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Search Results (517)

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Keywords = dry powder particles

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16 pages, 931 KiB  
Article
Evaluation of the Effects of Drying Techniques on the Physical and Nutritional Characteristics of Cricket (Gryllus bimaculatus) Powder for Use as Animal Feedstuff
by Warin Puangsap, Padsakorn Pootthachaya, Mutyarsih Oryza, Anusorn Cherdthong, Vibuntita Chankitisakul, Bundit Tengjaroensakul, Pheeraphong Phaengphairee and Sawitree Wongtangtintharn
Insects 2025, 16(8), 814; https://doi.org/10.3390/insects16080814 - 6 Aug 2025
Abstract
This study aimed to evaluate the effects of three drying methods, namely sun drying, microwave–vacuum drying, and hot-air-oven drying, on the physical and nutritional properties of cricket powder for use in poultry feed. The results showed that the drying method significantly affected color [...] Read more.
This study aimed to evaluate the effects of three drying methods, namely sun drying, microwave–vacuum drying, and hot-air-oven drying, on the physical and nutritional properties of cricket powder for use in poultry feed. The results showed that the drying method significantly affected color parameters (L*, a*, and b*; p < 0.05), and particle size distribution at 850 µm and 250 µm (p = 0.04 and p = 0.02, respectively). Microwave–vacuum drying produced the lightest powder with a higher proportion of coarse particles, while sun drying resulted in a darker color and greater particle retention at 850 µm. Hot-air-oven drying yielded the lowest moisture content (1.99%) and the highest gross energy (6126.43 kcal/kg), with no significant differences observed in crude protein (p = 0.61), ether extract (p = 0.08), crude fiber (p = 0.14), ash (p = 0.22), or amino acid profiles (p > 0.05). These findings indicate that all drying methods preserved the nutritional value of cricket powder, and based on the overall results, hot-air-oven drying is the most suitable method for producing high-quality cricket meal with optimal physical properties and feed value, while also providing a practical balance between drying efficiency and cost. Full article
(This article belongs to the Section Role of Insects in Human Society)
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16 pages, 1265 KiB  
Article
Enhancing Stability of Boesenbergia rotunda Bioactive Compounds: Microencapsulation via Spray-Drying and Its Physicochemical Evaluation
by Fahmi Ilman Fahrudin, Suphat Phongthai and Pilairuk Intipunya
Foods 2025, 14(15), 2699; https://doi.org/10.3390/foods14152699 - 31 Jul 2025
Viewed by 249
Abstract
This study aimed to microencapsulate Boesenbergia rotunda (fingerroot) extract using maltodextrin (MD) and gum arabic (GA) as wall materials via spray-drying to improve powder physicochemical properties and protect bioactive compounds. MD and GA were employed as wall materials in varying ratios (MD:GA of [...] Read more.
This study aimed to microencapsulate Boesenbergia rotunda (fingerroot) extract using maltodextrin (MD) and gum arabic (GA) as wall materials via spray-drying to improve powder physicochemical properties and protect bioactive compounds. MD and GA were employed as wall materials in varying ratios (MD:GA of 1:0, 0:1, 1:1, 2:1, 1:2) to evaluate their effects on the physicochemical properties of the resulting microcapsules. Spray-dried microcapsules were evaluated for morphology, flowability, particle size distribution, moisture content, hygroscopicity, solubility, encapsulation efficiency, major bioactive compound retention, and thermal stability. The extract encapsulation using MD:GA at 1:1 ratio (MD1GA1) demonstrated a favorable balance, with high solubility (98.70%), low moisture content (8.69%), low hygroscopicity (5.08%), and uniform particle morphology, despite its moderate EE (75.06%). SEM images revealed spherical particles with fewer surface indentations in MD-rich formulations. Microencapsulation effectively retained pinostrobin and pinocembrin in all formulations with pinostrobin consistently retained at a higher value, indicating its higher stability. The balanced profile of physical and functional properties of fingerroot extract with MD1GA1 microcapsule makes it a promising candidate for food and nutraceutical applications. Full article
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16 pages, 4455 KiB  
Article
Durability and Microstructure Analysis of Loess-Based Composite Coal Gangue Porous Vegetation Concrete
by Manman Qiu, Wuyu Zhang, Shuaihua Ye, Xiaohui Li and Jingbang Li
Buildings 2025, 15(14), 2531; https://doi.org/10.3390/buildings15142531 - 18 Jul 2025
Viewed by 214
Abstract
In order to improve the durability of loess-based composite coal gangue porous planting concrete (LCPC), the effects of fly ash and slag powder content on the durability and microstructure of LCPC were studied. In this paper, fly ash and slag powder were mixed [...] Read more.
In order to improve the durability of loess-based composite coal gangue porous planting concrete (LCPC), the effects of fly ash and slag powder content on the durability and microstructure of LCPC were studied. In this paper, fly ash and slag powder were mixed into LCPC, and freeze-thaw cycle and dry-wet cycle tests were carried out. The compressive strength, dynamic elastic modulus, and mass change were used as evaluation indices to determine the optimal mix ratio for LCPC durability. Scanning electron microscopy (SEM) was performed, and the experimental design was carried out with the water–cement ratio, fly ash, and slag powder content as variables. The microstructure characteristics of LCPC were analyzed. The results show that the maximum number of freeze-thaw cycles can reach 35 times and the maximum number of dry-wet cycles can reach 50 when 5% fly ash and 20% slag powder are used. With an increase in the water-cement ratio, the skeleton of the loess gradually became complete, and its structure became more compact. In the micro-morphology diagram, the mixed fly ash and slag powder particles are not obvious, but with an increase in dosage, the size of the cracks and pores gradually decreases. The incorporation of fly ash and slag powder can play a positive role in the durability of LCPC and improvement of its microstructure. The results of this study are crucial for improving the application performance of ecological restoration, soil improvement, and long-term stability of structures, and can provide a scientific basis for the sustainable development of environmentally friendly building materials. Full article
(This article belongs to the Special Issue Soil–Structure Interactions for Civil Infrastructure)
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19 pages, 2622 KiB  
Article
Three-Compartment Pharmacokinetics of Inhaled and Injected Sinapine Thiocyanate Manifest Prolonged Retention and Its Therapeutics in Acute Lung Injury
by Zixin Li, Caifen Wang, Huipeng Xu, Qian Wu, Ningning Peng, Lu Zhang, Hui Wang, Li Wu, Zegeng Li, Qinjun Yang and Jiwen Zhang
Pharmaceutics 2025, 17(7), 909; https://doi.org/10.3390/pharmaceutics17070909 - 14 Jul 2025
Viewed by 411
Abstract
Background: Acute lung injury (ALI) is driven by inflammatory cascades and reactive oxygen species (ROS) generation, with the progression to severe cases markedly increasing mortality. Sinapine thiocyanate (ST), a bioactive natural compound isolated from Sinapis Semen Albae (SSA), demonstrates both anti-inflammatory and [...] Read more.
Background: Acute lung injury (ALI) is driven by inflammatory cascades and reactive oxygen species (ROS) generation, with the progression to severe cases markedly increasing mortality. Sinapine thiocyanate (ST), a bioactive natural compound isolated from Sinapis Semen Albae (SSA), demonstrates both anti-inflammatory and antioxidant pharmacological activities. However, no monotherapeutic formulation of ST has been developed to date. A dry powder inhaler (DPI) enables targeted pulmonary drug delivery with excellent stability profiles and high inhalation efficiency. Methods: ST was purified and prepared as inhalable dry powder particles via an antisolvent crystallization technique. The therapeutic mechanisms of ST against ALI were elucidated by network pharmacology and pharmacokinetic analyses, with the therapeutic efficacy of the ST DPI in ALI mitigation being validated using LPS-induced rat models. Results: The ST DPI showed ideal aerodynamic characteristics. Notably, ST exhibited a three-compartment (triexponential) pharmacokinetic profile following both intravenous tail vein injection and inhalation administration. Furthermore, the inhaled formulation displayed a prolonged systemic residence time, which confers therapeutic advantages for pulmonary disease management. Furthermore, the inhalation administration of ST demonstrated a 2.7-fold increase in AUC compared with oral gavage, with a corresponding enhancement in systemic exposure. The ST DPI formulation demonstrated significant therapeutic efficacy against ALI in rats by downregulating inflammatory cytokines and modulating oxidative stress levels, mechanistically achieved through the MAPK-mediated regulation of cellular apoptosis via a positive feedback loop. Conclusions: The unique triexponential plasma level profiles of an ST DPI provide a promising pharmacokinetics-based therapeutic strategy for ALI, leveraging its marked efficacy in attenuating inflammation, oxidative stress, and pulmonary injury. Full article
(This article belongs to the Section Pharmacokinetics and Pharmacodynamics)
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22 pages, 2427 KiB  
Article
Cyclodextrin-Based Quercetin Powders for Potential Nose-to-Brain Transport: Formulation and In Vitro Assessment
by Elmina-Marina Saitani, Paraskevi Papakyriakopoulou, Theodora Bogri, Georgia Choleva, Kyriaki Kontopoulou, Spyridon Roboras, Maria Samiou, Antiopi Vardaxi, Stergios Pispas, Georgia Valsami and Natassa Pippa
Molecules 2025, 30(13), 2878; https://doi.org/10.3390/molecules30132878 - 7 Jul 2025
Viewed by 482
Abstract
Quercetin (Que) is widely recognized for its antioxidant and neuroprotective properties; however, its clinical potential remains limited due to poor solubility and low oral bioavailability. Nasal powders have emerged as a promising strategy to overcome these limitations, taking advantage of nose-to-brain delivery, offering [...] Read more.
Quercetin (Que) is widely recognized for its antioxidant and neuroprotective properties; however, its clinical potential remains limited due to poor solubility and low oral bioavailability. Nasal powders have emerged as a promising strategy to overcome these limitations, taking advantage of nose-to-brain delivery, offering a direct, non-invasive route to the central nervous system while bypassing first-pass metabolism. This study aims to extend previous work by systematically investigating the impact of different preparation methods (spray drying vs. lyophilization) and the incorporation of hydroxypropyl methylcellulose (HPMC) and mannitol/lecithin microparticles (MLMPs) on the physicochemical characteristics, structural properties, and in vitro diffusion behavior of HPβCD-based nasal powder formulations of Que. Thermal behavior and stability were analyzed using TGA, while morphology and particle distribution were assessed via Scanning Electron Microscopy. In vitro diffusion studies using Franz cells and regenerated cellulose membranes were conducted under simulated nasal conditions. Among all tested formulations, the spray-dried HPβCD/Que powder (F4) showed the highest permeation (0.11 ± 0.01 mg/cm2 at 120 min). The inclusion of HPMC improved thermal stability but reduced Que diffusion, likely due to increased viscosity and matrix formation. Blending with MLMPs enhanced powder flow and dose placement, although it modestly reduced diffusion efficiency. Overall, this study highlights the potential of HPβCD-based spray-dried powders for nasal Que delivery and demonstrates how HPMC and MLMPs can be strategically employed to tailor performance characteristics. Full article
(This article belongs to the Section Macromolecular Chemistry)
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22 pages, 2559 KiB  
Article
Viability of Microencapsulated Probiotics in Cross-Linked Alginate Matrices and Chia Seed or Flaxseed Mucilage During Spray-Drying and Storage
by Mariela Bustamante, B. Dave Oomah, César Burgos-Díaz, Daniela Vergara, Liset Flores and Carolina Shene
Microorganisms 2025, 13(7), 1457; https://doi.org/10.3390/microorganisms13071457 - 23 Jun 2025
Cited by 1 | Viewed by 739
Abstract
Interest in probiotics has not diminished, and techniques to protect them from the environment in which they are found are constantly being innovated. Spray-drying is the most studied and industrially used technique to encapsulate probiotics. Recently, a new process has been developed in [...] Read more.
Interest in probiotics has not diminished, and techniques to protect them from the environment in which they are found are constantly being innovated. Spray-drying is the most studied and industrially used technique to encapsulate probiotics. Recently, a new process has been developed in which particle formation, alginate cross-linking, and drying are carried out in a single step. In this study, Bifidobacterium infantis, Bifidobacterium longum, Lactobacillus plantarum, and Lactobacillus rhamnosus were microencapsulated by spray-drying using a cross-linked alginate matrix supplemented with chia seed mucilage (CM) or flaxseed mucilage (FM) as the coating material. All formulations evaluated, supplemented with 0.4% (w/v) of CM or FM, including the control formulation showed high survival rates, varying between 87% and 97%. The viability of microencapsulated probiotics was affected by storage temperature. At 4 °C, viability decreased slightly, and after 90 days, the viable probiotic count ranged from 7 to 11 Log CFU/g of dry powder. Meanwhile, viability did not exceed 4 Log CFU/g of dry powder at 37 °C. Probiotic microencapsulation in cross-linked alginate matrices and chia or flaxseed mucilage by spray-drying is presented as a promising alternative for their protection, potentially improving the long-term stability and efficacy of the probiotic product. Full article
(This article belongs to the Section Food Microbiology)
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26 pages, 8375 KiB  
Article
Water-Soluble Formulations of Curcumin and Eugenol Produced by Spray Drying
by Iskra Z. Koleva, Katya Kamenova, Petar D. Petrov and Christo T. Tzachev
Pharmaceuticals 2025, 18(7), 944; https://doi.org/10.3390/ph18070944 - 23 Jun 2025
Viewed by 588
Abstract
Background/Objectives: In this study, we present a green, scalable platform for the production of water-dispersible powders co-encapsulating the lipophilic bioactives curcumin (Cur) and eugenol (Eug) within the amphiphilic polymer Soluplus® (SP) via low-temperature spray drying. Methods: The amount of Cur [...] Read more.
Background/Objectives: In this study, we present a green, scalable platform for the production of water-dispersible powders co-encapsulating the lipophilic bioactives curcumin (Cur) and eugenol (Eug) within the amphiphilic polymer Soluplus® (SP) via low-temperature spray drying. Methods: The amount of Cur (1%, 5%, and 10%) and Eug (5%, 10%, 15%, and 20%) was varied to achieve single- and double-loaded water-soluble powders with the maximum amount of active substances. The powders containing a higher loading of Cur, 5% and 10% (and Eug), were obtained from water/ethanol mixtures (2:1 and 5:1 v/v ratio), while the formulation with 1% of Cur was spray-dried by using water as a solvent. Results: By leveraging aqueous or aqueous–ethanolic feed systems, we achieved high loading of the bioactive substances—up to 10% Cur and 20% Eug (w/w)—while minimizing organic solvent use. Myo-inositol was incorporated as a stabilizing excipient to modulate particle morphology, improve powder flowability, and enhance redispersibility. Physicochemical characterization revealed nanoscale micellization (53–127 nm), amorphization of both actives as confirmed by XRD and DSC, and the absence of crystalline residue. Encapsulation efficiencies exceeded 95% for Cur and 93% for Eug. Dissolution tests demonstrated a rapid release from the 5% Cur/5% Eug formulation (>85% in 5 min), while higher-loaded single-formulations showed progressively slower release (up to 45 min). Conclusions: This work demonstrates a robust and environmentally responsible encapsulation strategy, suitable for delivering poorly water-soluble phytochemicals with potential applications in oral nutraceuticals and pharmaceutical dosage forms. Full article
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17 pages, 1201 KiB  
Article
Valorization of Spent Osmotic Solutions by Production of Powders by Spray Drying
by Katarzyna Samborska, Alicja Barańska-Dołomisiewicz, Aleksandra Jedlińska, Rui Costa, Konstantinos Klimantakis, Ioannis Mourtzinos and Małgorzata Nowacka
Appl. Sci. 2025, 15(12), 6927; https://doi.org/10.3390/app15126927 - 19 Jun 2025
Viewed by 364
Abstract
Spent osmotic solutions (sucrose, buckwheat honey, acacia honey, apple juice concentrate, chokeberry juice concentrate, cherry juice concentrate, and mannitol) were tested for their valorization to produce powders by spray drying. Simultaneously, the application of inulin as an alternative carrier was verified. The drying [...] Read more.
Spent osmotic solutions (sucrose, buckwheat honey, acacia honey, apple juice concentrate, chokeberry juice concentrate, cherry juice concentrate, and mannitol) were tested for their valorization to produce powders by spray drying. Simultaneously, the application of inulin as an alternative carrier was verified. The drying yield varied from 6 to 92%. For acacia honey, apple juice concentrate, chokeberry juice concentrate, and cherry juice concentrate, high stickiness was observed, which resulted in low yield and the production of significantly bigger particles of regular size distribution, higher hygroscopicity and bulk density, and better flowability. Sucrose, acacia honey, and mannitol were dried with lower stickiness, and the physical properties of the powders were acceptable. However, the yield of mannitol drying was low due to very small particles, low bulk density, and low cyclone efficiency. Therefore, sucrose and buckwheat honey solutions can be successfully spray dried using inulin as a carrier to produce powders suitable for further food applications. However, for the other tested materials, alternative carriers should be considered to reduce stickiness during drying. Full article
(This article belongs to the Special Issue Advances in Drying Technologies for Food Processing)
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17 pages, 3077 KiB  
Article
Development of Mannitol-Based Microparticles for Dry Powder Inhalers: Enhancing Pulmonary Delivery of NSAIDs
by Petra Party, Zsófia Ilona Piszman and Rita Ambrus
Pharmaceuticals 2025, 18(6), 923; https://doi.org/10.3390/ph18060923 - 19 Jun 2025
Viewed by 580
Abstract
Background/Objectives: Chronic lung diseases are among the leading causes of death worldwide. In the treatment of these diseases, non-steroidal anti-inflammatory drugs can be effective. We have previously developed an excipient formulation alongside a modern manufacturing protocol, which we aim to further investigate. We [...] Read more.
Background/Objectives: Chronic lung diseases are among the leading causes of death worldwide. In the treatment of these diseases, non-steroidal anti-inflammatory drugs can be effective. We have previously developed an excipient formulation alongside a modern manufacturing protocol, which we aim to further investigate. We have chosen two new model drugs, meloxicam (MX) and its water-soluble salt, meloxicam-potassium (MXP). The particles in dry powder inhaler (DPI) formulation were expected to have a spherical shape, fast drug release, and good aerodynamic properties. Methods: The excipients were poloxamer-188, mannitol, and leucine. The samples were prepared by spray drying, preceded by solution preparation and wet grinding. Particle size was determined by laser diffraction, shape by scanning electron microscopy (SEM), crystallinity by powder X-ray diffraction (PXRD), interactions by Fourier-transform infrared spectroscopy (FT-IR), in vitro drug dissolution by paddle apparatus, and in vitro aerodynamic properties by Andersen cascade impactor and Spraytec® device. Results: We achieved the proper particle size (<5 μm) and spherical shape according to laser diffraction and SEM. The XRPD showed partial amorphization. FT-IR revealed no interaction between the materials. During the in vitro dissolution tests, more than 90% of MX and MXP were released within the first 5 min. The best products exhibited an aerodynamic diameter of around 4 µm, a fine particle fraction around 50%, and an emitted fraction over 95%. The analysis by Spraytec® supported the suitability for lung targeting. Conclusions: The developed preparation process and excipient system can be applied in the development of different drugs containing DPIs. Full article
(This article belongs to the Special Issue Recent Advances in Inhalation Therapy)
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15 pages, 1002 KiB  
Article
Preparing O/W/O Emulsion for Curcumin (Curcuma longa) Delivery and In Vitro Digestibility Assay
by Kristýna Opustilová, Barbora Lapčíková, Daniela Sumczynski and Richard Adámek
Int. J. Mol. Sci. 2025, 26(12), 5639; https://doi.org/10.3390/ijms26125639 - 12 Jun 2025
Viewed by 378
Abstract
In this study, simple oil-in-water emulsions (O/W) and multiple O/W/O emulsions were employed as carriers for a curcumin delivery system. The stability of emulsions was evaluated using DSC (differential scanning calorimetry), accompanied by particle size measurement by DLS (dynamic light scattering) and rheological [...] Read more.
In this study, simple oil-in-water emulsions (O/W) and multiple O/W/O emulsions were employed as carriers for a curcumin delivery system. The stability of emulsions was evaluated using DSC (differential scanning calorimetry), accompanied by particle size measurement by DLS (dynamic light scattering) and rheological analysis. The amount of freezable water (Wfs) in O/W emulsion was determined to be 80.4%, while that in O/W/O emulsion was 23.7%. Multiple emulsions had a more complex structure than simple emulsions, being characterized by higher stability with predominant loss modulus over storage modulus (G” > G’). The mean surface diameter for O/W emulsion was 198.7 ± 9.8 nm, being approximately two times lower than that for multiple emulsions. Curcumin in vitro digestibility was observed for both emulsions and, additionally, the digestibility of fresh and dried curcuma root powders was investigated. Multiple emulsions were found to be a superior matrix for curcumin delivery, with higher stability and emulsion digestibility of 50.6% for the stomach and small intestine. In vitro digestion of dried curcuma powders and curcuma root samples was monitored by HPLC (high-performance liquid chromatography). The DMD (dry matter digestibility) for dried curcuma powders ranged between 52.9% to 78.8%, and for fresh curcuma (KF) was 95.5%. Full article
(This article belongs to the Special Issue Functions and Applications of Natural Products)
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18 pages, 5213 KiB  
Article
Lung Delivery of Lactose-Free Microparticles Loaded with Azithromycin for the Treatment of Bacterial Infections
by Gracia Molina, Dolores R. Serrano, María Auxiliadora Dea-Ayuela, Carmina Rodriguez, Elena González-Burgos and Brayan J. Anaya
Pharmaceutics 2025, 17(6), 770; https://doi.org/10.3390/pharmaceutics17060770 - 11 Jun 2025
Viewed by 560
Abstract
Background/Objectives: Respiratory bacterial infections remain a significant global health challenge, with effective drug delivery to the lungs being crucial for successful treatment. This study aimed to develop a lactose-free dry powder inhaler (DPI) formulation containing azithromycin (AZM) microparticles for enhanced pulmonary delivery. Methods: [...] Read more.
Background/Objectives: Respiratory bacterial infections remain a significant global health challenge, with effective drug delivery to the lungs being crucial for successful treatment. This study aimed to develop a lactose-free dry powder inhaler (DPI) formulation containing azithromycin (AZM) microparticles for enhanced pulmonary delivery. Methods: Using a quality-by-design approach, an optimized formulation (4% AZM, 20% leucine, and 76% mannitol) was achieved. Results: The formulation demonstrated excellent aerodynamic properties with a mass median aerodynamic diameter (MMAD) of 2.72 μm ± 0.01 μm and fine particle fraction (FPF) (<5 μm) of 65.42% ± 5.12%. AZM-loaded microparticles exhibited enhanced efficacy against Pseudomonas aeruginosa with a two-fold reduction in the minimum bactericidal concentration (7.81 μg/mL vs. 15.62 μg/mL) compared to unprocessed AZM, while maintaining activity against Streptococcus pneumoniae. AZM microparticles demonstrated good biocompatibility with red blood cells and bronchial epithelial cells at therapeutic concentrations. Conclusions: These findings establish a promising lactose-free antibiotic formulation for targeted pulmonary delivery with enhanced antimicrobial efficacy. Full article
(This article belongs to the Special Issue Inhaled Treatment of Respiratory Infections, 2nd Edition)
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13 pages, 1626 KiB  
Article
Impact of Different Hydrate Forms of Magnesium Stearate as a Flow Control Agent on the Physical Stability and Inhalation Efficiency of Carrier-Based Formulations
by Jin-Hyuk Jeong, Jaewoon Son, Ji-Hyeon Kwon, Chang-Soo Han and Chun-Woong Park
Pharmaceutics 2025, 17(6), 711; https://doi.org/10.3390/pharmaceutics17060711 - 28 May 2025
Viewed by 620
Abstract
Objectives: This study aimed to evaluate the impact of the different hydration states of magnesium stearate (Mg.st) anhydrate (AH), monohydrate (MH), and dihydrate (DH) on the aerodynamic performance and stability of carrier-based dry powder inhalation (DPI) formulations using arformoterol and budesonide as model [...] Read more.
Objectives: This study aimed to evaluate the impact of the different hydration states of magnesium stearate (Mg.st) anhydrate (AH), monohydrate (MH), and dihydrate (DH) on the aerodynamic performance and stability of carrier-based dry powder inhalation (DPI) formulations using arformoterol and budesonide as model drugs. Methods: DPI formulations were prepared using Inhalac 251 lactose and Mg.st in various hydrated forms. The physicochemical properties of Mg.st were characterized using powder X-ray diffraction, differential scanning calorimetry, Fourier-transform infrared spectroscopy, Karl Fischer titration, dynamic vapor absorption, and Raman imaging. The aerodynamic performance was assessed employing a next-generation impactor under initial and accelerated conditions (40 °C, 75% relative humidity). Results: Mg.st-MH exhibited the highest crystallinity and the most stable moisture sorption profile, and showed the smallest particle size within the formulation as observed in the Raman images. Formulations containing Mg.st-MH demonstrated significantly higher fine particle fractions for both arformoterol (51.02 ± 5.16%) and budesonide (61.98 ± 4.09%) compared to formulations with Mg.st-AH or -DH forms. Mg.st-MH also exhibited improved performance retention under accelerated conditions, correlating with its physicochemical stability. Conclusions: The monohydrate form of magnesium stearate was the most effective force control agent, which reduced interparticulate interactions, thereby enhancing the inhalation efficiency and formulation stability. Thus, selecting an appropriate hydration form of Mg.st can improve DPI performance. Full article
(This article belongs to the Section Physical Pharmacy and Formulation)
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22 pages, 1321 KiB  
Article
Assessment of Innovative Dry Powders for Inhalation of a Synergistic Combination Against Mycobacterium tuberculosis in Infected Macrophages and Mice
by Faustine Ravon, Emilie Berns, Isaline Lambert, Céline Rens, Pierre-Yves Adnet, Mehdi Kiass, Véronique Megalizzi, Cédric Delporte, Alain Baulard, Vanessa Mathys, Samira Boarbi, Nathalie Wauthoz and Véronique Fontaine
Pharmaceutics 2025, 17(6), 705; https://doi.org/10.3390/pharmaceutics17060705 - 27 May 2025
Viewed by 564
Abstract
Background/Objectives: In vitro, vancomycin (VAN) and tetrahydrolipstatin (THL) together have been shown to synergistically inhibit Mycobacterium tuberculosis (Mtb), the world’s most infectious killer. The poor oral bioavailability of VAN and THL and predominant tropism of Mtb infection to the lungs and alveolar macrophages [...] Read more.
Background/Objectives: In vitro, vancomycin (VAN) and tetrahydrolipstatin (THL) together have been shown to synergistically inhibit Mycobacterium tuberculosis (Mtb), the world’s most infectious killer. The poor oral bioavailability of VAN and THL and predominant tropism of Mtb infection to the lungs and alveolar macrophages make pulmonary administration highly attractive. This study aimed to develop and assess the efficacy of dry powders for inhalation of VAN microparticles embedded with THL. Methods: The dry powders produced by spray-drying, with or without hydrogenated castor oil (HCO), were characterized for their physicochemical properties among others by HPLC-DAD. The fast-screening impactor was used to determine powder aerodynamic properties, and VAN and THL releases were established from the paddle over disk method. Biological activities were assessed in a new M. bovis-infected macrophage model and in Mtb-infected mice. Results and Discussion: The addition of 25% HCO enables co-deposition (fine particle dose) at the desired weight ratio and co-releasing of VAN and THL in aqueous media. Microparticles with 0% to 50% HCO drastically reduced cytoplasmic Mycobacterium bovis survival (99.9% to 62.5%, respectively), with higher efficacy at low HCO concentration. Consequently, VAN/THL with or without 25% HCO was evaluated in Mtb-infected mice. Although no decrease in Mtb lung burden was observed after two weeks of administration, the endotracheal administration of VAN 500 mg/kg and THL 50 mg/kg with 25% HCO administrated three times during five days concomitantly with daily oral rifampicin (10 mg/kg) demonstrated 2-fold bacterial burden reduction compared to the group treated with RIF alone. Conclusions: HCO was crucial for obtaining a fine particle dose at the synergistic weight ratio (VAN/THL 10:1) and for releasing both drugs in aqueous media. With oral administration of the first-line rifampicin, the dry powder VAN/THL/25% HCO was able to exert a potential anti-tubercular effect in vivo in Mtb-infected mice after five days. Full article
(This article belongs to the Special Issue Inhaled Treatment of Respiratory Infections, 2nd Edition)
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15 pages, 1289 KiB  
Article
The Particle Size to Modulate the Techno-Functional Properties of Fava Bean Pod Powder
by Abel I. Barrial-Lujan, María del Mar Camacho, Eva García-Martínez, Alberto Yuste and Nuria Martínez-Navarrete
Powders 2025, 4(2), 14; https://doi.org/10.3390/powders4020014 - 15 May 2025
Viewed by 444
Abstract
Plant by-products are undervalued as they are an important source of nutrients and bioactive compounds with potential health benefits, which also contribute to aroma and color. Therefore, their use in human food is a challenging field of study that deserves to be explored. [...] Read more.
Plant by-products are undervalued as they are an important source of nutrients and bioactive compounds with potential health benefits, which also contribute to aroma and color. Therefore, their use in human food is a challenging field of study that deserves to be explored. This study proposes the conversion of fava bean pods into a powdered product as a high-quality, stable, and easy-to-handle food ingredient, thus contributing to the sustainability of the food industry within the framework of the circular economy. The powdered product was obtained by freeze-drying and grinding. As the particle size of powders is a determinant of their quality and functionality, some properties of two bean pod powder samples with mean particle sizes of 102.9 and 45.3 μm, obtained by sieving at 200 and 45 μm, respectively, are compared. The results obtained indicate good flowability of both powders. However, the sample with the largest size showed, in addition to a greener tone, lower interparticle porosity related to a better packing capacity, lower hygroscopicity, and much better wettability, along with its higher swelling capacity and water and oil retention capacity. Nevertheless, in this case, the extraction of proteins and phenols decreased by 18% and 25%, respectively, without compromising the total fiber content. Considering the use of fava bean pod powder as a versatile food ingredient, the largest size of those studied, 102.9 μm, is recommended. Only if the objective is to obtain a healthy food supplement would it be more desirable to grind it to a smaller particle size. Full article
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19 pages, 3400 KiB  
Article
Preparation of Carrier-Free Inhalable Dry Powder of Rivaroxaban Using Two-Step Milling for Lung-Targeted Delivery
by Young-Jin Kim, Jaewoon Son, Chang-Soo Han and Chun-Woong Park
Pharmaceutics 2025, 17(5), 634; https://doi.org/10.3390/pharmaceutics17050634 - 9 May 2025
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Abstract
Background/Objectives: This study aimed to develop a dry powder inhalation (DPI) formulation of rivaroxaban (RVX) using a combination of bead milling (BM) and jet milling (JM) to enhance lung-targeted delivery for the effective treatment of pulmonary embolism while minimizing systemic exposure. Methods [...] Read more.
Background/Objectives: This study aimed to develop a dry powder inhalation (DPI) formulation of rivaroxaban (RVX) using a combination of bead milling (BM) and jet milling (JM) to enhance lung-targeted delivery for the effective treatment of pulmonary embolism while minimizing systemic exposure. Methods: A carrier-free DPI formulation of RVX was developed using sequential BM and JM, with L-leucine incorporated at various concentrations (1%, 5%, and 10%) as a force control agent. The formulations were characterized for particle morphology, size distribution, crystallinity, and thermal properties. The in-vitro aerodynamic performance was evaluated using a next-generation impactor, while ex-vivo studies assessed anticoagulant activity. Pharmacokinetic and tissue distribution studies were carried out in Sprague Dawley rats following intratracheal administration, and the effects of inhaled RVX were compared with those of oral administration. Results: The optimized BM-JM-5L formulation achieved a Dv50 of 2.58 ± 0.01 µm and a fine particle fraction of 72.10 ± 2.46%, indicating suitability for pulmonary delivery. The two-step milling effectively reduced particle size and enhanced dispersibility without altering RVX’s physicochemical properties. Ex-vivo anticoagulation tests confirmed maintained or improved activity. In-vivo studies showed that pulmonary administration (5 mg/kg) led to a 493-fold increase in lung drug concentration and 2.56-fold higher relative bioavailability vs. oral dosing, with minimal heart tissue accumulation, confirming targeted lung delivery. Conclusions: The two-step milled RVX DPI formulations, particularly BM-JM-5L with 5% leucine, demonstrated significant potential for pulmonary administration by achieving high local drug concentrations, rapid onset, and improved bioavailability at lower doses. These findings highlight the feasibility of RVX as a DPI formulation for pulmonary delivery in treating pulmonary embolism. Full article
(This article belongs to the Section Drug Delivery and Controlled Release)
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