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1.
Mol Pharm ; 2024 Oct 08.
Artículo en Inglés | MEDLINE | ID: mdl-39378315

RESUMEN

This study aims to develop an innovative microencapsulation method for coated Polymyxin B, utilizing various polysaccharides such as hydroxypropyl ß-cyclodextrin, alginate, and chitosan, implemented through a three-fluid nozzle (3FN) spray drying process. High-performance liquid chromatography (HPLC) analysis revealed that formulations with a high ratio of sugar cage, hydroxypropyl ß-cyclodextrin (HPßCD), and sodium alginate (coded as ALGHCDHPLPM) resulted in a notable 16-fold increase in Polymyxin B recovery compared to chitosan microparticles. Morphological assessments using fluorescence labeling confirmed successful microparticle formation with core/shell structures. Alginate-based formulations exhibited distinct layers, while chitosan formulations showed uniform fluorescence throughout the microparticles. Focused beam reflectance and histograms from fluorescence microscopic measurements provided insights into physical size analysis, indicating consistent sizes of 6.8 ± 1.2 µm. Fourier-transform infrared (FTIR) spectra unveiled hydrogen bonding between Polymyxin B and other components within the microparticle structures. The drug release study showed sodium alginate's sustained release capability, reaching 26 ± 3% compared to 94 ± 3% from the free solution at the 24 h time point. Furthermore, the antimicrobial properties of the prepared microparticles against two Gram-negative bacteria, Escherichia coli and Pseudomonas aeruginosa, were investigated. The influence of various key excipients on the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values was evaluated. Results demonstrated effective bactericidal effects of ALGHCDHPLPM against both E. coli and P. aeruginosa. Additionally, the antibiofilm assay highlighted the potential efficacy of ALGHCDHPLPM against the biofilm viability of E. coli and P. aeruginosa, with concentrations ranging from 3.9 to 500 µg/m. This signifies a significant advancement in antimicrobial drug delivery systems, promising improved precision and efficacy in combating bacterial infections.

2.
Food Res Int ; 195: 114932, 2024 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-39277219

RESUMEN

Capsicum oleoresin has potential health benefits, particularly against obesity markers. Due to its high pungency, few studies have been done to explore the intake of this ingredient. The objective of this study was to use the Capsicum oleoresin (CO) microencapsulated into a high-fat diet to evaluate its metabolic effect on mice. Two formulation containing 15 % solids were prepared: the first (F1) with 5% CO and 95% emulsifier, and the second (F2) with 2.5% corn oil, 2.5% CO, and 95% emulsifier. These formulation were atomized in a spray dryer. Ultra-Performance Liquid Chromatography determined the capsaicin content for both formulations. Mice were divided into two groups: lean control (normocaloric AIN diet, n = 10) and high fat (HF diet: hypercaloric, n = 30), which were subdivided into three subgroups: HF control diet (n = 10); diet F1: HF + 20 % CO oleoresin microparticles (n = 10); and diet F2: HF + 20 % CO microparticles containing corn oil (n = 10). The animals treated with the microparticles showed lower glucose levels than the HF control. Mice fed with HF-containing CO microparticles had cholesterol blood levels similar to that of the lean group and lower (<100 mg/dL) than that of the HF control group (150 mg/dL). Capsicum oleoresin microparticles added to high-fat diets promoted lower weight gain and protected the liver against hepatic steatosis. Leptin levels for mice fed with HF diet plus CO microparticles averaged between 2 and 5 ng/ml, whereas the fat control group developed leptin resistance. Capsicum microparticles evidenced a protective effect against dyslipidemia compared to the fat control group, which suggests their use as a potential ingredient for the control of obesity.


Asunto(s)
Capsicum , Dieta Alta en Grasa , Obesidad , Extractos Vegetales , Animales , Capsicum/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Dieta Alta en Grasa/efectos adversos , Masculino , Ratones , Capsaicina/farmacología , Ratones Endogámicos C57BL , Hígado/metabolismo , Hígado/efectos de los fármacos , Enfermedades Metabólicas/prevención & control
3.
Foods ; 13(17)2024 Aug 26.
Artículo en Inglés | MEDLINE | ID: mdl-39272465

RESUMEN

This study developed functional white chocolate enriched with free (WC-F) and encapsulated ß-carotene using whey protein isolate (WPI) and pullulan (PUL) blends through spray drying (WC-SP), freeze drying (WC-LP), and coaxial electrospinning (WC-EL). The thermal properties, rheological properties, hardness, and color of the chocolates were evaluated, and the stability of ß-carotene was monitored over 4 months at 25 °C. No significant differences were found in melting profile temperatures among samples; however, WC-LP and WC-EL exhibited higher melting energies (30.88 J/g and 16.00 J/g) compared to the control (12.42 J/g). WC-F and WC-SP showed rheological behaviors similar to those of the control, while WC-LP and WC-EL displayed altered flow characteristics. Hardness was unaffected in WC-F and WC-SP (7.77 N/mm2 and 9.36 N/mm2), increased slightly in WC-LP (10.28 N/mm2), and decreased significantly in WC-EL (5.89 N/mm2). Over storage, melting point, rheological parameters, and hardness increased slightly, while color parameters decreased. ß-carotene degradation followed a first-order reaction model, with degradation rate constants (k) of 0.0066 day-1 for WC-SP, 0.0094 day-1 for WC-LP, and 0.0080 day-1 for WC-EL, compared to 0.0164 day-1 for WC-F. WC-SP provided the best ß-carotene retention, extending the half-life period by 2 times compared to WC-F (126.04 days vs. 61.95 days). Practical implications: The findings suggest that WC-SP, with its superior ß-carotene stability, is particularly suitable for the development of functional confectionery products with extended shelf life, offering potential benefits in industrial applications where product stability is crucial. Future research directions: Further studies could explore the incorporation of additional bioactive compounds in white chocolate using similar encapsulation methods, as well as consumer acceptance and sensory evaluation of these enriched products.

4.
Eur J Pharm Biopharm ; : 114507, 2024 Sep 18.
Artículo en Inglés | MEDLINE | ID: mdl-39303952

RESUMEN

Increasing resistance to antiviral drugs approved for the treatment of influenza urges the development of novel compounds. Ideally, this should be complemented by a careful consideration of the administration route. 6'siallyllactosamine-functionalized ß-cyclodextrin (CD-6'SLN) is a novel entry inhibitor that acts as a mimic of the primary attachment receptor of influenza, sialic acid. In this study, we aimed to develop a dry powder formulation of CD-6'SLN to assess its in vivo antiviral activity after administration via the pulmonary route. By means of spray drying the compound together with trileucine, a dispersion enhancer, we created a powder that retained the antiviral effect of the drug, remained stable under elevated temperature conditions and performed well in a dry powder inhaler. To test the efficacy of the dry powder drug against influenza infection in vivo, infected mice were treated with CD-6'SLN using an aerosol generator that allowed for the controlled administration of powder formulations to the lungs of mice. CD-6'SLN was effective in mitigating the course of the disease compared to the control groups, reflected by lower disease activity scores and by the prevention of virus-induced IL-6 production. Our data show that CD-6'SLN can be formulated as a stable dry powder that is suitable for use in a dry powder inhaler and is effective when administered via the pulmonary route to influenza-infected mice.

5.
Eur J Pharm Sci ; 202: 106891, 2024 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-39233259

RESUMEN

Pulmonary fibrosis, a disabling lung disease, results from the fibrotic transformation of lung tissue. This fibrotic transformation leads to a deterioration of lung capacity, resulting in significant respiratory distress and a reduction in overall quality of life. Currently, the frontline treatment of pulmonary fibrosis remains limited, focusing primarily on symptom relief and slowing disease progression. Bacterial infections with Pseudomonas aeruginosa are contributing to a severe progression of idiopathic pulmonary fibrosis. Phytic acid, a natural chelator of zinc, which is essential for the activation of metalloproteinase enzymes involved in pulmonary fibrosis, shows potential inhibition of LasB, a virulence factor in P. aeruginosa, and mammalian metalloproteases (MMPs). In addition, phytic acid has anti-inflammatory properties believed to result from its ability to capture free radicals, inhibit certain inflammatory enzymes and proteins, and reduce the production of inflammatory cytokines, key signaling molecules that promote inflammation. To achieve higher local concentrations in the deep lung, phytic acid was spray dried into an inhalable powder. Challenges due to its hygroscopic and low melting (25 °C) nature were mitigated by converting it to sodium phytate to improve crystallinity and powder characteristics. The addition of leucine improved aerodynamic properties and reduced agglomeration, while mannitol served as carrier matrix. Size variation was achieved by modifying process parameters and were evaluated by tools such as the Next Generation Impactor (NGI), light diffraction methods, and scanning electron microscopy (SEM). An inhibition assay for human MMP-1 (collagenase-1) and MMP-2 (gelatinase A) allowed estimation of the biological effect on tissue remodeling enzymes. The activity was also assessed with respect to inhibition of bacterial LasB. The formulated phytic acid demonstrated an IC50 of 109.7 µg/mL for LasB with viabilities > 80 % up to 188 µg/mL on A549 cells. Therefore, inhalation therapy with phytic acid-based powder shows promise as a treatment for early-stage Pseudomonas-induced pulmonary fibrosis.


Asunto(s)
Fibrosis Pulmonar , Zinc , Humanos , Zinc/administración & dosificación , Zinc/química , Fibrosis Pulmonar/tratamiento farmacológico , Administración por Inhalación , Ácido Fítico/química , Ácido Fítico/administración & dosificación , Ácido Fítico/farmacología , Pseudomonas aeruginosa/efectos de los fármacos , Secado por Pulverización , Proteínas Bacterianas , Polvos , Células A549 , Quelantes/administración & dosificación , Quelantes/farmacología , Quelantes/química , Tamaño de la Partícula , Metaloendopeptidasas
6.
Pharmaceuticals (Basel) ; 17(9)2024 Aug 31.
Artículo en Inglés | MEDLINE | ID: mdl-39338319

RESUMEN

Herein, we present an elegant and simple method for significant improvement of eugenol water solubility using the polymers Soluplus® and Lutrol F 127 as carriers and spray drying as an encapsulation method. The formulations were optimized by adding myo-inositol-a sweetening agent-and Aerosil® 200 (colloidal, fumed silica)-an anticaking agent. The highest encapsulation efficiency of 97.9-98.2% was found for the samples containing 5% eugenol with respect to the mass of Soluplus®. The encapsulation efficiencies of the spray-dried samples with 15% eugenol are around 90%. Although lowering the yield, the addition of Lutrol F 127 results in a more regular particle shape and enhanced powder flowability. The presence of Aerosil® 200 and myo-inositol also improves the rheological powder properties. The obtained formulations can be used in various dosage forms like powders, granules, capsules, creams, and gels.

7.
Pharmaceutics ; 16(9)2024 Aug 31.
Artículo en Inglés | MEDLINE | ID: mdl-39339194

RESUMEN

The pursuit of targeted therapies for cytokine-dependent diseases has led to the discovery of Janus kinase (JAK) inhibitors, a promising class of drugs. Among them, CPL409116, a selective dual JAK and rho-associated protein kinase inhibitor (ROCK), has demonstrated potential for treating conditions such as pulmonary fibrosis exacerbated by the COVID-19 pandemic. This study investigated the feasibility of delivering CPL409116 via inhalation, with the aim of minimizing the systemic adverse effects associated with oral administration. Two micronization methods, jet milling and spray drying, were assessed for CPL409116, with spray drying chosen for its ability to produce an amorphous form of the compound. Moreover, parameters such as the mixing energy, drug load, and force control agent significantly influenced the fine particle fraction (FPF), a critical parameter for pulmonary drug delivery. This study provides insights into optimizing the formulation parameters to enhance the delivery efficiency of CPL409116 to the lungs, offering potential for improved therapeutic outcomes in cytokine-dependent pulmonary diseases.

8.
Insects ; 15(9)2024 Sep 19.
Artículo en Inglés | MEDLINE | ID: mdl-39336684

RESUMEN

Research into mosquito-borne illnesses faces hurdles because feeding fresh animal blood to rear female mosquitoes presents logistical, economic, and safety challenges. In this study, a shelf-stable additive (spray-dried porcine blood; SDPB) hypothesized to supply accessible hemoglobin was evaluated within an alternative meal (AM) containing whey powder and PBS for rearing the yellow fever mosquito Aedes aegypti. LC-MS/MS proteomics, microbial assays, and particle reduction techniques confirmed and characterized the functionality of hemoglobin in SDPB, while engorgement, fecundity, egg viability, and meal stability bioassays assessed AM performance. Chemical assays supported hemoglobin as the phagostimulant in SDPB with aggregates partially solubilized in the AM that can be more accessible via particle reduction. Unpaired two-tailed t-tests indicate that the AM stimulates oogenesis (t11 = 13.6, p = 0.003) and is stable under ambient (1+ y; t12 = 0.576, p = 0.575) and aqueous (14 d; t12 = 0.515, p = 0.639) conditions without decreasing fecundity. Egg hatch rates for the ninth generation of AM-reared Ae. aegypti were 50-70+%. With further development, this meal may serve as a platform for mass rearing or studying effects of nutritional additives on mosquito fitness due to its low cost and stability. Future work may examine tuning spray drying parameters and resulting impacts on hemoglobin agglomeration and feeding.

9.
Int J Pharm ; 665: 124755, 2024 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-39321902

RESUMEN

Rifampicin (RIF) is commonly used in the treatment of tuberculosis (TB), a bacterium that currently infects one fourth of the world's population. Despite the effectiveness of RIF in treating TB, current RIF treatment regimens require frequent and prolonged dosing, leading to decreased patient compliance and, ultimately, increased mortality rates. This project aims to provide an alternative to oral RIF by means of an inhalable spray-dried formulation. TB uses alveolar macrophages to hide and replicate until the cells rupture, further spreading the bacteria. Therefore, delivering RIF directly to the lungs can increase the drug concentration at the site of infection while reducing off-site side effects. Cyclodextrin (CD) was used to create a RIF-CD inclusion complex to increase RIF solubility and biodegradable RIF-loaded NP (RIF NP) were developed to provide sustained release of RIF. RIF NP and RIF-CD inclusion complex were spray dried to form a dry powder nanocomposite microparticles (nCmP) formulation (RIF-CD nCmP). RIF-CD nCmP displayed appropriate aerosol dispersion characteristics for effective deposition in the alveolar region of the lungs (4.0 µm) with a fine particle fraction of 89 %. The nCmP provided both a burst release of RIF due to the RIF-CD complex and pH-sensitive release of RIF due to the RIF NP incorporated into the formulation. RIF-CD nCmP did not adversely affect lung epithelial cell viability and RIF NP were able to effectively redisperse from the nCmP after spray drying. These results suggest that RIF-CD nCmP can successfully deliver RIF to the site of TB infection while providing both immediate and sustained release of RIF. Overall, the RIF-CD nCmP formulation has the potential to improve the efficacy for the treatment of TB.


Asunto(s)
Aerosoles , Ciclodextrinas , Nanocompuestos , Rifampin , Rifampin/administración & dosificación , Rifampin/química , Nanocompuestos/química , Nanocompuestos/administración & dosificación , Administración por Inhalación , Humanos , Ciclodextrinas/química , Ciclodextrinas/administración & dosificación , Antibióticos Antituberculosos/administración & dosificación , Antibióticos Antituberculosos/química , Liberación de Fármacos , Solubilidad , Tamaño de la Partícula , Composición de Medicamentos , Enfermedades Pulmonares/tratamiento farmacológico , Secado por Pulverización , Pulmón/metabolismo , Pulmón/efectos de los fármacos , Animales , Polvos , Supervivencia Celular/efectos de los fármacos , Química Farmacéutica/métodos , Preparaciones de Acción Retardada/química
10.
ACS Appl Mater Interfaces ; 16(40): 54344-54358, 2024 Oct 09.
Artículo en Inglés | MEDLINE | ID: mdl-39325628

RESUMEN

Acute lung injury (ALI) is a severe inflammatory syndrome, which was caused by diverse factors. The COVID-19 pandemic has resulted in a higher mortality rate of these conditions. Currently, effective treatments are lacking. Although siRNA nucleotide-based drugs are promising therapeutic approaches, their poor stability and inability to efficiently reach target cells limit their clinical translation. This study identified a peptide from known cell-penetrating peptides that can form an efficient anti-inflammatory complex with TNF-α siRNA, termed SAR6EW/TNF-α siRNA. This complex can effectively transport TNF-α siRNA into the cytoplasm and achieve potent gene silencing in vitro as well as in vivo. By using lactose and triarginine as coexcipients and optimizing the spray-drying process, a powder was produced with micrometer-scale spherical and porous structures, enhancing aerosol release and lung delivery efficiency. The dry powder formulation and process preserve the stability and integrity of the siRNA. When administered intratracheally to ALI model mice, the complex powder demonstrated specific pulmonary gene silencing activity and significantly reduced inflammation symptoms caused by ALI, suggesting a potential strategy for the clinical therapeutic approach of respiratory diseases.


Asunto(s)
Lesión Pulmonar Aguda , COVID-19 , Nanopartículas , Polvos , ARN Interferente Pequeño , Factor de Necrosis Tumoral alfa , Lesión Pulmonar Aguda/tratamiento farmacológico , Lesión Pulmonar Aguda/terapia , Animales , ARN Interferente Pequeño/química , Ratones , Nanopartículas/química , Polvos/química , Humanos , Factor de Necrosis Tumoral alfa/metabolismo , Factor de Necrosis Tumoral alfa/genética , Transfección/métodos , Pulmón/patología , Pulmón/metabolismo , Silenciador del Gen/efectos de los fármacos , SARS-CoV-2 , Masculino , Péptidos de Penetración Celular/química
11.
J Pharm Sci ; 2024 Sep 19.
Artículo en Inglés | MEDLINE | ID: mdl-39306037

RESUMEN

This study investigates the compatibility of excipients with the model system SDI-X and their role in the induced crystallization of the amorphous compound-X in tablet formulations. We aimed to establish a straightforward and practical screening approach for evaluating excipient-induced crystallization of SDI in tablet matrices. Three methodologies-binary powder mixture, binary compact, and bilayer tablets-were employed to qualitatively and quantitatively evaluate the recrystallization of SDI-X with various excipients under accelerated storage conditions. The results demonstrated that binary compacts, providing direct physical contact between SDI-X and excipients, are superior in reflecting realistic drug-excipient contact within pharmaceutical tablets, enabling a more accurate assessment of excipient-induced crystallization for SDI-X. In contrast, the broadly used conventional binary blends can significantly underestimate this risk due to insufficient proximity. In addition, the bilayer tablets further confirmed that crystallization initiates at the contact surface between SDI-X and the excipients. The study highlighted that not only hygroscopicity but also the type of excipient and its physical contact with SDI-X significantly influence the recrystallization extent and rate of SDI-X. Interestingly, less hygroscopic diluents such as mannitol and lactose induced much higher levels of crystallization of SDIs, contrary to expectations based on moisture content alone. This suggests that the excipient type and contact surface are more critical in inducing recrystallization than just the level of moisture. The findings emphasize the need for careful excipient selection, study design, and sample preparation to enable appropriate assessments of SDI-excipient compatibility.

12.
J Food Sci ; 2024 Sep 26.
Artículo en Inglés | MEDLINE | ID: mdl-39327544

RESUMEN

Ginsenosides are the primary active substance in ginseng plants and have a variety of benefits. However, its light and heat stability are weak and easy to decompose. This study used gum arabic (GA) and maltodextrin (MD) as wall materials, and 1% Tween 80 was used as emulsifier. Response surface methodology was used to optimize the preparation process of total saponins in the stems-leaves of Panax notoginseng (SLPNs) (SSLP) microcapsules by spray drying and freeze drying techniques. Under optimal process conditions, the two microcapsules have better solubility and lower moisture content (MC). The color of spray-dried SSLP microcapsules was greener and bluer, and the color was brighter. In morphology, the spray-dried SSLP microcapsules were spherical with a slightly shrunk surface, whereas the freeze-dried ones were lamellar and porous. The two microcapsules have strong stability under different storage conditions and in vitro gastrointestinal digestion simulation. In addition, both microcapsules and free SSLP contained multiple ginsenosides. At the same time, both microcapsules had good free radical scavenging ability. These results indicate that the microencapsulation technology could improve the stability and bioavailability of SSLP, which is expected to provide a reference for the intensive processing of the SLPN. PRACTICAL APPLICATION: After microencapsulation, the stem and leaf extract of Panax notoginseng improved its stability and taste, which laid a foundation for making more nutritious and better tasting food of the stem and leaf of P. notoginseng.

13.
AAPS PharmSciTech ; 25(7): 221, 2024 Sep 24.
Artículo en Inglés | MEDLINE | ID: mdl-39317842

RESUMEN

This study aims to enhance the solubility of Olaparib, classified as biopharmaceutical classification system (BCS) class IV due to its low solubility and bioavailability using a solid self-nanoemulsifying drug delivery system (S-SNEDDS). For this purpose, SNEDDS formulations were created using Capmul MCM as the oil, Tween 80 as the surfactant, and PEG 400 as the co-surfactant. The SNEDDS formulation containing olaparib (OLS-352), selected as the optimal formulation, showed a mean droplet size of 87.0 ± 0.4 nm and drug content of 5.53 ± 0.09%. OLS-352 also demonstrated anticancer activity against commonly studied ovarian (SK-OV-3) and breast (MCF-7) cancer cell lines. Aerosil® 200 and polyvinylpyrrolidone (PVP) K30 were selected as solid carriers, and S-SNEDDS formulations were prepared using the spray drying method. The drug concentration in S-SNEDDS showed no significant changes (98.4 ± 0.30%, 25℃) with temperature fluctuations during the 4-week period, demonstrating improved storage stability compared to liquid SNEDDS (L-SNEDDS). Dissolution tests under simulated gastric and intestinal conditions revealed enhanced drug release profiles compared to those of the raw drug. Additionally, the S-SNEDDS formulation showed a fourfold greater absorption in the Caco-2 assay than the raw drug, suggesting that S-SNEDDS could improve the oral bioavailability of poorly soluble drugs like olaparib, thus enhancing therapeutic outcomes. Furthermore, this study holds significance in crafting a potent and cost-effective pharmaceutical formulation tailored for the oral delivery of poorly soluble drugs.


Asunto(s)
Disponibilidad Biológica , Sistemas de Liberación de Medicamentos , Emulsiones , Ftalazinas , Piperazinas , Solubilidad , Piperazinas/química , Piperazinas/administración & dosificación , Piperazinas/farmacocinética , Humanos , Ftalazinas/química , Ftalazinas/administración & dosificación , Ftalazinas/farmacocinética , Ftalazinas/farmacología , Emulsiones/química , Sistemas de Liberación de Medicamentos/métodos , Línea Celular Tumoral , Estabilidad de Medicamentos , Química Farmacéutica/métodos , Tamaño de la Partícula , Antineoplásicos/administración & dosificación , Antineoplásicos/farmacocinética , Antineoplásicos/química , Antineoplásicos/farmacología , Tensoactivos/química , Portadores de Fármacos/química , Polietilenglicoles/química , Células MCF-7 , Liberación de Fármacos , Nanopartículas/química , Composición de Medicamentos/métodos
14.
J Food Sci ; 2024 Sep 25.
Artículo en Inglés | MEDLINE | ID: mdl-39323284

RESUMEN

Pingyin rose is an edible flower rich in anthocyanins. In this study, antioxidant capacity and color were used as the main evaluation indexes to investigate the effects of common physical and chemical factors on the stability of rose anthocyanin extracts (RAEs). In addition, the physicochemical properties of the whey protein isolate (WPI)-RAEs complex after spray drying were studied. Vitamin C, temperature, and some metal ions can cause different degrees of discoloration of RAEs solution. More importantly, heat treatment, as well as most metal ions and sugars, had no significant effect on the antioxidant capacity of RAEs solution (p > 0.05). Moreover, compared to spray-dried pure WPI, the WPI-RAEs powder was delicate and uniform, and had higher particle size, bulk density, moisture activity, and better gel properties. The release rate of all WPI-RAEs sol/gel to RAEs reached about 89% in the intestinal digestion stage, but the WPI-RAEs interaction reduced the digestibility of protein in the intestinal digestion stage. We hope that this study can provide a theoretical basis for the development and utilization of WPI-RAEs as food ingredients.

15.
AAPS PharmSciTech ; 25(7): 220, 2024 Sep 23.
Artículo en Inglés | MEDLINE | ID: mdl-39313719

RESUMEN

Ketoconazole (K) is a poorly water-soluble drug that faces significant challenges in achieving therapeutic efficacy. This study aimed to enhance the dissolution rate of ketoconazole by depositing spray-dried ketoconazole (SK) onto the surface of ground trehalose dihydrate (T) using spray drying. Ketoconazole-trehalose surface solid dispersions (SKTs) were prepared in ratios of 1:1 (SK1T1), 1:4 (SK1T4), and 1:10 (SK1T10), and characterized them using particle size analysis, scanning electron microscopy, powder X-ray diffraction, and in vitro dissolution studies. Results showed that the dissolution rates of the dispersions were significantly higher than those of pure ketoconazole, with the 1:10 ratio showing the highest dissolution rate. The improved dissolution was attributed to the formation of a new crystalline phase and better dispersion of ketoconazole particles. These findings suggest that the surface solid dispersion approach could be a valuable method for enhancing the bioavailability of poorly water-soluble drugs.


Asunto(s)
Cetoconazol , Tamaño de la Partícula , Solubilidad , Trehalosa , Difracción de Rayos X , Cetoconazol/química , Cetoconazol/administración & dosificación , Trehalosa/química , Difracción de Rayos X/métodos , Microscopía Electrónica de Rastreo/métodos , Secado por Pulverización , Química Farmacéutica/métodos , Polvos/química , Disponibilidad Biológica , Composición de Medicamentos/métodos , Antifúngicos/química , Antifúngicos/administración & dosificación
16.
Food Chem ; 463(Pt 3): 141352, 2024 Sep 19.
Artículo en Inglés | MEDLINE | ID: mdl-39316903

RESUMEN

In this study, we investigated the protein structures, powder characteristics, as well as rehydration and emulsifying properties of spray-dried egg yolk powder after short-time lactic acid fermentation (3.5 h). Results indicate that fermentation improved the rehydration and emulsifying properties of yolk powder. Limosilactobacillus reuteri-fermented yolk powder exhibited better wettability due to the porous structure of particles and higher hydrophilicity. Lacticaseibacillus rhamnosus-fermented yolk powder had an enhanced coefficient of stability due to its smaller particles and higher surface charge. The higher water solubility of fermented yolk powder samples is mainly attributed to their lower hydrophobicity and higher zeta potential. The enhanced emulsifying activity of fermented yolk powder samples is primarily related to their increased ß-turn structure and better solubility. Furthermore, fermentation treatment altered powder moisture content and bulk densities, while not affecting its flow behavior and thermal stability. This study provides an effective approach to improving the quality of yolk powder.

17.
Entropy (Basel) ; 26(9)2024 Sep 23.
Artículo en Inglés | MEDLINE | ID: mdl-39330142

RESUMEN

Spray drying is an energy-intensive process in industrial use, making energy recovery a critical focus for improving overall efficiency. This study investigates the potential of integrating heat-recovery systems, including an innovative air reheater, into a closed-loop spray-drying unit to maximise energy savings. Through detailed pinch analysis, the system achieved a very low approach temperature, averaging 3.48 K, which is significantly lower than that of conventional open-loop systems. The study quantifies the energy-recovery potential by demonstrating that the integration of heat-recovery components can reduce the external heating demand by up to 30%. This not only enhances heat-transfer efficiency but also lowers operational costs and reduces the system's environmental impact. The results suggest that closed-loop systems with air reheaters offer a scalable solution for improving energy efficiency across different industrial applications. The research highlights a new paradigm: focusing on latent energy within the system rather than adjusting individual operational variables.

18.
Eur J Pharm Biopharm ; : 114512, 2024 Sep 25.
Artículo en Inglés | MEDLINE | ID: mdl-39332746

RESUMEN

The use of inhalable nanoparticulate-based systems in the treatment of lung cancer allows for efficient localized delivery to the lungs with less undesirable systemic exposure. For this to be attained, the inhaled particles should have optimum properties for deposition and at the same time avoid pulmonary clearance mechanisms. Drug delivery to solid tumors is furthermore challenging, due to dense extracellular matrix (ECM) formation, which hinders the penetration and diffusion of therapeutic agents. To this end, the aim of the current work is to develop an ECM-modulating nano-structured microparticulate carrier, that not only enables the delivery of therapeutic nanoparticles (NPs) to the lungs, but also enhances their intratumoral penetration. The system is composed of acetalated maltodextrin (AcMD) NPs embedded into a water-soluble trehalose/leucine matrix, in which collagenase was loaded with different mass concentrations (10 %, 30 % and 50 %). The collagenase-containing AcMD nano-structured microparticles (MPs) exhibited suitable median volume diameters (2.58 ±â€¯1.35 to 3.01 ±â€¯0.68 µm), hollow corrugated morphology, sufficient redispersibility, low residual moisture content (2.71 ±â€¯0.17 % to 3.10 ±â€¯0.20 %), and favorable aerodynamic properties (Mass median aerodynamic diameter (MMAD): 1.93 ±â€¯0.06 to 2.80 ±â€¯0.10 µm and fine particle fraction (FPF): 68.02 ±â€¯6.86 % to 69.62 ±â€¯2.01 %). Importantly, collagenase retained as high as 89.5 ±â€¯6.7 % of its enzymatic activity after spray drying. MPs containing 10 % mass content of collagenase did not show signs of cytotoxicity on either human lung adenocarcinoma A549 cells or lung MRC-5 fibroblasts. The nanoparticle penetration was tested using adenocarcinoma A549/MRC-5 co-culture spheroid model, where the inclusion of collagenase resulted in deeper penetration depth of AcMD-NPs.

19.
Food Sci Biotechnol ; 33(13): 2937-2951, 2024 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-39220307

RESUMEN

Micro- and nano-encapsulation techniques, such as microfluidization, spray drying, and centrifugal extrusion, have been widely utilized in various industries, including pharmaceuticals, food, cosmetics, and agriculture, to improve the stability, shelf life, and bioavailability of active ingredients, such as vitamin A. Emulsion-based delivery platforms offer feasible and appropriate alternatives for safeguarding, encapsulating, and transporting bioactive compounds. Therefore, there is a need to enrich our basic diet to prevent vitamin A deficiency within a population. This review focused on addressing vitamin A shortages, encapsulation techniques for improving the delivery of vital vitamins A and their food applications. Additionally, more studies are required to guarantee the security of nano-delivery strategies, as they proliferate in the food and beverage sector.

20.
Food Sci Biotechnol ; 33(12): 2777-2788, 2024 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-39184992

RESUMEN

Spray drying process was optimized for the development of probiotic finger millet milk powder. The independent parameters considered were inlet air temperature, maltodextrin content, and feed rate depending upon the preliminary trials. The major dependent quality parameters considered in the current work were moisture content, water activity, powder yield, encapsulation efficiency, and viability reduction. The desirability function was considered as a basis for the optimization of spray drying process. At the optimum process conditions of 151.68 °C of inlet air temperature, 100 mL/h of feed rate, and 29.32% of maltodextrin content, probiotic finger millet milk powder with 43.81% of powder yield and 84.97% of higher encapsulation efficiency could be achieved. The SEM analysis of the spray-dried powder confirmed the proper encapsulation of viable cells in the powder matrix. XRD analysis showed the amorphous powder structure suitable for other food applications. The promising results could be further utilized to produce non-dairy probiotic finger millet milk powder.

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