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1.
Methods Mol Biol ; 2843: 163-175, 2024.
Article in English | MEDLINE | ID: mdl-39141300

ABSTRACT

Extracellular vesicles are nanosized lipid-bilayered spheres secreted from every living cell and they serve physiological and pathophysiological functions. Bacterial membrane vesicles are shed from both Gram-negative and Gram-positive bacteria and harbor many virulence factors, nuclear material, polysaccharides, proteins, and antigenic determinants, which are essential for immune recognition and evasion. Hence, bacterial membrane vesicles are very promising vaccine candidates. Spray drying is a well-established pharmaceutical technique to produce inhalable dry powders with enhanced stability for formulations of vaccines. In this chapter, we illustrate general guidelines for spray drying of bacterial extracellular vesicles to improve their stability without compromising their immunogenic protective effect. We discuss some of the most important experiments to characterize the generated spray-dried bacterial membrane vesicle powder vaccine.


Subject(s)
Extracellular Vesicles , Extracellular Vesicles/chemistry , Extracellular Vesicles/metabolism , Extracellular Vesicles/immunology , Bacterial Vaccines/immunology , Bacterial Vaccines/chemistry , Spray Drying , Powders/chemistry , Humans , Cell Membrane/metabolism , Cell Membrane/chemistry , Animals
2.
Molecules ; 29(15)2024 Jul 30.
Article in English | MEDLINE | ID: mdl-39124991

ABSTRACT

The study investigated the impact of Lonicera caerulea L. juice matrix modification and drying techniques on powder characteristics. The evaluation encompassed phenolics (514.7-4388.7 mg/100 g dry matter), iridoids (up to 337.5 mg/100 g dry matter), antioxidant and antiglycation capacity, as well as anti-ageing properties of powders produced using maltodextrin, inulin, trehalose, and palatinose with a pioneering role as a carrier. Spray drying proved to be competitive with freeze drying for powder quality. Carrier application influenced the fruit powder properties. Trehalose protected the phenolics in the juice extract products, whereas maltodextrin showed protective effect in the juice powders. The concentrations of iridoids were influenced by the matrix type and drying technique. Antiglycation capacity was more affected by the carrier type in juice powders than in extract products. However, with carrier addition, the latter showed approximately 12-fold higher selectivity for acetylcholinesterase than other samples. Understanding the interplay between matrix composition, drying techniques, and powder properties provides insights for the development of plant-based products with tailored attributes, including potential health-linked properties.


Subject(s)
Freeze Drying , Lonicera , Plant Extracts , Powders , Spray Drying , Freeze Drying/methods , Powders/chemistry , Lonicera/chemistry , Plant Extracts/chemistry , Antioxidants/chemistry , Antioxidants/analysis , Fruit and Vegetable Juices/analysis , Polysaccharides/chemistry , Polysaccharides/analysis , Phenols/analysis , Phenols/chemistry
3.
Food Res Int ; 192: 114804, 2024 Sep.
Article in English | MEDLINE | ID: mdl-39147504

ABSTRACT

This study investigated spray drying a method for microencapsulating Lacticaseibacillus rhamnosus GG using a gastrointestinal resistant composite matrix. An encapsulate composite matrix comprising green banana flour (GBF) blended with maltodextrin (MD) and gum arabic (GA). The morphology of resulted microcapsules revealed a near-spherical shape with slight dents and no surface cracks. Encapsulation efficiency and product yield varied significantly among the spray-dried microencapsulated probiotic powder samples (SMPPs). The formulation with the highest GBF concentration (FIV) exhibited maximum post-drying L. rhamnosus GG viability (12.57 ± 0.03 CFU/g) and best survivability during simulated gastrointestinal digestion (9.37 ± 0.05 CFU/g). Additionally, glass transition temperature (Tg) analysis indicated good thermal stability of SMPPs (69.3 - 92.9 ℃), while Fourier Transform infrared (FTIR) spectroscopy confirmed the structural integrity of functional groups within microcapsules. The SMPPs characterization also revealed significant variation in moisture content, water activity, viscosity, and particle size. Moreover, SMPPs exhibited differences in total phenolic and flavonoid, along with antioxidant activity and color values throughout the study. These results suggested that increasing GBF concentration within the encapsulating matrix, while reducing the amount of other composite materials, may offer enhanced protection to L. rhamnosus GG during simulated gastrointestinal conditions, likely due to the gastrointestinal resistance properties of GBF.


Subject(s)
Drug Compounding , Gum Arabic , Lacticaseibacillus rhamnosus , Musa , Polysaccharides , Powders , Probiotics , Spray Drying , Lacticaseibacillus rhamnosus/chemistry , Gum Arabic/chemistry , Polysaccharides/chemistry , Musa/chemistry , Particle Size , Capsules , Flour/analysis , Spectroscopy, Fourier Transform Infrared , Digestion , Viscosity , Gastrointestinal Tract/metabolism , Microbial Viability
4.
Eur J Pharm Biopharm ; 202: 114396, 2024 Sep.
Article in English | MEDLINE | ID: mdl-38971201

ABSTRACT

Proteins have recently caught attention as potential excipients for amorphous solid dispersions (ASDs) to improve oral bioavailability of poorly water-soluble drugs. Notably, the studies have highlighted whey protein isolates, particularly ß-lactoglobulin (BLG), as promising candidates in amorphous stabilization, dissolution and solubility enhancement, achieving drug loadings of 50 wt% and higher. Consequently, investigations into the mechanisms underlying the solid-state stabilization of amorphous drugs and the enhancement of drug solubility in solution have been conducted. This graphical review provides a comprehensive overview of recent findings concerning BLG-based ASDs. Firstly, the dissolution performance of BLG-based ASDs is compared to more traditional polymer-based ASDs. Secondly, the drug loading onto BLG and the resulting amorphous stabilization mechanisms is summarized. Thirdly, interactions between BLG and drug molecules in solution are described as the mechanisms governing the improvement of drug solubility. Lastly, we outline the impact of the spray drying process on the secondary structure of BLG, and the resulting differences in amorphous stabilization and drug dissolution performance between α-helix-rich and ß-sheet-rich BLG-based ASDs.


Subject(s)
Excipients , Lactoglobulins , Solubility , Lactoglobulins/chemistry , Excipients/chemistry , Biological Availability , Drug Compounding/methods , Chemistry, Pharmaceutical/methods , Drug Liberation , Drug Stability , Polymers/chemistry , Spray Drying
5.
Food Chem ; 459: 140336, 2024 Nov 30.
Article in English | MEDLINE | ID: mdl-39003859

ABSTRACT

The cell membrane, consisting of a phospholipid bilayer, is an important defense system of lactic acid bacteria (LAB) against adverse conditions. However, this membrane gets damaged during the process of spray drying of LAB into powder. In this study, two strains of Lactobacillus bulgaricus L9-7 and L4-2-12 with significantly different survival rates of about 22.49% and 0.43% after spray drying were explored at the cell membrane level. A total of 65 significantly different lipid species were screened from the cell membranes of two strains, with cardiolipin (CL) 15:1_22:6_24:0_28:0 being the crucial lipid species affecting membrane resistance. Finally, the KEGG enrichment analysis revealed that glycerophospholipid metabolism was the most predominant pathway, and eleven lipid species were annotated, including CL. Overall, this paper provides valuable insights into enhancing the heat tolerance of LAB.


Subject(s)
Lactobacillus delbrueckii , Lipidomics , Membrane Lipids , Lactobacillus delbrueckii/metabolism , Lactobacillus delbrueckii/chemistry , Membrane Lipids/chemistry , Membrane Lipids/metabolism , Spray Drying , Microbial Viability , Cell Membrane/chemistry , Cell Membrane/metabolism
6.
Int J Pharm ; 662: 124466, 2024 Sep 05.
Article in English | MEDLINE | ID: mdl-39009288

ABSTRACT

Biopharmaceuticals are labile biomolecules that must be safeguarded to ensure the safety, quality, and efficacy of the product. Batch freeze-drying is an established means of manufacturing solid biopharmaceuticals but alternative technologies such as spray-drying may be more suitable for continuous manufacturing of inhalable biopharmaceuticals. Here we assessed the feasibility of spray-drying Olipudase alfa, a novel parenteral therapeutic enzyme, by evaluating some of its critical quality attributes (CQAs) in a range of excipients, namely, trehalose, arginine (Arg), and arginine hydrochloride (Arg-HCl) in the sucrose/methionine base formulation. The Arg-HCl excipient produced the best gain in CQAs of spray-dried Olipudase with a 63% reduction in reconstitution time and 83% reduction in the optical density of the solution. Molecular dynamics simulations revealed the atomic-scale mechanism of the protein-excipient interactions, substantiating the experimental results. The Arg-HCl effect was explained by the calculated thermal stability and structural order of the protein wherein Arg-HCl acted as a crowding agent to suppress protein aggregation and promote stabilization of Olipudase post-spray-drying. Therefore, by rational selection of appropriate excipients, our experimental and modelling dataset confirms spray-drying is a promising technology for the manufacture of Olipudase and demonstrates the potential to accelerate development of continuous manufacturing of parenteral biopharmaceuticals.


Subject(s)
Arginine , Excipients , Molecular Dynamics Simulation , Recombinant Proteins , Excipients/chemistry , Arginine/chemistry , Recombinant Proteins/chemistry , Spray Drying , Drug Compounding/methods , Chemistry, Pharmaceutical/methods , Trehalose/chemistry , Sucrose/chemistry
7.
Molecules ; 29(14)2024 Jul 19.
Article in English | MEDLINE | ID: mdl-39064978

ABSTRACT

Edible flowers are a potential source of bioactive ingredients and are also an area of scientific research. Particularly noteworthy are Cyani flos, which have a wide range of uses in herbal medicine. The below study aimed to investigate the influence of selected soluble fiber fractions on the selected properties of physical and biochemical powders obtained during spray drying a water extract of Cyani flos. The drying efficiency for the obtained powders was over 60%. The obtained powders were characterized by low moisture content (≤4.99%) and water activity (≤0.22). The increase in the addition of pectin by the amount of 2-8% in the wall material resulted in a decrease in hygroscopicity, water solubility, and protection of flavonoids and anthocyanins both before and after digestion in the tested powders in comparison to the sample with only inulin as a carrier. Additionally, it was noted that all samples were characterized by high bioaccessibility when determining antioxidant properties and xanthine oxidase inhibition.


Subject(s)
Antioxidants , Flowers , Plant Extracts , Powders , Spray Drying , Plant Extracts/chemistry , Powders/chemistry , Flowers/chemistry , Antioxidants/chemistry , Antioxidants/pharmacology , Flavonoids/chemistry , Solubility , Anthocyanins/chemistry
8.
Food Res Int ; 191: 114677, 2024 Sep.
Article in English | MEDLINE | ID: mdl-39059906

ABSTRACT

Vitamin D3(cholecalciferol)plays a crucial role in various physiological processes. However, vitamin D3 deficiency is a major public health problem affecting millions of people. Therefore, it is important to develop effective strategies that ensure the protection and stability of this important vitamin for food supplementation and fortification. This work aimed to impregnate intact and plasmolyzedSaccharomyces pastorianus brewer's yeast biomass with cholecalciferol using a biosorption process followed by spray drying to characterize the obtained material in terms of morphology, average particle size, zeta potential, moisture, water activity, FT-IR, and the stability of the encapsulated vitamin during the drying and storage process. Plasmolysis proved to be an effective method for improving the biosorption efficiency, retention during spray drying, and stability of vitamin D3. In addition, this process promoted an increase in cell size, which favored the dispersion stability of the system, as evidenced by the zeta potential values. These results contribute to the understanding of a new method for delivering this vitamin that conforms to environmentally conscious practices.


Subject(s)
Biomass , Cholecalciferol , Particle Size , Saccharomyces cerevisiae , Saccharomyces cerevisiae/metabolism , Spectroscopy, Fourier Transform Infrared , Spray Drying , Desiccation/methods
9.
Food Res Int ; 191: 114646, 2024 Sep.
Article in English | MEDLINE | ID: mdl-39059932

ABSTRACT

Docosahexaenoic acid (DHA), an essential omega-3 fatty acid, offers significant health benefits but faces challenges such as distinct odor, oxidation susceptibility, and limited intestinal permeability, hindering its broad application. Microencapsulation, widely employed, enhances DHA performance by facilitating controlled release, digestion, and absorption in the gastrointestinal tract. Despite extensive studies on DHA microcapsules and related delivery systems, understanding the mechanisms governing encapsulated DHA release, digestion, and absorption, particularly regarding the influence of wall materials and DHA sources, remains limited. This review starts with an overview of current techniques commonly applied for DHA microencapsulation. It then proceeds to outline up-to-date advances in the release, digestion and absorption of DHA microcapsules, highlighting the roles of wall materials and DHA sources. Importantly, it proposes strategies for overcoming challenges and exploiting opportunities to enhance the bioavailability of DHA microcapsules. Notably, spray drying dominates DHA microencapsulation (over 90 % usage), while complex coacervation shows promise for future applications. The combination of proteins and carbohydrates or phospholipids as wall material exhibits potential in controlling release and digestion of DHA microcapsules. The source of DHA, particularly algal oil, demonstrates higher lipid digestibility and absorptivity of free fatty acids (FFAs) than fish oil. Future advancements in DHA microcapsule development include formulation redesign (e.g., using plant proteins as wall material and algal oil as DHA source), technique optimization (such as co-microencapsulation and pre-digestion), and creation of advanced in vitro systems for assessing DHA digestion and absorption kinetics.


Subject(s)
Biological Availability , Capsules , Digestion , Docosahexaenoic Acids , Docosahexaenoic Acids/chemistry , Humans , Drug Compounding , Intestinal Absorption , Spray Drying
10.
AAPS PharmSciTech ; 25(6): 164, 2024 Jul 13.
Article in English | MEDLINE | ID: mdl-38997569

ABSTRACT

This study employed a Quality by Design (QbD) approach to spray dry amorphousclotrimazole nanosuspension (CLT-NS) consisting of Soluplus® and microcrystallinecellulose. Using the Box-Behnken Design, a systematic evaluation was conducted toanalyze the impact of inlet temperature, % aspiration, and feed rate on the criticalquality attributes (CQAs) of the clotrimazole spray-dried nanosuspension (CLT-SDNS). In this study, regression analysis and ANOVA were employed to detect significantfactors and interactions, enabling the development of a predictive model for the spraydrying process. Following optimization, the CLT-SD-NS underwent analysis using Xraypowder diffraction (XRPD), Fourier transform infrared spectroscopy (FTIR), Dynamic Scanning Calorimetry (DSC), and in vitro dissolution studies. The resultsshowed significant variables, including inlet temperature, feed rate, and aspiration rate,affecting yield, redispersibility index (RDI), and moisture content of the final product. The models created for critical quality attributes (CQAs) showed statistical significanceat a p-value of 0.05. XRPD and DSC confirmed the amorphous state of CLT in theCLT-SD-NS, and FTIR indicated no interactions between CLT and excipients. In vitrodissolution studies showed improved dissolution rates for the CLT-SD-NS (3.12-foldincrease in DI water and 5.88-fold increase at pH 7.2 dissolution media), attributed torapidly redispersing nanosized amorphous CLT particles. The well-designed studyutilizing the Design of Experiments (DoE) methodology.


Subject(s)
Clotrimazole , Nanoparticles , Suspensions , Clotrimazole/chemistry , Clotrimazole/administration & dosage , Nanoparticles/chemistry , Suspensions/chemistry , Spray Drying , Chemistry, Pharmaceutical/methods , Solubility , Spectroscopy, Fourier Transform Infrared/methods , Particle Size , Calorimetry, Differential Scanning/methods , Temperature , Drug Compounding/methods , Polyvinyls/chemistry , X-Ray Diffraction/methods , Polyethylene Glycols
11.
Int J Biol Macromol ; 275(Pt 1): 133626, 2024 Aug.
Article in English | MEDLINE | ID: mdl-38964691

ABSTRACT

Low-viscosity hydroxypropyl methylcellulose (HPMC) was obtained by electron beam irradiation, and its use as an excipient for improving the properties of spray dried pharmaceutical powders was investigated. The minimum molecular weight of HPMC which could maintain the capacity of encapsulation and powder modification was explored. As the irradiation dose was increased from 10 to 200 kGy, the molecular weight and viscosity of HPMC decreased linearly. However, its main structure and degrees of methoxy and hydroxypropyl substitution were not significantly affected. The irradiated HPMC could encapsulate particles during spray drying and, thus, modify powder properties. Furthermore, the water content of spray-dried powders with irradiated HPMC was lower than that with parent HPMC. After the spray-dried powder with irradiated HPMC was prepared into granules, their dissolution rate was also faster. However, in order to achieve high encapsulation, the molecular weight of HPMC should be ensured to be above 7.5 kDa. The designated low-viscosity HPMC obtained by electron beam irradiation is a suitable powder-modification material for use in spray drying, and it shows promise as a superior excipient in medicine, food, paint industries, among others.


Subject(s)
Electrons , Hypromellose Derivatives , Molecular Weight , Spray Drying , Hypromellose Derivatives/chemistry , Viscosity , Powders , Particle Size , Excipients/chemistry , Water/chemistry
12.
Arch Microbiol ; 206(7): 320, 2024 Jun 22.
Article in English | MEDLINE | ID: mdl-38907882

ABSTRACT

The mining and metallurgical industry represents one of the leading causes of environmental pollution. In this context, the optimization of mineral waste management and the efficient extraction of metals of interest becomes an imperative priority for a sustainable future. Microorganisms such as Acidithiobacillus thiooxidans have represented a sustainable and economical alternative in recent years due to their capacity for environmental remediation in bioleaching processes because of their sulfur-oxidizing capacity and sulfuric acid generation. However, its use has been limited due to the reluctance of mine operators because of the constant reproduction of the bacterial culture in suitable media and the care that this entails. In this work, the central objective was to evaluate the functional characteristics of A. thiooxidans, microencapsulated and stored at room temperature for three years in vacuum bags, using a spray drying process with gum arabic as a wall vector. Growth kinetics showed a survival of 80 ± 0.52% after this long period of storage. Also, a qualitative fluorescence technique with a 5-cyano-2-3 ditolyl tetrazolium (CTC) marker was used to determine the respiratory activity of the microorganisms as soon as it was resuspended. On the other hand, the consumption of resuspended sulfur was evaluated to corroborate the correct metabolic functioning of the bacteria, with results of up to 50% sulfur reduction in 16 days and sulfate generation of 513.85 ± 0.4387 ppm and 524.15 ± 0.567 ppm for microencapsulated and non-microencapsulated cultures, respectively. These results demonstrate the success after three years of the microencapsulation process and give guidelines for its possible application in the mining-metallurgical industry.


Subject(s)
Acidithiobacillus thiooxidans , Gum Arabic , Mining , Acidithiobacillus thiooxidans/metabolism , Acidithiobacillus thiooxidans/growth & development , Gum Arabic/chemistry , Spray Drying , Biotechnology/methods , Sulfur/metabolism
13.
Food Chem ; 457: 140073, 2024 Nov 01.
Article in English | MEDLINE | ID: mdl-38909456

ABSTRACT

The phytochemical composition and physicochemical attributes of polyphenol-enriched protein particle ingredients produced with pulse proteins (e.g. chickpea protein, pea protein, and a chickpea-pea protein blend) and polyphenols recovered from wild blueberry pomace were investigated for colloidal and interfacial properties. Anthocyanins were the major polyphenol fraction (27.74-36.47 mg C3G/g) of these polyphenol-rich particles (44.95-62.08 mg GAE/g). Dispersions of pea protein-polyphenol particles showed a superior phase stability before and after heat treatment compared to the chickpea pea protein-polyphenol system. This observation was independent of the added amount of NaCl in the dispersion. In general, at quasi equilibrium state, pulse protein-polyphenol particles and parental pulse protein ingredients showed similar oil-water interfacial tension. However, pea protein-polyphenol particles demonstrated a reduced diffusion-driven oil-water interfacial adsorption rate constant compared to the parental pea protein ingredient. Overall, the obtained results suggest application potential of pea protein-polyphenol particles as a functional food/beverage ingredient.


Subject(s)
Colloids , Polyphenols , Polyphenols/chemistry , Colloids/chemistry , Plant Proteins/chemistry , Cicer/chemistry , Spray Drying , Particle Size , Pisum sativum/chemistry , Pea Proteins/chemistry , Fruit/chemistry , Plant Extracts/chemistry
14.
J Pharm Sci ; 113(9): 2764-2774, 2024 Sep.
Article in English | MEDLINE | ID: mdl-38944343

ABSTRACT

The incorporation of leucine (Leu), a hydrophobic amino acid, into pharmaceutically relevant particles via spray-drying can improve the physicochemical and particulate properties, stability, and ultimately bioavailability of the final product. More specifically, Leu has been proposed to form a shell on the surface of spray-dried (SD) particles. The aim of this study was to explore the potential of Leu in the SD protein/trehalose (Tre) formulation to control the water uptake and moisture-induced recrystallization of amorphous Tre, using lysozyme (LZM) as a model protein. LZM/Tre (1:1, w/w) was dissolved in water with varied amounts of Leu (0 - 40%, w/w) and processed by spray-drying. The solid form, residual moisture content (RMC), hygroscopicity, and morphology of SD LZM/Tre/Leu powders were evaluated, before and after storage under 22°C/55% RH conditions for 90 and 180 days. The X-ray powder diffraction results showed that Leu was in crystalline form when the amount of Leu in the formulation was at least 20% (w/w). Thermo-gravimetric analysis and scanning electron microscopy results showed that 0%, 5%, and 10% (w/w) Leu formulations led to comparable RMC and raisin-like round particles. In contrast, higher Leu contents resulted in a lower RMC and increased surface corrugation of the SD particles. Dynamic vapor sorption analysis showed that partial recrystallization of amorphous Tre to crystalline Tre·dihydrate occurred in the 0% Leu formulation. However, adding as little as 5% (w/w) Leu inhibited this recrystallization during the water sorption/desorption cycle. In addition, after storage, the formulations with higher Leu contents showed reduced water uptake. Instead of observing recrystallization of amorphous Tre in 0%, 5%, and 10% (w/w) Leu formulations, recrystallization of amorphous Leu was noted in the 5% and 10% (w/w) Leu formulations after storage. In summary, our study demonstrated that the addition of Leu has the potential to reduce water uptake and inhibit moisture-induced recrystallization of amorphous Tre in the SD protein/Tre powder system.


Subject(s)
Crystallization , Excipients , Leucine , Muramidase , Powders , Trehalose , Leucine/chemistry , Excipients/chemistry , Muramidase/chemistry , Powders/chemistry , Trehalose/chemistry , Water/chemistry , Spray Drying , Chemistry, Pharmaceutical/methods , X-Ray Diffraction/methods , Drug Compounding/methods , Particle Size , Drug Stability , Proteins/chemistry
15.
Nutrients ; 16(11)2024 May 21.
Article in English | MEDLINE | ID: mdl-38892489

ABSTRACT

A bioactive Pleurotus eryngii aqueous extract powder (SPAE) was obtained by spray drying and its performance in terms of physicochemical properties, in vitro digestion, inflammatory factors, and modulation of the intestinal microbiota was explored. The results indicated that the SPAE exhibited a more uniform particle size distribution than P. eryngii polysaccharide (PEP). Meanwhile, a typical absorption peak observed at 843 cm-1 in the SPAE FTIR spectra indicated the existence of α-glycosidic bonds. SPAE exhibited higher antioxidant abilities and superior resistance to digestion in vitro. In addition, SPAE supplementation to mice significantly reduced the release of factors that promote inflammation, enhanced the secretion of anti-inflammatory factors, and sustained maximum production of short-chain fatty acids (SCFAs). Additionally, it significantly enhanced the relative abundance of SCFAs-producing Akkermansia and reduced the abundance of Ruminococcus and Clostridiides in intestines of mice. These results show the potential of SPAE as a novel material with prebiotic effects for the food and pharmaceutical industries.


Subject(s)
Gastrointestinal Microbiome , Pleurotus , Powders , Prebiotics , Spray Drying , Pleurotus/chemistry , Animals , Gastrointestinal Microbiome/drug effects , Mice , Fatty Acids, Volatile/metabolism , Antioxidants/pharmacology , Male , Particle Size , Digestion/drug effects , Anti-Inflammatory Agents/pharmacology , Polysaccharides/pharmacology , Polysaccharides/chemistry
16.
Int J Pharm ; 660: 124309, 2024 Jul 20.
Article in English | MEDLINE | ID: mdl-38848797

ABSTRACT

Delivering novel antimycobacterial agents through the pulmonary route using nanoparticle-based systems shows promise for treating diseases like tuberculosis. However, creating dry powder inhaler (DPI) with suitable aerodynamic characteristics while preserving nanostructure integrity and maintaining bioactivity until the active ingredient travels deeply into the lungs is a difficult challenge. We developed DPI formulations containing levofloxacin-loaded solid lipid nanoparticles (SLNs) via spray-drying technique with tailored aerosolization characteristics for effective inhalation therapy. A range of biophysical techniques, including transmission electron microscopy, confocal microscopy, and scanning electron microscopy were used to measure the morphologies and sizes of the spray-dried microparticles that explored both the geometric and aerodynamic properties. Spray drying substantially reduced the particle sizes of the SLNs while preserving their nanostructural integrity and enhancing aerosol dispersion with efficient mucus penetration. Despite a slower uptake rate compared to plain SLNs, the polyethylene glycol modified formulations exhibited enhanced cellular uptake in both A549 and NR8383 cell lines. The percent viability of Mycobacterium bovis had dropped to nearly 0 % by day 5 for both types of SLNs. Interestingly, the levofloxacin-loaded SLNs demonstrated a lower minimum bactericidal concentration (0.25 µg/mL) compared with pure levofloxacin (1 µg/mL), which indicated the formulations have potential as effective treatments for tuberculosis.


Subject(s)
Antitubercular Agents , Dry Powder Inhalers , Levofloxacin , Nanoparticles , Particle Size , Tuberculosis , Levofloxacin/administration & dosage , Levofloxacin/chemistry , Levofloxacin/pharmacology , Nanoparticles/chemistry , Administration, Inhalation , Humans , Antitubercular Agents/administration & dosage , Antitubercular Agents/chemistry , Antitubercular Agents/pharmacology , Antitubercular Agents/pharmacokinetics , Tuberculosis/drug therapy , Lipids/chemistry , Mycobacterium bovis/drug effects , Cell Line , Aerosols , A549 Cells , Animals , Spray Drying , Microbial Sensitivity Tests , Drug Carriers/chemistry , Polyethylene Glycols/chemistry , Anti-Bacterial Agents/administration & dosage , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Liposomes
17.
Int J Pharm ; 660: 124354, 2024 Jul 20.
Article in English | MEDLINE | ID: mdl-38897486

ABSTRACT

During recent years there have been shortages of certain drugs due to problems in raw material supply. These are often related to active ingredients but could also affect excipients. Lactose is one of the most used excipients in tableting and comes in two anomeric and several solid-state forms. The aim of this study was to utilize lactose from a dairy side-stream and compare it against a commercial reference in direct compression. This would be a sustainable option and would secure domestic availability during crises. Two types of lactose, spray-dried and freeze-dried, were evaluated. Lactose was mixed with microcrystalline cellulose in different ratios together with lubricant and glidant, and flowability and tabletability of the formulations was characterized. The fully amorphous and small particle-sized spray-dried lactose flowed inadequately but exhibited good tabletability. The larger particle-sized, freeze-dried lactose exhibited sufficient flow and better tabletability than the commercial reference. However, disintegration and drug release were slower when using the investigational lactose formulations. This was most likely due to remaining milk proteins, especially caseins, in the lactose. Overall, the investigational lactose provides promise for the use of such a side-stream product during crisis situations but enhancing their properties and/or purity would be needed.


Subject(s)
Cellulose , Drug Compounding , Drug Liberation , Excipients , Freeze Drying , Lactose , Tablets , Lactose/chemistry , Excipients/chemistry , Cellulose/chemistry , Drug Compounding/methods , Proof of Concept Study , Particle Size , Spray Drying , Dairying , Chemistry, Pharmaceutical/methods
18.
Appl Microbiol Biotechnol ; 108(1): 361, 2024 Jun 05.
Article in English | MEDLINE | ID: mdl-38837050

ABSTRACT

Lactobacillus delbrueckii subsp. bulgaricus and Lactiplantibacillus plantarum are two lactic acid bacteria (LAB) widely used in the food industry. The objective of this work was to assess the resistance of these bacteria to freeze- and spray-drying and study the mechanisms involved in their loss of activity. The culturability and acidifying activity were measured to determine the specific acidifying activity, while membrane integrity was studied by flow cytometry. The glass transitions temperature and the water activity of the dried bacterial suspensions were also determined. Fourier transform infrared (FTIR) micro-spectroscopy was used to study the biochemical composition of cells in an aqueous environment. All experiments were performed after freezing, drying and storage at 4, 23 and 37 °C. The results showed that Lb. bulgaricus CFL1 was sensitive to osmotic, mechanical, and thermal stresses, while Lpb. plantarum WCFS1 tolerated better the first two types of stress but was more sensitive to thermal stress. Moreover, FTIR results suggested that the sensitivity of Lb. bulgaricus CFL1 to freeze-drying could be attributed to membrane and cell wall degradation, whereas changes in nucleic acids and proteins would be responsible of heat inactivation of both strains associated with spray-drying. According to the activation energy values (47-85 kJ/mol), the functionality loss during storage is a chemically limited reaction. Still, the physical properties of the glassy matrix played a fundamental role in the rates of loss of activity and showed that a glass transition temperature 40 °C above the storage temperature is needed to reach good preservation during storage. KEY POINTS: • Specific FTIR bands are proposed as markers of osmotic, mechanic and thermal stress • Lb. bulgaricus CFL1 was sensitive to all three stresses, Lpb. plantarum WCFS1 to thermal stress only • Activation energy revealed chemically limited reactions ruled the activity loss in storage.


Subject(s)
Freeze Drying , Freeze Drying/methods , Spectroscopy, Fourier Transform Infrared , Spray Drying , Microbial Viability , Lactobacillus plantarum/metabolism , Lactobacillus plantarum/physiology , Lactobacillus delbrueckii/metabolism , Lactobacillus delbrueckii/physiology , Lactobacillales/metabolism , Lactobacillales/physiology , Desiccation
19.
Sci Rep ; 14(1): 14802, 2024 06 26.
Article in English | MEDLINE | ID: mdl-38926468

ABSTRACT

Long-chain polyunsaturated fatty acids (LCPUFA) are of interest due to their potential health properties and have a significant role in reducing the risk of various chronic diseases in humans. It is commonly used as a supplement. However, lipid oxidation is an important negative factor caused by environmental, processing, and limited water solubility of LCPUFA, making them difficult to incorporate into food products. The objective of this research work was to prevent oxidation, extend shelf life, enhance the stability of fatty acids, and to achieve controlled release by preparing spray-dried powder (SDM). For spray-drying, aqueous emulsion blends were formulated using a 1:1 ratio of chia seed oil (CSO) and fish oil (FO) and using a laboratory-scale spray-dryer with varying conditions: inlet air temperature (IAT, 125-185 °C), wall material (WM, 5-25%), pump speed (PS, 3-7 mL/min), and needle speed (NS, 3-11 s). The maximum alpha-linolenic acid (ALA) content was 33 ± 1%. The highest values of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in the microcapsules were 8.4 ± 0.4 and 13 ± 1%, respectively. Fourier transform infrared and X-Ray diffraction analysis results indicated that SDM was successfully formulated with Gum Arabic and maltodextrin (MD). The blending without encapsulation of CSO and FO was digested more efficiently and resulted in more oil being released with simulated gastric fluid (SGF), simulated intestinal fluid (SIF), and SGF + SIF conditions without heating. No significant changes were observed for saturated, monounsaturated, and LCPUFA, whether exposed or not to gastrointestinal conditions. However, compared to the release of SDM, it can be useful for designing delivery systems for the controlled release of essential fatty acids.


Subject(s)
Capsules , Fish Oils , Spray Drying , Fish Oils/chemistry , Plant Oils/chemistry , Salvia/chemistry , Fatty Acids/chemistry , Humans
20.
Int J Biol Macromol ; 273(Pt 2): 133139, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38878929

ABSTRACT

The microencapsulation of polysaturated fatty acids by spray drying remains a challenge due to their susceptibility to oxidation. In this work, antioxidant Pickering emulsions were attempted as feeds to produce oxidation stable tuna oil microcapsules. The results indicated that the association between chitosan (CS) and ovalbumin (OVA) was a feasible way to fabricate antioxidant and wettable complexes and a high CS percentage favored these properties. The particles could yield tuna oil Pickering emulsions with enhanced oxidation stability through high-pressure homogenization, which were successfully spray dried to produce microcapsules with surface oil content of 8.84 % and microencapsulation efficiency of 76.65 %. The microcapsules exhibited significantly improved oxidation stability and their optimum peroxide values after storage at 50 °C, 85 % relative humidity, or natural light for 15 d were 48.67 %, 60.07 %, and 39.69 % respectively lower than the powder derived from the OVA-stabilized emulsion. Hence, Pickering emulsions stabilized by the CS/OVA polyelectrolyte complexes are potential in the production of oxidation stable polyunsaturated fatty acid microcapsules by spray drying.


Subject(s)
Capsules , Chitosan , Emulsions , Ovalbumin , Oxidation-Reduction , Spray Drying , Tuna , Chitosan/chemistry , Emulsions/chemistry , Ovalbumin/chemistry , Animals , Fish Oils/chemistry , Polyelectrolytes/chemistry , Antioxidants/chemistry , Particle Size
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