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1.
Methods Mol Biol ; 2843: 163-175, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39141300

RESUMO

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.


Assuntos
Vesículas Extracelulares , Vesículas Extracelulares/química , Vesículas Extracelulares/metabolismo , Vesículas Extracelulares/imunologia , Vacinas Bacterianas/imunologia , Vacinas Bacterianas/química , Secagem por Atomização , Pós/química , Humanos , Membrana Celular/metabolismo , Membrana Celular/química , Animais
2.
Artigo em Inglês | MEDLINE | ID: mdl-39133299

RESUMO

Spray drying is an important industrial method for the preparation of B. thuringiensis powder from fermentation liquor. The effect of spray drying on the crystal proteins, however, has not been reported in the literature so far. The present study systematically investigated the effect of inlet air temperature, outlet air temperature, atomizing air pressure and additives (including organic and inorganic auxiliaries) on the thermal destruction of crystal proteins of B. thuringiensis. The results indicated that the content of crystal proteins of B. thuringiensis powder decreased with increased inlet air temperature, outlet air temperature and atomising air pressure. The pseudo-z values for inlet air temperature, outlet air temperature and atomizing air pressure were 826.4 â„ƒ, 204.0 â„ƒ and 4.74 MPa, respectively. Among them, the outlet air temperature was a major parameter influencing the thermal destruction of crystal proteins, therefore, the decrease of the outlet air temperature was beneficial to increase the protein content in powder. Although the spray drying had an adverse effect on crystal proteins, the crystal protein content in spray-dried powder approached that in freeze-dried powder when the inlet air temperature of 165 â„ƒ, outlet air temperature of 70 â„ƒ and atomizing air pressure of 0.15 MPa were employed. The addition of some organic and inorganic auxiliaries to fermentation liquor can protect the crystal proteins from heat damage.

3.
Molecules ; 29(15)2024 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-39124996

RESUMO

Encapsulation revolutionizes industries through enhanced stability, controlled release, and targeted performance of active ingredients. The novel aspect of this study explores the impact of the wall material-to-active (WM:A) ratio on the stability of ascorbic acid (AA) encapsulated in a maltodextrin (MD) and gum arabic (GA) blend (2:1 w/w). Microparticles were spray-dried and analyzed using SEM, TGA, DSC, thermal stability, and antioxidant activity assessments. Stability tests under different conditions revealed that a higher WM:A ratio (7:1) improved the active stability and antioxidant activity during storage, highlighting its importance in the encapsulation process. SEM analysis confirmed particles with no cracks, and the particles demonstrated excellent thermal stability up to 200 °C with minimal degradation. These findings underscore the critical role of the WM:A ratio in determining the stability of encapsulated AA within a carbohydrate matrix, offering valuable insights for advancing encapsulation technologies.

4.
Food Chem ; 460(Pt 3): 140755, 2024 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-39121768

RESUMO

In this paper, tiger nut oil-loaded microcapsules (TNOMs) were prepared by complexation soybean protein isolate (SPI) and maltodextrin (MD) as wall materials using the spray drying method with tiger nut oil (TNO) as the core material, and its physicochemical properties and stabilities were characterized and analyzed. Under the optimum conditions, the encapsulation efficiency (EE) of TNOMs could reach up to 91.23%. Of note, after 60 days of storage at 60 °C, the peroxide value (PV) of TNO was almost 21.8 times as much as that of TNO encapsulated. Furthermore, TNOMs had good thermal stability below 200 °C and are sufficient for the general food processing needs. By fitting Arrhenius oxidation kinetics model, it was predicted that the shelf life of the product stored at 25 °C was 352.48 d. Therefore, it is promised to be applied to the development of high oleic acid food in the future. This study offered a theoretical framework for utilization and broadening the range of applications of TNO in the food industry.

5.
Heliyon ; 10(13): e33544, 2024 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-39040403

RESUMO

AÒ«ai fruit is characterized by the properties of its bioactive compounds; however, this fruit is highly perishable and its compounds are sensitive when exposed to non-optimal environmental factors. Therefore, the objective of this study was to encapsulate the fruit pulp by spray drying to improve the nutritional value and extend the shelf life of the products derived from acai fruit. Maltodextrin was used as a wall material and the process was optimized to obtain the desirable values of the response variables. For this, a central compound design (CCD) was developed to determine the influence of temperature (110-170 °C) and the wall material proportion (5-15 %) on dependent variables: the retention of ascorbic acid, moisture percentage, hygroscopicity, solubility, water activity, and yield. Furthermore, the effects of spray drying on bioactive compounds (AA, TPC, TFC, TA, TCC, GA, CT, and QC) and antioxidant activity (ABTS, DPPH, and ORAC) were evaluated. The maximum design temperature (170 °C) and wall material proportion (15 %) significantly influenced the response variables where encapsulation was applied, with high ascorbic acid retention (96.886 %), low moisture (0.303 %), low hygroscopicity (7.279 g/100 g), low level of water activity (0.255), a water solubility index of 23.206 %, and a high yield of 70.285 %. The bioactive compounds analyzed and the antioxidant capacity presented significant retention values for AA (96.86 %), TPC (65.13 %), TFC (82.09 %), TA (62.46 %), TCC (7.28 %), GA (35.02 %), CT (49.03 %), QC (37.57 %), ABTS (81.24 %), DPPH (75.11 %), and ORAC (15.68 %). Therefore, it is concluded that the powder obtained under these conditions has desirable physical properties, and the drying process preserved a notable retention of bioactive compounds and their antioxidant activities.

6.
J Sep Sci ; 47(14): e2400141, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-39054594

RESUMO

Hydroxyapatite (HAp) is a calcium phosphate ceramic, widely used as a matrix for protein chromatography. The crystal structure of HAp is amenable to a wide range of substitutions, thus allowing for the alteration of its properties. In this study, nickel-ion substituted HAp (NiSHAp) was synthesized using a wet-precipitation method, followed by spray drying. This resulted in the structural incorporation of nickel ions within well-defined microspheres, which were suitable for chromatographic applications. The chromatographic experiments were conducted with NiSHAp and compared with spray-dried hydroxyapatite (SHAp) matrices. Protein purification experiments were conducted using refolded recombinant L-asparaginase (L-Asp), which was produced as inclusion bodies in Escherichia coli. The results showed that NiSHAp effectively adsorbed L-Asp, which was selectively eluted using a phosphate buffer, surpassing the efficiency of imidazole-based elution. In contrast, SHAp showed weaker binding and lower selectivity. The significance of this study lies in developing a scalable NiSHAp matrix for protein purification, especially for large-scale applications. The NiSHAp matrix offers a cost-effective alternative to commercial immobilized metal affinity chromatography (IMAC) adsorbents, especially for purifying His-tagged proteins. This innovative approach exhibits the advantages of mixed-mode chromatography by combining the properties of hydroxyapatite and IMAC in a single matrix, with the potential of improved industrial-scale protein purification.


Assuntos
Cromatografia de Afinidade , Durapatita , Níquel , Proteínas Recombinantes , Durapatita/química , Cromatografia de Afinidade/métodos , Níquel/química , Proteínas Recombinantes/química , Proteínas Recombinantes/isolamento & purificação , Escherichia coli/química , Adsorção
7.
Int J Biol Macromol ; 276(Pt 1): 133736, 2024 Jul 09.
Artigo em Inglês | MEDLINE | ID: mdl-38992543

RESUMO

Pea peptides can lead to degradation through oxidation, deamidation, hydrolysis, or cyclization during production, processing, and storage, which in turn limit their broader application. To stabilize pea peptides, this study employed spray drying technology to create a pea peptide micro-encapsule using maltodextrin, gum tragacanth, and pea peptides. Four key factors, including polysaccharide ratio, glycopeptide ratio, solid-liquid ratio, and inlet temperature, were optimized to enhance the antioxidant properties of the pea peptide micro-encapsule. The results indicated that the utilization of maltodextrin and gum tragacanth significantly improves the storage stability and antioxidant activity of pea peptides. Moreover, optimal storage stability for pea peptides was achieved with a polysaccharide ratio of 9:1, a glycopeptide ratio of 10:1, a solid-liquid ratio of 4:40, and an inlet temperature of 180 °C. After 60 days of storage, the encapsulated pea peptides maintained 70.22 %, 25.19 %, and 40.32 % for scavenging abilities to hydroxyl radical, superoxide anion, and ABTS radical, respectively. In contrast, the unencapsulated pea peptides showed a decline to 47.02 %, 0 %, and 24.46 % in the same antioxidant activities after storage. These findings underscore the potential of spray drying technology to enhance the functional properties of pea peptides for various applications.

8.
AAPS PharmSciTech ; 25(6): 164, 2024 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-38997569

RESUMO

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.


Assuntos
Clotrimazol , Nanopartículas , Suspensões , Clotrimazol/química , Clotrimazol/administração & dosagem , Nanopartículas/química , Suspensões/química , Secagem por Atomização , Química Farmacêutica/métodos , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Tamanho da Partícula , Varredura Diferencial de Calorimetria/métodos , Temperatura , Composição de Medicamentos/métodos , Polivinil/química , Difração de Raios X/métodos , Polietilenoglicóis
9.
Polymers (Basel) ; 16(13)2024 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-39000673

RESUMO

The aim of the study was to develop casein-fucoidan composite nanostructures through the method of polyelectrolyte complexation and subsequent spray drying. To determine the optimal parameters for the preparation of the composite structures and to investigate the influence of the production and technological parameters on the main structural and morphological characteristics of the obtained structures, 3(k-p) fractional factorial design was applied. The independent variables (casein to fucoidan ratio, glutaraldehyde concentration, and spray intensity) were varied at three levels (low, medium, and high) and their effect on the yield, the average particle size, and the zeta potential were evaluated statistically. Based on the obtained results, models C1F1G1Sp.30, C1F1G2Sp.40, and C1F1G3Sp.50, which have an average particle size ranging from (0.265 ± 0.03) µm to (0.357 ± 0.02) µm, a production yield in the range (48.9 ± 2.9) % to (66.4 ± 2.2) %, and a zeta potential varying from (-20.12 ± 0.9) mV to (-25.71 ± 1.0) mV, were selected as optimal for further use as drug delivery systems.

10.
Int J Mol Sci ; 25(13)2024 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-39000223

RESUMO

Microparticles as a multicompartment drug delivery system are beneficial for poorly soluble drugs. Mucoadhesive polymers applied in microparticle technology prolong the contact of the drug with the mucosa surface enhancing drug bioavailability and extending drug activity. Sodium alginate (ALG) and hydroxypropyl methylcellulose (hypromellose, HPMC) are polymers of a natural or semi-synthetic origin, respectively. They are characterized by mucoadhesive properties and are applied in microparticle technology. Spray drying is a technology employed in microparticle preparation, consisting of the atomization of liquid in a stream of gas. In this study, the pharmaceutical properties of spray-dried ALG/HPMC microparticles with posaconazole were compared with the properties of physical mixtures of powders with equal qualitative and quantitative compositions. Posaconazole (POS) as a relatively novel antifungal was utilized as a model poorly water-soluble drug, and hard gelatin capsules were applied as a reservoir for designed formulations. A release study in 0.1 M HCl showed significantly prolonged POS release from microparticles compared to a mixture of powders. Such a relationship was not followed in simulated vaginal fluid (SVF). Microparticles were also characterized by stronger mucoadhesive properties, an increased swelling ratio, and prolonged residence time compared to physical mixtures of powders. The obtained results indicated that the pharmaceutical properties of hard gelatin capsules filled with microparticles were significantly different from hard gelatin capsules with mixtures of powders.


Assuntos
Alginatos , Cápsulas , Sistemas de Liberação de Medicamentos , Gelatina , Derivados da Hipromelose , Triazóis , Alginatos/química , Gelatina/química , Derivados da Hipromelose/química , Sistemas de Liberação de Medicamentos/métodos , Triazóis/química , Triazóis/administração & dosagem , Triazóis/farmacocinética , Liberação Controlada de Fármacos , Preparações de Ação Retardada/química , Antifúngicos/administração & dosagem , Antifúngicos/química , Antifúngicos/farmacocinética , Microesferas
11.
Food Chem ; 459: 140336, 2024 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-39003859

RESUMO

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.

12.
Mar Drugs ; 22(7)2024 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-39057417

RESUMO

To improve probiotics' survivability during gastrointestinal digestion and heat treatment, Lactobacillus plantarum was microencapsulated by spray-drying using Laminaria japonica polysaccharide/sodium caseinate/gelatin (LJP/SC/GE) composites. Thermogravimetry and differential scanning calorimetry results revealed that the denaturation of LJP/SC/GE microcapsules requires higher thermal energy than that of SC/GE microcapsules, and the addition of LJP may improve thermal stability. Zeta potential measurements indicated that, at low pH of the gastric fluid, the negatively charged LJP attracted the positively charged SC/GE, helping to maintain an intact microstructure without disintegration. The encapsulation efficiency of L. plantarum-loaded LJP/SC/GE microcapsules reached about 93.4%, and the survival rate was 46.9% in simulated gastric fluid (SGF) for 2 h and 96.0% in simulated intestinal fluid (SIF) for 2 h. In vitro release experiments showed that the LJP/SC/GE microcapsules could protect the viability of L. plantarum in SGF and release probiotics slowly in SIF. The cell survival of LJP/SC/GE microcapsules was significantly improved during the heat treatment compared to SC/GE microcapsules and free cells. LJP/SC/GE microcapsules can increase the survival of L. plantarum by maintaining the lactate dehydrogenase and Na+-K+-ATPase activity. Overall, this study demonstrates the great potential of LJP/SC/GE microcapsules to protect and deliver probiotics in food and pharmaceutical systems.


Assuntos
Cápsulas , Temperatura Alta , Lactobacillus plantarum , Laminaria , Polissacarídeos , Laminaria/química , Polissacarídeos/farmacologia , Polissacarídeos/química , Probióticos/farmacologia , Probióticos/administração & dosagem , Digestão/efeitos dos fármacos , Trato Gastrointestinal/efeitos dos fármacos , Trato Gastrointestinal/microbiologia , Concentração de Íons de Hidrogênio , Gelatina/química , Gelatina/farmacologia , Viabilidade Microbiana/efeitos dos fármacos , Algas Comestíveis
13.
Pharmaceutics ; 16(7)2024 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-39065558

RESUMO

The study aimed to develop encapsulation systems to maintain the preservation of everlasting (Helichrysum plicatum) flower extract polyphenols. Spray-dried encapsulates were formulated using ß-cyclodextrin (BCD) and 2-hydroxypropyl-ß-cyclodextrin (HPBCD) as supramolecular hosts, and their macromolecule mixtures with the conventional carriers, maltodextrin (MD) and whey protein (WP). The obtained microparticles were comparatively assessed regarding technological, physicochemical, and phytochemical properties. The highest yields were achieved by combining cyclodextrins with whey protein (73.96% for WP+BCD and 75.50% for WP+HPBCD compared to 62.48% of pure extract). The extract-carrier interactions and thermal stability were evaluated by FTIR and DSC analysis, suggesting successful entrapment within the carriers. Carriers reduced the particle diameter (3.99 to 4.86 µm compared to 6.49 µm of pure extract), classifying all encapsulates as microsystems. Carrier blends made the particle size distribution uniform, while SEM analysis revealed the production of more spherical and less aggregated particles. The HPBCD provided the highest encapsulation efficiency, with the highest content of detected aglycones and slightly lower values of their glycosylated forms. An analysis of the dual macromolecule encapsulation systems revealed the highest bioactive preservation potential for SHE+MD+BCD and SHE+WP+HPBCD. Overall, macromolecule combinations of cyclodextrins and conventional biopolymers in the spray-drying process can enhance the functional properties of H. plicatum extract.

14.
Pharmaceutics ; 16(7)2024 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-39065621

RESUMO

PROTACs, proteolysis targeting chimeras, are bifunctional molecules inducing protein degradation through a unique proximity-based mode of action. While offering several advantages unachievable by classical drugs, PROTACs have unfavorable physicochemical properties that pose challenges in application and formulation. In this study, we show the solubility enhancement of two PROTACs, ARV-110 and SelDeg51, using Poly(vinyl alcohol). Hereby, we apply a three-fluid nozzle spray drying set-up to generate an amorphous solid dispersion with a 30% w/w drug loading with the respective PROTACs and the hydrophilic polymer. Dissolution enhancement was achieved and demonstrated for t = 0 and t = 4 weeks at 5 °C using a phosphate buffer with a pH of 6.8. A pH shift study on ARV-110-PVA is shown, covering transfer from simulated gastric fluid (SGF) at pH 2.0 to fasted-state simulated intestinal fluid (FaSSIF) at pH 6.5. Additionally, activity studies and binding assays of the pure SelDeg51 versus the spray-dried SelDeg51-PVA indicate no difference between both samples. Our results show how modern enabling formulation technologies can partially alleviate challenging physicochemical properties, such as the poor solubility of increasingly large 'small' molecules.

15.
Foods ; 13(14)2024 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-39063288

RESUMO

Cheese powder is a product resulting from the removal of moisture from cheese. At first, cheese emulsion is prepared by dissolving cheese(s) with water and calcium sequestering salts followed by drying. The desirable characteristics of cheese powder are high solubility, no lumps, storage stability, and imparting a typical cheesy flavor to the final product. Many current studies on cheese powder are focused on reducing calcium-sequestering salts (CSSs) to reduce the sodium content of cheese powder. This review discusses the production processes and physio-chemical properties of cheese emulsions and powders, aiming to enhance current understanding and identifying potential research gaps. Furthermore, strategies for producing cheese powder without CSSs, including pH adjustment, homogenization, and addition of dairy components such as buttermilk powder and sodium caseinate, are elaborated upon. Processing variables such as heating conditions during the preparation of cheese emulsion may vary with the type and age of the cheese used and product formulation. These conditions also effect the characteristics of cheese powders. On the other hand, producing a stable cheese emulsion without CSSs is challenging due to impaired emulsification of fat. The combined use of buttermilk powder and sodium caseinate among various alternatives has shown promising results in producing cheese powder without CSSs. However, future research on replacing CSSs should focus on combining two or more strategies together to produce cheese powder without CSSs. The combination of pH adjustment and dairy ingredients and the use of novel processing technologies with different ingredients are interesting alternatives.

16.
Water Res ; 261: 121998, 2024 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-38996735

RESUMO

The presence of active pharmaceutical ingredients (APIs) in wastewater effluents and natural aquatic systems threatens ecological and human health. While activated carbon-based adsorbents, such as GAC and PAC, are widely used for API removal, they exhibit certain deficiencies, including reduced performance due to the presence of natural organic macromolecules (NOMs) and high regeneration costs. There is growing demand for a robust, stable, and self-regenerative adsorbent designed for API removal in various environments. In this study, we synthesized a self-generating metal oxide nano-composite (S-MGC) containing titanium dioxide (TiO2) and silicon dioxide (SiO2) combined with 3D graphene oxide (GO) to adsorb APIs and undergo regeneration via light illumination. We determined optimal TiO2:SiO2:GO compositions for the S-MGCs through experiments using a model contaminant, methylene blue. The physical and chemical properties of S-MGCs were characterized, and their adsorption and photodegradation capabilities were studied using five model APIs, including sulfamethoxazole, carbamazepine, ketoprofen, valsartan, and diclofenac, both in single-component and multi-component mixtures. In the absence of TiO2/SiO2, 3D graphene oxide (CGB) displayed better adsorption performance compared to GAC, and S-MGCs further improve CGB's adsorption capacity. This performance remained consistent in two complex water environments: aqueous solutions at varying NOM levels and artificial urine. TiO2 supported on the GO surface exhibits similar photocatalytic activity to suspended TiO2. In a continuous fixed-bed column test, S-MGCs demonstrated robust API adsorption performance that is maintained in the presence of NOM or urine, and can be regenerated through multiple cycles of adsorption and light illumination.


Assuntos
Grafite , Poluentes Químicos da Água , Grafite/química , Adsorção , Poluentes Químicos da Água/química , Purificação da Água/métodos , Preparações Farmacêuticas/química , Dióxido de Silício/química , Titânio/química
17.
Int J Biol Macromol ; : 133754, 2024 Jul 17.
Artigo em Inglês | MEDLINE | ID: mdl-39084984

RESUMO

Hibiscus extract exhibits considerable antioxidant activity and a high anthocyanin content, which suggesting potential health benefits. However, these compounds are highly susceptible to environmental factors. The aim of this study was to establish the optimal conditions for the encapsulation of Hibiscus sabdariffa extract (HSE) using mixed porous maize starch-gum Arabic to enhance the stability of bioactive compounds under accelerated aging conditions. Response surface methodology (RSM) was used to optimize microencapsulation conditions through spray drying. The optimal conditions for microencapsulation of HSE by RSM were determined to be 126 °C at the inlet temperature (IT) and 8.5 % at the total solid content (TSC). Using these conditions, the amount of bioactive compounds in optimized microcapsules (OMs) was 2368 mg GAE/100 g, 694 mg QE/100 g, and 930 mg EC3G/100 g, of phenolic compounds, flavonoids, and anthocyanin, respectively. The release rate of anthocyanins during in vitro digestion was more effectively regulated in the OM sample, which retained up to 40 % of anthocyanins compared with 10 % in the HSE. The experimental values in this study exhibit high assertiveness, which renders the optimization model technologically and financially viable for the encapsulation of bioactive compounds with potential use in the food and pharmaceutical industries.

18.
Int J Pharm ; 662: 124466, 2024 Jul 14.
Artigo em Inglês | MEDLINE | ID: mdl-39009288

RESUMO

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.

19.
Int J Biol Macromol ; 275(Pt 2): 133615, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38960221

RESUMO

Microencapsulation has emerged as a promising strategy to enhance the stability and protection of bioactive compounds. In this work, roasted mate tea was microencapsulated using 15 % maltodextrin and lasiodiplodan (0.5-1.25 %) as wall coating materials. The microcapsules were characterized for encapsulation efficiency, hygroscopicity, moisture, water activity, water solubility, dissolubility, scanning electron microscopy, FT-IR spectroscopy, thermal analysis, colorimetry, antioxidant activity, as well as quantification of phenolic compounds and caffeine. Microencapsulation yields ranged from 44.92 to 56.39 %, and encapsulation efficiency varied from 66.54 to 70.16 by increasing the lasiodiplodan concentration. FT-IR revealed phenolic acids, flavonoids, and polyphenolics. Minor color variations were observed among the samples. Thermal analysis demonstrated the microencapsulates exhibited good thermal stability with no degradation below 250 °C. Encapsulated samples showed high levels of bioactive compounds, suggesting that microencapsulation by spray-drying was a favorable process, where maltodextrin, a low-cost protective agent, when combined with the properties of lasiodiplodan, can be a good option for stabilizing mate extracts.


Assuntos
Antioxidantes , Composição de Medicamentos , Polissacarídeos , Chá , Polissacarídeos/química , Composição de Medicamentos/métodos , Antioxidantes/química , Antioxidantes/farmacologia , Chá/química , Extratos Vegetais/química , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Cápsulas , beta-Glucanas/química , Polifenóis/química , Cafeína/química
20.
Int J Biol Macromol ; 275(Pt 1): 133626, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38964691

RESUMO

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.


Assuntos
Elétrons , Derivados da Hipromelose , Peso Molecular , Secagem por Atomização , Derivados da Hipromelose/química , Viscosidade , Pós , Tamanho da Partícula , Excipientes/química , Água/química
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