the antioxidant capacity. Within the appropriate concentration range, cell viability and the activity of glutathione S-transferase, superoxide dismutase, and catalase were increased, while the oxidation products of malondialdehyde and the level of intracellular reactive oxygen species were obviously reduced. Thus, oxidative stress was relieved, and cellular antioxidant levels were improved. Finally, response surface optimization was carried out for EPA, ALA, and DHA, and the model was established. The antioxidant capacity of the cells was highest at EPA, ALA, and DHA concentrations of 145.46, 405.05, and 551.52 µM, respectively. These findings lay the foundation for further exploration of the interactive mechanisms of n-3 PUFAs in the body, as well as their applications in nutraceutical food.


Asunto(s)
Antioxidantes , Supervivencia Celular , Ácidos Docosahexaenoicos , Ácido Eicosapentaenoico , Ácidos Grasos Omega-3 , Hepatocitos , Estrés Oxidativo , Especies Reactivas de Oxígeno , Superóxido Dismutasa , Animales , Ratones , Hepatocitos/metabolismo , Hepatocitos/efectos de los fármacos , Antioxidantes/farmacología , Antioxidantes/metabolismo , Estrés Oxidativo/efectos de los fármacos , Ácidos Grasos Omega-3/farmacología , Ácido Eicosapentaenoico/farmacología , Ácidos Docosahexaenoicos/farmacología , Especies Reactivas de Oxígeno/metabolismo , Supervivencia Celular/efectos de los fármacos , Superóxido Dismutasa/metabolismo , Catalasa/metabolismo , Malondialdehído/metabolismo , Ácido alfa-Linolénico/farmacología , Glutatión Transferasa/metabolismo
18.
Turk J Pharm Sci ; 21(3): 199-210, 2024 Jul 12.
Artículo en Inglés | MEDLINE | ID: mdl-38994813

RESUMEN

Objectives: Olmesartan medoxomil (OLM) is a low bioavailability antihypertensive drug. This study aimed to prepare and optimize an OLM niosomal gel and investigate drug permeation via a chicken buccal pouch. Materials and Methods: OLM-loaded niosome were prepared using a film hydration technique. The vesicle size, zeta potential, entrapment efficiency, and percentage cumulative drug release of niosome were evaluated. The niosomes were incorporated into a Carbopol 974P (1.5% w/v) gel, and the drug permeability of the niosomal gel was evaluated. The formulations of the niosomal gel were optimized using the Box-Behnken design. The optimized formulation was further characterized by transmission electron microscopy (TEM) and Fourier transform infrared radiation analysis. Results: The particle size and zeta potential of the optimized niosomal formulations were 296.4 nm and -38.4 mV, respectively. Based on TEM analysis, the niosomes were found to be spherical in shape. The permeability, flux, and permeability coefficient of the optimized niosomal gel were 0.507 mg/cm2, 0.083 mg/cm2 × hour, and 041 cm/hour, respectively. Histopathological evaluation revealed that the niosomal gel had better permeability than the OLM gel. Conclusion: Based on the results of the OLM niosomal gel, it can be concluded that the formulation can be beneficial in increasing bioavailability, resulting in better therapeutic efficacy.

19.
Environ Sci Pollut Res Int ; 31(32): 45441-45451, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38951392

RESUMEN

Bisphenol A diglycidyl ether (BADGE), a derivative of the well-known endocrine disruptor Bisphenol A (BPA), is a potential threat to long-term environmental health due to its prevalence as a micropollutant. This study addresses the previously unexplored area of BADGE toxicity and removal. We investigated, for the first time, the biodegradation potential of laccase isolated from Geobacillus thermophilic bacteria against BADGE. The laccase-mediated degradation process was optimized using a combination of response surface methodology (RSM) and machine learning models. Degradation of BADGE was analyzed by various techniques, including UV-Vis spectrophotometry, high-performance liquid chromatography (HPLC), Fourier transform infrared (FTIR) spectroscopy, and gas chromatography-mass spectrometry (GC-MS). Laccase from Geobacillus stearothermophilus strain MB600 achieved a degradation rate of 93.28% within 30 min, while laccase from Geobacillus thermoparafinivorans strain MB606 reached 94% degradation within 90 min. RSM analysis predicted the optimal degradation conditions to be 60 min reaction time, 80°C temperature, and pH 4.5. Furthermore, CB-Dock simulations revealed good binding interactions between laccase enzymes and BADGE, with an initial binding mode selected for a cavity size of 263 and a Vina score of -5.5, which confirmed the observed biodegradation potential of laccase. These findings highlight the biocatalytic potential of laccases derived from thermophilic Geobacillus strains, notably MB600, for enzymatic decontamination of BADGE-contaminated environments.


Asunto(s)
Compuestos de Bencidrilo , Biodegradación Ambiental , Geobacillus stearothermophilus , Geobacillus , Lacasa , Lacasa/metabolismo , Geobacillus stearothermophilus/enzimología , Geobacillus/enzimología , Compuestos de Bencidrilo/metabolismo , Fenoles/metabolismo , Compuestos Epoxi/metabolismo
20.
Molecules ; 29(13)2024 Jun 27.
Artículo en Inglés | MEDLINE | ID: mdl-38999001

RESUMEN

The root of Adenophora tetraphylla (Thunb.) Fisch. is a common Chinese materia medica and the polysaccharides which have been isolated from the plant are important active components for medicinal purposes. The objective of the current study was to optimize the extraction parameters and evaluate the glucose consumption activity for Adenophorae root polysaccharides (ARPs). The optimization of ARP extraction was evaluated with preliminary experiments and using response surface methodology (RSM). The conditions investigated were 35-45 °C extraction temperature, 20-30 (v/w) water-to-solid ratio, and 3-5 h extraction time. The antidiabetic effects of ARPs for the glucose consumption activity were evaluated in HepG2 cells. The statistical analyses of the experiments indicated that temperature, water-to-solid ratio, and extraction time significantly affected ARP yield (p < 0.01). The correlation analysis revealed that the experimental data were well-aligned with a quadratic polynomial model, as evidenced by the mathematical regression model's fit. The optimal conditions for maximum ARP yield were 45 °C extraction temperature and 28.47:1 (mL/g) water-to-solid ratio with a 4.60 h extraction time. Extracts from these conditions showed significant activity of promoting cell proliferation from 11.26% (p < 0.001) to 32.47% (p < 0.001) at a dose of 50 µg/mL to 800 µg/mL and increasing glucose consumption to 75.86% (p < 0.001) at 250 µg/mL on HepG2 cells. This study provides a sustainable alternative for the industry since it allowed simplified handling and a specific quantity of ARPs. Furthermore, ARPs might directly stimulate the glucose consumption in the liver and showed no cytotoxicity; therefore, ARPs probably could be taken as a potential natural source of antidiabetic materials.


Asunto(s)
Glucosa , Raíces de Plantas , Polisacáridos , Agua , Humanos , Células Hep G2 , Polisacáridos/farmacología , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Glucosa/metabolismo , Raíces de Plantas/química , Agua/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Solubilidad , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación
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