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1.
Int J Mol Sci ; 25(15)2024 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-39125974

RESUMO

There is currently a growing interest in health-promoting foods. The beneficial effects of food on human health are actively promoted by health professionals and nutritionists. This growing awareness is influencing the increasing range of functional foods and the pursuit of more innovative solutions. Recent research indicates that spherical nanoparticles have the potential to be used as functional biomaterials in the food industry, particularly for encapsulating hydrophobic natural phytochemicals. Techniques and systems based on micro- and nano-encapsulation are of great importance in the food and pharmaceutical industries. It is of paramount importance that encapsulation materials are safe for use in food. The aim of this study was to obtain micelles containing extracts from chokeberry fruit pomace using egg yolk powder (EYP) for emulsification (as a source of lecithin) and egg white powder (EWP) for stabilisation. The structural properties of the micelles in the resulting powders were characterised using Fourier transform infrared spectroscopy (FTIR). Scanning electron microscopy (SEM) analysis confirmed the presence of spherical micellar structures between 500 and 1000 nm in size. The water activity and water content of the obtained powders were determined, and the thermal (DSC) and antioxidant properties were investigated. The results indicated that the powder with the micellar structures had a higher stability compared to the powder obtained by simple mixing without the use of encapsulation techniques.


Assuntos
Antioxidantes , Clara de Ovo , Gema de Ovo , Frutas , Micelas , Extratos Vegetais , Extratos Vegetais/química , Gema de Ovo/química , Frutas/química , Clara de Ovo/química , Antioxidantes/química , Antioxidantes/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Nanopartículas/química , Fenômenos Químicos , Pós/química
2.
Zhongguo Zhong Yao Za Zhi ; 49(14): 3868-3877, 2024 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-39099360

RESUMO

The study investigated the effect of Compound Shougong Powder(CSGP) on the biological functions of triple-negative breast cancer(TNBC) cells and whether its mechanism of action was related to the epithelial-mesenchymal transition(EMT) signaling pathway. TNBC cells(MDA-MB-231 and BT-549) were treated with different concentrations of CSGP-containing serum. MTS assay was used to detect the effect of CSGP on the proliferation of TNBC cells. The EdU staining was used to detect the effect of CSGP on the proliferation of TNBC cells. Flow cytometry was used to examine the impact of CSGP on apoptosis of TNBC cells. Wound-healing and Transwell assays were used to evaluate the effects of different concentrations of CSGP on the migration and invasion capabilities of TNBC cells. RNA sequencing technology was utilized to elucidate its mechanism. Subsequently, qRT-PCR was performed to measure the mRNA expression levels of E-cadherin, N-cadherin, Slug, Snail, Vimentin, Twist, Zinc finger E-box-Binding homeobox 1(Zeb1), and Zinc finger E-box-Binding homeobox 2(Zeb2). Western blot was used to assess the protein expression levels of Slug, Vimentin, and E-cadherin. After intervention with CSGP, the proliferation of MDA-MB-231 and BT-549 cells significantly decreased, while the apoptosis rate markedly increased. The expression levels of the epithelial marker protein E-cadherin significantly increased, while the expression levels of the EMT-related transcription factors Slug and Vimentin showed a decrease. In conclusion, CSGP inhibits the EMT, thereby suppressing the malignant progression of TNBC.


Assuntos
Apoptose , Proliferação de Células , Medicamentos de Ervas Chinesas , Transição Epitelial-Mesenquimal , Neoplasias de Mama Triplo Negativas , Transição Epitelial-Mesenquimal/efeitos dos fármacos , Humanos , Neoplasias de Mama Triplo Negativas/tratamento farmacológico , Neoplasias de Mama Triplo Negativas/genética , Neoplasias de Mama Triplo Negativas/metabolismo , Neoplasias de Mama Triplo Negativas/patologia , Medicamentos de Ervas Chinesas/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Feminino , Apoptose/efeitos dos fármacos , Movimento Celular/efeitos dos fármacos , Pós/química , Caderinas/genética , Caderinas/metabolismo
3.
Biomacromolecules ; 25(7): 4177-4191, 2024 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-38866384

RESUMO

After RNAi was first discovered over 20 years ago, siRNA-based therapeutics are finally becoming reality. However, the delivery of siRNA has remained a challenge. In our previous research, we found that spermine-based poly(ß-amino ester)s are very promising for siRNA delivery. However, the role of hydrophobic modification in siRNA delivery of spermine-based poly(ß-amino ester)s is not fully understood yet. In the current work, we synthesized spermine-based poly(ß-amino ester)s with different percentages of oleylamine side chains, named P(SpOABAE). The chemical structures of the polymers were characterized by 1H NMR. The polymers showed efficient siRNA encapsulation determined by SYBR Gold assays. The hydrodynamic diameters of the P(SpOABAE) polyplexes from charge ratio N/P 1 to 20 were 30-100 nm except for aggregation phenomena observed at N/P 3. Morphology of the polyplexes was visualized by atomic force microscopy, and cellular uptake was determined by flow cytometry in H1299 cells, where all the polyplexes showed significantly higher cellular uptake than hyperbranched polyethylenimine (25 kDa). The most hydrophobic P(SpOABAE) polyplexes were able to achieve more than 90% GFP knockdown in H1299/eGFP cells. The fact that gene silencing efficacy increased with hydrophobicity but cellular uptake was affected by both charge and hydrophobic interactions highlights the importance of endosomal escape. For pulmonary administration and improved storage stability, the polyplexes were spray-dried. Results confirmed the maintained siRNA activity after storage for 3 months at room temperature, indicating potential for dry powder inhalation.


Assuntos
Interações Hidrofóbicas e Hidrofílicas , RNA Interferente Pequeno , Espermina , RNA Interferente Pequeno/química , RNA Interferente Pequeno/administração & dosagem , RNA Interferente Pequeno/farmacologia , Espermina/química , Humanos , Administração por Inalação , Polímeros/química , Pós/química , Linhagem Celular Tumoral
4.
Int J Pharm ; 657: 124190, 2024 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-38701910

RESUMO

Lubricants are essential for most tablet formulations as they assist powder flow, prevent adhesion to tableting tools and facilitate tablet ejection. Magnesium stearate (MgSt) is an effective lubricant but may compromise tablet strength and disintegratability. In the design of orodispersible tablets, tablet strength and disintegratability are critical attributes of the dosage form. Hence, this study aimed to conduct an in-depth comparative study of MgSt with alternative lubricants, namely sodium lauryl sulphate (SLS), stearic acid (SA) and hydrogenated castor oil (HCO), for their effects on the tableting process as well as tablet properties. Powder blends were prepared with lactose, sodium starch glycolate or crospovidone as the disintegrant, and a lubricant at different concentrations. Angle of repose was determined for the mixtures. Comparative evaluation was carried out based on the ejection force, tensile strength, liquid penetration and disintegratability of the tablets produced. As the lubricant concentration increased, powder flow and tablet ejection improved. The lubrication efficiency generally decreased as follows: MgSt > HCO > SA > SLS. Despite its superior lubrication efficacy, MgSt is the only lubricant of four evaluated that reduced tablet tensile strength. Tablet disintegration time was strongly determined by tensile strength and liquid penetration, which were in turn affected by the lubricant type and concentration. All the above factors should be taken into consideration when deciding the type and concentration of lubricant for an orodispersible tablet formulation.


Assuntos
Excipientes , Lubrificantes , Ácidos Esteáricos , Comprimidos , Resistência à Tração , Lubrificantes/química , Ácidos Esteáricos/química , Excipientes/química , Composição de Medicamentos/métodos , Pós/química , Dodecilsulfato de Sódio/química , Óleo de Rícino/química , Povidona/química , Amido/química , Amido/análogos & derivados , Lactose/química , Administração Oral , Solubilidade , Química Farmacêutica/métodos
5.
Food Chem ; 453: 139539, 2024 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-38788638

RESUMO

The aim of this study was to investigate the effects of dietary Allium mongolicum Regel powder (AMRP) supplementation on the growth performance, meat quality, antioxidant capacity and muscle fibre characteristics of fattening Angus calves. Growth performance data and longissimus thoracis (LT) samples were collected from four groups of fattening Angus, which were fed either a basal diet (CON) or a basal diet supplemented with an AMRP dose of 10 (LAMR), 15 (MAMR), or 20 g/animal/day AMRP (HAMR) for 120 days before slaughter. AMRP addition to the feed improved growth performance and meat quality and altered muscle fibre type. Some responses to AMRP supplementation were dose dependent, whereas others were not. Together, the results of this study demonstrated that dietary supplementation with 10 g/animal/day AMRP was the optimal dose in terms of fattening calf growth performance, while 20 g/animal/day AMRP supplementation was the optimal dose in terms of meat quality.


Assuntos
Ração Animal , Antioxidantes , Suplementos Nutricionais , Carne , Animais , Bovinos/metabolismo , Bovinos/crescimento & desenvolvimento , Antioxidantes/metabolismo , Suplementos Nutricionais/análise , Ração Animal/análise , Carne/análise , Fibras Musculares Esqueléticas/metabolismo , Fibras Musculares Esqueléticas/efeitos dos fármacos , Pós/química , Masculino , Resposta ao Choque Térmico/efeitos dos fármacos , Allium/química , Allium/crescimento & desenvolvimento , Allium/metabolismo , Temperatura Alta
6.
Chem Res Toxicol ; 37(6): 873-877, 2024 Jun 17.
Artigo em Inglês | MEDLINE | ID: mdl-38780306

RESUMO

Emerging evidence showing urothelial cancer in herbalists is linked to aristolochic acid (AA) exposure; however, the exposure pathway remains unclear. Here, we show that dermal contact and inhalation of fine powders of AA-containing herbs are significant occupational AA exposure pathways for herbalists. We initiated the study by quantifying the amount of AA in the AA-containing powder deposited on gloves and face masks worn by the operators of an AA-containing herb grinding machine. Then, we measured the kinetics of dermal absorption and dissolution of AA from fine powders of AA-containing herbs into artificial sweat and surrogate lung fluid. Lastly, we quantified the mutagenic AA-DNA adduct levels formed in the kidneys of mice exposed to AA-containing fine powders through dermal contact. Our findings highlight an urgent occupational risk that should demand implementation of safety standards for herbalists exposed to AA-containing fine powders.


Assuntos
Ácidos Aristolóquicos , Exposição Ocupacional , Pós , Ácidos Aristolóquicos/análise , Exposição Ocupacional/efeitos adversos , Pós/química , Animais , Humanos , Camundongos , Adutos de DNA/análise , Exposição por Inalação/efeitos adversos , Urotélio/efeitos dos fármacos , Urotélio/patologia , Profissionais de Medicina Tradicional
7.
Food Chem ; 449: 139233, 2024 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-38593725

RESUMO

This investigation was focused on the impact of cold plasma (CP) on the extraction of curcumin and bioactive compounds of turmeric powder (TP). TP was treated with CP at different applied voltages (10, 20, and 30 kV), with various exposure times (10, 20, and 30 min). The curcumin content was highest at 30 kV for 10 min with a yield of 46.49 mg/g of TP. Total phenols significantly (p < 0.05) enhanced from 163.91 to 360.78 mg GAE/g DW accompanied by a remarkable 16% increment in total flavonoids, paralleled by a 26% increment in antioxidants as of control. Nuclear magnetic resonance spectra justified the extraction of curcuminoids. Moreover, micrographs displayed cell lysis in the treated powder. CP has exhibited a positive effect on surface colour parameters and thermal properties of TP. Overall, CP technology can be tailored for better curcumin extraction and the enhancement of phytochemicals.


Assuntos
Antioxidantes , Curcuma , Curcumina , Compostos Fitoquímicos , Extratos Vegetais , Gases em Plasma , Pós , Curcuma/química , Curcumina/química , Curcumina/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Gases em Plasma/química , Gases em Plasma/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Pós/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
8.
Int J Pharm ; 653: 123896, 2024 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-38346602

RESUMO

The therapeutic potential of pharmaceutical cocrystals in intranasal applications remains largely unexplored despite progressive advancements in cocrystal research. We present the application of spray freeze drying (SFD) in successful fabrication of a favipiravir-pyridinecarboxamide cocrystal nasal powder formulation for potential treatment of broad-spectrum antiviral infections. Preliminary screening via mechanochemistry revealed that favipiravir (FAV) can cocrystallize with isonicotinamide (INA), but not nicotinamide (NCT) and picolinamide (PIC) notwithstanding their structural similarity. The cocrystal formation was characterized by differential scanning calorimetry, Fourier-transform infrared spectroscopy, and unit cell determination through Rietveld refinement of powder X-ray analysis. FAV-INA crystalized in a monoclinic space group P21/c with a unit cell volume of 1223.54(3) Å3, accommodating one FAV molecule and one INA molecule in the asymmetric unit. The cocrystal was further reproduced as intranasal dry powders by SFD, of which the morphology, particle size, in vitro drug release, and nasal deposition were assessed. The non-porous flake shaped FAV-INA powders exhibited a mean particle size of 19.79 ± 2.61 µm, rendering its suitability for intranasal delivery. Compared with raw FAV, FAV-INA displayed a 3-fold higher cumulative fraction of drug permeated in Franz diffusion cells at 45 min (p = 0.001). Dose fraction of FAV-INA deposited in the nasal fraction of a customized 3D-printed nasal cast reached over 80 %, whereas the fine particle fraction remained below 6 % at a flow rate of 15 L/min, suggesting high nasal deposition whilst minimal lung deposition. FAV-INA was safe in RPMI 2650 nasal and SH-SY5Y neuroblastoma cells without any in vitro cytotoxicity observed. This study demonstrated that combining the merits of cocrystallization and particle engineering via SFD can propel the development of advanced dry powder formulations for intranasal drug delivery.


Assuntos
Amidas , Química Farmacêutica , Neuroblastoma , Pirazinas , Humanos , Química Farmacêutica/métodos , Pós/química , Liofilização/métodos , Tamanho da Partícula , Inaladores de Pó Seco , Administração por Inalação , Aerossóis
9.
Biometals ; 37(4): 859-875, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38267777

RESUMO

The processed forms of milk, branded liquid, and power milk available in Dhaka city, the capital of Bangladesh, were investigated for essential and trace metal/metalloids regarding nutritional and human health risk aspects. For this, the potential nutritional contribution, estimated daily intake (EDI) and non-carcinogenic risk for six different life stages with male and female categories, as well as the carcinogenic risk for children and adults of both genders, were addressed. In total, 46 branded liquid and powder milk samples were considered for this analysis employing atomic absorption spectroscopy. The concentration of essential elements showed the trends of K > Ca > Na > Mg > Fe > Zn > Mn > Cu and K > Ca > Na > Mg > Fe > Cu > Mn > Zn for liquid and powder milk samples, respectively, but the potentially hazardous one showed the same trends (Cr > Pb > Hg > As > Cd) for both items. Except for Cr, Hg, and Fe, the elemental compositions of both milk categories differed considerably (< 0.05). Compared to the threshold values for milk samples (liquid and powder), Fe (19% and 27%), Mn (100% and 63%), Cu (0% and 23%), Zn (94% and 0%), Pb (25% and 13%), and Cr (0% and 3%) showed above the permissible limits. The nutrient input was the highest for Ca (27.2% and 18.7%), followed by Mg, K, and Na. The EDI of studied elements was within the daily permissible limit in both the milk category (except age group (≤ 3) and the female category). The non-carcinogenic risk assessment showed that the age groups ≤ 3 for liquid milk and ≤ 3 and 3 < X ≤ 14 with female categories for powder milk exceeded the threshold level (> 1) in the case of Cr, Cd, As, Zn, and Mn. The probable carcinogenic risks indicated an unacceptable risk level (< 1.00E-04) for the ingestion of Cr through powder milk samples for children in male and female categories. Finally, it believes that green cow farming practices and green milk processing technology, as well as continuous monitoring of toxic metals, can limit the ultimate risk worldwide.


Assuntos
Leite , Oligoelementos , Humanos , Bangladesh , Leite/química , Animais , Feminino , Masculino , Criança , Adulto , Oligoelementos/análise , Medição de Risco , Pré-Escolar , Metaloides/análise , Contaminação de Alimentos/análise , Adolescente , Lactente , Metais/análise , Adulto Jovem , Pós/química
10.
Int J Pharm ; 651: 123757, 2024 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-38160992

RESUMO

Extracellular vesicles (EVs) are endogenous vesicles that comprise a variety of submicron vesicular structures. Among these, exosomes have been widely investigated as delivery systems for small and large molecules. Herein, the thin-film freeze-drying technology was utilized to engineer aerosolizable dry powders of miR-335-laden induced EVs (iEV-335) generated in B cells for potential delivery into the lung to treat primary lung cancer and/or pulmonary metastases. The size distribution, structure, and morphology of iEV-335 were preserved after they were subjected to thin-film freeze-drying with the proper excipients. Importantly, iEV-335, in liquid or reconstituted from thin-film freeze-dried powders, were equally effective in downregulating SOX4 gene expression in LM2 human triple-negative mammary cancer cells. The iEV-335 dry powder compositions showed mass median aerodynamic diameters (MMAD) of around 1.2 µm with > 60 % of the emitted doses had an MMAD of ≤ 3 µm, indicating that the powders can potentially achieve efficient deposition within the alveolar region following oral inhalation, which is desirable for treatment of primary lung cancer and pulmonary metastases. Overall, it is concluded that it is feasible to apply thin-film freeze-drying to prepare aerosolizable dry powders of iEVs for pulmonary delivery.


Assuntos
Vesículas Extracelulares , Neoplasias Pulmonares , MicroRNAs , Humanos , Pós/química , Liofilização , Administração por Inalação , Tamanho da Partícula , Inaladores de Pó Seco , Aerossóis e Gotículas Respiratórios , Fatores de Transcrição SOXC
11.
Eur J Pharm Biopharm ; 193: 218-226, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37956785

RESUMO

In an ideal world, pharmaceutical drugs would have infinite shelf life, no susceptibility to degradation, chemical reactions or loss of efficacy. In reality, these processes occur, however, making it desirable to extend a drugs' shelf life. Nucleic acid-based drugs are most commonly stored as aqueous suspension where they are vulnerable to microbial growth and degradation processes. Drying procedures, such as lyophilization and spray drying, help to reduce the products' residual moisture while increasing the products' shelf life and stability. The present study was designed to evaluate 90 days of storage of spray-dried siRNA-lipid nanoparticles (LNPs) at 4 °C and 25 °C. An updated Onpattro® composition modified with a positively charged helper lipid was used as the LNP carrier system. In an attempt to further reduce the residual moisture of our previously reported formulations, all LNP samples were subjected to a secondary drying step in the spray drying tower for 20 min. The measurement of physicochemical properties of spray-dried and subsequently dried LNPs resulted in sizes of 180 nm, PDI values of 0.1-0.15 and zeta potentials of + 3 mV. Spray drying resulted in residual moisture levels of 3.6-4 % and was reduced by subsequent drying to 2.8-3.1 %. Aerodynamic properties after storage showed discrepancies depending on the storage conditions. MMADs remained at 2.8 µm when stored at 4 °C, whereas an increase to 5 µm at 25 °C was observed. Subsequent drying led to sizes of 3.6-3.8 µm, independent of the storage conditions. Spray-dried LNPs maintained bioactivity resulting in > 95 % protein downregulation and confirming the lack of cytotoxic effects in a lung adenocarcinoma cell line. Furthermore, the spray-dried and subsequently dried LNPs stored for 3 months at 4 °C and 25 °C achieved up to 50 % gene silencing of the house-keeping gene GAPDH after deposition on the mucus layer of Calu-3 cells. This study confirms the stability of spray-dried and subsequently dried LNPs over at least 90 days at 4 °C and 25 °C emphasizing the potential of dry powder inhalation of RNA-loaded LNPs as a therapy option for pulmonary diseases.


Assuntos
Dessecação , Nanopartículas , Administração por Inalação , Nanopartículas/química , RNA Interferente Pequeno , Pós/química
12.
Eur J Pharm Biopharm ; 189: 264-275, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37392870

RESUMO

Low oral absorption and extensive first pass metabolism of progesterone is reported for many oral formulations which warrants investigation into other routes of administration. It is the aim of this study to investigate the generation of inhaled formulations of progesterone though a spray drying approach with a focus on how spray drying impacts the physicochemical properties of progesterone. Formulations of progesterone with L-leucine and hydroxypropyl methylcellulose acetate succinate (HPMCAS) are reported to this aim. X-ray diffraction, spectroscopy and thermal analysis were used to characterise these formulations and confirmed that progesterone crystallises as the Form II polymorph during spray drying regardless of the solvent used. The resultant formulations showed higher aqueous solubility than progesterone Form I starting material and the addition of HPMCAS was shown to temporarily enable a supersaturated state. Thermal analysis was used to show that the Form II polymorph was sensitive to transformation to Form I during heating. The addition of L-leucine to the formulations reduced the temperature for the polymorphic transformation by âˆ¼ 10 °C. However, when HPMCAS was added to the formulation, the Form II polymorph was prevented from transforming to the Form I polymorph. Cascade impaction was used to determine the aerosol performance of the spray dried powders and showed promising lung deposition profiles (mass median aerodynamic diameter 5 µm) with significant variation depending on the organic solvent used and the ratio of organic to aqueous phase in the feedstock. However, further optimisation of formulations was required to direct more progesterone into the alveolar regions. The addition of HPMCAS was seen to increase the alveolar deposition and therefore formed a formulation with a lower fine particle fraction and mass median aerodynamic diameter. The most suitable formulation for inhalation was formed from a 50:50 acetone:water mixture and showed an ED, FPF and FPD of 81.7%, 44.5% and 7.3 mg respectively. Therefore, HPMCAS is suggested as a suitable excipient to increase solubility, prevent polymorphic transformation and improve inhalation properties of spray dried progesterone formulations. This study highlights the use of spray drying to form inhalable progesterone powders with higher solubility which may broaden the application of this medicine.


Assuntos
Excipientes , Progesterona , Pós/química , Leucina/química , Excipientes/química , Administração por Inalação , Aerossóis/química , Solventes , Tamanho da Partícula , Inaladores de Pó Seco/métodos
13.
J Mater Chem B ; 11(31): 7502-7513, 2023 08 09.
Artigo em Inglês | MEDLINE | ID: mdl-37458109

RESUMO

Magnetic bioactive glass-ceramic (MGC) powders with nominal compositions of (45 - x)SiO224.5CaO24.5Na2O6P2O5xFe2O3 (x = 2, 4, 6, 8, 10, and 15 wt%) have been synthesized by a sol-gel route by systematically substituting silicon dioxide with iron oxide in Hench's 45S5 glass composition. Powder X-ray diffraction studies revealed a variation in the percentage of combeite (Ca2Na2Si3O9), magnetite (Fe3O4), and hematite (Fe2O3) nanocrystalline phases in MGC powders as a function of composition. Zeta potential measurements showed that MGC containing up to 10 wt% iron oxide formed stable suspensions. The saturation magnetization and heat generation capacity of MGC fluids increased with an increase in iron oxide content. Degradation of MGC powders was investigated in phosphate buffered saline (PBS). The in vitro bioactivity of the MGC powders taken in pellet form was confirmed by observing the pH variation as well as hydroxyapatite layer (HAp) formation upon soaking in modified simulated body fluid. These studies showed a decrement in the overall bioactivity in samples with high iron oxide content due to the proportional decrease in the silanol group. Monitoring the proliferation of MG-63 osteoblast cells in Dulbecco's Modified Eagle Medium (DMEM) revealed that MGC with up to 10 wt% iron oxide exhibited acceptable viability. The systematic study revealed that the MGC with 10 wt% iron oxide exhibited optimal cell viability, magnetic properties and induction heating capacity, which were better than those of FluidMag-CT, which is used for hyperthermia treatment.


Assuntos
Cerâmica , Durapatita , Pós/química , Durapatita/química , Cerâmica/química
14.
Biomater Adv ; 153: 213525, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37352744

RESUMO

The upsurge of bacterial resistance to conventional antibiotics turned a well-recognized public health threat. The need of developing new biomaterials of effective practical use in order to tackle bacterial resistance became urgent. In this study, a submicrometric bioparticle of known antibacterial activity was produced in powder form with suitable texture and appealing characteristics for effective oral administration. Through complex coacervating a natural-source antimicrobial polypeptide with chitosan-N-arginine and alginate, the bioactive polypeptide was physically incorporated to the bioparticle whose structure positively responds to the pH variations found in gastrointestinal tract. The powder formulation presented high palatability that was evaluated using fish as in vivo animal model. A thorough survey of the fish intestinal tissues, following a systematic oral administration, revealed high penetration potential of the biomaterial through epithelial cells and deeper intestine layers. Despite, no cytotoxic effect was observed in analyzing the tissues through different histology methods. The absence of intestinal damage was corroborated by immune histochemistry, being the integrity of epithelial motor myosin Vb and related traffic proteins preserved. Hematology further endorsed absence of toxicity in blood cells whose morphology was evaluated in detail. The study evidenced the applicability potential of a new biomaterial of appealing and safe oral administration of antibacterial polypeptide.


Assuntos
Antibacterianos , Peptídeos , Peptídeos/química , Peptídeos/farmacologia , Antibacterianos/química , Antibacterianos/farmacologia , Administração Oral , Pós/química , Peixes-Gato , Animais , Tamanho da Partícula , Concentração de Íons de Hidrogênio
15.
Int J Pharm ; 642: 123117, 2023 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-37315636

RESUMO

The past decades have witnessed tremendous expansion in utilization of plant-derived medicines as resveratrol (RES) in treating several diseases like idiopathic pulmonary fibrosis (IPF). RES can exhibit its role in treating IPF via its outstanding antioxidant and anti-inflammatory activities. The goal of this work was to formulate RES-loaded spray-dried composite microparticles (SDCMs) suitable for pulmonary delivery via dry powder inhaler (DPI). They were prepared by spray drying of a previously prepared RES-loaded bovine serum albumin nanoparticles (BSA NPs) dispersion using different carriers. RES-loaded BSA NPs, prepared by the desolvation technique, acquired suitable particle size of 177.67 ± 0.95 nm and entrapment efficiency of 98.7 ± 0.35% with perfectly uniform size distribution and high stability. Considering the attributes of the pulmonary route, NPs were co-spray dried with compatible carriers viz. mannitol, dextran, trehalose, leucine, glycine, aspartic acid, and glutamic acid to fabricate SDCMs. All formulations showed suitable mass median aerodynamic diameter<5 µm; that is suitable for deep lung deposition. However, the best aerosolization behavior was attained from using leucine with fine particle fraction (FPF) of 75.74%, followed by glycine with FPF of 54.7%. Finally, a pharmacodynamic study was conducted on bleomycin-induced mice, and it strongly revealed the role of the optimized formulations in alleviating PF through suppressing the levels of hydroxyproline, tumor necrosis factor-α and matrix metalloproteinase-9 with obvious improvements in the treated lung histopathology. These findings indicate that in addition to leucine, the glycine amino acid, which is not commonly used yet, is very promising in the formulation of DPIs.


Assuntos
Portadores de Fármacos , Fibrose Pulmonar Idiopática , Camundongos , Animais , Portadores de Fármacos/química , Resveratrol , Leucina/química , Administração por Inalação , Soroalbumina Bovina , Fibrose Pulmonar Idiopática/tratamento farmacológico , Tamanho da Partícula , Inaladores de Pó Seco , Pós/química , Aerossóis e Gotículas Respiratórios
16.
Eur J Pharm Biopharm ; 188: 243-253, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37224929

RESUMO

Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive, and often fatal lung disease caused by multiple factors. Currently, safe, and effective drugs for the treatment of IPF have been extremely scarce. Baicalin (BA) is used to treat pulmonary fibrosis, IPF, chronic obstructive pulmonary disease, and other lung diseases. Ambroxol hydrochloride (AH), a respiratory tract lubricant and expectorant, is often used to treat chronic respiratory diseases, such as bronchial asthma, emphysema, tuberculosis, and cough. The combination of BA and AH can relieve cough and phlegm, improve lung function, and potentially treat IPF and its symptoms. However, given the extremely low solubility of BA, its bioavailability for oral absorptions is also low. AH, on the other hand, has been associated with certain side effects, such as gastrointestinal tract and acute allergic reactions, which limit its applicability. Therefore, an efficient drug delivery system is urgently needed to address the mentioned problems. This study combined BA and AH as model drugs with L-leucine (L-leu) as the excipient to prepare BA/AH dry powder inhalations (BA/AH DPIs) using the co-spray drying method. We the performed modern pharmaceutical evaluation, which includes particle size, differential scanning calorimetry analysis, X-ray diffraction, scanning electron microscope, hygroscopicity, in vitro aerodynamic analysis, pharmacokinetics, and pharmacodynamics. Notably, BA/AH DPIs were found to be advantageous over BA and AH in treating IPF and had better efficacy in improving lung function than did the positive drug pirfenidone. The BA/AH DPI is a promising preparation for the treatment of IPF given its lung targeting, rapid efficacy, and high lung bioavailability.


Assuntos
Ambroxol , Fibrose Pulmonar Idiopática , Humanos , Pós/química , Tosse , Aerossóis e Gotículas Respiratórios , Administração por Inalação , Pulmão , Fibrose Pulmonar Idiopática/tratamento farmacológico , Inaladores de Pó Seco , Tamanho da Partícula
17.
Food Chem ; 419: 135989, 2023 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-37027977

RESUMO

This study aimed to explore the impacts of different anticaking agents on the moisture adsorption, caking, and flowability of silkworm pupae peptide powders (SPPP). The characteristics of water distributions in SPPP with anticaking agents were investigated by LF NMR. The morphological observation of powders was analyzed by scanning electron microscope. Moisture sorption curves and moisture sorption isotherm curves indicated that calcium stearate, silicon dioxide and calcium silicate of 20 % reduced hygroscopicity and increased critical relative humidity. The angle of repose analysis revealed that anticaking agents could also increase flowability (45°-49°). LF NMR analysis indicated that anticaking agents reduced the moisture adsorption ability of SPPP. Scanning electron microscope observations demonstrated different shapes and surface morphology of SPPP using different anticaking agents. Notably, silicon dioxide served as the most effective anticaking agent by forming a physical barrier. Overall, anticaking agents can effectively delay moisture adsorption and deliquescence of SPPP by different anticaking fashions.


Assuntos
Bombyx , Animais , Pós/química , Pupa , Adsorção , Dióxido de Silício , Peptídeos , Água/química , Tamanho da Partícula
18.
Int J Biol Macromol ; 238: 124340, 2023 May 31.
Artigo em Inglês | MEDLINE | ID: mdl-37028633

RESUMO

Bioactive compounds can be protected from degradation through encapsulation, increasing their bioavailability and shelf life. Spray drying is an advanced encapsulation technique mainly used for the processing of food-based bioactives. In this study, Box-Behnken design (BBD)-based response surface methodology (RSM) was used to study the effects of combined polysaccharide carrier agents and other spray drying parameters on encapsulating date fruit sugars obtained from a supercritical assisted aqueous extraction. The spray drying parameters were set at various levels: Air inlet temperature (150-170 °C), feed flow rate (3-5 mL/min), and carrier agent concentration (30-50 %). Under the optimized conditions (inlet temperature of 170 °C, the feed flow rate of 3 mL/min, and carrier agent concentration of 44 %), a maximum sugar powder yield of 38.62 % with 3.5 % moisture, 18.2 % hygroscopicity and 91.3 % solubility was obtained. The tapped density and particle density of the dried date sugar were estimated as 0.575 g cm-3 and 1.81 g cm-3, respectively, showing its potential for easy storage. In addition, scanning electron microscope (SEM) and X-ray diffraction (XRD) analysis revealed better microstructural stability of the fruit sugar product, which is essential for commercial applications. Thus, the hybrid carrier agent system (maltodextrin and gum arabic) can be considered a potential carrier agent for producing stable date sugar powder with longer shelf-life and desirable characteristics in the food industry.


Assuntos
Goma Arábica , Phoeniceae , Frutas , Goma Arábica/química , Extratos Vegetais , Polissacarídeos/química , Pós/química , Açúcares
19.
Food Res Int ; 168: 112783, 2023 06.
Artigo em Inglês | MEDLINE | ID: mdl-37120229

RESUMO

Jet milling is a common technique in ultrafine powder preparation field. It has never been used to design delivery systems. Cannabidiol (CBD) is an important cannabinoid of hemp but poor aqueous solubility limited its applications. In this study, solid dispersion (SD) technique was combined with cyclodextrin complexation technique, and jet milling was used for the first time to prepare SDs for improving CBD solubility. Different characterizations demonstrated that the dispersion effect and complexation structure of CBD SD3 prepared by jet milling were comparable to that of CBD SD2 prepared by spray drying (a common solution-based method), and were better than that of CBD SD1 prepared by cogrinding. The water solubility of CBD was increased to 20.902 µg/mL (909-fold) in CBD SD3. Besides, the antioxidant activity and cytotoxicity to tumor cells of CBD were enhanced by dispersion. This work indicated that jet milling, as a new technique with low cost and excellent applicability, could be further developed for the delivery of food functional factors or bioactive molecules.


Assuntos
Canabidiol , Canabidiol/química , Solubilidade , Água/química , Pós/química
20.
Pharm Res ; 40(5): 1073-1086, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36869245

RESUMO

INTRODUCTION: The emergence of multidrug-resistant (MDR) Mycobacterium tuberculosis (Mtb) posed a severe challenge to tuberculosis (TB) management. The treatment of MDR-TB involves second-line anti-TB agents, most of which are injectable and highly toxic. Previous metabolomics study of the Mtb membrane revealed that two antimicrobial peptides, D-LAK120-A and D-LAK120-HP13, can potentiate the efficacy of capreomycin against mycobacteria. AIMS: As both capreomycin and peptides are not orally available, this study aimed to formulate combined formulations of capreomycin and D-LAK peptides as inhalable dry powder by spray drying. METHODS AND RESULTS: A total of 16 formulations were prepared with different levels of drug content and capreomycin to peptide ratios. A good production yield of over 60% (w/w) was achieved in most formulations. The co-spray dried particles exhibited spherical shape with a smooth surface and contained low residual moisture of below 2%. Both capreomycin and D-LAK peptides were enriched at the surface of the particles. The aerosol performance of the formulations was evaluated with Next Generation Impactor (NGI) coupled with Breezhaler®. While no significant difference was observed in terms of emitted fraction (EF) and fine particle fraction (FPF) among the different formulations, lowering the flow rate from 90 L/min to 60 L/min could reduce the impaction at the throat and improve the FPF to over 50%. CONCLUSIONS: Overall, this study showed the feasibility of producing co-spray dried formulation of capreomycin and antimicrobial peptides for pulmonary delivery. Future study on their antibacterial effect is warranted.


Assuntos
Mycobacterium tuberculosis , Tuberculose Resistente a Múltiplos Medicamentos , Humanos , Capreomicina/química , Capreomicina/uso terapêutico , Pós/química , Peptídeos Antimicrobianos , Tuberculose Resistente a Múltiplos Medicamentos/tratamento farmacológico , Tuberculose Resistente a Múltiplos Medicamentos/microbiologia , Aerossóis/química , Peptídeos/farmacologia , Inaladores de Pó Seco/métodos , Tamanho da Partícula , Administração por Inalação
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