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Sample records for advanced spray-dried inhalable

  1. Design and physicochemical characterization of advanced spray-dried tacrolimus multifunctional particles for inhalation

    PubMed Central

    Wu, Xiao; Hayes, Don; Zwischenberger, Joseph B; Kuhn, Robert J; Mansour, Heidi M

    2013-01-01

    The aim of this study was to design, develop, and optimize respirable tacrolimus microparticles and nanoparticles and multifunctional tacrolimus lung surfactant mimic particles for targeted dry powder inhalation delivery as a pulmonary nanomedicine. Particles were rationally designed and produced at different pump rates by advanced spray-drying particle engineering design from organic solution in closed mode. In addition, multifunctional tacrolimus lung surfactant mimic dry powder particles were prepared by co-dissolving tacrolimus and lung surfactant mimic phospholipids in methanol, followed by advanced co-spray-drying particle engineering design technology in closed mode. The lung surfactant mimic phospholipids were 1,2-dipalmitoyl-sn-glycero-3-phosphocholine and 1,2-dipalmitoyl-sn-glycero-3-[phosphor-rac-1-glycerol]. Laser diffraction particle sizing indicated that the particle size distributions were suitable for pulmonary delivery, whereas scanning electron microscopy imaging indicated that these particles had both optimal particle morphology and surface morphology. Increasing the pump rate percent of tacrolimus solution resulted in a larger particle size. X-ray powder diffraction patterns and differential scanning calorimetry thermograms indicated that spray drying produced particles with higher amounts of amorphous phase. X-ray powder diffraction and differential scanning calorimetry also confirmed the preservation of the phospholipid bilayer structure in the solid state for all engineered respirable particles. Furthermore, it was observed in hot-stage micrographs that raw tacrolimus displayed a liquid crystal transition following the main phase transition, which is consistent with its interfacial properties. Water vapor uptake and lyotropic phase transitions in the solid state at varying levels of relative humidity were determined by gravimetric vapor sorption technique. Water content in the various powders was very low and well within the levels necessary

  2. Physicochemical characterization and water vapor sorption of organic solution advanced spray-dried inhalable trehalose microparticles and nanoparticles for targeted dry powder pulmonary inhalation delivery.

    PubMed

    Li, Xiaojian; Mansour, Heidi M

    2011-12-01

    Novel advanced spray-dried inhalable trehalose microparticulate/nanoparticulate powders with low water content were successfully produced by organic solution advanced spray drying from dilute solution under various spray-drying conditions. Laser diffraction was used to determine the volumetric particle size and size distribution. Particle morphology and surface morphology was imaged and examined by scanning electron microscopy. Hot-stage microscopy was used to visualize the presence/absence of birefringency before and following particle engineering design pharmaceutical processing, as well as phase transition behavior upon heating. Water content in the solid state was quantified by Karl Fisher (KF) coulometric titration. Solid-state phase transitions and degree of molecular order were examined by differential scanning calorimetry (DSC) and powder X-ray diffraction, respectively. Scanning electron microscopy showed a correlation between particle morphology, surface morphology, and spray drying pump rate. All advanced spray-dried microparticulate/nanoparticulate trehalose powders were in the respirable size range and exhibited a unimodal distribution. All spray-dried powders had very low water content, as quantified by KF. The absence of crystallinity in spray-dried particles was reflected in the powder X-ray diffractograms and confirmed by thermal analysis. DSC thermal analysis indicated that the novel advanced spray-dried inhalable trehalose microparticles and nanoparticles exhibited a clear glass transition (T(g)). This is consistent with the formation of the amorphous glassy state. Spray-dried amorphous glassy trehalose inhalable microparticles and nanoparticles exhibited vapor-induced (lyotropic) phase transitions with varying levels of relative humidity as measured by gravimetric vapor sorption at 25°C and 37°C.

  3. Design, Characterization, and Aerosol Dispersion Performance Modeling of Advanced Spray-Dried Microparticulate/Nanoparticulate Mannitol Powders for Targeted Pulmonary Delivery as Dry Powder Inhalers

    PubMed Central

    Li, Xiaojian; Vogt, Frederick G.; Hayes, Don

    2014-01-01

    Abstract Background: The purpose was to design and characterize inhalable microparticulate/nanoparticulate dry powders of mannitol with essential particle properties for targeted dry powder delivery for cystic fibrosis mucolytic treatment by dilute organic solution spray drying, and, in addition, to tailor and correlate aerosol dispersion performance delivered as dry powder inhalers based on spray-drying conditions and solid-state physicochemical properties. Methods: Organic solution advanced spray drying from dilute solution followed by comprehensive solid-state physicochemical characterization and in vitro dry powder aerosolization were used. Results: The particle size distribution of the spray-dried (SD) powders was narrow, unimodal, and in the range of ∼500 nm to 2.0 μm. The particles possessed spherical particle morphology, relatively smooth surface morphology, low water content and vapor sorption (crystallization occurred at exposure above 65% relative humidity), and retention of crystallinity by polymorphic interconversion. The emitted dose, fine particle fraction (FPF), and respirable fraction (RF) were all relatively high. The mass median aerodynamic diameters were below 4 μm for all SD mannitol aerosols. Conclusion: The in vitro aerosol deposition stage patterns could be tailored based on spray-drying pump rate. Positive linear correlation was observed between both FPF and RF values with spray-drying pump rates. The interplay between various spray-drying conditions, particle physicochemical properties, and aerosol dispersion performance was observed and examined, which enabled tailoring and modeling of high aerosol deposition patterns. PMID:24502451

  4. Design, characterization, and aerosolization of organic solution advanced spray-dried moxifloxacin and ofloxacin dipalmitoylphosphatidylcholine (DPPC) microparticulate/nanoparticulate powders for pulmonary inhalation aerosol delivery

    PubMed Central

    Duan, Jinghua; Vogt, Frederick G; Li, Xiaojian; Hayes, Don; Mansour, Heidi M

    2013-01-01

    The aim of this study was to design and develop respirable antibiotics moxifloxacin (MOXI) hydrochloride and ofloxacin (OFLX) microparticles and nanoparticles, and multifunctional antibiotics particles with or without lung surfactant 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) for targeted dry powder inhalation delivery as a pulmonary nanomedicine. Particles were rationally designed and produced by advanced spray-drying particle engineering from an organic solution in closed mode (no water) from dilute solution. Scanning electron microscopy indicated that these particles had both optimal particle morphology and surface morphology, and the particle size distributions were suitable for pulmonary delivery. Comprehensive and systematic physicochemical characterization and in vitro aerosol dispersion performance revealed significant differences between these two fluoroquinolone antibiotics following spray drying as drug aerosols and as cospray-dried antibiotic drug: DPPC aerosols. Fourier transform infrared spectroscopy and confocal Raman microspectroscopy were employed to probe composition and interactions in the solid state. Spray-dried MOXI was rendered noncrystalline (amorphous) following organic solution advanced spray drying. This was in contrast to spray-dried OFLX, which retained partial crystallinity, as did OFLX:DPPC powders at certain compositions. Aerosol dispersion performance was conducted using inertial impaction with a dry powder inhaler device approved for human use. The present study demonstrates that the use of DPPC offers improved aerosol delivery of MOXI as cospray-dried microparticulate/nanoparticulate powders, whereas residual partial crystallinity influenced aerosol dispersion of OFLX and most of the compositions of OFLX:DPPC inhalation powders. PMID:24092972

  5. Characterization and aerosol dispersion performance of advanced spray-dried chemotherapeutic PEGylated phospholipid particles for dry powder inhalation delivery in lung cancer.

    PubMed

    Meenach, Samantha A; Anderson, Kimberly W; Zach Hilt, J; McGarry, Ronald C; Mansour, Heidi M

    2013-07-16

    Pulmonary inhalation chemotherapeutic drug delivery offers many advantages for lung cancer patients in comparison to conventional systemic chemotherapy. Inhalable particles are advantageous in their ability to deliver drug deep in the lung by utilizing optimally sized particles and higher local drug dose delivery. In this work, spray-dried and co-spray dried inhalable lung surfactant-mimic PEGylated lipopolymers as microparticulate/nanoparticulate dry powders containing paclitaxel were rationally designed via organic solution advanced spray drying (no water) in closed-mode from dilute concentration feed solution. Dipalmitoylphosphatidylcholine (DPPC) and dipalmitoylphosphatidylethanolamine poly(ethylene glycol) (DPPE-PEG) with varying PEG chain length were mixed with varying amounts of paclitaxel in methanol to produce co-spray dried microparticles and nanoparticles. Scanning electron microscopy showed the spherical particle morphology of the inhalable particles. Thermal analysis and X-ray powder diffraction confirmed the retention of the phospholipid bilayer structure in the solid-state following spray drying, the degree of solid-state molecular order, and solid-state phase transition behavior. The residual water content of the particles was very low as quantified analytically Karl Fisher titration. The amount of paclitaxel loaded into the particles was quantified which indicated high encapsulation efficiencies (43-99%). Dry powder aerosol dispersion performance was measured in vitro using the Next Generation Impactor (NGI) coupled with the Handihaler dry powder inhaler device and showed mass median aerodynamic diameters in the range of 3.4-7 μm. These results demonstrate that this novel microparticulate/nanoparticulate chemotherapeutic PEGylated phospholipid dry powder inhalation aerosol platform has great potential in lung cancer drug delivery.

  6. Physicochemical characterization and aerosol dispersion performance of organic solution advanced spray-dried cyclosporine A multifunctional particles for dry powder inhalation aerosol delivery.

    PubMed

    Wu, Xiao; Zhang, Weifen; Hayes, Don; Mansour, Heidi M

    2013-01-01

    In this systematic and comprehensive study, inhalation powders of the polypeptide immunosuppressant drug - cyclosporine A - for lung delivery as dry powder inhalers (DPIs) were successfully designed, developed, and optimized. Several spray drying pump rates were rationally chosen. Comprehensive physicochemical characterization and imaging was carried out using scanning electron microscopy, hot-stage microscopy, differential scanning calorimetry, powder X-ray diffraction, Karl Fischer titration, laser size diffraction, and gravimetric vapor sorption. Aerosol dispersion performance was conducted using a next generation impactor with a Food and Drug Administration-approved DPI device. These DPIs displayed excellent aerosol dispersion performance with high values in emitted dose, respirable fraction, and fine particle fraction. In addition, novel multifunctional inhalation aerosol powder formulations of cyclosporine A with lung surfactant-mimic phospholipids were also successfully designed and developed by advanced organic solution cospray drying in closed mode. The lung surfactantmimic phospholipids were 1,2-dipalmitoyl-sn-glycero-3-phosphocholine and 1,2-dipalmitoyl-snglycero- 3-(phosphor-rac-1-glycerol). These cyclosporine A lung surfactant-mimic aerosol powder formulations were comprehensively characterized. Powder X-ray diffraction and differential scanning calorimetry confirmed that the phospholipid bilayer structure in the solid state was preserved following advanced organic solution spray drying in closed mode. These novel multifunctional inhalation powders were optimized for DPI delivery with excellent aerosol dispersion performance and high aerosol performance parameters.

  7. Physicochemical characterization and aerosol dispersion performance of organic solution advanced spray-dried cyclosporine A multifunctional particles for dry powder inhalation aerosol delivery

    PubMed Central

    Wu, Xiao; Zhang, Weifen; Hayes, Don; Mansour, Heidi M

    2013-01-01

    In this systematic and comprehensive study, inhalation powders of the polypeptide immunosuppressant drug – cyclosporine A – for lung delivery as dry powder inhalers (DPIs) were successfully designed, developed, and optimized. Several spray drying pump rates were rationally chosen. Comprehensive physicochemical characterization and imaging was carried out using scanning electron microscopy, hot-stage microscopy, differential scanning calorimetry, powder X-ray diffraction, Karl Fischer titration, laser size diffraction, and gravimetric vapor sorption. Aerosol dispersion performance was conducted using a next generation impactor with a Food and Drug Administration-approved DPI device. These DPIs displayed excellent aerosol dispersion performance with high values in emitted dose, respirable fraction, and fine particle fraction. In addition, novel multifunctional inhalation aerosol powder formulations of cyclosporine A with lung surfactant-mimic phospholipids were also successfully designed and developed by advanced organic solution cospray drying in closed mode. The lung surfactantmimic phospholipids were 1,2-dipalmitoyl-sn-glycero-3-phosphocholine and 1,2-dipalmitoyl-snglycero- 3-(phosphor-rac-1-glycerol). These cyclosporine A lung surfactant-mimic aerosol powder formulations were comprehensively characterized. Powder X-ray diffraction and differential scanning calorimetry confirmed that the phospholipid bilayer structure in the solid state was preserved following advanced organic solution spray drying in closed mode. These novel multifunctional inhalation powders were optimized for DPI delivery with excellent aerosol dispersion performance and high aerosol performance parameters. PMID:23569375

  8. Advanced spray-dried design, physicochemical characterization, and aerosol dispersion performance of vancomycin and clarithromycin multifunctional controlled release particles for targeted respiratory delivery as dry powder inhalation aerosols.

    PubMed

    Park, Chun-Woong; Li, Xiaojian; Vogt, Frederick G; Hayes, Don; Zwischenberger, Joseph B; Park, Eun-Seok; Mansour, Heidi M

    2013-10-15

    Respirable microparticles/nanoparticles of the antibiotics vancomycin (VCM) and clarithromycin (CLM) were successfully designed and developed by novel organic solution advanced spray drying from methanol solution. Formulation optimization was achieved through statistical experimental design of pump feeding rates of 25% (Low P), 50% (Medium P) and 75% (High P). Systematic and comprehensive physicochemical characterization and imaging were carried out using scanning electron microscopy (SEM), hot-stage microscopy (HSM), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Karl Fischer titration (KFT), laser size diffraction (LSD), gravimetric vapor sorption (GVS), confocal Raman microscopy (CRM) and spectroscopy for chemical imaging mapping. These novel spray-dried (SD) microparticulate/nanoparticulate dry powders displayed excellent aerosol dispersion performance as dry powder inhalers (DPIs) with high values in emitted dose (ED), respirable fraction (RF), and fine particle fraction (FPF). VCM DPIs displayed better aerosol dispersion performance compared to CLM DPIs which was related to differences in the physicochemical and particle properties of VCM and CLM. In addition, organic solution advanced co-spray drying particle engineering design was employed to successfully produce co-spray-dried (co-SD) multifunctional microparticulate/nanoparticulate aerosol powder formulations of VCM and CLM with the essential lung surfactant phospholipid, dipalmitoylphosphatidylcholine (DPPC), for controlled release pulmonary nanomedicine delivery as inhalable dry powder aerosols. Formulation optimization was achieved through statistical experimental design of molar ratios of co-SD VCM:DPPC and co-SD CLM:DPPC. XRPD and DSC confirmed that the phospholipid bilayer structure in the solid-state was preserved following spray drying. Co-SD VCM:DPPC and co-SD CLM:DPPC dry powder aerosols demonstrated controlled release of antibiotic drug that was fitted to various

  9. Design, physicochemical characterization, and optimization of organic solution advanced spray-dried inhalable dipalmitoylphosphatidylcholine (DPPC) and dipalmitoylphosphatidylethanolamine poly(ethylene glycol) (DPPE-PEG) microparticles and nanoparticles for targeted respiratory nanomedicine delivery as dry powder inhalation aerosols.

    PubMed

    Meenach, Samantha A; Vogt, Frederick G; Anderson, Kimberly W; Hilt, J Zach; McGarry, Ronald C; Mansour, Heidi M

    2013-01-01

    Novel advanced spray-dried and co-spray-dried inhalable lung surfactant-mimic phospholipid and poly(ethylene glycol) (PEG)ylated lipopolymers as microparticulate/nanoparticulate dry powders of biodegradable biocompatible lipopolymers were rationally formulated via an organic solution advanced spray-drying process in closed mode using various phospholipid formulations and rationally chosen spray-drying pump rates. Ratios of dipalmitoylphosphatidylcholine (DPPC) and dipalmitoylphosphatidylethanolamine PEG (DPPE-PEG) with varying PEG lengths were mixed in a dilute methanol solution. Scanning electron microscopy images showed the smooth, spherical particle morphology of the inhalable particles. The size of the particles was statistically analyzed using the scanning electron micrographs and SigmaScan® software and were determined to be 600 nm to 1.2 μm in diameter, which is optimal for deep-lung alveolar penetration. Differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) were performed to analyze solid-state transitions and long-range molecular order, respectively, and allowed for the confirmation of the presence of phospholipid bilayers in the solid state of the particles. The residual water content of the particles was very low, as quantified analytically via Karl Fischer titration. The composition of the particles was confirmed using attenuated total-reflectance Fourier-transform infrared (ATR-FTIR) spectroscopy and confocal Raman microscopy (CRM), and chemical imaging confirmed the chemical homogeneity of the particles. The dry powder aerosol dispersion properties were evaluated using the Next Generation Impactor™ (NGI™) coupled with the HandiHaler® dry powder inhaler device, where the mass median aerodynamic diameter from 2.6 to 4.3 μm with excellent aerosol dispersion performance, as exemplified by high values of emitted dose, fine particle fraction, and respirable fraction. Overall, it was determined that the pump rates defined in the

  10. Physicochemical characterization and aerosol dispersion performance of organic solution advanced spray-dried microparticulate/nanoparticulate antibiotic dry powders of tobramycin and azithromycin for pulmonary inhalation aerosol delivery.

    PubMed

    Li, Xiaojian; Vogt, Frederick G; Hayes, Don; Mansour, Heidi M

    2014-02-14

    The purpose of this study was to systematically design pure antibiotic drug dry powder inhalers (DPIs) for targeted antibiotic pulmonary delivery in the treatment of pulmonary infections and comprehensively correlate the physicochemical properties in the solid-state and spray-drying conditions effects on aerosol dispersion performance as dry powder inhalers (DPIs). The two rationally chosen model antibiotic drugs, tobramycin (TOB) and azithromycin (AZI), represent two different antibiotic drug classes of aminoglycosides and macrolides, respectively. The particle size distributions were narrow, unimodal, and in the microparticulate/nanoparticulate size range. The SD particles possessed relatively spherical particle morphology, smooth surface morphology, low residual water content, and the absence of long-range molecular order. The emitted dose (ED%), fine particle fraction (FPF%) and respirable fraction (RF%) were all excellent. The MMAD values were in the inhalable range (<10 μm) with smaller MMAD values for SD AZI powders in contrast to SD TOB powders. Positive linear correlations were observed between the aerosol dispersion performance parameter of FPF with increasing spray-drying pump rates and also with the difference between thermal parameters expressed as Tg-To (i.e. the difference between the glass transition temperature and outlet temperature) for SD AZI powders. The aerosol dispersion performance for SD TOB appeared to be influenced by its high water vapor sorption behavior (hygroscopicity) and pump rates or To. Aerosol dispersion performance of SD powders were distinct for both antibiotic drug aerosol systems and also between different pump rates for each system.

  11. Design, characterization, and aerosol dispersion performance modeling of advanced co-spray dried antibiotics with mannitol as respirable microparticles/nanoparticles for targeted pulmonary delivery as dry powder inhalers.

    PubMed

    Li, Xiaojian; Vogt, Frederick G; Hayes, Don; Mansour, Heidi M

    2014-09-01

    Dry powder inhalation aerosols of antibiotic drugs (a first-line aminoglycoside, tobramycin, and a first-line macrolide, azithromycin) and a sugar alcohol mucolytic agent (mannitol) as co-spray dried (co-SD) particles at various molar ratios of drug:mannitol were successfully produced by organic solution advanced co-spray drying from dilute solute concentration. These microparticulate/nanoparticulate aerosols consisting of various antibiotic drug:mannitol molar ratios were rationally designed with a narrow and unimodal primary particle size distribution, spherical particle shape, relatively smooth particle surface, and very low residual water content to minimize the interparticulate interactions and enhance in vitro aerosolization. These microparticulate/nanoparticulate inhalation powders were high-performing aerosols as reflected in the aerosol dispersion performance parameters of emitted dose, fine particle fraction (FPF), respirable fraction (RF), and mass median aerodynamic diameter (MMAD). The glass transition temperature (Tg) values were significantly above room temperature, which indicated that the co-SD powders were all in the amorphous glassy state. The Tg values for co-SD tobramycin:mannitol powders were significantly lower than those for co-SD azithromycin:mannitol powders. The interplay between aerosol dispersion performance parameters and Tg was modeled where higher Tg values (i.e., more ordered glass) were correlated with higher values in FPF and RF and lower values in MMAD.

  12. Spray drying of siRNA-containing PLGA nanoparticles intended for inhalation.

    PubMed

    Jensen, Ditte Marie Krohn; Cun, Dongmei; Maltesen, Morten Jonas; Frokjaer, Sven; Nielsen, Hanne Mørck; Foged, Camilla

    2010-02-25

    Local delivery of small interfering RNA (siRNA) to the lungs constitutes a promising new area in drug delivery. The present study evaluated parameters of importance for spray drying of siRNA-loaded poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles (NPs) into nanocomposite microparticles intended for inhalation. The spray drying process was optimised using a statistical design of experiment and by evaluating powder characteristics upon systematic variation of the formulation parameters. Concentration, carbohydrate excipient (trehalose, lactose and mannitol) and the ratio of NP to excipient were varied to monitor the effects on moisture content, particle morphology, particle size and powder yield. The identified optimum conditions were applied for spray drying of siRNA-loaded nanocomposite microparticles, resulting in a product with a low water content (0.78% w/w) and an aerodynamic particle diameter considered suitable for inhalation. The use of mannitol in the formulation allowed a significantly lower moisture content than trehalose and lactose. The inclusion of 50% (w/w) or higher amounts of NPs resulted in a marked change in the surface morphology of the spray-dried particles. Importantly, the integrity and biological activity of the siRNA were preserved during the spray drying process. In conclusion, the present results show that spray drying is a suitable technique for producing nanocomposite microparticles comprising siRNA-containing PLGA NPs for potential use in inhalation therapy.

  13. Inhalable spray-dried formulation of D-LAK antimicrobial peptides targeting tuberculosis.

    PubMed

    Kwok, Philip Chi Lip; Grabarek, Adam; Chow, Michael Y T; Lan, Yun; Li, Johnny C W; Casettari, Luca; Mason, A James; Lam, Jenny K W

    2015-08-01

    Tuberculosis (TB) is a global disease that is becoming more difficult to treat due to the emergence of multidrug resistant (MDR) Mycobacterium tuberculosis. Inhalable antimicrobial peptides (AMPs) are potentially useful alternative anti-TB agents because they can overcome resistance against classical antibiotics, reduce systemic adverse effects, and achieve local targeting. The aims of the current study were to produce inhalable dry powders containing d-enantiomeric AMPs (D-LAK120-HP13 and D-LAK120-A) and evaluate their solid state properties, aerosol performance, and structural conformation. These two peptides were spray dried with mannitol as a bulking agent at three mass ratios (peptide:mannitol 1:99, 1:49, and 1:24) from aqueous solutions. The resultant particles were spherical, with those containing D-LAK120-HP13 being more corrugated than those with D-LAK120-A. The median volumetric diameter of the particles was approximately 3μm. The residual water content of all powders were <3% w/w and crystalline, due to the low hygroscopicity and crystallinity of mannitol, respectively. The mannitol changed from a mixture of alpha- and beta-forms to delta form with an increasing proportion of AMP in the formulation. The emitted fraction and fine particle fraction of the powders when dispersed from an Osmohaler(®) at 90L/min were about 80% and 50-60% of the loaded dose, respectively, indicating good aerosol performance. Circular dichroism data showed that D-LAK120-HP13 dissolved in Tris buffer at pH 7.15 was of a disordered conformation. In contrast, D-LAK120-A showed greater α-helical conformation. Since the conformations of the AMPs were comparable to the controls (unprocessed peptides), the spray drying process did not substantially affect their secondary structures. In conclusion, spray dried powders containing d-enantiomeric AMPs with preserved secondary molecular structures and good aerosol performance could be successfully produced. They may potentially be used

  14. Spray dried amikacin powder for inhalation in cystic fibrosis patients: a quality by design approach for product construction.

    PubMed

    Belotti, Silvia; Rossi, Alessandra; Colombo, Paolo; Bettini, Ruggero; Rekkas, Dimitrios; Politis, Stavros; Colombo, Gaia; Balducci, Anna Giulia; Buttini, Francesca

    2014-08-25

    An amikacin product for convenient and compliant inhalation in cystic fibrosis patients was constructed by spray-drying in order to produce powders of pure drug having high respirability and flowability. An experimental design was applied as a statistical tool for the characterization of amikacin spray drying process, through the establishment of mathematical relationships between six Critical Quality Attributes (CQAs) of the finished product and five Critical Process Parameters (CPPs). The surface-active excipient, PEG-32 stearate, studied for particle engineering, in general did not benefit the CQAs of the spray dried powders for inhalation. The spray drying feed solution required the inclusion of 10% (v/v) ethanol in order to reach the desired aerodynamic performance of powders. All desirable function solutions indicated that the favourable concentration of amikacin in the feed solution had to be kept at 1% w/v level. It was found that when the feed rate of the sprayed solution was raised, an increase in the drying temperature to the maximum value (160 °C) was required to maintain good powder respirability. Finally, the increase in drying temperature always led to an evident increase in emitted dose (ED) without affecting the desirable fine particle dose (FPD) values. The application of the experimental design enabled us to obtain amikacin powders with both ED and FPD, well above the regulatory and scientific references. The finished product contained only the active ingredient, which keeps low the mass to inhale for dose requirement.

  15. Physicochemical and in vitro deposition properties of salbutamol sulphate/ipratropium bromide and salbutamol sulphate/excipient spray dried mixtures for use in dry powder inhalers.

    PubMed

    Corrigan, Deirdre O; Corrigan, Owen I; Healy, Anne Marie

    2006-09-28

    The physicochemical and aerodynamic properties of spray dried powders of the drug/drug mixture salbutamol sulphate/ipratropium bromide were investigated. The in vitro deposition properties of spray dried salbutamol sulphate and the spray dried drug/excipient mixtures salbutamol sulphate/lactose and salbutamol sulphate/PEG were also determined. Spray drying ipratropium bromide monohydrate resulted in a crystalline material from both aqueous and ethanolic solution. The product spray dried from aqueous solution consisted mainly of ipratropium bromide anhydrous. There was evidence of the presence of another polymorphic form of ipratropium bromide. When spray dried from ethanolic solution the physicochemical characterisation suggested the presence of an ipratropium bromide solvate with some anhydrous ipratropium bromide. Co-spray drying salbutamol sulphate with ipratropium bromide resulted in amorphous composites, regardless of solvent used. Particles were spherical and of a size suitable for inhalation. Twin impinger studies showed an increase in the fine particle fraction (FPF) of spray dried salbutamol sulphate compared to micronised salbutamol sulphate. Co-spray dried salbutamol sulphate:ipratropium bromide 10:1 and 5:1 systems also showed an increase in FPF compared to micronised salbutamol sulphate. Most co-spray dried salbutamol sulphate/excipient systems investigated demonstrated FPFs greater than that of micronised drug alone. The exceptions to this were systems containing PEG 4000 20% or PEG 20,000 40% both of which had FPFs not significantly different from micronised salbutamol sulphate. These two systems were crystalline unlike most of the other spray dried composites examined which were amorphous in nature.

  16. Biologic comparison of inhaled insulin formulations: Exubera™ and novel spray-dried engineered particles of dextran-10.

    PubMed

    Kuehl, Philip J; Cherrington, Alan; Dobry, Dan E; Edgerton, Dale; Friesen, Dwayne T; Hobbs, Charles; Leach, Chet L; Murri, Brice; Neal, Doss; Lyon, David K; Vodak, David T; Reed, Matthew D

    2014-12-01

    Inhaled peptides and proteins have promise for respiratory and systemic disease treatment. Engineered spray-dried powder formulations have been shown to stabilize peptides and proteins and optimize aerosol properties for pulmonary delivery. The current study was undertaken to investigate the in vitro and in vivo inhalation performance of a model spray-dried powder of insulin and dextran 10 in comparison to Exubera™. Dextrans are a class of glucans that are generally recognized as safe with optimum glass transition temperatures well suited for spray drying. A 70% insulin particle loading was prepared by formulating with 30% (w/v) dextran 10. Physical characterization revealed a "raisin like" particle. Both formulations were generated to produce a similar bimodal particle size distribution of less than 3.5 μm MMAD. Four female Beagle dogs were exposed to each powder in a crossover design. Similar presented and inhaled doses were achieved with each powder. Euglycemia was achieved in each dog prior and subsequent to dosing and blood samples were drawn out to 245 min post-exposure. Pharmacokinetic analyses of post-dose insulin levels were similar for both powders. Respective dextran 10-insulin and Exubera exposures were similar producing near identical area under the curve (AUC), 7,728 ± 1,516 and 6,237 ± 2,621; concentration maximums (C max), 126 and 121 (μU/mL), and concentration-time maximums, 20 and 14 min, respectively. These results suggest that dextran-10 and other dextrans may provide a novel path for formulating peptides and proteins for pulmonary delivery.

  17. Preparation and characterization of spray-dried inhalable powders containing nanoaggregates for pulmonary delivery of anti-tubercular drugs.

    PubMed

    Kaur, Ranjot; Garg, Tarun; Das Gupta, Umesh; Gupta, Pushpa; Rath, Goutam; Goyal, Amit Kumar

    2016-01-01

    This study aims to prepare spray-dried inhalable powders containing anti-tubercular drugs-loaded HPMC nanoaggregates for sustained delivery of drugs to the lung. Nanoaggregates were prepared by precipitation technique. Results showed that the powders obtained had excellent aerosolization property. High drug encapsulation efficiency was achieved in HPMC nano aggregates, ranging from 60% to 70%. A single pulmonary dose resulted in therapeutic drug concentrations 40% to 60% in the lungs and in other organs (< 5%) for 24 h. From this study, we can conclude that delivering drugs through pulmonary route is advantageous for local action in lungs.

  18. Spray dried inhalable ciprofloxacin powder with improved aerosolisation and antimicrobial activity.

    PubMed

    Osman, Rihab; Kan, Pei Lee; Awad, Gehanne; Mortada, Nahed; El-Shamy, Abd-Elhameed; Alpar, Oya

    2013-06-05

    In this study, the spray drying technique was used to prepare ciprofloxacin microparticles (CFX-MPs) for pulmonary administration. By virtue of its amphoteric properties, CFX was dissolved in either a slightly alkaline or acidic solution depending on the used polymer. Dextran and chitosan were used to prepare the MPs and modify the release characteristics of the drug. Particle surface modification was done with either DPPC or PEG. The effects of the manufacturing and formulation parameters on the drug-polymer interactions were investigated by thermal analysis and infrared spectroscopy. CFX-MPs showed improved aerosolisation properties and the encapsulated drug possessed high antimicrobial activity against two of the common and resistant respiratory pathogens: Pseudomonas aeruginosa and Staphylococus aureus. MPs were safe on the lung epithelial cells. Modulation of particle characteristics and drug release was possible by altering not only the polymer but also the type of the acid from which the powders were spray dried. MPs prepared with glutamic and aspartic acids showed better characteristics than those prepared with acetic and hydrochloric acids. Dextran modified particles showed improved aerosolisation properties and safety on lung epithelial cells.

  19. Single step spray drying method to develop proliposomes for inhalation: a systematic study based on quality by design approach.

    PubMed

    Patil-Gadhe, Arpana; Pokharkar, Varsha

    2014-04-01

    Quality by Design (QbD) is a systematic approach to develop drug products which includes evaluation of formulation parameters to achieve defined final product quality. In the present study principles of QbD were extended to the preparation, in-vitro and in-vivo performance of rifapentine-loaded proliposomes for pulmonary inhalation where final product needs to comply with specific properties. The rifapentine-loaded proliposomes for the treatment of tuberculosis were prepared in single step by spray drying method and independent variables were optimized using factorial design approach. Contour plots and multiple regression analysis were used to study the effect of selected independent variables on dependent variables. The effect of presence of drug: hydrogenated soya phosphatidylcholine (HSPC) and type of charged lipid in the formulation at three levels were studied on mass median diameter (MMD), liposomal vesicle size, % encapsulation efficiency (% EE), mass median aerodynamic diameter (MMAD) and fine particle fraction (FPF) as critical quality attributes. Optimized formulation (R-LDPI-7) with drug: HSPC ratio of 1:2 and stearyl amine as charged lipid were found to give respirable proliposomes with MMAD of 1.56 ± 0.16 μm and FPF of 92.5 ± 1.5%. Sustained drug release with Higuchi diffusion kinetics was achieved from liposomally encapsulated rifapentine. Pulmonary pharmacokinetics of optimized batch R-LDPI-7 revealed longer retention of drug in lungs with 7 fold increase in both, the mean residence time and t1/2 as compared to R-DPI-0. The study results demonstrated the application of QbD principles and design of experiment (DOE) approach to develop drug encapsulated proliposomes for inhalation by spray drying in single step.

  20. Preparation of theophylline inhalable microcomposite particles by wet milling and spray drying: The influence of mannitol as a co-milling agent.

    PubMed

    Malamatari, Maria; Somavarapu, Satyanarayana; Kachrimanis, Kyriakos; Bloxham, Mark; Taylor, Kevin M G; Buckton, Graham

    2016-11-30

    Inhalable theophylline particles with various amounts of mannitol were prepared by combining wet milling in isopropanol followed by spray drying. The effect of mannitol as a co-milling agent on the micromeritic properties, solid state and aerosol performance of the engineered particles was investigated. Crystal morphology modelling and geometric lattice matching calculations were employed to gain insight into the intermolecular interactions that may influence the mechanical properties of theophylline and mannitol. The addition of mannitol facilitated the size reduction of the needle-like crystals of theophylline and also their assembly in microcomposites by forming a porous structure of mannitol nanocrystals wherein theophylline particles are embedded. The microcomposites were found to be in the same crystalline state as the starting material(s) ensuring their long-term physical stability upon storage. Incorporation of mannitol resulted in microcomposite particles with smaller size, more spherical shape and increased porosity. The aerosol performance of the microcomposites was markedly enhanced compared to the spray-dried suspension of theophylline wet milled without mannitol. Overall, wet co-milling with mannitol in an organic solvent followed by spray drying may be used as a formulation approach for producing respirable particles of water-soluble drugs or drugs that are prone to crystal transformation in an aqueous environment (i.e. formation of hydrates).

  1. Preparation and physicochemical characterization of spray-dried and jet-milled microparticles containing bosentan hydrate for dry powder inhalation aerosols.

    PubMed

    Lee, Hyo-Jung; Kang, Ji-Hyun; Lee, Hong-Goo; Kim, Dong-Wook; Rhee, Yun-Seok; Kim, Ju-Young; Park, Eun-Seok; Park, Chun-Woong

    2016-01-01

    The objectives of this study were to prepare bosentan hydrate (BST) microparticles as dry powder inhalations (DPIs) via spray drying and jet milling under various parameters, to comprehensively characterize the physicochemical properties of the BST hydrate microparticles, and to evaluate the aerosol dispersion performance and dissolution behavior as DPIs. The BST microparticles were successfully prepared for DPIs by spray drying from feeding solution concentrations of 1%, 3%, and 5% (w/v) and by jet milling at grinding pressures of 2, 3, and 4 MPa. The physicochemical properties of the spray-dried (SD) and jet-milled (JM) microparticles were determined via scanning electron microscopy, atomic force microscopy, dynamic light scattering particle size analysis, Karl Fischer titration, surface analysis, pycnometry, differential scanning calorimetry, powder X-ray diffraction, and Fourier transform infrared spectroscopy. The in vitro aerosol dispersion performance and drug dissolution behavior were evaluated using an Anderson cascade impactor and a Franz diffusion cell, respectively. The JM microparticles exhibited an irregular corrugated surface and a crystalline solid state, while the SD microparticles were spherical with a smooth surface and an amorphous solid state. Thus, the in vitro aerosol dispersion performance and dissolution behavior as DPIs were considerably different due to the differences in the physicochemical properties of the SD and JM microparticles. In particular, the highest grinding pressures under jet milling exhibited excellent aerosol dispersion performance with statistically higher values of 56.8%±2.0% of respirable fraction and 33.8%±2.3% of fine particle fraction and lower mass median aerodynamic diameter of 5.0±0.3 μm than the others (P<0.05, analysis of variance/Tukey). The drug dissolution mechanism was also affected by the physicochemical properties that determine the dissolution kinetics of the SD and JM microparticles, which were well

  2. Preparation and physicochemical characterization of spray-dried and jet-milled microparticles containing bosentan hydrate for dry powder inhalation aerosols

    PubMed Central

    Lee, Hyo-Jung; Kang, Ji-Hyun; Lee, Hong-Goo; Kim, Dong-Wook; Rhee, Yun-Seok; Kim, Ju-Young; Park, Eun-Seok; Park, Chun-Woong

    2016-01-01

    The objectives of this study were to prepare bosentan hydrate (BST) microparticles as dry powder inhalations (DPIs) via spray drying and jet milling under various parameters, to comprehensively characterize the physicochemical properties of the BST hydrate microparticles, and to evaluate the aerosol dispersion performance and dissolution behavior as DPIs. The BST microparticles were successfully prepared for DPIs by spray drying from feeding solution concentrations of 1%, 3%, and 5% (w/v) and by jet milling at grinding pressures of 2, 3, and 4 MPa. The physicochemical properties of the spray-dried (SD) and jet-milled (JM) microparticles were determined via scanning electron microscopy, atomic force microscopy, dynamic light scattering particle size analysis, Karl Fischer titration, surface analysis, pycnometry, differential scanning calorimetry, powder X-ray diffraction, and Fourier transform infrared spectroscopy. The in vitro aerosol dispersion performance and drug dissolution behavior were evaluated using an Anderson cascade impactor and a Franz diffusion cell, respectively. The JM microparticles exhibited an irregular corrugated surface and a crystalline solid state, while the SD microparticles were spherical with a smooth surface and an amorphous solid state. Thus, the in vitro aerosol dispersion performance and dissolution behavior as DPIs were considerably different due to the differences in the physicochemical properties of the SD and JM microparticles. In particular, the highest grinding pressures under jet milling exhibited excellent aerosol dispersion performance with statistically higher values of 56.8%±2.0% of respirable fraction and 33.8%±2.3% of fine particle fraction and lower mass median aerodynamic diameter of 5.0±0.3 μm than the others (P<0.05, analysis of variance/Tukey). The drug dissolution mechanism was also affected by the physicochemical properties that determine the dissolution kinetics of the SD and JM microparticles, which were well

  3. Optimisation of spray-drying process variables for dry powder inhalation (DPI) formulations of corticosteroid/cyclodextrin inclusion complexes.

    PubMed

    Cabral-Marques, Helena; Almeida, Rita

    2009-09-01

    This study aims to develop and characterise a beclomethasone diproprionate:gamma-cyclodextrin (BDP:gamma-CYD) complex and to optimise the variables on the spray-drying process, in order to obtain a powder with the most suitable characteristics for lung delivery. The spray-dried powder--in a mass ratio of 2:5 (BDP:gamma-CYD)--was physically mixed with three carriers of different particle sizes and in different ratios. Particle-size distribution, shape and morphology, moisture content, and uniformity in BDP content of formulations were studied. In vitro aerolisation behaviour of the formulations was evaluated using the Rotahaler, and the performance was characterised based on the uniformity of emitted dose and aerodynamic particle-size distribution (respirable fraction (RF), as a percentage of nominal dose (RFN) and emitted dose (RFE)). The most suitable conditions for the preparation of BDP:gamma-CYD complexes were obtained with the solution flow of 5 ml/min, T(in) of 70 degrees C and T(out) of 50 degrees C. Statistically significant differences in the aerodynamic performances were obtained for formulations containing BDP:gamma-CYD complexes prepared using different solution flows and different T(in) (p<0.05). RFN and RFE vary in direct proportion with T(in), while an inverse relationship was observed for the solution flow. A direct correlation between the RFE and the T(out) was identified. Performance of the formulations was compared with an established commercial product (Beclotaide Rotacaps 100 microg) with improved performance of RF: formulations with respitose carrier attained RFN and RFE twofold greater, and formulations based on 63-90 microm fraction lactose and trehalose achieved a threefold improvement; also, all formulations showed that the percentage of dose of BDP deposited in the "oropharynx" compartment was reduced to half.

  4. A comparison between spray drying and spray freeze drying for dry powder inhaler formulation of drug-loaded lipid-polymer hybrid nanoparticles.

    PubMed

    Wang, Yajie; Kho, Katherine; Cheow, Wean Sin; Hadinoto, Kunn

    2012-03-15

    Lipid-polymer hybrid nanoparticles - polymeric nanoparticles enveloped by lipid layers - have emerged as a potent therapeutic nano-carrier alternative to liposomes and polymeric nanoparticles. Herein we perform comparative studies of employing spray drying (SD) and spray freeze drying (SFD) to produce inhalable dry-powder form of drug-loaded lipid-polymer hybrid nanoparticles. Poly(lactic-co-glycolic acid), lecithin, and levofloxacin are employed as the polymer, lipid, and drug models, respectively. The hybrid nanoparticles are transformed into micro-scale nanoparticle aggregates (or nano-aggregates) via SD and SFD, where the effects of (1) different excipients (i.e. mannitol, polyvinyl alcohol (PVA), and leucine), and (2) nanoparticle to excipient ratio on nano-aggregate characteristics (e.g. size, flowability, aqueous reconstitution, aerosolization efficiency) are examined. In both methods, PVA is found more effective than mannitol for aqueous reconstitution, whereas hydrophobic leucineis needed to achieve effective aerosolization as it reduces nano-aggregate agglomeration. Using PVA, both methods are equally capable of producing nano-aggregates having size, density, flowability, yield and reconstitutibility in the range ideal for inhaled delivery. Nevertheless, nano-aggregates produced by SFD are superior to SD in terms of their aerosolization efficiency manifested in the higher emitted dose and fine particle fraction with lower mass median aerodynamic diameter.

  5. No Heat Spray Drying Technology

    SciTech Connect

    Beetz, Charles

    2016-06-15

    No Heat Spray Drying Technology. ZoomEssence has developed our Zooming™ spray drying technology that atomizes liquids to powders at ambient temperature. The process of drying a liquid into a powder form has been traditionally achieved by mixing a heated gas with an atomized (sprayed) fluid within a vessel (drying chamber) causing the solvent to evaporate. The predominant spray drying process in use today employs air heated up to 400° Fahrenheit to dry an atomized liquid into a powder. Exposing sensitive, volatile liquid ingredients to high temperature causes molecular degradation that negatively impacts solubility, stability and profile of the powder. In short, heat is detrimental to many liquid ingredients. The completed award focused on several areas in order to advance the prototype dryer to a commercial scale integrated pilot system. Prior to the award, ZoomEssence had developed a prototype ‘no-heat’ dryer that firmly established the feasibility of the Zooming™ process. The award focused on three primary areas to improve the technology: (1) improved ability to formulate emulsions for specific flavor groups and improved understanding of the relationship of emulsion properties to final dry particle properties, (2) a new production atomizer, and (3) a dryer controls system.

  6. Spray drying formulation of amorphous solid dispersions.

    PubMed

    Singh, Abhishek; Van den Mooter, Guy

    2016-05-01

    Spray drying is a well-established manufacturing technique which can be used to formulate amorphous solid dispersions (ASDs) which is an effective strategy to deliver poorly water soluble drugs (PWSDs). However, the inherently complex nature of the spray drying process coupled with specific characteristics of ASDs makes it an interesting area to explore. Numerous diverse factors interact in an inter-dependent manner to determine the final product properties. This review discusses the basic background of ASDs, various formulation and process variables influencing the critical quality attributes (CQAs) of the ASDs and aspects of downstream processing. Also various aspects of spray drying such as instrumentation, thermodynamics, drying kinetics, particle formation process and scale-up challenges are included. Recent advances in the spray-based drying techniques are mentioned along with some future avenues where major research thrust is needed.

  7. Solid-state stability of spray-dried insulin powder for inhalation: chemical kinetics and structural relaxation modeling of Exubera above and below the glass transition temperature.

    PubMed

    Sadrzadeh, Negar; Miller, Danforth P; Lechuga-Ballesteros, David; Harper, Nancy J; Stevenson, Cynthia L; Bennett, David B

    2010-09-01

    The effect of temperature on the chemical stability of an amorphous spray-dried insulin powder formulation (Exubera) was evaluated in the solid state at constant moisture content. The chemical stability of the powder was assessed using reversed-phase high-performance liquid chromatography (RP-HPLC) and high-performance-size exclusion chromatography (HP-SEC). The major degradants in spray-dried insulin produced during heat stressing were identified as A21-desamidoinsulin (A21) and high molecular weight protein (HMWP). As expected, the rates of formation of A21 and HMWP were observed to increase with temperature. A stretched-time kinetic model (degradation rate is proportional to the square root of time) was applied to the degradant profiles above and below the glass transition temperature (T(g)) and apparent reaction rate constants were determined. Below T(g), isothermal enthalpy of relaxation measurements were used to assess the effect of temperature on molecular mobility. The formation of A21 and HMWP was found to follow an Arrhenius temperature dependence above and below the T(g). Comparison of reaction rate constants to those estimated from structural relaxation experiments suggests that the reaction pathways to form A21 and HMWP below the T(g) may be coupled with the molecular motions involved in structural relaxation.

  8. Review of patents and application of spray drying in pharmaceutical, food and flavor industry.

    PubMed

    Patel, Bhavesh B; Patel, Jayvadan K; Chakraborty, Subhashis

    2014-04-01

    Spray drying has always remained an energetic field of innovation in pharmaceutical, food and flavor industry since last couple of decades. The current communication embodies an in-depth application of spray drying in pulmonary drug delivery for production of uniform and respirable size particles suitable for nebulizers, dry powder inhalers (DPI) and pressurized metered dose inhalers (pMDI). The review also highlights spray drying application in the manufacturing of mucoadhesive formulation suitable for nasal cavities to improve the drug absorption and bioavailability. Recent research works and patents filed by various researchers on spray drying technology for solubility enhancement have also been accentuated. Benefits of spray drying in production of dry flavorings to meet a product with maximum yield and least flavor loss are also discussed. The use of spray drying in production of various food products like milk or soymilk powder, tomato pulp, dry fruit juice etc, and in encapsulation of vegetable oil or fish oil and dry creamer has been discussed. Current review also highlights the application of spray drying in the biotechnology field like production of dry influenza or measles vaccine as well as application in ceramic industry. Spray drying based patents issued by the U.S. Patent and Trademark Office in the area of drug delivery have also been included in the current review to emphasize importance of spray drying in the recent research scenario.

  9. Pharmaceutical Particle Engineering via Spray Drying

    PubMed Central

    2007-01-01

    This review covers recent developments in the area of particle engineering via spray drying. The last decade has seen a shift from empirical formulation efforts to an engineering approach based on a better understanding of particle formation in the spray drying process. Microparticles with nanoscale substructures can now be designed and their functionality has contributed significantly to stability and efficacy of the particulate dosage form. The review provides concepts and a theoretical framework for particle design calculations. It reviews experimental research into parameters that influence particle formation. A classification based on dimensionless numbers is presented that can be used to estimate how excipient properties in combination with process parameters influence the morphology of the engineered particles. A wide range of pharmaceutical application examples—low density particles, composite particles, microencapsulation, and glass stabilization—is discussed, with specific emphasis on the underlying particle formation mechanisms and design concepts. PMID:18040761

  10. Investigation of the Changes in Aerosolization Behavior Between the Jet-Milled and Spray-Dried Colistin Powders Through Surface Energy Characterization.

    PubMed

    Jong, Teresa; Li, Jian; Morton, David A V; Zhou, Qi Tony; Larson, Ian

    2016-03-01

    This study aimed to investigate the surface energy factors behind improved aerosolization performance of spray-dried colistin powder formulations compared with those produced by jet milling. Inhalable colistin powder formulations were produced by jet milling or spray drying (with or without l-leucine). Scanning electron micrographs showed the jet-milled particles had irregularly angular shapes, whereas the spray-dried particles were more spherical. Significantly higher fine particle fractions were measured for the spray-dried (43.8%-49.6%) versus the jet-milled formulation (28.4%) from a Rotahaler at 60 L/min; albeit the size distribution of the jet-milled powder was smaller. Surprisingly, addition of l-leucine in the spray drying feed solution gave no significant improvement in fine particle fraction. As measured by inverse gas chromatography, spray-dried formulations had significantly (p < 0.001) lower dispersive, specific, and total surface energy values and more uniform surface energy distributions than the jet-milled powder. Interestingly, no significant difference was measured in the specific and total surface energy values between the spray-dried formulation with or without l-leucine. Based on our previous findings in the self-assembling behavior of colistin in aqueous solution and the surface energy data obtained here, we propose the self-assembly of colistin molecules during spray drying contributed significantly to the reduction of surface free energy and the superior aerosolization performance.

  11. Investigation of the changes in aerosolization behavior between the jet-milled and spray-dried colistin powders through surface energy characterization

    PubMed Central

    Jong, Teresa; Li, Jian; Mortonx, David A.V.; Zhou, Qi (Tony); Larson, Ian

    2016-01-01

    This study aimed to investigate the surface energy factors behind improved aerosolization performance of spray-dried colistin powder formulations compared to those produced by jet-milling. Inhalable colistin powder formulations were produced by jet-milling or spray-drying (with or without L-leucine). Scanning electron micrographs showed the jet-milled particles had irregularly angular shapes, while the spray-dried particles were more spherical. Significantly higher fine particle fractions (FPFs) were measured for the spray-dried (43.8-49.6%) vs. the jet-milled formulation (28.4 %) from a Rotahaler at 60L/min; albeit the size distribution of the jet-milled powder was smaller. Surprisingly, addition of L-leucine in the spray drying feed-solution gave no significant improvement in FPF. As measured by inverse gas chromatography, spray-dried formulations had significantly (p<0.001) lower dispersive, specific and total surface energy values and more uniform surface energy distributions than the jet-milled powder. Interestingly, no significant difference was measured in the specific and total surface energy values between the spray-dried formulation with or without L-leucine. Based upon our previous findings in the self-assembling behavior of colistin in aqueous solution and the surface energy data obtained here, we propose the self-assembly of colistin molecules during spray-drying, contributed significantly to the reduction of surface free energy and the superior aerosolization performance. PMID:26886330

  12. Aerosolization properties, surface composition and physical state of spray-dried protein powders.

    PubMed

    Bosquillon, Cynthia; Rouxhet, Paul G; Ahimou, François; Simon, Denis; Culot, Christine; Préat, Véronique; Vanbever, Rita

    2004-10-19

    Powder aerosols made of albumin, dipalmitoylphosphatidylcholine (DPPC) and a protein stabilizer (lactose, trehalose or mannitol) were prepared by spray-drying and analyzed for aerodynamic behavior, surface composition and physical state. The powders exited a Spinhaler inhaler as particle aggregates, the size of which depending on composition, spray-drying parameters and airflow rate. However, due to low bulk powder tap density (<0.15 g/cm3), the aerodynamic size of a large fraction of aggregates remained respirable (<5 microm). Fine particle fractions ranged between 21% and 41% in an Andersen cascade impactor operated at 28.3 l/min, with mannitol and lactose providing the most cohesive and free-flowing powders, respectively. Particle surface analysis by X-ray photoelectron spectroscopy (XPS) revealed a surface enrichment with DPPC relative to albumin for powders prepared under certain spray-drying conditions. DPPC self-organized in a gel phase in the particle and no sugar or mannitol crystals were detected by X-ray diffraction. Water sorption isotherms showed that albumin protected lactose from moisture-induced crystallization. In conclusion, a proper combination of composition and spray-drying parameters allowed to obtain dry powders with elevated fine particle fractions (FPFs) and a physical environment favorable to protein stability.

  13. Preparation of nanoscale pulmonary drug delivery formulations by spray drying.

    PubMed

    Bohr, Adam; Ruge, Christian A; Beck-Broichsitter, Moritz

    2014-01-01

    Advances in preparation technologies for nanomedicines have provided novel formulations for pulmonary drug delivery. Application of drugs via the lungs can be considered as one of the most attractive implementations of nanoparticles for therapeutic use due to the unique anatomy and physiology of the lungs. The colloidal nature of nanoparticles provides important advantages to the formulation of drugs, which are normally difficult to administer due to poor stability or uptake, partly because nanoparticles protect the drug from the physiological milieu, facilitate transport across biological barriers and can offer controlled drug release. There are numerous methods for producing therapeutic nanoparticles, each with their own advantages and suitable application. Liquid atomization techniques such as spray drying can produce nanoparticle formulations in a dry powder form suitable for pulmonary administration in a direct one-step process. This chapter describes the different state-of-the-art techniques used to prepare drug nanoparticles (with special emphasize on spray drying techniques) and the strategies for administering such unique formulations to the pulmonary environment.

  14. Spray Drying of Mosambi Juice in Lab

    NASA Astrophysics Data System (ADS)

    Singh, S. V.; Verma, A.

    2014-01-01

    The studies on spray drying of mosambi juice were carried out with Laboratory spray dryer set-up (LSD-48 MINI SPRAY DRYER-JISL). Inlet and outlet air temperature and maltodextrin (drying agent) concentration was taken as variable parameters. Experiments were conducted by using 110 °C to 140 °C inlet air temperature, 60 °C to 70 °C outlet air temperature and 5-7 % maltodextrin concentration. The free flow powder of mosambi juice was obtained with 7 % maltodextrin at 140 °C inlet air temperature and 60 °C outlet air temperature. Fresh and reconstituted juices were evaluated for vitamin C, titrable acidity and sensory characteristics. The reconstituted juice was found slightly acceptable by taste panel.

  15. Quality characteristic of spray-drying egg white powders.

    PubMed

    Ma, Shuang; Zhao, Songning; Zhang, Yan; Yu, Yiding; Liu, Jingbo; Xu, Menglei

    2013-10-01

    Spray drying is a useful method for developing egg process and utilization. The objective of this study was to evaluate effects on spray drying condition of egg white. The optimized conditions were spraying flow 22 mL/min, feeding temperature 39.8 °C and inlet-air temperature 178.2 °C. Results of sulfydryl (SH) groups measurement indicated conformation structure have changed resulting in protein molecule occur S-S crosslinking phenomenon when heating. It led to free SH content decreased during spray drying process. There was almost no change of differential scanning calorimetry between fresh egg white and spray-drying egg white powder (EWP). For a given protein, the apparent SH reactivity is in turn influenced by the physico-chemical characteristics of the reactant. The phenomenon illustrated the thermal denaturation of these proteins was unrelated to their free SH contents. Color measurement was used to study browning level. EWP in optimized conditions revealed insignificant brown stain. Swelling capacity and scanning electron micrograph both proved well quality characteristic of spray-drying EWP. Results suggested spray drying under the optimized conditions present suitable and alternative method for egg processing industrial implementation. Egg food industrialization needs new drying method to extend shelf-life. The purpose of the study was to provide optimal process of healthy and nutritional instant spray-drying EWP and study quality characteristic of spray-drying EWP.

  16. The preparation of steatite suspension for spray drying

    NASA Technical Reports Server (NTRS)

    Jirousek, L.; Spicak, K.

    1983-01-01

    Liquifying agents were investigated for preparation of highly concentrated steatite suspensions which are to be spray-dried. Organic additives for improving the molding properties and strength of green compacts are described. Demands on properties of the spray-dried granules are defined with regard to shrinkage of the molded compacts.

  17. Microencapsulation of Lactobacillus casei by spray drying.

    PubMed

    Dos Santos, Rebeka Cristiane Silva; Finkler, Leandro; Finkler, Christine Lamenha Luna

    2014-01-01

    This study evaluates the use of spray drying to produce microparticles of Lactobacillus casei. Microorganism was cultivated in shaken flasks and the microencapsulation process was performed using a laboratory-scale spray dryer. A rotational central composite design was employed to optimise the drying conditions. High cell viability (1.1 × 10(10) CFU/g) was achieved using an inlet air temperature of 70 °C and 25% (w/v) of maltodextrin. Microparticles presented values of solubility, wettability, water activity, hygroscopicity and humidity corresponding to 97.03 ± 0.04%, 100% (in 1.16 min), 0.14 ± 0.0, 35.20 g H2O/100 g and 4.80 ± 0.43%, respectively. The microparticles were spherical with a smooth surface and thermally stable. Encapsulation improved the survival of L. casei during storage. After 60 days, the samples stored at -8 °C showed viable cell concentrations of 1.0 × 10(9) CFU/g.

  18. Feasibility of spray drying bacteriophages into respirable powders to combat pulmonary bacterial infections.

    PubMed

    Vandenheuvel, Dieter; Singh, Abhishek; Vandersteegen, Katrien; Klumpp, Jochen; Lavigne, Rob; Van den Mooter, Guy

    2013-08-01

    The use of bacterial viruses for antibacterial treatment (bacteriophage therapy) is currently being reevaluated. In this study, we analyze the potential of processing bacteriophages in a dry powder formulation, using a laboratory spray dryer. The phages were dried in the presence of lactose, trehalose or dextran 35, serving as an excipient to give the resulting powder the necessary bulk mass and offer protection to the delicate phage structure. Out of the three excipients tested, trehalose was found to be the most efficient in protecting the phages from temperature and shear stress throughout the spray drying process. A low inlet air temperature and atomizing force appeared to be the best parameter conditions for phage survival. Pseudomonas podovirus LUZ19 was remarkably stable, suffering less than 1 logarithmic unit reduction in phage titer. The phage titer of Staphyloccus phage Romulus-containing powders, a member of the Myoviridae family, showed more than 2.5 logarithmic units reduction. On the other hand, Romulus-containing powders showed more favorable characteristics for pulmonary delivery, with a high percentage of dry powder particles in the pulmonary deposition fraction (1-5 μm particle diameter). Even though the parameters were not optimized for spray drying all phages, it was demonstrated that spray drying phages with this industrial relevant and scalable set up was possible. The resulting powders had desirable size ranges for pulmonary delivery of phages with dry powder inhalers (DPIs).

  19. Spray drying of fruit and vegetable juices--a review.

    PubMed

    Verma, Anjali; Singh, Satya Vir

    2015-01-01

    The main cause of spray drying is to increase the shelf life and easy handling of juices. In the present paper, the studies carried out so far on spray drying of various fruits and vegetables are reported. The major fruit juices dried are mango, banana, orange, guava, bayberry, watermelon, pineapple, etc. However, study on vegetable juices is limited. In spray drying, the major optimized parameters are inlet air temperature, relative humidity of air, outlet air temperature, and atomizer speed that are given for a particular study. The juices in spray drying require addition of drying agents that include matlodextrin, liquid glucose, etc. The drying agents are added to increase the glass transition temperature. Different approaches for spray dryer design have also been discussed in the present work.

  20. Encapsulation of alcohol dehydrogenase in mannitol by spray drying.

    PubMed

    Shiga, Hirokazu; Joreau, Hiromi; Neoh, Tze Loon; Furuta, Takeshi; Yoshii, Hidefumi

    2014-03-24

    The retention of the enzyme activity of alcohol dehydrogenase (ADH) has been studied in various drying processes such as spray drying. The aim of this study is to encapsulate ADH in mannitol, either with or without additive in order to limit the thermal denaturation of the enzyme during the drying process. The retention of ADH activity was investigated at different drying temperatures. When mannitol was used, the encapsulated ADH was found inactive in all the dried powders. This is presumably due to the quick crystallization of mannitol during spray drying that resulted in the impairment of enzyme protection ability in comparison to its amorphous form. Maltodextin (dextrose equivalent = 11) was used to reduce the crystallization of mannitol. The addition of maltodextrin increased ADH activity and drastically changed the powder X-ray diffractogram of the spray-dried powders.

  1. Encapsulation of shiitake (Lenthinus edodes) flavors by spray drying.

    PubMed

    Shiga, Hirokazu; Yoshii, Hidefumi; Ohe, Hisashi; Yasuda, Masahumi; Furuta, Takeshi; Kuwahara, Hiroshige; Ohkawara, Masaaki; Linko, Pekka

    2004-01-01

    Powdery encapsulation of shiitake flavors, extracted from dried shiitake, was investigated by spray drying. Flavor retention increased with an increase in drying air temperature and solid content, and decreased with an increase in dextrose equivalents of maltodextrin. A heat-treatment of the extract liquid made the lenthionine concentration increase, but did not influence the concentrations of the other flavors. The formation of lenthionine with heat-treatment could be described by the consecutive unimolecular-type first order reaction. Lenthionine content in a spray-dried powder prepared with the heated extracted liquid significantly increased. alpha-Cyclodextrin was the most suitable encapsulant of alpha-, beta-, and gamma-cyclodextrins to prepare the spray-dried powder, including lenthionine. The flavor retentions were markedly increased by using of alpha-cyclodextrin and maltodextrin in combination as an encapsulant.

  2. Roll compaction of mannitol: compactability study of crystalline and spray-dried grades.

    PubMed

    Wagner, Carl Moritz; Pein, Miriam; Breitkreutz, Jörg

    2013-09-10

    Purpose of this project was to investigate the roll compaction behavior of various mannitol grades. Therefore, five spray-dried grades as well as unprocessed β-d-mannitol were roll compacted with different compaction forces. The resulting granules were characterized with regard to their particle size distribution, flow properties, and BET surface area and compressed to tablets. Granules of unprocessed mannitol, even when applying high compaction forces during dry granulation, were characterized by a high amount of fines (about 21%), a small surface area (0.83 m(2)/g), and solely fair flowability (ffc=7.2). Tablets revealed either high friability or insufficient disintegration behavior. However, the use of spray-dried mannitol led to better results. Granules showed improved flow properties and a reduced amount of fines. Robust tablets with low friability were produced. Within the various spray-dried grades huge differences concerning the compactability were observed. Large BET surface areas of the granules resulted in advanced tensile strengths of the tablets, but acceptable disintegration behavior was maintained. These findings are relevant for the development of mannitol based drug formulations, in particular (oro)dispersible tablets containing a low dose or poor flowing active pharmaceutical ingredient, where direct compression is inappropriate and a granulation process prior to tableting is mandatory.

  3. Spray drying technique. I: Hardware and process parameters.

    PubMed

    Cal, Krzysztof; Sollohub, Krzysztof

    2010-02-01

    Spray drying is a transformation of feed from a fluid state into a dried particulate form by spraying the feed into a hot drying medium. The main aim of drying by this method in pharmaceutical technology is to obtain dry particles with desired properties. This review presents the hardware and process parameters that affect the properties of the dried product. The atomization devices, drying chambers, air-droplet contact systems, the collection of dried product, auxiliary devices, the conduct of the spray drying process, and the significance of the individual parameters in the drying process, as well as the obtained product, are described and discussed.

  4. Powder compression mechanics of spray-dried lactose nanocomposites.

    PubMed

    Hellrup, Joel; Nordström, Josefina; Mahlin, Denny

    2017-02-25

    The aim of this study was to investigate the structural impact of the nanofiller incorporation on the powder compression mechanics of spray-dried lactose. The lactose was co-spray-dried with three different nanofillers, that is, cellulose nanocrystals, sodium montmorillonite and fumed silica, which led to lower micron-sized nanocomposite particles with varying structure and morphology. The powder compression mechanics of the nanocomposites and physical mixtures of the neat spray-dried components were evaluated by a rational evaluation method with compression analysis as a tool, using the Kawakita equation and the Shapiro-Konopicky-Heckel equation. Particle rearrangement dominated the initial compression profiles due to the small particle size of the materials. The strong contribution of particle rearrangement in the materials with fumed silica continued throughout the whole compression profile, which prohibited an in-depth material characterization. However, the lactose/cellulose nanocrystals and the lactose/sodium montmorillonite nanocomposites demonstrated high yield pressure compared with the physical mixtures indicating increased particle hardness upon composite formation. This increase has likely to do with a reinforcement of the nanocomposite particles by skeleton formation of the nanoparticles. In summary, the rational evaluation of mechanical properties done by applying powder compression analysis proved to be a valuable tool for mechanical evaluation for this type of spray-dried composite materials, unless they demonstrate particle rearrangement throughout the whole compression profile.

  5. Protective effect of sucrose on spray drying of oxyhemoglobin.

    PubMed

    Labrude, P; Rasolomanana, M; Vigneron, C; Thirion, C; Chaillot, B

    1989-03-01

    As far as we know, spray drying has previously not been applied to oxyhemoglobin, undoubtedly because of the sensitivity of oxyhemoglobin to temperature and oxidation. Our experience with freeze drying encouraged us to perform spray-drying trials in order to compare the results of the two methods, in the absence and the presence of protective compounds. Spray drying of hemoglobin without a protective compound led, as in freeze drying, to formation of a percentage of methemoglobin (50%) that makes it unsuitable for transporting oxygen. In the presence of 0.25 M sucrose (optimum) and at 80-100 degrees C, the functional properties of the hemoglobin were well preserved (methemoglobin approximately 4%), and the residual humidity was limited to approximately 3%. Structural investigation by optical circular dichroism confirmed the results obtained by freeze drying: in the presence of an effective protector, the spectra were similar to those of control hemoglobin and the immediate environment of the heme did not undergo any major change. Electron spin resonance absorption bands in all samples were similar for each value of the spectral decomposition factor, g. This suggests that the structure of the heme is not altered by desiccation and that the protector does not penetrate into the heme pocket since it would have disturbed the symmetry of the crystalline field. Fundamentally, these results are equivalent or similar to those observed with freeze drying; since spray drying is a different process of dehydration, the results indicate a lack of specificity in the phenomena of oxidation or of protection affecting hemoglobin.

  6. Formation of monodisperse mesoporous silica microparticles via spray-drying.

    PubMed

    Waldron, Kathryn; Wu, Winston Duo; Wu, Zhangxiong; Liu, Wenjie; Selomulya, Cordelia; Zhao, Dongyuan; Chen, Xiao Dong

    2014-03-15

    In this work, a protocol to synthesize monodisperse mesoporous silica microparticles via a unique microfluidic jet spray-drying route is reported for the first time. The microparticles demonstrated highly ordered hexagonal mesostructures with surface areas ranging from ~900 up to 1500 m(2)/g and pore volumes from ~0.6 to 0.8 cm(3)/g. The particle size could be easily controlled from ~50 to 100 μm from the same diameter nozzle via changing the initial solute content, or changing the drying temperature. The ratio of the surfactant (CTAB) and silica (TEOS), and the amount of water in the precursor were found to affect the degree of ordering of mesopores by promoting either the self-assembly of the surfactant-silica micelles or the condensation of the silica as two competing processes in evaporation induced self-assembly. The drying rate and the curvature of particles also affected the self-assembly of the mesostructure. The particle mesostructure is not influenced by the inlet drying temperature in the range of 92-160 °C, with even a relatively low temperature of 92 °C producing highly ordered mesoporous microparticles. The spray-drying derived mesoporous silica microparticles, while of larger sizes and more rapidly synthesized, showed a comparable performance with the conventional mesoporous silica MCM-41 in controlled release of a dye, Rhodamine B, indicating that these spray dried microparticles could be used for the immobilisation and controlled release of small molecules.

  7. [Study on totai flavonoids of Epimedium assisted with soybean polysaccharide spray-drying powder].

    PubMed

    Yan, Hong-mei; Jia, Xiao-bin; Zhang, Zhen-hai; Sun, E; Deng, Jia-hui

    2015-08-01

    In order to evaluate the characteristics of the spray drying of total flavonoids of Epimedium extracts assisted with soybean polysaccharide, a certain percentage of soybean polysaccharide or polyvidone were added to the total flavonoids of Epimedium extract to conduct the spray drying. The effect of soybean polysaccharides against the wall sticking effect of the spray drying was detected, as well as the powder property of total flavonoids of Epimedium spray drying powder and the dissolution in vitro behavior of the effective component. Compared with the total flavonoids of Epimedium spray drying powder, soybean polysaccharide revealed a significant anti-wall sticking effect. The spray drying power which had no notable change in the grain size made a increase in the fluidity, improvement in the moisture absorption and remarkable rise in the dissolution in vitro behavior. It was worth further studying the application of soybean polysaccharide in spray drying power of traditional Chinese medicine.

  8. Compare and contrast the effects of surfactants (PluronicF-127 and CremophorEL) and sugars (β-cyclodextrin and inulin) on properties of spray dried and crystallised lysozyme.

    PubMed

    Haj-Ahmad, Rita Rochdy; Elkordy, Amal Ali; Chaw, Cheng Shu; Moore, Adrian

    2013-07-16

    promising protectant of proteins. The improved stability of the spray dried and crystallised protein containing PluronicF-127 shows promise for delivery of proteins via inhalation (in a spray dried form which has particle size range suitable for inhalation as revealed by particle size analysis and SEM) and injectable routes (in spray dried and crystallised forms). The way excipients react with proteins is different in the case of spray drying and crystallisation techniques, hence the choice of the additives and the processing techniques play a great role in controlling protein properties, activity and stability as shown in this study.

  9. [Study on Xinyueshu spray drying assisted with copovidone and its effect on powder property].

    PubMed

    Jiang, Yan-Rong; Zhang, Zhen-Hai; Ding, Dong-Mei; Yan, Hong-Mei; Hu, Shao-Ying; Jia, Xiao-Bin

    2013-12-01

    To study the application characteristics of copovidone (PVP-S630) in Xinyueshu extracts during the spray drying process, and its effect on such pharmaceutical properties as micromeritics and drug release behavior. PVP-S630 was added into Xinyueshu extracts to study on the spray drying, the effect of different dosages of PVP-S630 against the wall sticking effect of the spray drying, as well as the power property of Xinyueshu spray drying power and the dissolution in vitro behavior of the effective component of hyperoside. The results showed that PVP-S630 revealed a significant anti-wall sticking effect, with no notable change in the grain size of the spray drying power, increase in the fluidity, improvement in the moisture absorption and remarkable rise in the dissolution in vitro behavior of hyperoside. It was worth further studying the application of PVP-S630 in spray drying power of traditional Chinese medicine.

  10. Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions.

    PubMed

    Adebisi, Adeola O; Kaialy, Waseem; Hussain, Tariq; Al-Hamidi, Hiba; Nokhodchi, Ali; Conway, Barbara R; Asare-Addo, Kofi

    2016-10-01

    This work explores the use of both spray drying and d-glucosamine HCl (GLU) as a hydrophilic carrier to improve the dissolution rate of piroxicam (PXM) whilst investigating the electrostatic charges associated with the spray drying process. Spray dried PXM:GLU solid dispersions were prepared and characterised (XRPD, DSC, SEM). Dissolution and triboelectric charging were also conducted. The results showed that the spray dried PXM alone, without GLU produced some PXM form II (DSC results) with no enhancement in solubility relative to that of the parent PXM. XRPD results also showed the spray drying process to decrease the crystallinity of GLU and solid dispersions produced. The presence of GLU improved the dissolution rate of PXM. Spray dried PXM: GLU at a ratio of 2:1 had the most improved dissolution. The spray drying process generally yielded PXM-GLU spherical particles of around 2.5μm which may have contributed to the improved dissolution. PXM showed a higher tendency for charging in comparison to the carrier GLU (-3.8 versus 0.5nC/g for untreated material and -7.5 versus 3.1nC/g for spray dried materials). Spray dried PXM and spray dried GLU demonstrated higher charge densities than untreated PXM and untreated GLU, respectively. Regardless of PXM:GLU ratio, all spray dried PXM:GLU solid dispersions showed a negligible charge density (net-CMR: 0.1-0.3nC/g). Spray drying of PXM:GLU solid dispersions can be used to produce formulation powders with practically no charge and thereby improving handling as well as dissolution behaviour of PXM.

  11. Fungitoxicity of lyophilized and spray-dried garlic extracts.

    PubMed

    Tedeschi, Paola; Maietti, Annalisa; Boggian, Marisa; Vecchiati, Giorgio; Brandolini, Vincenzo

    2007-01-01

    Among the compounds discussed for anti-microbial and anti-fungal use allicin (allylthiosulfinate, diallyl disulfide-S-monoxide), an active ingredient of garlic, has attracted considerable attention. The objective of this study is to determine the antifungal activity of a local garlic ecotype (Voghiera) extracts against different pathogens. Primary screening was carried out by the agar plates technique using ethanol garlic extract at four final concentrations against the following organisms: Alternaria alternata, Aspergillus spp., Colletotrichum acutatum, Didymella bryoniae, Fusarium culmorum, Fusarium avenaceum, Fusarium gramineareum, Gliocladium roseum 47, Pythium splendens, Rhizoctonia solani, Sclerotium rolfsii, Stemphylium vesicarium, Trichoderma longibranchiatum, and Botrytis cinerea. Secondary screening was carried out using a lyophilized and a spray-dried preparation at different concentrations against the organisms selected for the high inhibition garlic effect in the primary screening and compared with the commercial fungicides mancozeb and iprodione. The best results were observed for the spray-dried garlic compound that showed a good fungicidal activity at the concentration of 1.5 g/10 mL while lyophilized garlic at the same concentration exhibited less inhibition activity against the four fungi analyzed in the second screening.

  12. Crystal coating via spray drying to improve powder tabletability.

    PubMed

    Vanhoorne, V; Peeters, E; Van Snick, B; Remon, J P; Vervaet, C

    2014-11-01

    A continuous crystal coating method was developed to improve both flowability and tabletability of powders. The method includes the introduction of solid, dry particles into an atomized spray during spray drying in order to coat and agglomerate individual particles. Paracetamol was used as a model drug as it exhibits poor flowability and high capping tendency upon compaction. The particle size enlargement and flowability were evaluated by the mean median particle size and flow index of the resulting powders. The crystal coating coprocessing method was successful for the production of powders containing 75% paracetamol with excellent tableting properties. However, the extent of agglomeration achieved during coprocessing was limited. Tablets compressed on a rotary tablet press in manual mode showed excellent compression properties without capping tendency. A formulation with 75% paracetamol, 5% PVP and 20% amorphous lactose yielded a tensile strength of 1.9 MPa at a compression pressure of 288 MPa. The friability of tablets compressed at 188 MPa was only 0.6%. The excellent tabletability of this formulation was attributed to the coating of paracetamol crystals with amorphous lactose and PVP through coprocessing and the presence of brittle and plastic components in the formulation. The coprocessing method was also successfully applied for the production of directly compressible lactose showing improved tensile strength and friability in comparison to a spray dried direct compression lactose grade.

  13. Microencapsulation of soybean oil by spray drying using oleosomes

    NASA Astrophysics Data System (ADS)

    Maurer, S.; Ghebremedhin, M.; Zielbauer, B. I.; Knorr, D.; Vilgis, T. A.

    2016-02-01

    The food industry has discovered that oleosomes are beneficial as carriers of bioactive ingredients. Oleosomes are subcellular oil droplets typically found in plant seeds. Within seeds, they exist as pre-emulsified oil high in unsaturated fatty acids, stabilised by a monolayer of phospholipids and proteins, called oleosins. Oleosins are anchored into the oil core with a hydrophobic domain, while the hydrophilic domains remain on the oleosome surface. To preserve the nutritional value of the oil and the function of oleosomes, microencapsulation by means of spray drying is a promising technique. For the microencapsulation of oleosomes, maltodextrin was used. To achieve a high oil encapsulation efficiency, optimal process parameters needed to be established. In order to better understand the mechanisms of drying behind powder formation and the associated powder properties, the findings obtained using different microscopic and spectroscopic measurements were correlated with each other. By doing this, it was found that spray drying of pure oleosome emulsions resulted in excessive component segregation and thus in a poor encapsulation efficiency. With the addition of maltodextrin, the oil encapsulation efficiency was significantly improved.

  14. Amorphous and nanostructured silica and aluminosilicate spray-dried microspheres

    NASA Astrophysics Data System (ADS)

    Todea, M.; Turcu, R. V. F.; Frentiu, B.; Tamasan, M.; Mocuta, H.; Ponta, O.; Simon, S.

    2011-08-01

    Amorphous silica and aluminosilicate microspheres with diameters in the 0.1-20 μm range were produced by spray drying method. SEM, TEM and AFM images showed the spherical shape of the obtained particles. Based on thermal analysis data, several heat treatments have been applied on the as-prepared samples in order to check the amorphous state stability of the microspheres and to develop nanosized crystalline phases. As-prepared microspheres remain amorphous up to 1400 °C. By calcination at 1400 °C, cristobalite type nanocrystals are developed on silica sample, while in aluminosilicate sample first are developed mullite type nanocrystals and only after prolonged treatment are developed also cristobalite type nanocrystals. 29Si and 27Al MAS NMR results show that the local order around aluminum and silicon atoms strongly depend on the thermal history of the microspheres.

  15. Clay as a matrix former for spray drying of drug nanosuspensions.

    PubMed

    Dong, Yuancai; Ng, Wai Kiong; Hu, Jun; Shen, Shoucang; Tan, Reginald B H

    2014-04-25

    Utilization of sugars (e.g. lactose, sucrose) as matrix formers for spray drying of drug nanosuspensions is associated with two drawbacks: (1) sugars are incapable of preventing agglomeration of drug nanoparticles (NPs) in the suspension state; and (2) the spray-dried sugars are usually amorphous and hygroscopic. This work aimed to apply a clay, montmorillonite (MMT) as an alternative matrix former for spray drying of drug nanosuspensions with fenofibrate (feno) as a model compound. Drug nanosuspensions were synthesized by liquid antisolvent precipitation with different amount of MMT followed by spray drying. It is found that MMT is able to reduce the agglomeration of drug nanoparticles in the suspension state, as observed from the gradual alleviation of the clogging with the increased clay during the spray drying. The spray-dried feno NPs/MMT powders exhibited a much lower moisture sorption than spray-dried feno NPs/lactose powders as evidenced by the dynamic vapor sorption (DVS) analysis. The dissolution within 5 min for the spray-dried feno NPs/MMT powders at drug:MMT weight ratio of 1:3 was 81.4 ± 1.8% and the total dissolution within 60 min was 93.4 ± 0.9%. Our results demonstrate that MMT is a useful matrix former for preservation of the high dissolution rate of nanosized drug particles after drying.

  16. 40 CFR 417.150 - Applicability; description of the manufacture of spray dried detergents subcategory.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... manufacture of spray dried detergents subcategory. 417.150 Section 417.150 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) EFFLUENT GUIDELINES AND STANDARDS SOAP AND DETERGENT MANUFACTURING POINT SOURCE CATEGORY Manufacture of Spray Dried Detergents Subcategory § 417.150...

  17. 40 CFR 417.150 - Applicability; description of the manufacture of spray dried detergents subcategory.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... manufacture of spray dried detergents subcategory. 417.150 Section 417.150 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) EFFLUENT GUIDELINES AND STANDARDS SOAP AND DETERGENT MANUFACTURING POINT SOURCE CATEGORY Manufacture of Spray Dried Detergents Subcategory § 417.150...

  18. 40 CFR 417.150 - Applicability; description of the manufacture of spray dried detergents subcategory.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... manufacture of spray dried detergents subcategory. 417.150 Section 417.150 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) EFFLUENT GUIDELINES AND STANDARDS SOAP AND DETERGENT MANUFACTURING POINT SOURCE CATEGORY Manufacture of Spray Dried Detergents Subcategory § 417.150...

  19. 40 CFR 417.150 - Applicability; description of the manufacture of spray dried detergents subcategory.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... manufacture of spray dried detergents subcategory. 417.150 Section 417.150 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) EFFLUENT GUIDELINES AND STANDARDS SOAP AND DETERGENT MANUFACTURING POINT SOURCE CATEGORY Manufacture of Spray Dried Detergents Subcategory § 417.150...

  20. 40 CFR 417.150 - Applicability; description of the manufacture of spray dried detergents subcategory.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... manufacture of spray dried detergents subcategory. 417.150 Section 417.150 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) EFFLUENT GUIDELINES AND STANDARDS SOAP AND DETERGENT MANUFACTURING POINT SOURCE CATEGORY Manufacture of Spray Dried Detergents Subcategory § 417.150...

  1. Effect of spray drying on the properties of amylose-hexadecylammonium chloride inclusion complexes

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Water soluble amylose-hexadecyl ammonium chloride complexes were prepared from high amylose corn starch and hexadecyl ammonium chloride by excess steam jet cooking. Amylose inclusion complexes were spray dried to determine the viability of spray drying as a production method. The variables tested in...

  2. Spray-Dried Multiscale Nano-biocomposites Containing Living Cells.

    PubMed

    Johnson, Patrick E; Muttil, Pavan; MacKenzie, Debra; Carnes, Eric C; Pelowitz, Jennifer; Mara, Nathan A; Mook, William M; Jett, Stephen D; Dunphy, Darren R; Timmins, Graham S; Brinker, C Jeffrey

    2015-07-28

    Three-dimensional encapsulation of cells within nanostructured silica gels or matrices enables applications as diverse as biosensors, microbial fuel cells, artificial organs, and vaccines; it also allows the study of individual cell behaviors. Recent progress has improved the performance and flexibility of cellular encapsulation, yet there remains a need for robust scalable processes. Here, we report a spray-drying process enabling the large-scale production of functional nano-biocomposites (NBCs) containing living cells within ordered 3D lipid-silica nanostructures. The spray-drying process is demonstrated to work with multiple cell types and results in dry powders exhibiting a unique combination of properties including highly ordered 3D nanostructure, extended lipid fluidity, tunable macromorphologies and aerodynamic diameters, and unexpectedly high physical strength. Nanoindentation of the encasing nanostructure revealed a Young's modulus and hardness of 13 and 1.4 GPa, respectively. We hypothesized this high strength would prevent cell growth and force bacteria into viable but not culturable (VBNC) states. In concordance with the VBNC state, cellular ATP levels remained elevated even over eight months. However, their ability to undergo resuscitation and enter growth phase greatly decreased with time in the VBNC state. A quantitative method of determining resuscitation frequencies was developed and showed that, after 36 weeks in a NBC-induced VBNC, less than 1 in 10,000 cells underwent resuscitation. The NBC platform production of large quantities of VBNC cells is of interest for research in bacterial persistence and screening of drugs targeting such cells. NBCs may also enable long-term preservation of living cells for applications in cell-based sensing and the packaging and delivery of live-cell vaccines.

  3. Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers.

    PubMed

    Sosnik, Alejandro; Seremeta, Katia P

    2015-09-01

    Spray-drying is a rapid, continuous, cost-effective, reproducible and scalable process for the production of dry powders from a fluid material by atomization through an atomizer into a hot drying gas medium, usually air. Often spray-drying is considered only a dehydration process, though it also can be used for the encapsulation of hydrophilic and hydrophobic active compounds within different carriers without substantial thermal degradation, even of heat-sensitive substances due to fast drying (seconds or milliseconds) and relatively short exposure time to heat. The solid particles obtained present relatively narrow size distribution at the submicron-to-micron scale. Generally, the yield% of spray-drying at laboratory scale with conventional spray-dryers is not optimal (20-70%) due to the loss of product in the walls of the drying chamber and the low capacity of the cyclone to separate fine particles (<2 μm). Aiming to overcome this crucial drawback in early development stages, new devices that enable the production of submicron particles with high yield, even for small sample amounts, have been introduced into the market. This review describes the most outstanding advantages and challenges of the spray-drying method for the production of pure drug particles and drug-loaded polymeric particles and discusses the potential of this technique and the more advanced equipment to pave the way toward reproducible and scalable processes that are critical to the bench-to-bedside translation of innovative pharmaceutical products.

  4. Inhalants

    MedlinePlus

    ... place a chemical- soaked rag in their mouth. Abusers may also inhale fumes from a balloon or ... by inhalants usually lasts just a few minutes, abusers often try to prolong it by continuing to ...

  5. Inhalants

    MedlinePlus

    ... Drug Facts Chat Day: Inhalants Drug Facts Chat Day: Inhalants Print Can you get high off of ... Cool Order Free Materials National Drugs & Alcohol Chat Day Newsletter Sign up to receive National Drug & Alcohol ...

  6. Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying.

    PubMed

    Craye, Goedele; Löbmann, Korbinian; Grohganz, Holger; Rades, Thomas; Laitinen, Riikka

    2015-12-03

    In this study, spray drying from aqueous solutions, using the surface-active agent sodium lauryl sulfate (SLS) as a solubilizer, was explored as a production method for co-amorphous simvastatin-lysine (SVS-LYS) at 1:1 molar mixtures, which previously have been observed to form a co-amorphous mixture upon ball milling. In addition, a spray-dried formulation of SVS without LYS was prepared. Energy-dispersive X-ray spectroscopy (EDS) revealed that SLS coated the SVS and SVS-LYS particles upon spray drying. X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) showed that in the spray-dried formulations the remaining crystallinity originated from SLS only. The best dissolution properties and a "spring and parachute" effect were found for SVS spray-dried from a 5% SLS solution without LYS. Despite the presence of at least partially crystalline SLS in the mixtures, all the studied formulations were able to significantly extend the stability of amorphous SVS compared to previous co-amorphous formulations of SVS. The best stability (at least 12 months in dry conditions) was observed when SLS was spray-dried with SVS (and LYS). In conclusion, spray drying of SVS and LYS from aqueous surfactant solutions was able to produce formulations with improved physical stability for amorphous SVS.

  7. Spray Dried Aerosol Particles of Pyrazinoic Acid Salts for Tuberculosis Therapy. [Corrected].

    PubMed

    Durham, P G; Zhang, Y; German, N; Mortensen, N; Dhillon, J; Mitchison, D A; Fourie, P B; Hickey, A J

    2015-08-03

    Tuberculosis is the most serious infectious disease caused by a single organism, Mycobacterium tuberculosis (Mtb). The standard of care is a protracted and complex drug treatment regimen made more complicated and of longer duration by the incidence of multiple and extensively drug resistant disease. Pulmonary delivery of aerosols as a supplement to the existing regimen offers the advantage of delivering high local drug doses to the initial site of infection and most prominent organ system involved in disease. Pyrazinamide is used in combination with other drugs to treat tuberculosis. It is postulated that the action of pyrazinoic acid (POA), the active moiety of pyrazinamide, may be enhanced by local pH adjustment, when presented as a salt form. POA was prepared as leucine (POA-leu) and ammonium salts (POA-NH4), spray dried, and characterized in terms of physicochemical properties (melting point, crystallinity, moisture content), aerodynamic performance (aerodynamic particle size distribution, emitted dose), and in vitro inhibitory effect on two mycobacteria (Mtb and Mycobacterium bovis). Particles were prepared in sizes suitable for inhalation (3.3 and 5.4 μm mass median aerodynamic diameter and 61 and 40% of the aerodynamic particle size distribution less than 4.46 μm, as measured by inertial impaction, for POA-leu and POA-NH4, respectively) and with properties (stoichiometric 1:1 ratio of salt to drug, melting points at ∼180 °C, with water content of <1%) that would support further development as an inhaled dosage form. In addition, POA salts demonstrated greater potency in inhibiting mycobacterial growth compared with POA alone, which is promising for therapy.

  8. Clarithromycin and N-Acetylcysteine co-spray-dried powders for pulmonary drug delivery: A focus on drug solubility.

    PubMed

    Manniello, Michele Dario; Del Gaudio, Pasquale; Aquino, Rita P; Russo, Paola

    2017-04-01

    Cystic fibrosis (CF) lungs are usually susceptible to Pseudomonas aeruginosa colonization and this bacterium is resistant to immune system clearance and drug control. Particularly, the biofilm mode of growth protects several microorganisms from host defenses and antibacterial drugs, mainly due to a delayed penetration of the drug through the biofilm matrix. Biofilm, together with lung mucus viscosity and tenacity, reduces, therefore, the effectiveness of conventional antibiotic therapy in CF. The aim of this research was to design and develop a stable, portable, easy to use dry powder inhaler (DPI) for CF patients, able to release directly to the lung an association of macrolide antibiotics (clarithromycin) and a mucolytic agent (N-Acetyl-Cysteine). Its effectiveness is based on the counteracting of the characteristics of P. aeruginosa infections in CF (lung bacterial adhesion to lung epithelium, biofilm formation and mucus viscosity) and the ability to let the antimicrobial drug exert their pharmacological action. A solution of these two drugs, without any excipients, was spray-dried to obtain respirable microparticles, characterized by aerodynamic diameters suitable for inhalation (<5.0μm). The morphology evaluation evidenced a particles shape dependent on water content in the spray drying feeds, with wrinkle particles more evident with higher water content. Moreover, thanks to the presence of N-acetylcysteine which can interact with clarithromycin dimethyl-amino group, a consistent enhancement of drug solubility was obtained, compared to raw material and to the drug sprayed alone. The mucolytic agent added in the DPI may improve the macrolide diffusion into the mucus, enabling its action.

  9. Fabrication of polyacrylate core-shell nanoparticles via spray drying method

    NASA Astrophysics Data System (ADS)

    Chen, Pengpeng; Cheng, Zenghui; Chu, Fuxiang; Xu, Yuzhi; Wang, Chunpeng

    2016-05-01

    Fine polyacrylate particles are thought to be environmental plastisols for car industry. However, these particles are mainly dried through demulsification of the latexes, which is not reproducible and hard to be scaled up. In this work, a spray drying method had been applied to the plastisols-used acrylate latex. By adjusting the core/shell ratio, spray drying process of the latex was fully studied. Scanning electronic microscopy observation of the nanoparticles before and after spray drying indicated that the core-shell structures could be well preserved and particles were well separated by spray drying if the shell was thick enough. Otherwise, the particles fused into each other and core-shell structures were destroyed. Polyacrylate plastisols were developed using diisononylphthalate as a plasticizer, and plastigels were obtained after heat treatment of the sols. Results showed that the shell thickness also had a great influence on the storage stability of the plastisols and mechanical properties of the plastigels.

  10. Effect of whey protein agglomeration on spray dried microcapsules containing Saccharomyces boulardii.

    PubMed

    Duongthingoc, Diep; George, Paul; Katopo, Lita; Gorczyca, Elizabeth; Kasapis, Stefan

    2013-12-01

    This work investigates the effect of whey protein agglomeration on the survivability of Saccharomyces boulardii within spray dried microcapsules. It attempts to go beyond phenomenological observations by establishing a relationship between physicochemical characteristics of the polymeric matrix and its effect on probiotic endurance upon spray drying. It is well known that this type of thermal shock has lethal consequences on the yeast cells. To avoid such undesirable outcome, we take advantage of the early agglomeration phenomenon observed for whey protein by adjusting the pH value of preparations close to isoelectric point (pH 4-5). During the subsequent process of spray drying, development of whey protein agglomerates induces formation of an early crust, and the protein in this molten globular state creates a cohesive network encapsulating the yeast cells. It appears that the early crust formation at a given sample pH and temperature regime during spray drying benefits the survivability of S. boulardii within microcapsules.

  11. Effect of oil droplet size on the oxidative stability of spray-dried flaxseed oil powders.

    PubMed

    Shiga, Hirokazu; Loon Neoh, Tze; Ninomiya, Ai; Adachi, Sae; Pasten, Ignacio Lopez; Adachi, Shuji; Yoshii, Hidefumi

    2017-04-01

    The effect of the size of oil droplets on the oxidative stability of flaxseed oil in spray-dried powders was investigated. Maltodextrin with a dextrose equivalent of 25 was used as a wall material, and sodium caseinate and transglutaminase-polymerized sodium caseinate were used as emulsifiers. The oxidative stability of flaxseed oil encapsulated in the spray-dried powders was evaluated using lipid oxidation and conductometric determination tests at 105 °C. The powders containing larger oil droplets exhibited higher surface oil content after spray drying, and higher peroxide value and conductivity after storage at 105 °C. Removal of the surface oil from the powders by washing with hexane significantly decreased the conductivity. The results indicated that the surface oil of the spray-dried flaxseed oil powders affected the oxidation stability.

  12. Development of "all natural" layer-by-layer redispersible solid lipid nanoparticles by nano spray drying technology.

    PubMed

    Wang, Taoran; Hu, Qiaobin; Zhou, Mingyong; Xia, Yan; Nieh, Mu-Ping; Luo, Yangchao

    2016-10-01

    Solid lipid nanoparticles (SLNs) have gained tremendous attraction as carriers for controlled drug delivery. Despite numerous advances in the field, one long-standing historical challenge for their practical applications remains unmet: redispersibility after drying. In this work, a novel design of SLNs using a layer-by-layer (LbL) technique was developed and the formulations were optimized by surface response methodology (Box-Behnken design). To the best of our knowledge, this is the first study reporting the fabrication of SLNs from all natural ingredients in the absence of any synthetic surfactants or coatings. The SLNs were prepared by a combined solvent-diffusion and hot homogenization method, with soy lecithin as natural emulsifier (first layer), followed by the subsequent coating with sodium caseinate (second layer) and pectin (third layer), both of which are natural food biopolymers. The adsorption of pectin coating onto caseinate was reinforced by hydrophobic and electrostatic interactions induced by a pH-driven process along with thermal treatment. The innovative nano spray drying technology was further explored to obtain ultra-fine powders of SLNs. Compared to uncoated or single-layer coated SLNs powders, which showed severe aggregation after spray drying, the well-separated particles with spherical shape and smooth surface were obtained for layer-by-layer (LbL) SLNs, which were redispersible into water without variation of dimension, shape and morphology. The SLNs were characterized by Fourier transform infrared and high-performance differential scanning calorimetry for their physical properties. The LbL-coated SLNs based on all natural ingredients have promising features for future applications as drug delivery systems, overcoming the major obstacles in conventional spray drying and redispersing SLNs-based formulations.

  13. Effect of liquid retentate storage on flavor of spray-dried whey protein concentrate and isolate.

    PubMed

    Whitson, M; Miracle, R E; Bastian, E; Drake, M A

    2011-08-01

    The objective of this study was to determine the effects of holding time of liquid retentate on flavor of spray-dried whey proteins: Cheddar whey protein isolate (WPI) and Mozzarella 80% whey protein concentrate (WPC80). Liquid WPC80 and WPI retentate were manufactured and stored at 3°C. After 0, 6, 12, 24, and 48h, the product was spray-dried (2kg) and the remaining retentate held until the next time point. The design was replicated twice for each product. Powders were stored at 21°C and evaluated every 4 mo throughout 12 mo of storage. Flavor profiles of rehydrated proteins were documented by descriptive sensory analysis. Volatile components were analyzed with solid phase microextraction coupled with gas chromatography mass spectrometry. Cardboard flavors increased in both spray-dried products with increased retentate storage time and cabbage flavors increased in WPI. Concurrent with sensory results, lipid oxidation products (hexanal, heptanal, octanal) and sulfur degradation products (dimethyl disulfide, dimethyl trisulfide) increased in spray-dried products with increased liquid retentate storage time, whereas diacetyl decreased. Shelf stability was decreased in spray-dried products from longer retentate storage times. For maximum quality and shelf life, liquid retentate should be held for less than 12h before spray drying.

  14. Effect of spray drying on the properties of amylose-hexadecylammonium chloride inclusion complexes.

    PubMed

    Hay, William T; Behle, Robert W; Fanta, George F; Felker, Frederick C; Peterson, Steven C; Selling, Gordon W

    2017-02-10

    Water soluble amylose-hexadecyl ammonium chloride complexes were prepared from high amylose corn starch and hexadecyl ammonium chloride by excess steam jet cooking. Amylose inclusion complexes were spray dried to determine the viability of spray drying as a production method. The variables tested in the spray drying process were the% solids of the amylose-hexadecyl ammonium chloride complex being fed into the spray dryer, feed rate and the spray dryer outlet temperature. The amylose-inclusion complexes remained intact in all spray drying conditions tested as determined by X-ray diffraction. The rheological properties of solutions of the spray dried amylose-complexes remained unchanged when compared with the freeze dried control. Particle density and moisture content decreased with increased outlet temperature while particle size increased. X-ray diffraction and DSC analysis confirmed the formation of type II amylose inclusion complexes. Spray drying is a high throughput, low cost continuous commercial production method, which when coupled with excess steam jet cooking allows for the industrial scale production of cationic amylose-hexadecyl ammonium chloride complexes which may have value as flocculating and filtration enhancing agents and other aspects of paper production.

  15. Competition of thermodynamic and dynamic factors during formation of multicomponent particles via spray drying.

    PubMed

    Kawakami, Kohsaku; Hasegawa, Yusuke; Deguchi, Kenzo; Ohki, Shinobu; Shimizu, Tadashi; Yoshihashi, Yasuo; Yonemochi, Etsuo; Terada, Katsuhide

    2013-02-01

    As psicose cannot be spray dried because of its low glass transition temperature (T(g)), additives have been used to manufacture spray-dried particles. Its thermodynamic miscibility with each additive was evaluated by thermal analysis and C solid-state nuclear magnetic resonance. Aspartame was miscible with psicose at all ratios, and spray-dried particles were obtained when T(g) of the mixture was higher than the outlet temperature of the spray dryer, where 30 wt % of psicose was loaded. poly(vinylpyrrolidone) and cluster dextrin were partially miscible with psicose, with a maximum loading of 40 wt %. When polymeric excipients were used, their mixing behavior with psicose was affected by the dynamic factor during the spray drying, that is, enhanced phase separation due to the molecular-weight difference. The T(g) value of the polymer-rich phases, which were likely to form shell layers on the surfaces, played an important role in determining availability of the spray-dried particles. Hydroxypropyl methylcellulose (HPMC) offered a very effective loading capacity of 80 wt %, due to distinct phase separation to form shell phase with a very high T(g). Because molecular weight of HPMC was the smallest among the polymeric excipients, the thermodynamic miscibility seemed to affect the dynamic phase separation. These results provide useful information for preparing multicomponent spray-dried particles.

  16. Use of cheese whey for biomass production and spray drying of probiotic lactobacilli.

    PubMed

    Lavari, Luisina; Páez, Roxana; Cuatrin, Alejandra; Reinheimer, Jorge; Vinderola, Gabriel

    2014-08-01

    The double use of cheese whey (culture medium and thermoprotectant for spray drying of lactobacilli) was explored in this study for adding value to this wastewater. In-house formulated broth (similar to MRS) and dairy media (cheese and ricotta whey and whey permeate) were assessed for their capacity to produce biomass of Lactobacillus paracasei JP1, Lb. rhamnosus 64 and Lb. gasseri 37. Simultaneously, spray drying of cheese whey-starch solution (without lactobacilli cells) was optimised using surface response methodology. Cell suspensions of the lactobacilli, produced in in house-formulated broth, were spray-dried in cheese whey-starch solution and viability monitored throughout the storage of powders for 2 months. Lb. rhamnosus 64 was able to grow satisfactorily in at least two of the in-house formulated culture media and in the dairy media assessed. It also performed well in spray drying. The performance of the other strains was less satisfactory. The growth capacity, the resistance to spray drying in cheese whey-starch solution and the negligible lost in viability during the storage (2 months), makes Lb. rhamnosus 64 a promising candidate for further technological studies for developing a probiotic dehydrated culture for foods, utilising wastewaters of the dairy industry (as growth substrate and protectant) and spray drying (a low-cost widely-available technology).

  17. Preparation and characterization of microparticles of piroxicam by spray drying and spray chilling methods

    PubMed Central

    Dixit, M.; Kini, A.G.; Kulkarni, P.K.

    2010-01-01

    Piroxicam, an anti-inflammatory drug, exhibits poor water solubility and flow properties, poor dissolution and poor wetting. Consequently, the aim of this study was to improve the dissolution of piroxicam. Microparticles containing piroxicam were produced by spray drying, using isopropyl alcohol and water in the ratio of 40:60 v/v as solvent system, and spray chilling technology by melting the drug and chilling it with a pneumatic nozzle to enhance dissolution rate. The prepared formulations were evaluated for in vitro dissolution and solubility. The prepared drug particles were characterized by scanning electron microscopy (SEM), differential scanning calorimeter, X-ray diffraction and Fourier transform infrared spectroscopy. Dissolution profile of the spray dried microparticles was compared with spray-chilled microparticles, pure and recrystallized samples. Spray dried microparticles and spray chilled microparticles exhibited decreased crystallinity and improved micromeritic properties. The dissolution of the spray dried microparticle and spray chilled particles were improved compared with recrystallized and pure sample of piroxicam. Consequently, it was believed that spray drying of piroxicam is a useful tool to improve dissolution but not in case of spray chilling. This may be due to the degradation of drug or variations in the resonance structure or could be due to minor distortion of bond angles. Hence, this spray drying technique can be used for formulation of tablets of piroxicam by direct compression with directly compressible tablet excipients. PMID:21589797

  18. Characterization of Phase Separation Propensity for Amorphous Spray Dried Dispersions.

    PubMed

    McNamara, Daniel; Yin, Shawn; Pan, Duohai; Crull, George; Timmins, Peter; Vig, Balvinder

    2017-02-06

    A generalized screening approach, applying isothermal calorimetry at 37 °C 100% RH, to formulations of spray dried dispersions (SDDs) for two active pharmaceutical ingredients (APIs) (BMS-903452 and BMS-986034) is demonstrated. APIs 452 and 034, with similar chemotypes, were synthesized and promoted during development for oral dosing. Both APIs were formulated as SDDs for animal exposure studies using the polymer hydroxypropylmethlycellulose acetyl succinate M grade (HPMCAS-M). 452 formulated at 30% (wt/wt %) was an extremely robust SDD that was able to withstand 40 °C 75% RH open storage conditions for 6 months with no physical evidence of crystallization or loss of dissolution performance. Though 034 was a chemical analogue with similar physical chemical properties to 452, a physically stable SDD of 034 could not be formulated in HPMCAS-M at any of the drug loads attempted. This study was used to develop experience with specific physical characterization laboratory techniques to evaluate the physical stability of SDDs and to characterize the propensity of SDDs to phase separate and possibly crystallize. The screening strategy adopted was to stress the formulated SDDs with a temperature humidity screen, within the calorimeter, and to apply orthogonal analytical techniques to gain a more informed understanding of why these SDDs formulated with HPMCAS-M demonstrated such different physical stability. Isothermal calorimetry (thermal activity monitor, TAM) was employed as a primary stress screen wherein the SDD formulations were monitored for 3 days at 37 °C 100% RH for signs of phase separation and possible crystallization of API. Powder X-ray diffraction (pXRD), modulated differential scanning calorimetry (mDSC), Fourier transform infrared spectroscopy (FTIR), and solid state nuclear magnetic resonance (ssNMR) were all used to examine formulated SDDs and neat amorphous drug. 452 SDDs formulated at 30% (wt/wt %) or less did not show phase separation behavior upon

  19. L-Leucine as an excipient against moisture on in vitro aerosolization performances of highly hygroscopic spray-dried powders.

    PubMed

    Li, Liang; Sun, Siping; Parumasivam, Thaigarajan; Denman, John A; Gengenbach, Thomas; Tang, Patricia; Mao, Shirui; Chan, Hak-Kim

    2016-05-01

    L-Leucine (LL) has been widely used to enhance the dispersion performance of powders for inhalation. LL can also protect powders against moisture, but this effect is much less studied. The aim of this study was to investigate whether LL could prevent moisture-induced deterioration in in vitro aerosolization performances of highly hygroscopic spray-dried powders. Disodium cromoglycate (DSCG) was chosen as a model drug and different amounts of LL (2-40% w/w) were added to the formulation, with the aim to explore the relationship between powder dispersion, moisture protection and physicochemical properties of the powders. The powder formulations were prepared by spray drying of aqueous solutions containing known concentrations of DSCG and LL. The particle sizes were measured by laser diffraction. The physicochemical properties of fine particles were characterized by X-ray powder diffraction (XRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and dynamic vapor sorption (DVS). The surface morphology and chemistry of fine particles were analyzed by scanning electron microscopy (SEM), X-ray photoelectron spectroscopy (XPS), and time-of-flight secondary ion mass spectrometry (ToF-SIMS). In vitro aerosolization performances were evaluated by a next generation impactor (NGI) after the powders were stored at 60% or 75% relative humidity (RH), and 25°C for 24h. Spray-dried (SD) DSCG powders were amorphous and absorbed 30-45% (w/w) water at 70-80% RH, resulting in deterioration in the aerosolization performance of the powders. LL did not decrease the water uptake of DSCG powders, but it could significantly reduce the effect of moisture on aerosolization performances. This is due to enrichment of crystalline LL on the surface of the composite particles. The effect was directly related to the percentage of LL coverage on the surface of particles. Formulations having 61-73% (molar percent) of LL on the particle surface (which correspond to 10-20% (w

  20. The spray-drying process is sufficient to inactivate infectious porcine epidemic diarrhea virus in plasma.

    PubMed

    Gerber, Priscilla F; Xiao, Chao-Ting; Chen, Qi; Zhang, Jianqiang; Halbur, Patrick G; Opriessnig, Tanja

    2014-11-07

    Porcine epidemic diarrhea virus (PEDV) is considered an emergent pathogen associated with high economic losses in many pig rearing areas. Recently it has been suggested that PEDV could be transmitted to naïve pig populations through inclusion of spray-dried porcine plasma (SDPP) into the nursery diet which led to a ban of SDPP in several areas in North America and Europe. To determine the effect of spray-drying on PEDV infectivity, 3-week-old pigs were intragastrically inoculated with (1) raw porcine plasma spiked with PEDV (RAW-PEDV-CONTROL), (2) porcine plasma spiked with PEDV and then spray dried (SD-PEDV-CONTROL), (3) raw plasma from PEDV infected pigs (RAW-SICK), (4) spray-dried plasma from PEDV infected pigs (SD-SICK), or (5) spray-dried plasma from PEDV negative pigs (SD-NEG-CONTROL). For the spray-drying process, a tabletop spray-dryer with industry-like settings for inlet and outlet temperatures was used. In the RAW-PEDV-CONTROL group, PEDV RNA was present in feces at day post infection (dpi) 3 and the pigs seroconverted by dpi 14. In contrast, PEDV RNA in feces was not detected in any of the pigs in the other groups including the SD-PEDV-CONTROL group and none of the pigs had seroconverted by termination of the project at dpi 28. This work provides direct evidence that the experimental spray-drying process used in this study was effective in inactivating infectious PEDV in the plasma. Additionally, plasma collected from PEDV infected pigs at peak disease did not contain infectious PEDV. These findings suggest that the risk for PEDV transmission through commercially produced SDPP is minimal.

  1. Inhalants

    MedlinePlus

    ... Alerts Alcohol Club Drugs Cocaine Hallucinogens Heroin Inhalants Marijuana MDMA (Ecstasy/Molly) Methamphetamine Opioids Prescription Drugs & Cold ... Notes Articles Adolescent Cigarette, Alcohol Use Declines as Marijuana Use Rises ( February 2013 ) Program Helps Troubled Boys ...

  2. A user-friendly model for spray drying to aid pharmaceutical product development.

    PubMed

    Grasmeijer, Niels; de Waard, Hans; Hinrichs, Wouter L J; Frijlink, Henderik W

    2013-01-01

    The aim of this study was to develop a user-friendly model for spray drying that can aid in the development of a pharmaceutical product, by shifting from a trial-and-error towards a quality-by-design approach. To achieve this, a spray dryer model was developed in commercial and open source spreadsheet software. The output of the model was first fitted to the experimental output of a Büchi B-290 spray dryer and subsequently validated. The predicted outlet temperatures of the spray dryer model matched the experimental values very well over the entire range of spray dryer settings that were tested. Finally, the model was applied to produce glassy sugars by spray drying, an often used excipient in formulations of biopharmaceuticals. For the production of glassy sugars, the model was extended to predict the relative humidity at the outlet, which is not measured in the spray dryer by default. This extended model was then successfully used to predict whether specific settings were suitable for producing glassy trehalose and inulin by spray drying. In conclusion, a spray dryer model was developed that is able to predict the output parameters of the spray drying process. The model can aid the development of spray dried pharmaceutical products by shifting from a trial-and-error towards a quality-by-design approach.

  3. Generation of 1:1 Carbamazepine:Nicotinamide cocrystals by spray drying.

    PubMed

    Patil, Shashank P; Modi, Sameer R; Bansal, Arvind K

    2014-10-01

    The present study investigates the potential of spray drying as a technique for generation of pharmaceutical cocrystals. Carbamazepine-Nicotinamide cocrystal (CNC) was chosen as model cocrystal system for this study. Firstly, CNC was generated using liquid assisted grinding and used for generation of phase solubility diagram (PSD) and ternary phase diagram (TPD). Both PSD and TPD were carefully evaluated for phase behavior of CNC when equilibrated with solvent. The undersaturated region with respect to CNC, as depicted by TPD, was selected as target region to initiate cocrystallization experiments. Various points in this region, representative of different compositions of Carbamazepine, Nicotinamide and CNC, were selected and spray drying was carried out. The spray dried product was characterized for solid state properties and was compared with CNC generated by liquid assisted grinding. Spray drying successfully generated CNC of similar quality as those generated by liquid assisted grinding. Moreover, there was no significant impact of process variables on formation of CNC. Spray drying, owing to its simplicity and industrial scalability, can be a promising method for large scale cocrystal generation.

  4. Standardization of spray-dried powder of Piper betle hot water extract.

    PubMed

    Arawwawala, Liyanage Dona Ashanthi Menuka; Hewageegana, Horadugoda Gamage Sujatha Pushpakanthi; Arambewela, Lakshmi Sriyani Rajapaksha; Ariyawansa, Hettiarachchige Sami

    2011-04-01

    The leaves of Piper betle Linn. (Family: Piperaceae) possess several bioactivities and are used in the Traditional Medical systems of Sri Lanka. The present investigation was carried out to standardize the spray-dried powder of P. betle by (a) determination of physicochemical parameters, presence or absence of heavy metals, and microbial contamination; (b) screening for phytochemicals; and (c) development of High Pressure Liquid Chromatography (HPLC) fingerprint and densitogram. The percentages of moisture content, total ash, acid insoluble ash, water-soluble ash, and ethanol extractable matter of spray-dried powder of P. betle were 2.2-2.5, 6.8-7.0, 0.003-0.005, 4.1-4.3, and 15.8-16.2, respectively. The concentrations of all the tested heavy metals were below the WHO acceptable limits and bacterial species, such as Escherichia coli, Salmonella spp, Staphylococcus aureus, and Pseudomonas aeroginosa were not present in the P. betle spray-dried powder. Phenolic compounds, tannins, flavonoids steroids, and alkaloids were found to be present in the spray-dried powder of P. betle and HPLC fingerprint and densitogram clearly demonstrated the proportional differences of these chemical constituents. In conclusion, the results obtained from this study can be used to standardize the spray-dried powder of P. betle.

  5. Revealing facts behind spray dried solid dispersion technology used for solubility enhancement

    PubMed Central

    Patel, Bhavesh B.; Patel, Jayvadan K.; Chakraborty, Subhashis; Shukla, Dali

    2013-01-01

    Poor solubility and bioavailability of an existing or newly synthesized drug always pose challenge in the development of efficient pharmaceutical formulation. Numerous technologies can be used to improve the solubility and among them amorphous solid dispersion based spray drying technology can be successfully useful for development of product from lab scale to commercial scale with a wide range of powder characteristics. Current review deals with the importance of spray drying technology in drug delivery, basically for solubility and bioavailability enhancement. Role of additives, selection of polymer, effect of process and formulation parameters, scale up optimization, and IVIVC have been covered to gain the interest of readers about the technology. Design of experiment (DoE) to optimize the spray drying process has been covered in the review. A lot more research work is required to evaluate spray drying as a technology for screening the right polymer for solid dispersion, especially to overcome the issue related to drug re-crystallization and to achieve a stable product both in vitro and in vivo. Based on the recent FDA recommendation, the need of the hour is also to adopt Quality by Design approach in the manufacturing process to carefully optimize the spray drying technology for its smooth transfer from lab scale to commercial scale. PMID:27134535

  6. Stabilisation of proteins via mixtures of amino acids during spray drying.

    PubMed

    Ajmera, Ankur; Scherließ, Regina

    2014-03-10

    Biologicals are often formulated as solids in an effort to preserve stability which generally requires stabilising excipients for proper drying. The purpose of this study was to screen amino acids and their combinations for their stabilising effect on proteins during spray drying. Catalase, as model protein, was spray dried in 1+1 or 1+2 ratios with amino acids. Some amino acids namely arginine, glycine and histidine showed good retention of catalase functionality after spray drying and subsequent storage stress. A 1+1 combination of arginine and glycine in a 1+2 ratio with catalase resulted in a tremendously good stabilising effect. Storage at high temperature/humidity also showed beneficial effects of this combination. To evaluate whether this was a general principle, these findings were transferred to an antigenic protein of comparable size and supramolecular structure (haemagglutinin) as well as to a smaller enzyme (lysozyme). Upon spray drying with the combination of amino acids it could be shown that both proteins remain more stable especially after storage compared to the unprotected protein. The combination of arginine and glycine is tailored to the needs of protein stabilisation during spray drying and may hence be utilised in dry powder formulation of biomolecules with superior stability characteristics.

  7. A User-Friendly Model for Spray Drying to Aid Pharmaceutical Product Development

    PubMed Central

    Grasmeijer, Niels; de Waard, Hans; Hinrichs, Wouter L. J.; Frijlink, Henderik W.

    2013-01-01

    The aim of this study was to develop a user-friendly model for spray drying that can aid in the development of a pharmaceutical product, by shifting from a trial-and-error towards a quality-by-design approach. To achieve this, a spray dryer model was developed in commercial and open source spreadsheet software. The output of the model was first fitted to the experimental output of a Büchi B-290 spray dryer and subsequently validated. The predicted outlet temperatures of the spray dryer model matched the experimental values very well over the entire range of spray dryer settings that were tested. Finally, the model was applied to produce glassy sugars by spray drying, an often used excipient in formulations of biopharmaceuticals. For the production of glassy sugars, the model was extended to predict the relative humidity at the outlet, which is not measured in the spray dryer by default. This extended model was then successfully used to predict whether specific settings were suitable for producing glassy trehalose and inulin by spray drying. In conclusion, a spray dryer model was developed that is able to predict the output parameters of the spray drying process. The model can aid the development of spray dried pharmaceutical products by shifting from a trial-and-error towards a quality-by-design approach. PMID:24040240

  8. Nano-amorphous spray dried powder to improve oral bioavailability of itraconazole.

    PubMed

    Kumar, Sumit; Shen, Jie; Burgess, Diane J

    2014-10-28

    The objective of this study was to formulate nano-amorphous spray-dried powders of itraconazole to enhance its oral bioavailability. A combination approach of solvent-antisolvent precipitation followed by spray drying was used. DoE studies were utilized to understand the critical processing parameters: antisolvent-to-solvent ratio, drug concentration and stabilizer concentration. Particle size was the critical quality attribute. Spray drying of the nano-precipitated formulation was performed with several auxiliary excipients to obtain nano-sized amorphous powder formulations. PLM, DSC and PXRD were utilized to characterize the spray-dried powders. In vitro dissolution and in vivo bioavailability studies of the nano-amorphous powders were performed. The particle size of the nano-formulations was dependent on the drug concentration. The smallest size precipitates were obtained with low drug concentration. All high molecular weight auxiliary excipients and mannitol containing formulations were unstable and crystallized during spray drying. Formulations containing disaccharides were amorphous and non-aggregating. In vitro dissolution testing and in vivo studies showed the superior performance of nano-amorphous formulations compared to melt-quench amorphous and crystalline itraconazole formulations. This study shows superior oral bioavailability of nano-amorphous powders compared to macro-amorphous powders. The nano-amorphous formulation showed similar bioavailability to the nano-crystalline formulation but with a faster absorption profile.

  9. Revealing facts behind spray dried solid dispersion technology used for solubility enhancement.

    PubMed

    Patel, Bhavesh B; Patel, Jayvadan K; Chakraborty, Subhashis; Shukla, Dali

    2015-09-01

    Poor solubility and bioavailability of an existing or newly synthesized drug always pose challenge in the development of efficient pharmaceutical formulation. Numerous technologies can be used to improve the solubility and among them amorphous solid dispersion based spray drying technology can be successfully useful for development of product from lab scale to commercial scale with a wide range of powder characteristics. Current review deals with the importance of spray drying technology in drug delivery, basically for solubility and bioavailability enhancement. Role of additives, selection of polymer, effect of process and formulation parameters, scale up optimization, and IVIVC have been covered to gain the interest of readers about the technology. Design of experiment (DoE) to optimize the spray drying process has been covered in the review. A lot more research work is required to evaluate spray drying as a technology for screening the right polymer for solid dispersion, especially to overcome the issue related to drug re-crystallization and to achieve a stable product both in vitro and in vivo. Based on the recent FDA recommendation, the need of the hour is also to adopt Quality by Design approach in the manufacturing process to carefully optimize the spray drying technology for its smooth transfer from lab scale to commercial scale.

  10. Modification of the solid-state nature of sulfathiazole and sulfathiazole sodium by spray drying.

    PubMed

    Bianco, Stefano; Caron, Vincent; Tajber, Lidia; Corrigan, Owen I; Nolan, Lorraine; Hu, Yun; Healy, Anne Marie

    2012-06-01

    Solid-state characterisation of a drug following pharmaceutical processing and upon storage is fundamental to successful dosage form development. The aim of the study was to investigate the effects of using different solvents, feed concentrations and spray drier configuration on the solid-state nature of the highly polymorphic model drug, sulfathiazole (ST) and its sodium salt (STNa). The drugs were spray-dried from ethanol, acetone and mixtures of these organic solvents with water. Additionally, STNa was spray-dried from pure water. The physicochemical properties including the physical stability of the spray-dried powders were compared to the unprocessed materials. Spray drying of ST from either acetonic or ethanolic solutions with the spray drier operating in a closed cycle mode yielded crystalline powders. In contrast, the powders obtained from ethanolic solutions with the spray drier operating in an open cycle mode were amorphous. Amorphous ST crystallised to pure form I at ≤35 % relative humidity (RH) or to polymorphic mixtures at higher RH values. The usual crystal habit of form I is needle-like, but spherical particles of this polymorph were generated by spray drying. STNa solutions resulted in an amorphous material upon processing, regardless of the solvent and the spray drier configuration employed. Moisture induced crystallisation of amorphous STNa to a sesquihydrate, whilst crystallisation upon heating gave rise to a new anhydrous polymorph. This study indicated that control of processing and storage parameters can be exploited to produce drugs with a specific/desired solid-state nature.

  11. Standardization of spray-dried powder of Piper betle hot water extract

    PubMed Central

    Arawwawala, Liyanage Dona Ashanthi Menuka; Hewageegana, Horadugoda Gamage Sujatha Pushpakanthi; Arambewela, Lakshmi Sriyani Rajapaksha; Ariyawansa, Hettiarachchige Sami

    2011-01-01

    The leaves of Piper betle Linn. (Family: Piperaceae) possess several bioactivities and are used in the Traditional Medical systems of Sri Lanka. The present investigation was carried out to standardize the spray-dried powder of P. betle by (a) determination of physicochemical parameters, presence or absence of heavy metals, and microbial contamination; (b) screening for phytochemicals; and (c) development of High Pressure Liquid Chromatography (HPLC) fingerprint and densitogram. The percentages of moisture content, total ash, acid insoluble ash, water-soluble ash, and ethanol extractable matter of spray-dried powder of P. betle were 2.2-2.5, 6.8-7.0, 0.003-0.005, 4.1-4.3, and 15.8-16.2, respectively. The concentrations of all the tested heavy metals were below the WHO acceptable limits and bacterial species, such as Escherichia coli, Salmonella spp, Staphylococcus aureus, and Pseudomonas aeroginosa were not present in the P. betle spray-dried powder. Phenolic compounds, tannins, flavonoids steroids, and alkaloids were found to be present in the spray-dried powder of P. betle and HPLC fingerprint and densitogram clearly demonstrated the proportional differences of these chemical constituents. In conclusion, the results obtained from this study can be used to standardize the spray-dried powder of P. betle. PMID:21716924

  12. Evaluation of some water-miscible organic solvents for spray-drying enzymes and carbohydrates.

    PubMed

    Sass, Anke; Lee, Geoffrey

    2014-06-01

    The spray-drying behaviour of 16 water-miscible organic solvents on a bench-scale machine (Büchi B290 with inert loop) was determined under mild-to-moderate process conditions, namely inlet gas temperature of 130 °C and liquid feed flow rate of ≤3 mL/min. The solvents with boiling points below the inlet gas temperature could be fully dried (Group 1 solvents). The two exceptions were DMSO and DMF which despite their higher boiling points could be fully dried. The remaining solvents with boiling points above the inlet gas temperature were not fully dried during passage through the spray-dryer (Group 2 solvents). Trypsin and lysozyme when spray-dried from Group 1 solvent binary mixtures with water showed similar inactivation and residual water content, independent of solvent. The level of residual solvent was, however, strongly dependent on solvent. Trehalose (20%) and mannitol (10%) could be spray-dried from DMSO/water binary mixtures, but the amorphous disaccharide required higher inlet gas temperature. Trehalose/trypsin and mannitol/trypsin formulations showed differing degrees of protection against enzyme inactivation when spray-dried from Group 1 solvent binary mixtures with water. In all solvents the mannitol protected as well, if not better, than the trehalose. This study identifies some suitable organic solvents for spray-drying protein formulations, but also shows the difficulties of remaining organic solvent under the moderate inlet gas temperature used.

  13. Spray drying for preservation of erythrocytes: effect of atomization on hemolysis.

    PubMed

    McLean, Mary; Han, Xiao-Yue; Higgins, Adam Z

    2013-04-01

    Spray drying has the potential to enable storage of erythrocytes at room temperature in the dry state. The spray drying process involves atomization of a liquid into small droplets and drying of the droplets in a gas stream. In this short report, we focus on the atomization process. To decouple atomization from drying, erythrocyte suspensions were sprayed with a two-fluid atomizer nozzle using humid nitrogen as the atomizing gas. The median droplet size was less than 100 μm for all of the spray conditions investigated, indicating that the suspensions were successfully atomized. Hemolysis was significantly affected by the hematocrit of the erythrocyte suspension, the suspension flow rate, and the atomizing gas flow rate (p<0.01 in all cases). Under appropriate conditions, it was possible to achieve less than 2% hemolysis, suggesting that spray drying may be a feasible option for erythrocyte biopreservation.

  14. Optimising the Encapsulation of an Aqueous Bitter Melon Extract by Spray-Drying

    PubMed Central

    Tan, Sing Pei; Kha, Tuyen Chan; Parks, Sophie; Stathopoulos, Costas; Roach, Paul D.

    2015-01-01

    Our aim was to optimise the encapsulation of an aqueous bitter melon extract by spray-drying with maltodextrin (MD) and gum Arabic (GA). The response surface methodology models accurately predicted the process yield and retentions of bioactive concentrations and activity (R2 > 0.87). The optimal formulation was predicted and validated as 35% (w/w) stock solution (MD:GA, 1:1) and a ratio of 1.5:1 g/g of the extract to the stock solution. The spray-dried powder had a high process yield (66.2% ± 9.4%) and high retention (>79.5% ± 8.4%) and the quality of the powder was high. Therefore, the bitter melon extract was well encapsulated into a powder using MD/GA and spray-drying. PMID:28231214

  15. Curcumin encapsulation in submicrometer spray-dried chitosan/Tween 20 particles.

    PubMed

    O'Toole, Martin G; Henderson, Richard M; Soucy, Patricia A; Fasciotto, Brigitte H; Hoblitzell, Patrick J; Keynton, Robert S; Ehringer, William D; Gobin, Andrea S

    2012-08-13

    Optimal curcumin delivery for medicinal applications requires a drug delivery system that both solubilizes curcumin and prevents degradation. To achieve this, curcumin has been encapsulated in submicrometer chitosan/Tween 20 particles via a benchtop spray-drying process. Spray-drying parameters have been optimized using a Taguchi statistical approach to minimize particle size and to favor spheroid particles with smooth surfaces, as evaluated with scanning electron microscopy (SEM) imaging. Nearly spherical particles with 285 ± 30 nm diameter and 1.21 axial ratio were achieved. Inclusion of curcumin in the spray-drying solution results in complete encapsulation of curcumin within the chitosan/Tween 20 particles. Release studies confirm that curcumin can be released completely from the particles over a 2 h period.

  16. Optimising the Encapsulation of an Aqueous Bitter Melon Extract by Spray-Drying.

    PubMed

    Tan, Sing Pei; Kha, Tuyen Chan; Parks, Sophie; Stathopoulos, Costas; Roach, Paul D

    2015-09-09

    Our aim was to optimise the encapsulation of an aqueous bitter melon extract by spray-drying with maltodextrin (MD) and gum Arabic (GA). The response surface methodology models accurately predicted the process yield and retentions of bioactive concentrations and activity (R² > 0.87). The optimal formulation was predicted and validated as 35% (w/w) stock solution (MD:GA, 1:1) and a ratio of 1.5:1 g/g of the extract to the stock solution. The spray-dried powder had a high process yield (66.2% ± 9.4%) and high retention (>79.5% ± 8.4%) and the quality of the powder was high. Therefore, the bitter melon extract was well encapsulated into a powder using MD/GA and spray-drying.

  17. Use of spray-dried zirconia microspheres in the separation of immunoglobulins from cell culture supernatant.

    PubMed

    Subramanian, A; Carr, P W; McNeff, C V

    2000-08-18

    A method suitable for the isolation of monoclonal antibodies (MAbs) on novel zirconia microspheres (20-30 microm) is described. Zirconia microspheres were generated by spray drying colloidal zirconia. Spray-dried zirconia microspheres were further classified and characterized by X-ray diffraction, BET porosimetry and scanning electron microscopy. Spray-dried zirconia microspheres were modified with ethylenediamine-N,N'-tetra(methylenephosphonic) acid (EDTPA) to create a cation-exchange chromatographic support. The chromatographic behavior of a semi-preparative column packed with EDTPA-modified zirconia microspheres was evaluated and implications for scale-up are provided. EDTPA-modified zirconia microspheres were further used to purify MAbs from cell culture supernatant. Analysis by enzyme linked immunosorbent assay and gel electrophoresis demonstrate that MAbs can be recovered from a cell culture supernatant at high yield (92-98%) and high purity (>95%) in a single chromatographic step.

  18. Synthesis of nickel oxide nanospheres by a facile spray drying method and their application as anode materials for lithium ion batteries

    SciTech Connect

    Xiao, Anguo Zhou, Shibiao; Zuo, Chenggang; Zhuan, Yongbing; Ding, Xiang

    2015-10-15

    Graphical abstract: NiO nanospheres prepared by a facile spray drying method show high lithium ion storage performance as anode of lithium ion battery. - Highlights: • NiO nanospheres are prepared by a spray drying method. • NiO nanospheres are composed of interconnected nanoparticles. • NiO nanospheres show good lithium ion storage properties. - Abstract: Fabrication of advanced anode materials is indispensable for construction of high-performance lithium ion batteries. In this work, nickel oxide (NiO) nanospheres are fabricated by a facial one-step spray drying method. The as-prepared NiO nanospheres show diameters ranging from 100 to 600 nm and are composed of nanoparticles of 30–50 nm. As an anode for lithium ion batteries, the electrochemical properties of the NiO nanospheres are investigated by cyclic voltammetry (CV) and galvanostatic charge/discharge tests. The specific reversible capacity of NiO nanospheres is 656 mA h g{sup −1} at 0.1 C, and 476 mA h g{sup −1} at 1 C. The improvement of electrochemical properties is attributed to nanosphere structure with large surface area and short ion/electron transfer path.

  19. Designing CAF-adjuvanted dry powder vaccines: spray drying preserves the adjuvant activity of CAF01.

    PubMed

    Ingvarsson, Pall Thor; Schmidt, Signe Tandrup; Christensen, Dennis; Larsen, Niels Bent; Hinrichs, Wouter Leonardus Joseph; Andersen, Peter; Rantanen, Jukka; Nielsen, Hanne Mørck; Yang, Mingshi; Foged, Camilla

    2013-05-10

    Dry powder vaccine formulations are highly attractive due to improved storage stability and the possibility for particle engineering, as compared to liquid formulations. However, a prerequisite for formulating vaccines into dry formulations is that their physicochemical and adjuvant properties remain unchanged upon rehydration. Thus, we have identified and optimized the parameters of importance for the design of a spray dried powder formulation of the cationic liposomal adjuvant formulation 01 (CAF01) composed of dimethyldioctadecylammonium (DDA) bromide and trehalose 6,6'-dibehenate (TDB) via spray drying. The optimal excipient to stabilize CAF01 during spray drying and for the design of nanocomposite microparticles was identified among mannitol, lactose and trehalose. Trehalose and lactose were promising stabilizers with respect to preserving liposome size, as compared to mannitol. Trehalose and lactose were in the glassy state upon co-spray drying with the liposomes, whereas mannitol appeared crystalline, suggesting that the ability of the stabilizer to form a glassy matrix around the liposomes is one of the prerequisites for stabilization. Systematic studies on the effect of process parameters suggested that a fast drying rate is essential to avoid phase separation and lipid accumulation at the surface of the microparticles during spray drying. Finally, immunization studies in mice with CAF01 in combination with the tuberculosis antigen Ag85B-ESAT6-Rv2660c (H56) demonstrated that spray drying of CAF01 with trehalose under optimal processing conditions resulted in the preservation of the adjuvant activity in vivo. These data demonstrate the importance of liposome stabilization via optimization of formulation and processing conditions in the engineering of dry powder liposome formulations.

  20. Utilization of spray drying technique for improvement of dissolution and anti-inflammatory effect of Meloxicam.

    PubMed

    Shazly, Gamal; Badran, Mohamed; Zoheir, Khairy; Alomrani, Abdullah

    2015-01-01

    Meloxicam (MLX) is a poorly water-soluble non steroidal anti-inflammatory drug (NSAID). The main objective of the present work was to enhance the dissolution of MLX and thus its bioavailability by the aid of additives. The novelty of this work rises from the utilization of spray drying technology to produce micro particulates solid dispersion systems containing MLX in the presence of small amount of additives. Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), and Scan Electron Microscope (SEM) were used for studying the physico-chemical and morphological properties of MLX samples. The dissolution of MLX samples was investigated in two different pH media. The morphology of MLX solid dispersion micro-particles was spherical in shape according to SEM. FT-IR profiles indicated that a complex was formed between MLX and the additives. DSC patterns of the MLX micro-particles suggested a reduction in the crystallinity of MLX and probability of presence of an interaction between MLX and the additives. The rate of dissolution of the spray-dried MLX enhanced as compared with the unprocessed MLX in both acidic and neutral media. It was found that 100% of the added MLX released within 5 min in phosphate buffer dissolution medium (pH 7.4) compared to that of the unprocessed MLX (15% in 60 min). Such increase rate in the dissolution of the spray dried MLX could be attributed to the increase in wettability of MLX particles and the hydrophilic nature of the additives. The anti-inflammatory effect of the spray dried MLX was explored using formalin induced rat paw edema model. The spray-dried samples showed an increase in the anti-inflammatory activity of MLX as compared to the unprocessed MLX. This work reveals that the spray drying technique is suitable for preparation of micro-particles with improved dissolution and anti-inflammatory effect of MLX.

  1. Cellulose acetate butyrate and polycaprolactone for ketoprofen spray-dried microsphere preparation.

    PubMed

    Giunchedi, P; Conti, B; Maggi, L; Conte, U

    1994-01-01

    Ketoprofen-loaded microspheres made with a polymeric blend were prepared by a spray-drying technique. Organic solutions of two polymers, cellulose acetate butyrate (CAB) and poly(epsilon-caprolactone) (PCL), in different weight ratios, and of ketoprofen (Ket) were prepared and sprayed, in different experimental conditions, achieving drug-loaded microspheres. The obtained spray-dried microspheres were characterized in terms of yield of production, shape, size, surface properties and drug content, and their in vitro drug release behaviours were determined at different pH values.

  2. Improvement of Physico-mechanical Properties of Partially Amorphous Acetaminophen Developed from Hydroalcoholic Solution Using Spray Drying Technique

    PubMed Central

    Sadeghi, Fatemeh; Torab, Mansour; Khattab, Mostafa; Homayouni, Alireza; Afrasiabi Garekani, Hadi

    2013-01-01

    Objective(s): This study was performed aiming to investigate the effect of particle engineering via spray drying of hydroalcoholic solution on solid states and physico-mechanical properties of acetaminophen. Materials and Methods: Spray drying of hydroalcoholic solution (25% v/v ethanol/water) of acetaminophen (5% w/v) in the presence of small amounts of polyninylpyrrolidone K30 (PVP) (0, 1.25, 2.5 and 5% w/w based on acetaminophen weight) was carried out. The properties of spray dried particles namely morphology, surface characteristics, particle size, crystallinity, dissolution rate and compactibility were evaluated. Results: Spray drying process significantly changed the morphology of acetaminophen crystals from acicular (rod shape) to spherical microparticle. Differential scanning calorimetery (DSC) and x-ray powder diffraction (XRPD) studies ruled out any polymorphism in spray dried samples, however, a major reduction in crystallinity up to 65%, especially for those containing 5% w/w PVP was observed. Spray dried acetaminophen particles especially those obtained in the presence of PVP exhibited an obvious improvement of the dissolution and compaction properties. Tablets produced from spray dried samples exhibited excellent crushing strengths and no tendency to cap. Conclusions: The findings of this study revealed that spray drying of acetaminophen from hydroalcoholic solution in the presence of small amount of PVP produced partially amorphous particles with improved dissolution and excellent compaction properties. PMID:24379968

  3. Spray drying of lipid-based systems loaded with Camellia sinensis polyphenols.

    PubMed

    Secolin, Vanessa A; Souza, Claudia R F; Oliveira, Wanderley P

    2017-03-01

    In this work, spray-dried lipid systems based on soy phosphatidylcholine, cholesterol and lauroyl polyoxylglycerides for entrapping Green tea polyphenols were produced. The aim was to study the effects of the encapsulating composition and spray drying conditions on the system performance and physicochemical product properties. The spray dryer powder production yield falls around 50.7 ± 2.8%, which is typical for lab scale spray dryers. Wrinkled and rounded particles, with low surface porosities were generated, independent of the drying carriers (trehalose or lactose) used. The product showed high encapsulation efficiency of Green tea polyphenols, which was promptly redispersible in water. It presented low density, and good compressive and flow properties. The results herein reported confirm the feasibility of the entrapment of Green tea polyphenols in lipid-based compositions by spray drying in presence of the drying carriers evaluated. The spray-dried microparticles show high potential to be used as additive in food, nutraceutical and pharmaceutical products.

  4. Effect of emulsification and spray-drying microencapsulation on the antilisterial activity of transcinnamaldehyde.

    PubMed

    Trinh, Nga-Thi-Thanh; Lejmi, Raja; Gharsallaoui, Adem; Dumas, Emilie; Degraeve, Pascal; Thanh, Mai Le; Oulahal, Nadia

    2015-01-01

    Spray-dried redispersible transcinnamaldehyde (TC)-in-water emulsions were prepared in order to preserve its antibacterial activity; 5% (w/w) TC emulsions were first obtained with a rotor-stator homogeniser in the presence of either soybean lecithin or sodium caseinate as emulsifiers. These emulsions were mixed with a 30% (w/w) maltodextrin solution before feeding a spray-dryer. The antibacterial activity of TC alone, TC emulsions with and without maltodextrin before and after spray-drying were assayed by monitoring the growth at 30 °C of Listeria innocua in their presence and in their absence (control). Whatever the emulsifier used, antilisterial activity of TC was increased following its emulsification. However, reconstituted spray-dried emulsions stabilised by sodium caseinate had a higher antibacterial activity suggesting that they better resisted to spray-drying. This was consistent with observation that microencapsulation efficiencies were 27.6% and 78.7% for emulsions stabilised by lecithin and sodium caseinate, respectively.

  5. A critical review on the spray drying of fruit extract: effect of additives on physicochemical properties.

    PubMed

    Krishnaiah, Duduku; Nithyanandam, Rajesh; Sarbatly, Rosalam

    2014-01-01

    Spray drying accomplishes drying while particles are suspended in the air and is one method in the family of suspended particle processing systems, along with fluid-bed drying, flash drying, spray granulation, spray agglomeration, spray reaction, spray cooling, and spray absorption. This drying process is unique because it involves both particle formation and drying. The present paper reviews spray drying of fruit extracts, such as acai, acerola pomace, gac, mango, orange, cactus pear, opuntia stricta fruit, watermelon, and durian, and the effects of additives on physicochemical properties such as antioxidant activity, total carotenoid content, lycopene and β-carotene content, hygroscopy, moisture content, volatile retention, stickiness, color, solubility, glass transition temperature, bulk density, rehydration, caking, appearance under electron microscopy, and X-ray powder diffraction. The literature clearly demonstrates that the effect of additives and encapsulation play a vital role in determining the physicochemical properties of fruit extract powder. The technical difficulties in spray drying of fruit extracts can be overcome by modifying the spray dryer design. It also reveals that spray drying is a novel technology for converting fruit extract into powder form.

  6. Properties of chitosan microencapsulated orange oil prepared by spray-drying and its stability to detergents

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Fragrance encapsulated in small particles of less than 20 µm diameter is preferred for use in textiles. In this study, aromatic orange oil was emulsified in a continuous phase of chitosan and spray-dried to produce microcapsules. The most effective combination of emulsifiers, ratio of chitosan to oi...

  7. Crystallization of spray-dried lactose/protein mixtures in humid air

    NASA Astrophysics Data System (ADS)

    Shawqi Barham, A.; Kamrul Haque, Md.; Roos, Yrjö H.; Kieran Hodnett, B.

    2006-10-01

    An in situ crystallization technique with X-ray diffraction analysis complemented by ex situ scanning electron microscopy and chromatographic analysis of the α/( α+ β) solid-state anomeric ratios has been developed to study the crystallization of lactose/protein mixtures in humid air. This technique was used to determine changes in phase composition and morphology during crystallization. Following an induction period during which water is sorbed, crystallization is rapid and the predominant phase observed using the in situ method in spray-dried lactose/sodium-caseinate, albumin and gelatin is α-lactose monohydrate. However, in the case of spray-dried lactose/whey protein isolate (WPI) the predominant phase that appears is the α/ β mixed phase with smaller amounts of α-lactose monohydrate. With pure lactose the α/ β mixed phase appears as a transient shortly after the onset of crystallization and α-lactose monohydrate and β-lactose both appear as stable crystalline phases at longer times. Another transient phase with 2 θ=12.2°, 20.7° and 21.8° was observed in spray-dried lactose/albumin. This phase decomposed as α-lactose monohydrate developed. Three phases seem to persist in the case of spray-dried lactose/gelatin, namely the phase with peaks at 2 θ=12.2°, 20.7° and 21.8°, α-lactose monohydrate and β-lactose for the duration of the in situ experiment.

  8. Spray drying of Pomegranate Juice using maltodextrin/cyclodextrin blends as the wall material

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Microencapsulation protects sensitive nutrients for preservation, masking flavors, or to enhance delivery. Ratios of maltodextrin and '-cyclodextrin (20:0, 19:1, and 17:3 % w/w) were dissolved in water and mixed with pomegranate juice for spray drying with inlet temperatures of 120, 140 and 160°C. ...

  9. Hot Melt Extrusion and Spray Drying of Co-amorphous Indomethacin-Arginine With Polymers.

    PubMed

    Lenz, Elisabeth; Löbmann, Korbinian; Rades, Thomas; Knop, Klaus; Kleinebudde, Peter

    2017-01-01

    Co-amorphous drug-amino acid systems have gained growing interest as an alternative to common amorphous formulations which contain polymers as stabilizers. Several preparation methods have recently been investigated, including vibrational ball milling on a laboratory scale or spray drying in a larger scale. In this study, the feasibility of hot melt extrusion for continuous manufacturing of co-amorphous drug-amino acid formulations was examined, challenging the fact that amino acids melt with degradation at high temperatures. Furthermore, the need for an addition of a polymer in this process was evaluated. After a polymer screening via the solvent evaporation method, co-amorphous indomethacin-arginine was prepared by a melting-solvent extrusion process without and with copovidone. The obtained products were characterized with respect to their solid-state properties, non-sink dissolution behavior, and stability. Results were compared to those of spray-dried formulations with the same compositions and to spray-dried indomethacin-copovidone. Overall, stable co-amorphous systems could be prepared by extrusion without or with copovidone, which exhibited comparable molecular interaction properties to the respective spray-dried products, while phase separation was detected by differential scanning calorimetry in several cases. The formulations containing indomethacin in combination with arginine and copovidone showed enhanced dissolution behavior over the formulations with only copovidone or arginine.

  10. The impact of atomization on the surface composition of spray-dried milk droplets.

    PubMed

    Foerster, Martin; Gengenbach, Thomas; Woo, Meng Wai; Selomulya, Cordelia

    2016-04-01

    The dominant presence of fat at the surface of spray-dried milk powders has been widely reported in the literature and described as resulting in unfavourable powder properties. The mechanism(s) causing this phenomenon are yet to be clearly identified. A systematic investigation of the component distribution in atomized droplets and spray-dried particles consisting of model milk systems with different fat contents demonstrated that atomization strongly influences the final surface composition. Cryogenic flash-freezing of uniform droplets from a microfluidic jet nozzle directly after atomization helped to distinguish the influence of the atomization stage from the drying stage. It was confirmed that the overrepresentation of fat on the surface is independent of the atomization technique, including a pressure-swirl single-fluid spray nozzle and a pilot-scale rotary disk spray dryer commonly used in industry. It is proposed that during the atomization stage a disintegration mechanism along the oil-water interface of the fat globules causes the surface predominance of fat. X-ray photoelectron spectroscopic measurements detected the outermost fat layer and some adjacent protein present on both atomized droplets and spray-dried particles. Confocal laser scanning microscopy gave a qualitative insight into the protein and fat distribution throughout the cross-sections, and confirmed the presence of a fat film along the particle surface. The film remained on the surface in the subsequent drying stage, while protein accumulated underneath, driven by diffusion. The results demonstrated that atomization induces component segregation and fat-rich surfaces in spray-dried milk powders, and thus these cannot be prevented by adjusting the spray drying conditions.

  11. Hot melt extrusion versus spray drying: hot melt extrusion degrades albendazole.

    PubMed

    Hengsawas Surasarang, Soraya; Keen, Justin M; Huang, Siyuan; Zhang, Feng; McGinity, James W; Williams, Robert O

    2017-05-01

    The purpose of this study was to enhance the dissolution properties of albendazole (ABZ) by the use of amorphous solid dispersions. Phase diagrams of ABZ-polymer binary mixtures generated from Flory-Huggins theory were used to assess miscibility and processability. Forced degradation studies showed that ABZ degraded upon exposure to hydrogen peroxide and 1 N NaOH at 80 °C for 5 min, and the degradants were albendazole sulfoxide (ABZSX), and ABZ impurity A, respectively. ABZ was chemically stable following exposure to 1 N HCl at 80 °C for one hour. Thermal degradation profiles show that ABZ, with and without Kollidon(®) VA 64, degraded at 180 °C and 140 °C, respectively, which indicated that ABZ could likely be processed by thermal processing. Following hot melt extrusion, ABZ degraded up to 97.4%, while the amorphous ABZ solid dispersion was successfully prepared by spray drying. Spray-dried ABZ formulations using various types of acids (methanesulfonic acid, sulfuric acid and hydrochloric acid) and polymers (Kollidon(®) VA 64, Soluplus(®) and Eudragit(®) E PO) were studied. The spray-dried ABZ with methanesulfonic acid and Kollidon(®) VA 64 substantially improved non-sink dissolution in acidic media as compared to bulk ABZ (8-fold), physical mixture of ABZ:Kollidon(®) VA 64 (5.6-fold) and ABZ mesylate salt (1.6-fold). No degradation was observed in the spray-dried product for up to six months and less than 5% after one-year storage. In conclusion, amorphous ABZ solid dispersions in combination with an acid and polymer can be prepared by spray drying to enhance dissolution and shelf-stability, whereas those made by melt extrusion are degraded.

  12. Impact of feed counterion addition and cyclone type on aerodynamic behavior of alginic-atenolol microparticles produced by spray drying.

    PubMed

    Ceschan, Nazareth Eliana; Bucalá, Verónica; Ramírez-Rigo, María Verónica; Smyth, Hugh David Charles

    2016-12-01

    The inhalatory route has emerged as an interesting non-invasive alternative for drug delivery. This allows both pulmonary (local) and systemic treatments (via alveolar absorption). Further advantages in terms of stability, dose and patient preference have often lead researchers to focus on dry powder inhaler delivery systems. Atenolol is an antihypertensive drug with low oral bioavailability and gastrointestinal side effects. Because atenolol possesses adequate permeation across human epithelial membranes, it has been proposed as a good candidate for inhalatory administration. In a previous work, atenolol was combined with alginic acid (AA) and microparticles were developed using spray-drying (SD) technology. Different AA/atenolol ratios, total feed solid content and operative variables were previously explored. In order to improve particle quality for inhalatory administration and the SD yield, in this work the AA acid groups not neutralized by atenolol were kept either free or neutralized to pH∼7 and two different SD cyclones were used. Particle morphology, flow properties, moisture uptake and in vitro aerosolization behavior at different pressure drops were studied. When the AA acid groups were neutralized, particle size decreased as a consequence of the lower feed viscosity. The SD yield and in vitro particle deposition significantly increased when a high performance cyclone was employed, and even when lactose carrier particles were not used. Although the in vitro particle deposition decreased when the storage relative humidity increased, the developed SD powders showed adequate characteristics to be administered by inhalatory route up to storage relative humidities of about 60%.

  13. Endospore production allows using spray-drying as a possible formulation system of the biocontrol agent Bacillus subtilis CPA-8.

    PubMed

    Yánez-Mendizabal, V; Viñas, I; Usall, J; Cañamás, T; Teixidó, N

    2012-04-01

    The role of endospore production by Bacillus subtilis CPA-8 on survival during spray-drying was investigated by comparison with a non-spore-forming biocontrol agent Pantoea agglomerans CPA-2. Endospore formation promoted heat resistance in CPA-8 depending on growth time (72 h cultures were more resistant than 24 h ones). The survival of CPA-8 and CPA-2 after spray-drying was determined after being grown in optimised media for 24 and 72 h. Spray-dried 72 h CPA-8 had the best survival (32%), while CPA-2 viability was less than 2%. CPA-8 survival directly related with its ability to produce endospores. Spray-dried CPA-8 reduced Monilinia fructicola conidia germination similarly to fresh cells, demonstrating that spray-drying did not adversely affect biocontrol efficacy. Endospore production thus improves CPA-8 resistance to spray-drying. These results can provide a reliable basis for optimising of the spray-drying formulation process for CPA-8 and other microorganisms.

  14. Development of a rapid screening protocol for selection of strains resistant to spray drying and storage in dry powder.

    PubMed

    Reimann, S; Grattepanche, F; Baggenstos, C; Rezzonico, E; Berger, B; Arigoni, F; Lacroix, C

    2010-06-01

    An efficient screening method for selection of Bifidobacterium longum strains resistant to spray drying and storage was developed based on randomly amplified polymorphic DNA (RAPD) for identification of the best survivors in mixed strains bacterial preparations. Three different primers were used to generate RAPD profiles of 22 B. longum strains. All strains were distinguished according to their RAPD profiles except for the strain NCC2705 and its H(2)O(2) resistant derivative variant. The 22 strains were grouped in 3 batches of 7, 7 and 8 strains and subjected to spray drying and storage at 30 and 37 °C under anaerobic conditions. Batch survival rates after spray drying reached 17.1±4.4%. Strains showing the highest prevalence and/or resistance to storage at 37 °C were selected from individual batches for subsequent spray drying and storage testing. After 67 days of storage, NCC572 was identified as the dominant strain in powder. The stability of strain NCC572 was confirmed by performing single spray drying and storage tests. Out of 22 B. longum strains, a robust strain was identified by combining RAPD with a simultaneous screening test for survival under spray drying and storage. The method allowed a fast screening of B. longum strains in mixture for resistance to spray drying and storage compared to traditional screening procedures carried out with individual strains, in the same conditions. This approach could be applied to other stress conditions.

  15. Preparation and In vitro / In vivo characterization of spray dried microsphere formulation encapsulating 4-chlorocurcumin

    PubMed Central

    Gogu, P. K.; Jithan, A. V.

    2010-01-01

    The objective of the present study was to prepare and characterize in vitro and in vivo performance of a sustained release microsphere formulation of 4-chlorocurcumin, a novel curcumin analogue. A spray dried technique with ethylcellulose as the polymer was used in the preparation of these microspheres. Microspheres were characterized for drug content, particle size and shape, in vitro drug release and the drug-polymer interaction. To assess in vivo performance, both pharmacokinetics and hepatoprotective activity were investigated. Results were compared with an equivalent i.v. solution. The microspheres of 4-chlorocurcumin with ethylcellulose were successfully prepared using a spray-dried technique. These microspheres were able to sustain the release of the drug both in vitro as well as in vivo. Microspheres offered better pharmacokinetic and hepatoprotective properties to the drug compared to its solution form. PMID:21188044

  16. Effect of sucrose on physical properties of spray-dried whole milk powder.

    PubMed

    Ma, U V Lay; Ziegler, G R; Floros, J D

    2008-11-01

    Spray-dried whole milk powders were prepared from whole condensed milk with various sucrose concentrations (0%, 2.5%, 5%, 7.5%, and 10% w/w), and their glass transition temperature and some physical properties of importance in chocolate manufacture were evaluated. In milk powder samples, the glass transition temperature and free-fat content decreased in a nonlinear manner with sucrose addition. Moreover, increasing sucrose concentration reduced the formation of dents on the particle surface. Addition of sucrose in whole condensed milk increased linearly the apparent particle density and in a nonlinear manner the particle size of spray-dried milk powders. The particle size volume distribution of milk powders with the highest sucrose concentration differed from the log-normal distribution of the other samples due to the formation of large agglomerates. Neither vacuole volume, nor the amorphous state of milk powders was affected by sucrose addition.

  17. Application of cashew tree gum on the production and stability of spray-dried fish oil.

    PubMed

    Botrel, Diego Alvarenga; Borges, Soraia Vilela; Fernandes, Regiane Victória de Barros; Antoniassi, Rosemar; de Faria-Machado, Adelia Ferreira; Feitosa, Judith Pessoa de Andrade; de Paula, Regina Celia Monteiro

    2017-04-15

    Evaluation of cashew gum compared to conventional materials was conducted regarding properties and oxidative stability of spray-dried fish oil. Emulsions produced with cashew gum showed lower viscosity when compared to Arabic gum. The particle size was larger (29.9μm) when cashew gum was used, and the encapsulation efficiency reached 76%, similar to that of modified starch but higher than that for Arabic gum (60%). The oxidation process for the surface oil was conducted and a relative lower formation of oxidation compounds was observed for the cashew gum treatment. GAB model was chosen to describe the moisture adsorption isotherm behaviours. Microparticles produced using Arabic and cashew gums showed greater water adsorption when exposed to higher relative humidities. Microparticles produced using cashew gum were more hygroscopic however encapsulation efficiency were higher and surface oil oxidation were less pronounced. Cashew gum can be further explored as an encapuslant material for spray drying processes.

  18. Instability of bacteriophages in spray-dried trehalose powders is caused by crystallization of the matrix.

    PubMed

    Vandenheuvel, Dieter; Meeus, Joke; Lavigne, Rob; Van den Mooter, Guy

    2014-09-10

    Spray drying is a valuable technique in pharmaceutical dosage formulation, capable of producing amorphous, spherical powders, suitable for pulmonary deposition and further downstream processing. In this study, we show that spray drying bacteriophages together with trehalose results in an amorphous powder matrix with high glass transition temperature (between 116 and 118°C), typical for amorphous trehalose. These powders are stable at low temperatures (4°C) and relative humidity (0%). However, high humidity causes crystallization of the amorphous matrix, destroying the embedded phages. Furthermore, storage at higher temperature (25°C) causes thermal instability of the embedded phages. The results show that storage conditions are important parameters to take into account in phage therapy development. The resulting particles are hollow spheres, with suitable aerodynamic diameters for deposition into the deep lungs. This opens possibilities to use these phage-containing powder formulations to tackle pulmonary infectious diseases, especially caused by antibiotic resistant pathogens.

  19. Functional properties and stability of spray-dried pigments from Bordo grape (Vitis labrusca) winemaking pomace.

    PubMed

    Souza, Volnei Brito de; Fujita, Alice; Thomazini, Marcelo; da Silva, Edson Roberto; Lucon, João Francisco; Genovese, Maria Inés; Favaro-Trindade, Carmen Sílvia

    2014-12-01

    The stability of anthocyanin and phenolic compounds, the antioxidant capacity, the antimicrobial activity and the capacity to inhibit arginase from Leishmania were evaluated in spray-dried powders from Bordo grape winemaking pomace extract. The pigments were produced using maltodextrin as the carrier agent at concentrations varying from 10% to 30% and air entrance temperatures varying from 130 to 170°C. A sample of freeze-dried extract without the carrier was also evaluated. The anthocyanins in the spray-dried samples showed good stability during storage, better than the freeze-dried and liquid extracts. The samples were capable of inhibiting the growth of Staphylococcus aureus and Listeria monocytogenes and showed high inhibitory capacity against the enzyme arginase from Leishmania. These results provide evidence that Bordo grapes from the winemaking process have the potential to be used as natural pigments with functional properties.

  20. Influence of emulsion composition and spray-drying conditions on microencapsulation of tilapia oil.

    PubMed

    Huang, Hui; Hao, Shuxian; Li, Laihao; Yang, Xianqing; Cen, Jianwei; Lin, Wanling; Wei, Ya

    2014-09-01

    The influence of processing conditions on the microencapsulation of tilapia oil by spray drying was studied. Trehalose, gelatin, sucrose and xanthan were used as emulsion composition. The experimental parameters of spray drying such as inlet air temperature, solid content, drying air flow rate and atomizing pressure were optimized using a central composite design. Encapsulation efficiency and lipid oxidation were determined. Bulk density, powder morphology and particle size were also analyzed. Trehalose improved the glass transition temperature of wall material significantly and prevented the oxidation of the fish oil. Encapsulation efficiency reached a maximum of 90 % under optimum conditions with an inlet air temperature of 121 °C, a drying air flow rate of 0.65 m(3)/min and a spray pressure of 100 kPa.

  1. Microencapsulation of bioactives in cross-linked alginate matrices by spray drying.

    PubMed

    Santa-Maria, Monica; Scher, Herbert; Jeoh, Tina

    2012-01-01

    Microencapsulation of biomolecules, cells and chemicals is widely used in the food and pharmaceutical industries to improve stability, delivery and to control the release of encapsulated moieties. Among encapsulation matrices, alginate is preferred due to its low cost, biodegradability and biocompatibility. Current methods for producing stable alginate gels involve dropping alginate suspensions into divalent cation solutions. This procedure is difficult to scale-up and produces undesirably large alginate beads. In our novel encapsulation method, alginate gelation occurs during spray drying upon volatilisation of a base and rapid release of otherwise unavailable calcium ions. The resulting particles, with median particle sizes in the range 15-120 µm, are insoluble in solution. Cellulase and hemicellulase activities encapsulated by this method were not compromised during spray drying and remained stable over prolonged storage. The procedure described here offers a one-step alternative to other encapsulation methods that are costly and difficult to scale-up.

  2. Characterisation of spray dried soy sauce powders made by adding crystalline carbohydrates to drying carrier.

    PubMed

    Wang, Wei; Zhou, Weibiao

    2015-02-01

    This study aimed to reduce stickiness and caking of spray dried soy sauce powders by introducing a new crystalline structure into powder particles. To perform this task, soy sauce powders were formulated by using mixtures of cellulose and maltodextrin or mixtures of waxy starch and maltodextrin as drying carriers, with a fixed carrier addition rate of 30% (w/v) in the feed solution. The microstructure, crystallinity, solubility as well as stickiness and caking strength of all the different powders were analysed and compared. Incorporating crystalline carbohydrates in the drying carrier could significantly reduce the stickiness and caking strength of the powders when the ratio of crystalline carbohydrates to maltodextrin was above 1:5 and 1:2, respectively. X-ray Diffraction (XRD) results showed that adding cellulose or waxy starch could induce the crystallinity of powders. Differential Scanning Calorimetry (DSC) results demonstrated that the native starch added to the soy sauce powders did not fully gelatinize during spray drying.

  3. Spray drying as a strategy for biosurfactant recovery, concentration and storage.

    PubMed

    Barcelos, Gisely S; Dias, Lívia C; Fernandes, Péricles L; Fernandes, Rita de Cássi R; Borges, Arnaldo C; Kalks, Karlos Hm; Tótola, Marcos R

    2014-01-01

    The objective of this study was to analyze the use of Spray Drying for concentration and preservation of biosurfactants produced by Bacillus subtilis LBBMA RI4914 isolated from a heavy oil reservoir. Kaolinite and maltodextrin 10DE or 20DE were tested as drying adjuvants. Surface activity of the biosurfactant was analyzed by preparing dilution x surface activity curves of crude biosurfactant, crude biosurfactant plus adjuvants and of the dried products, after their reconstitution in water. The shelf life of the dried products was also evaluated. Spray drying was effective in the recovery and concentration of biosurfactant, while keeping its surface activity. Drying adjuvants were required to obtain a solid product with the desired characteristics. These compounds did not interfere with tensoactive properties of the biosurfactant molecules. The dehydrated product maintained its surfactant properties during storage at room temperature during the evaluation period (120 days), with no detectable loss of activity.

  4. Production of monodisperse epigallocatechin gallate (EGCG) microparticles by spray drying for high antioxidant activity retention.

    PubMed

    Fu, Nan; Zhou, Zihao; Jones, Tyson Byrne; Tan, Timothy T Y; Wu, Winston Duo; Lin, Sean Xuqi; Chen, Xiao Dong; Chan, Peggy P Y

    2011-07-15

    Epigallocatechin gallate (EGCG) originated from green tea is well-known for its pharmaceutical potential and antiproliferating effect on carcinoma cells. For drug delivery, EGCG in a micro-/nanoparticle form is desirable for their optimized chemopreventive effect. In this study, first time reports that EGCG microparticles produced by low temperature spray drying can maintain high antioxidant activity. A monodisperse droplet generation system was used to realize the production of EGCG microparticles. EGCG microparticles were obtained with narrow size distribution and diameter of 30.24 ± 1.88 μM and 43.39 ± 0.69 μM for pure EGCG and lactose-added EGCG, respectively. The EC50 value (the amount of EGCG necessary to scavenge 50% of free radical in the medium) of spray dried pure EGCG particles obtained from different temperature is in the range of 3.029-3.075 μM compared to untreated EGCG with EC50 value of 3.028 μM. Varying the drying temperatures from 70°C and 130°C showed little detrimental effect on EGCG antioxidant activity. NMR spectrum demonstrated the EGCG did not undergo chemical structural change after spray drying. The major protective mechanism was considered to be: (1) the use of low temperature and (2) the heat loss from water evaporation that kept the particle temperature at low level. With further drier optimization, this monodisperse spray drying technique can be used as an efficient and economic approach to produce EGCG micro-/nanoparticles.

  5. Thermal behavior and stability of biodegradable spray-dried microparticles containing triamcinolone.

    PubMed

    da Silva, Arnóbio Antônio; de Matos, Jivaldo Rosário; Formariz, Thalita Pedroni; Rossanezi, Gustavo; Scarpa, Maria Virginia; do Egito, Eryvaldo Sócrates Tabosa; de Oliveira, Anselmo Gomes

    2009-02-23

    Thermal analysis has been widely used for obtaining information about drug-polymer interactions and for pre-formulation studies of pharmaceutical dosage forms. In this work, biodegradable microparticles of poly (d,L-lactide-co-glycolide) (PLGA) containing triamcinolone (TR) in various drug:polymer ratios were produced by spray drying. The main purpose of this study was to study the effect of the spray-drying process not only on the drug-polymer interactions but also on the stability of microparticles using differential scanning calorimetry (DSC), thermogravimetry (TG) and derivative thermogravimetry (DTG), X-ray analysis (XRD), and infrared spectroscopy (IR). The evaluation of drug-polymer interactions and the pre-formulation studies were assessed using the DSC, TG and DTG, and IR. The quantitative analysis of drugs entrapped in PLGA microparticles was performed by the HPLC method. The results showed high levels of drug-loading efficiency for all used drug:polymer ratio, and the polymorph used for preparing the microparticles was the form B. The DSC and TG/DTG profiles for drug-loaded microparticles were very similar to those for the physical mixtures of the components. Therefore, a correlation between drug content and the structural and thermal properties of drug-loaded PLGA microparticles was established. These data indicate that the spray-drying technique does not affect the physico-chemical stability of the microparticle components. These results are in agreement with the IR analysis demonstrating that no significant chemical interaction occurs between TR and PLGA in both physical mixtures and microparticles. The results of the X-ray analysis are in agreement with the thermal analysis data showing that the amorphous form of TR prevails over a small fraction of crystalline phase of the drug also present in the TR-loaded microparticles. From the pre-formulation studies, we have found that the spray-drying methodology is an efficient process for obtaining TR

  6. Inhibition of Recrystallization of Amorphous Lactose in Nanocomposites Formed by Spray-Drying.

    PubMed

    Hellrup, Joel; Alderborn, Göran; Mahlin, Denny

    2015-11-01

    This study aims at investigating the recrystallization of amorphous lactose in nanocomposites. In particular, the focus is on the influence of the nano- to micrometer length scale nanofiller arrangement on the amorphous to crystalline transition. Further, the relative significance of formulation composition and manufacturing process parameters for the properties of the nanocomposite was investigated. Nanocomposites of amorphous lactose and fumed silica were produced by co-spray-drying. Solid-state transformation of the lactose was studied at 43%, 84%, and 94% relative humidity using X-ray powder diffraction and microcalorimetry. Design of experiments was used to analyze spray-drying process parameters and nanocomposite composition as factors influencing the time to 50% recrystallization. The spray-drying process parameters showed no significant influence. However, the recrystallization of the lactose in the nanocomposites was affected by the composition (fraction silica). The recrystallization rate constant decreased as a function of silica content. The lowered recrystallization rate of the lactose in the nanocomposites could be explained by three mechanisms: (1) separation of the amorphous lactose into discrete compartments on a micrometer length scale (compartmentalization), (2) lowered molecular mobility caused by molecular interactions between the lactose molecules and the surface of the silica (rigidification), and/or (3) intraparticle confinement of the amorphous lactose.

  7. Scalable organic solvent free supercritical fluid spray drying process for producing dry protein formulations.

    PubMed

    Nuchuchua, O; Every, H A; Hofland, G W; Jiskoot, W

    2014-11-01

    In this study, we evaluated the influence of supercritical carbon dioxide (scCO2) spray drying conditions, in the absence of organic solvent, on the ability to produce dry protein/trehalose formulations at 1:10 and 1:4 (w/w) ratios. When using a 4L drying vessel, we found that decreasing the solution flow rate and solution volume, or increasing the scCO2 flow rate resulted in a significant reduction in the residual water content in dried products (Karl Fischer titration). The best conditions were then used to evaluate the ability to scale the scCO2 spray drying process from 4L to 10L chamber. The ratio of scCO2 and solution flow rate was kept constant. The products on both scales exhibited similar residual moisture contents, particle morphologies (SEM), and glass transition temperatures (DSC). After reconstitution, the lysozyme activity (enzymatic assay) and structure (circular dichroism, HP-SEC) were fully preserved, but the sub-visible particle content was slightly increased (flow imaging microscopy, nanoparticle tracking analysis). Furthermore, the drying condition was applicable to other proteins resulting in products of similar quality as the lysozyme formulations. In conclusion, we established scCO2 spray drying processing conditions for protein formulations without an organic solvent that holds promise for the industrial production of dry protein formulations.

  8. Nano and microparticle engineering of water insoluble drugs using a novel spray-drying process.

    PubMed

    Schafroth, Nina; Arpagaus, Cordin; Jadhav, Umesh Y; Makne, Sushil; Douroumis, Dennis

    2012-02-01

    In the current study nano and microparticle engineering of water insoluble drugs was conducted using a novel piezoelectric spray-drying approach. Cyclosporin A (CyA) and dexamethasone (DEX) were encapsulated in biodegradable poly(D,L-lactide-co-glycolide) (PLGA) grades of different molecular weights. Spray-drying studies carried out with the Nano Spray Dryer B-90 employed with piezoelectric driven actuator. The processing parameters including inlet temperature, spray mesh diameter, sample flow rate, spray rate, applied pressure and sample concentration were examined in order to optimize the particle size and the obtained yield. The process parameters and the solute concentration showed a profound effect on the particle engineering and the obtained product yield. The produced powder presented consistent and reproducible spherical particles with narrow particle size distribution. Cyclosporin was found to be molecularly dispersed while dexamethasone was in crystalline state within the PLGA nanoparticles. Further evaluation revealed excellent drug loading, encapsulation efficiency and production yield. In vitro studies demonstrated sustained release patterns for the active substances. This novel spray-drying process proved to be efficient for nano and microparticle engineering of water insoluble active substances.

  9. Arrhenius activation energy of damage to catalase during spray-drying.

    PubMed

    Schaefer, Joachim; Lee, Geoffrey

    2015-07-15

    The inactivation of catalase during spray-drying over a range of outlet gas temperatures could be closely represented by the Arrhenius equation. From this an activation energy for damage to the catalase could be calculated. The close fit to Arrhenius suggests that the thermally-induced part of inactivation of the catalase during the complex drying and particle-formation processes takes place at constant temperature. These processes are rapid compared with the residence time of the powder in the collecting vessel of the cyclone where dried catalase is exposed to a constant temperature equal to approximately the drying gas outlet temperature. A lower activation energy after spray drying with the ultrasonic nozzle was found than with the 2-fluid nozzle under otherwise identical spray drying conditions. It is feasible that the ultrasonic nozzle when mounted in the lid of the spray dryer heats up toward the drying gas inlet temperature much more that the air-cooled 2-fluid nozzle. Calculation of the Arrhenius activation energy also showed how the stabilizing efficacy of trehalose and mannitol on the catalase varies in strength across the range of drying gas inlet and outlet temperatures examined.

  10. Optimization of spray drying process for developing seabuckthorn fruit juice powder using response surface methodology.

    PubMed

    Selvamuthukumaran, Meenakshisundaram; Khanum, Farhath

    2014-12-01

    The response surface methodology was used to optimize the spray drying process for development of seabuckthorn fruit juice powder. The independent variables were different levels of inlet air temperature and maltodextrin concentration. The responses were moisture, solubility, dispersibility, vitamin C and overall color difference value. Statistical analysis revealed that independent variables significantly affected all the responses. The Inlet air temperature showed maximum influence on moisture and vitamin C content, while the maltodextrin concentration showed similar influence on solubility, dispersibility and overall color difference value. Contour plots for each response were used to generate an optimum area by superimposition. The seabuckthorn fruit juice powder was developed using the derived optimum processing conditions to check the validity of the second order polynomial model. The experimental values were found to be in close agreement to the predicted values and were within the acceptable limits indicating the suitability of the model in predicting quality attributes of seabuckthorn fruit juice powder. The recommended optimum spray drying conditions for drying 100 g fruit juice slurry were inlet air temperature and maltodextrin concentration of 162.5 °C and 25 g, respectively. The spray dried juice powder contains higher amounts of antioxidants viz., vitamin C, vitamin E, total carotenoids, total anthocyanins and total phenols when compared to commercial fruit juice powders and they are also found to be free flowing without any physical alterations such as caking, stickiness, collapse and crystallization by exhibiting greater glass transition temperature.

  11. Spray-dried voriconazole-cyclodextrin complexes: solubility, dissolution rate and chemical stability.

    PubMed

    Miletic, Tijana; Kyriakos, Kachrimanis; Graovac, Adrijana; Ibric, Svetlana

    2013-10-15

    The present work investigates the effect of complexation with hydroxypropyl-beta-cyclodextrin (HPBCD) and 2-O-methyl-beta-cyclodextrin (2-O-MBCD), on voriconazole solubility, dissolution rate and chemical stability. Drug-cyclodextrin complexes were prepared as aqueous solutions, which were spray-dried, and their properties were compared to wet ground samples and physical mixtures. DSC analysis revealed absence of crystalline voriconazole from spray-dried complexes. FTIR spectroscopy indicated changes in the H-bonding network of the hydroxyl groups of cyclodextrin following drug inclusion. Dissolution rate of voriconazole was significantly higher from spray-dried complexes with either cyclodextrin in comparison with free drug, physical mixtures, or wet ground mixtures. However, two degradation impurities were found in aged samples, with slightly higher impurity level with HPBCD. Performed solubility studies suggested that 2-O-MBCD is more efficient solubilizer. Molecular docking simulations showed a difference in the 1:1 binding affinities and sites, with HPBCD surprisingly forming complexes of much lower energy, thus suggesting a multiple rather than a 1:1 complexation.

  12. Ilex paraguariensis Pellets from a Spray-Dried Extract: Development, Characterization, and Stability.

    PubMed

    Yatsu, Francini K J; Borghetti, Greice S; Magalhães, Fagner; Ferraz, Humberto G; Schenkel, Eloir Paulo; Bassani, Valquiria L

    2016-04-01

    Several studies have shown the potential use of Ilex paraguariensis in developing products with the aim to protect biological systems against oxidative stress-mediated damages. In the same way, technological studies have demonstrated the feasibility of obtaining dry products, by spray-drying process, from aqueous extracts of I. paraguariensis in laboratory. The present work was designed to develop pellets by extrusion/spheronization process, from an I. paraguariensis spray-dried powder. The pellets were characterized with respect to their chemical, physical, and technological properties, and the thermal and the photostability of the main polyphenol constituents were investigated. The pellets exhibited adequate size, shape, and high process yield (78.7%), as well as a good recovery of the total polyphenols (>95%) and a good dissolution in water (89.44 to 100.05%). The polyphenols were stable against light when conditioned in amber glass bottles; unstable against heat when the samples were conditioned either in open glass bottles or in hermetically sealed glass bottles and demonstrated to be hygroscopic and sensible to the temperature, especially when stored in permeable flasks. These findings pointed to the relevance of reducing the residual moisture content of pellets as well as of conditioning them in opaque humidity tight packages under low temperatures. The feasibility of obtaining pellets from an I. paraguariensis spray-dried powder using extrusion/spheronization technique was, for the first time, demonstrated. This finding represents a novelty for the herbal products in both pharmaceutical and food fields.

  13. Spray Dried Formulation of 5-Fluorouracil Embedded with Probiotic Biomass: In Vitro and In Vivo Studies.

    PubMed

    Sharma, Anshul; Arora, Malika; Goyal, Amit K; Rath, Goutam

    2017-03-08

    The present study is utilizing the targeted therapeutic approach and antioxidant potential of selected probiotic biomass in mitigating toxic side effects of chemotherapeutic agents. Multicomponent carrier system consisting of 5-fluorouracil (5-FU) and selected probiotic strain with higher free radical scavenging activity was prepared using spray drying technique. Prepared spray dried microparticles were characterized for various physical, pharmaceutical, and biopharmaceutical properties including particle size, moisture content, entrapment efficiency, in vitro drug release, DSC, XRD, cell uptake, histopathology, and pharmacokinetic studies. In addition to the above, optimized formulation was subjected to in vivo targeting efficacy studies using radiographic technique. Optimized formulation meets the necessary physical requirement for pharmaceutical powder. X-ray studies revealed that the prepared spray dried formulations are able to target the colon. Pharmacokinetic endpoints with an extended t 1/2 and lower C max indicate lower systemic toxicity. Intact nature of colonic epithelium in experimental formulation clearly demonstrates the protective role of Lactobacillus rhamnosus in minimizing the harmful consequence induced by 5-FU. Existing outcomes provide the basis for a combination of targeted therapeutic approach with natural antioxidant capacity of potential probiotic strain which could help to mitigate the problems associated with traditional chemotherapy.

  14. A Model-Based Methodology for Spray-Drying Process Development.

    PubMed

    Dobry, Dan E; Settell, Dana M; Baumann, John M; Ray, Rod J; Graham, Lisa J; Beyerinck, Ron A

    2009-09-01

    Solid amorphous dispersions are frequently used to improve the solubility and, thus, the bioavailability of poorly soluble active pharmaceutical ingredients (APIs). Spray-drying, a well-characterized pharmaceutical unit operation, is ideally suited to producing solid amorphous dispersions due to its rapid drying kinetics. This paper describes a novel flowchart methodology based on fundamental engineering models and state-of-the-art process characterization techniques that ensure that spray-drying process development and scale-up are efficient and require minimal time and API. This methodology offers substantive advantages over traditional process-development methods, which are often empirical and require large quantities of API and long development times. This approach is also in alignment with the current guidance on Pharmaceutical Development Q8(R1). The methodology is used from early formulation-screening activities (involving milligrams of API) through process development and scale-up for early clinical supplies (involving kilograms of API) to commercial manufacturing (involving metric tons of API). It has been used to progress numerous spray-dried dispersion formulations, increasing bioavailability of formulations at preclinical through commercial scales.

  15. Production of spray-dried honey jackfruit (Artocarpus heterophyllus) powder from enzymatic liquefied puree.

    PubMed

    Wong, Chen Wai; Tan, Hong Hock

    2017-02-01

    This paper presents the enzymatic liquefaction process for honey jackfruit optimized with Pectinex(®) Ultra SP-L and Celluclast(®) 1.5 L individually or in combinations at different concentrations (0-2.5% v/w) and incubation time (0-2.5 h). Treatment with combinations of enzymes showed a greater effect in the reduction of viscosity (83.9-98.8%) as compared to single enzyme treatment (64.8-87.3%). The best parameter for enzymatic liquefaction was obtained with 1.0% (v/w) Pectinex(®) Ultra SP-L and 0.5% (v/w) Celluclast(®) 1.5 L for 1.5 h. Spray drying process was carried out using different inlet temperatures (140-180 °C) and maltodextrin concentrations (10-30% w/w). Results indicated that the spray-dried honey jackfruit powder produced at 160 °C with 30% w/w maltodextrin gave the highest product yield (66.90%) with good powder qualities in terms of water activity, solubility, moisture content, hygroscopicity, color and bulk density. The spray-dried honey jackfruit powder could potentially be incorporated into various food products.

  16. Towards an aerogel-based coating for aerospace applications: reconstituting aerogel particles via spray drying

    NASA Astrophysics Data System (ADS)

    Bheekhun, N.; Abu Talib, A. R.; Mustapha, S.; Ibrahim, R.; Hassan, M. R.

    2016-10-01

    Silica aerogel is an ultralight and highly porous nano-structured ceramic with its thermal conductivity being the lowest than any solids. Although aerogels possess fascinating physical properties, innovative solutions to tackle today's problems were limited due to their relative high manufacturing cost in comparison to conventional materials. Recently, some producers have brought forward quality aerogels at competitive costs, and thereby opening a panoply of applied research in this field. In this paper, the feasibility of spray-drying silica aerogel to tailor its granulometric property is studied for thermal spraying, a novel application of aerogels that is never tried before in the academic arena. Aerogel-based slurries with yttria stabilised zirconia as a secondary ceramic were prepared and spray-dried according to modified T aguchi experimental design in order to appreciate the effect of both the slurry formulation and drying conditions such as the solid content, the ratio of yttria stabilised zirconia:aerogel added, the amount of dispersant and binder, inlet temperature, atomisation pressure and feeding rate on the median particle size of the resulting spray-dried powder. The latter was found to be affected by all the aforementioned independent variables at different degree of significance and inclination. Based on the derived relationships, an optimised condition to achieve maximum median particle size was then predicted.

  17. Microencapsulation of menadione sodium bisulphite with polydimethylsiloxane by the spray-drying process: characterization by thermal analysis.

    PubMed

    Gronchi, P; Del Rosso, R; Centola, P; Cosentino, R F

    1992-01-01

    Menadione sodium bisulphite was microencapsulated with a polydimethylsiloxane membrane using spray-drying technology. Tests were performed using laboratory equipment and a Niro Atomizer pilot plant to scale up the process. The products were characterized with differential thermal analysis (DTA) and chemical and physical methods. Many differences between raw material and microencapsulated powder result from DTA data. The thermal characterization confirms that the spray-drying microcoating could be used to protect powder from the oxidative actions of the atmosphere.

  18. Preparation and evaluation of raloxifene-loaded solid dispersion nanoparticle by spray-drying technique without an organic solvent.

    PubMed

    Tran, Tuan Hiep; Poudel, Bijay K; Marasini, Nirmal; Chi, Sang-Cheol; Choi, Han-Gon; Yong, Chul Soon; Kim, Jong Oh

    2013-02-25

    The aim of this study was to improve the physicochemical properties and bioavailability of a poorly water-soluble drug, raloxifene by solid dispersion (SD) nanoparticles using the spray-drying technique. These spray-dried SD nanoparticles were prepared with raloxifene (RXF), polyvinylpyrrolidone (PVP) and Tween 20 in water. Reconstitution of optimized RXF-loaded SD nanoparticles in pH 1.2 medium showed a mean particle size of approximately 180 nm. X-ray diffraction and differential scanning calorimetry indicated that RXF existed in an amorphous form within spray-dried nanoparticles. The optimized formulation showed an enhanced dissolution rate of RXF at pH 1.2, 4.0, 6.8 and distilled water as compared to pure RXF powder. The improved dissolution of raloxifene from spray-dried SD nanoparticles appeared to be well correlated with enhanced oral bioavailability of raloxifene in rats. Furthermore, the pharmacokinetic parameters of the spray-dried SD nanoparticles showed increased AUC(0-∞) and C(max) of RXF by approximately 3.3-fold and 2.3-fold, respectively. These results suggest that the preparation of RXF-SD nanoparticles using the spray drying technique without organic solvents might be a promising approach for improving the oral bioavailability of RXF.

  19. A Design of Experiment approach to predict product and process parameters for a spray dried influenza vaccine.

    PubMed

    Kanojia, Gaurav; Willems, Geert-Jan; Frijlink, Henderik W; Kersten, Gideon F A; Soema, Peter C; Amorij, Jean-Pierre

    2016-09-25

    Spray dried vaccine formulations might be an alternative to traditional lyophilized vaccines. Compared to lyophilization, spray drying is a fast and cheap process extensively used for drying biologicals. The current study provides an approach that utilizes Design of Experiments for spray drying process to stabilize whole inactivated influenza virus (WIV) vaccine. The approach included systematically screening and optimizing the spray drying process variables, determining the desired process parameters and predicting product quality parameters. The process parameters inlet air temperature, nozzle gas flow rate and feed flow rate and their effect on WIV vaccine powder characteristics such as particle size, residual moisture content (RMC) and powder yield were investigated. Vaccine powders with a broad range of physical characteristics (RMC 1.2-4.9%, particle size 2.4-8.5μm and powder yield 42-82%) were obtained. WIV showed no significant loss in antigenicity as revealed by hemagglutination test. Furthermore, descriptive models generated by DoE software could be used to determine and select (set) spray drying process parameter. This was used to generate a dried WIV powder with predefined (predicted) characteristics. Moreover, the spray dried vaccine powders retained their antigenic stability even after storage for 3 months at 60°C. The approach used here enabled the generation of a thermostable, antigenic WIV vaccine powder with desired physical characteristics that could be potentially used for pulmonary administration.

  20. Design of salmon calcitonin particles for nasal delivery using spray-drying and novel supercritical fluid-assisted spray-drying processes.

    PubMed

    Cho, Wonkyung; Kim, Min-Soo; Jung, Min-Sook; Park, Junsung; Cha, Kwang-Ho; Kim, Jeong-Soo; Park, Hee Jun; Alhalaweh, Amjad; Velaga, Sitaram P; Hwang, Sung-Joo

    2015-01-15

    The overall aim of this study was to prepare a nasal powder formulation of salmon calcitonin (sCT) using an absorption enhancer to improve its bioavailability. In this work, powder formulations for nasal delivery of sCT were studied using various absorption enhancers and stabilizers. Powders were prepared by two different methods: conventional spray-drying (SD) and novel supercritical fluid-assisted spray-drying (SASD) to investigate the role of CO2 in the particle formation process. The prepared sCT powder formulations were characterized by several analyses; powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), and the Fourier transform infrared (FT-IR) spectroscopy method. The particle size distribution was also evaluated. In vivo absorption tests were carried out in Sprague-Dawley rat using the prepared powder formulations, and the results were compared to those of raw sCT. Quantitative analysis by high-performance liquid chromatography (HPLC) indicated that sCT was chemically stable after both the SD and SASD processes. Results of PXRD, SEM, and FT-IR did not indicate a strong interaction or defragmentation of sCT. The in vivo absorption test showed that SD- and SASD-processed sCT powders increased the bioavailability of the drug when compared to the nasal administration of raw sCT. In addition, SASD-processed sCT exhibited higher nasal absorption when compared with SD-processed sCT in all formulations due to a reduction of particle size. The results from this study illustrate that the preparation of nasal powders using the SASD process could be a promising approach to improve nasal absorption of sCT.

  1. Physical Properties and Effect in a Battery of Safety Pharmacology Models for Three Structurally Distinct Enteric Polymers Employed as Spray-Dried Dispersion Carriers

    PubMed Central

    Fryer, Ryan M.; Patel, Mita; Zhang, Xiaomei; Baum-Kroker, Katja S.; Muthukumarana, Akalushi; Linehan, Brian; Tseng, Yin-Chao

    2016-01-01

    Establishing a wide therapeutic index (TI) for pre-clinical safety is important during lead optimization (LO) in research, prior to clinical development, although is often limited by a molecules physiochemical characteristics. Recent advances in the application of the innovative vibrating mesh spray-drying technology to prepare amorphous solid dispersions may offer an opportunity to achieve high plasma concentrations of poorly soluble NCEs to enable testing and establishment of a wide TI in safety pharmacology studies. While some of the amorphous solid dispersion carriers are generally recognized as safe for clinical use, whether they are sufficiently benign to enable in vivo pharmacology studies has not been sufficiently demonstrated. Thus, the physical properties, and effect in a battery of in vivo safety pharmacology models, were assessed in three classes of polymers employed as spray-dried dispersion carriers. The polymers (HPMC-AS, Eudragit, PVAP) displayed low affinity with acetone/methanol, suitable for solvent-based spray drying. The water sorption of the polymers was moderate, and the degree of hysteresis of HPMC-AS was smaller than Eudragit and PVAP indicating the intermolecular interaction of water-cellulose molecules is weaker than water-acrylate or water-polyvinyl molecules. The polymer particles were well-suspended without aggregation with a mean particle size less than 3 μm in an aqueous vehicle. When tested in conscious Wistar Han rats in safety pharmacology models (n = 6–8/dose/polymer) investigating effects on CNS, gastrointestinal, and cardiovascular function, no liabilities were identified at any dose tested (30–300 mg/kg PO, suspension). In brief, the polymers had no effect in a modified Irwin test that included observational and evoked endpoints related to stereotypies, excitation, sedation, pain/anesthesia, autonomic balance, reflexes, and others. No effect of the polymers on gastric emptying or intestinal transit was observed when

  2. Physical Properties and Effect in a Battery of Safety Pharmacology Models for Three Structurally Distinct Enteric Polymers Employed as Spray-Dried Dispersion Carriers.

    PubMed

    Fryer, Ryan M; Patel, Mita; Zhang, Xiaomei; Baum-Kroker, Katja S; Muthukumarana, Akalushi; Linehan, Brian; Tseng, Yin-Chao

    2016-01-01

    Establishing a wide therapeutic index (TI) for pre-clinical safety is important during lead optimization (LO) in research, prior to clinical development, although is often limited by a molecules physiochemical characteristics. Recent advances in the application of the innovative vibrating mesh spray-drying technology to prepare amorphous solid dispersions may offer an opportunity to achieve high plasma concentrations of poorly soluble NCEs to enable testing and establishment of a wide TI in safety pharmacology studies. While some of the amorphous solid dispersion carriers are generally recognized as safe for clinical use, whether they are sufficiently benign to enable in vivo pharmacology studies has not been sufficiently demonstrated. Thus, the physical properties, and effect in a battery of in vivo safety pharmacology models, were assessed in three classes of polymers employed as spray-dried dispersion carriers. The polymers (HPMC-AS, Eudragit, PVAP) displayed low affinity with acetone/methanol, suitable for solvent-based spray drying. The water sorption of the polymers was moderate, and the degree of hysteresis of HPMC-AS was smaller than Eudragit and PVAP indicating the intermolecular interaction of water-cellulose molecules is weaker than water-acrylate or water-polyvinyl molecules. The polymer particles were well-suspended without aggregation with a mean particle size less than 3 μm in an aqueous vehicle. When tested in conscious Wistar Han rats in safety pharmacology models (n = 6-8/dose/polymer) investigating effects on CNS, gastrointestinal, and cardiovascular function, no liabilities were identified at any dose tested (30-300 mg/kg PO, suspension). In brief, the polymers had no effect in a modified Irwin test that included observational and evoked endpoints related to stereotypies, excitation, sedation, pain/anesthesia, autonomic balance, reflexes, and others. No effect of the polymers on gastric emptying or intestinal transit was observed when measured

  3. The effect of water to ethanol feed ratio on physical properties and aerosolization behavior of spray dried cromolyn sodium particles.

    PubMed

    Gilani, Kambiz; Najafabadi, Abdolhossien Rouholamini; Barghi, Mohammadali; Rafiee-Tehrani, Morteza

    2005-05-01

    Cromolyn sodium (CS) was spray dried under constant operation conditions from different water to ethanol feed ratios (50:50-0:100). The spray dried CS samples were characterized for their physicochemical properties including crystallinity, particle size distribution, morphology, density, and water/ethanol content. To determine quantitatively the crystallinity of the powders, an X-ray diffraction (XRD) method was developed using samples with different crystallinity prepared by physical mixing of 100% amorphous and 100% crystalline CS materials. The aerodynamic behavior of the CS samples was determined using an Andersen Cascade Impactor (ACI) with a Spinhaler at an air flow of 60 L/min. Binary mixtures of each spray dried CS powder and Pharmatose 325, a commercial alpha-lactose monohydrate available for DPI formulations, were prepared and in vitro aerosol deposition of the drug from the mixtures was analyzed using ACI to evaluate the effect of carrier on deposition profiles of the spray dried samples. CS spray dried from absolute ethanol exhibited XRD pattern characteristic for crystalline materials and different from patterns of the other samples. The crystallinity of spray dried CS obtained in the presence of water varied from 0% to 28.37%, depending on the ratio of water to ethanol in the feed suspensions. All samples presented different particle size, water/ethanol content, and bulk density values. CS particles spray dried from absolute ethanol presented uniform elongated shape whereas the other samples consisted mainly of particles with irregular shape. Overall, fine particle fraction increased significantly (p < 0.01) with decreasing d50% and water and ethanol content of spray dried CS samples. Significant difference (p < 0.01) in deposition profiles of the drug were observed between corresponding carrier free and carrier blended formulations. The difference in deposition profiles of CS aerosolized from various spray dried samples were described according to

  4. Microencapsulation by spray drying of nitrogen-fixing bacteria associated with lupin nodules.

    PubMed

    Campos, Daniela C; Acevedo, Francisca; Morales, Eduardo; Aravena, Javiera; Amiard, Véronique; Jorquera, Milko A; Inostroza, Nitza G; Rubilar, Mónica

    2014-09-01

    Plant growth promoting bacteria and nitrogen-fixing bacteria (NFB) used for crop inoculation have important biotechnological potential as a sustainable fertilization tool. However, the main limitation of this technology is the low inoculum survival rate under field conditions. Microencapsulation of bacterial cells in polymer matrices provides a controlled release and greater protection against environmental conditions. In this context, the aim of this study was to isolate and characterize putative NFB associated with lupin nodules and to evaluate their microencapsulation by spray drying. For this purpose, 21 putative NFB were isolated from lupin nodules and characterized (16S rRNA genes). Microencapsulation of bacterial cells by spray drying was studied using a mixture of sodium alginate:maltodextrin at different ratios (0:15, 1:14, 2:13) and concentrations (15 and 30% solids) as the wall material. The microcapsules were observed under scanning electron microscopy to verify their suitable morphology. Results showed the association between lupin nodules of diverse known NFB and nodule-forming bacteria belonging to Alphaproteobacteria, Betaproteobacteria, Gammaproteobacteria and Bacteroidetes. In microencapsulation assays, the 1:14 ratio of sodium alginate:maltodextrin (15% solids) showed the highest cell survival rate (79%), with a microcapsule yield of 27% and spherical microcapsules of 5-50 µm in diameter. In conclusion, diverse putative NFB genera and nodule-forming bacteria are associated with the nodules of lupine plants grown in soils in southern Chile, and their microencapsulation by spray drying using sodium alginate:maltodextrin represents a scalable process to generate a biofertilizer as an alternative to traditional nitrogen fertilization.

  5. Spray Dried Sodium Zirconate: A Rapid Absorption Powder for CO2 Capture with Superior Cyclic Stability.

    PubMed

    Bamiduro, Faith; Ji, Guozhao; Brown, Andy P; Valerie A Dupont, Valerie A; Zhao, Ming; Milne, Steve J

    2017-04-03

    Improved powders for capturing CO2 at high temperatures are required for H2 production using sorption enhanced steam reforming. This paper examines the relationship between particle structure and carbonation rate for two types of Na2ZrO3 powder. Hollow spray-dried micro-granules with a wall thickness of 100-300 nm corresponding to the dimensions of the primary acetate derived particles gave ~75 wt % theoretical CO2 conversion after a process-relevant 5 min exposure to 15 vol % CO2. A conventional powder prepared by solid state reaction carbonated more slowly, only achieving 50 % conversion due to a greater proportion of the reaction requiring bulk diffusion through the densely agglomerated particles. The hollow granular structure of the spray dried powder was retained post-carbonation but chemical segregation resulted in islands of an amorphous Na-rich phase (Na2CO3) within a crystalline ZrO2 particle matrix. Despite this phase separation, the reverse reaction to re-form Na2ZrO3 could be achieved by heating each powder to 900 °C in N2 (no dwell time). This resulted in a very stable multicycle performance in 40 cycle tests using TGA for both powders. Kinetic analysis of TGA data showed the carbonation process fits an Avrami-Erofeyev 2-D nucleation and nuclei growth model, consistent with microstructural evidence of a surface driven transformation. Thus, we demonstrate that spray-drying is a viable processing route to enhance the carbon capture performance of Na2ZrO3 powder.

  6. Scalable synthesis of mesoporous titania microspheres via spray-drying method.

    PubMed

    Pal, Manas; Wan, Li; Zhu, Yongheng; Liu, Yupu; Liu, Yang; Gao, Wenjun; Li, Yuhui; Zheng, Gengfeng; Elzatahry, Ahmed A; Alghamdi, Abdulaziz; Deng, Yonghui; Zhao, Dongyuan

    2016-10-01

    Mesoporous TiO2 has several potential applications due to its unique electronic and optical properties, although its structures and morphologies are typically difficult to tune because of its uncontrollable and fast sol-gel reaction. In this study we have coupled the template-directed-sol-gel-chemistry with the low-cost, scalable, and environmentally benign aerosol (spray-drying) one-pot preparation technique for the fabrication of hierarchically mesoporous TiO2 microspheres and Fe3O4@mesoporous TiO2-x microspheres in a large scale. Parameters during the pre-hydrolysis and spray-drying treatment were varied to successfully control the bead diameter, morphology, monodispersity, surface area and pore size for improving their effectiveness for better application. Unlike to the previous aerosol synthetic approaches, where mainly quite a high temperature gradient with the strict control of spray-drying precursor concentration is implied, our strategy is lying on comparatively low drying temperature with an additional post-ultrasonication (further hydrolysis and condensation) route of the pre-calcined TiO2 samples. As-synthesized mesoporous microspheres have a size distribution from 500nm to 5μm, specific surface areas ranging from 150 to 162m(2)g(-1) and mean pore sizes of several nanometers (4-6nm). Further Fe3O4@mesoporous TiO2-x microspheres were observed to show remarkable selective phosphopeptide-enrichment activity which might have significant importance in disease diagnosis and other biomedical applications.

  7. Effects of spray drying and size reduction of edible bird's nest on in-vitro digestibility

    NASA Astrophysics Data System (ADS)

    Muslim, Masitah; Babji, Abdul Salam; Mustapha, Wan Aida Wan

    2015-09-01

    The purpose of this study is to determine the effects of spray drying and size reduction of edible bird's nest (EBN) on in-vitro digestibility respectively. Sample prepared were EBN microparticulates; 710 µm (EBN710), 300 µm (EBN300) and 38 µm (EBN38), EBN spray died (EBNSD) and raw EBN (EBNraw) as control. Protein content and solubility were determined before the samples being subjected to in-vitro digestibility. Protein content of EBN710 (55.37±0.269%), EBN300 (56.57±0.163%) EBN38 (56.77±0.021%) and EBNraw (55.46±0.269%) was not significantly different (p>0.05) but EBNSD (60.33b+0.346%) was the highest (p<0.05). Solubility results showed that EBNSD had the highest solubility (94.38±1.24%) in water significantly (p<0.05) compared to EBNraw (16.01±0.231%), EBN710 (21.89+0.41%), EBN300 (22.52+0.072%) and EBN38 (27.51±0.321%). Digestibility of EBN300 (88.43±0.95%) was higher (p<0.05) compared to EBNSD (85.23±0.27%). However, treatment of microparticulates and spray drying were not significantly different with EBNraw (85.38±1.12%). Digestibility of EBN microparticulates and spray dried powder were all lower (p<0.05) than casein (98.36+0.95%). Lower EBN digestibility could be due to the nature of EBN protein as glycoprotein. Proteolytic (tryptic) digestion of native glycoprotein is often incomplete due to ste aric hindrance from the presence of bulky oligosaccharides.

  8. Optimization of Sour Cherry Juice Spray Drying as
Affected by Carrier Material and Temperature.

    PubMed

    Garofulić, Ivona Elez; Zorić, Zoran; Pedisić, Sandra; Dragović-Uzelac, Verica

    2016-12-01

    Response surface methodology was applied for optimization of the sour cherry Marasca juice spray drying process with 20, 30 and 40% of carriers maltodextrin with dextrose equivalent (DE) value of 4-7 and 13-17 and gum arabic, at three drying temperatures: 150, 175 and 200 °C. Increase in carrier mass per volume ratio resulted in lower moisture content and powder hygroscopicity, higher bulk density, solubility and product yield. Higher temperatures decreased the moisture content and bulk density of powders. Temperature of 200 °C and 27% of maltodextrin with 4-7 DE were found to be the most suitable for production of sour cherry Marasca powder.

  9. Culture and spray-drying of Tsukamurella paurometabola C-924: stability of formulated powders.

    PubMed

    Hernández, Armando; Weekers, Fréderic; Mena, Jesús; Pimentel, Eulogio; Zamora, Jesús; Borroto, Carlos; Thonart, Philippe

    2007-11-01

    The nematocidal agent, Tsukamurella paurometabola C-924, was cultured in a 300 l bioreactor. Spray-dried formulations of this microorganism were prepared using sucrose. At an outlet temperature 62 degrees C, survival rates between 12 and 85% were reached with sucrose up to 10% (w/w). The stability study of the powders showed that the best storage condition was at 4 degrees C under vacuum. A new method for the calculation of cell death order for bacteria stored at low temperatures was developed. Powders stored under vacuum showed an Arrhenius behavior in relation to cell death kinetics.

  10. Drug nano-domains in spray-dried ibuprofen-silica microspheres.

    PubMed

    Fatnassi, Mohamed; Tourné-Péteilh, Corine; Mineva, Tzonka; Devoisselle, Jean-Marie; Gaveau, Philippe; Fayon, Franck; Alonso, Bruno

    2012-09-21

    Silica microspheres encapsulating ibuprofen in separated domains at the nanometre scale are formed by spray-drying and sol-gel processes. A detailed (1)H and (13)C NMR study of these microspheres shows that ibuprofen molecules are mobile and are interacting through hydrogen bonds with other ibuprofen molecules. (1)H magnetisation exchange NMR experiments were employed to characterize the size of the ibuprofen domains at the nanometre scale. These domains are solely formed by ibuprofen, and their diameters are estimated to be ∼40 nm in agreement with TEM observations. The nature and formation of these particular texture and drug dispersion are discussed.

  11. Influence of granule characteristics on microstructure quality of compacts made from spray-dried powders

    NASA Astrophysics Data System (ADS)

    Balasubramanian, Sreeram

    Powder compaction is a widely used technique for the manufacture of high volume of ceramic components that have simple shapes and sizes. However, this technique is inherently prone to strength-limiting defects like large intergranular pores and remnants of the initial granule structure. These defects are a major obstacle that hinder the use of powder compaction to fabricate parts for applications where strength is an important criterion. The objective of this work is to understand the important factors that control the elimination of strength-limiting defects in compacts made from spray dried powders. The influence of granule density, internal lubricants, particle shape and external application of a plasticizer to already spray dried powders on compaction behavior was investigated. Emphasis was placed on role of these factors in the elimination of large intergranular pores and persistent granule interfaces. The powders were spray dried under varying conditions to tailor the granule characteristics, including granule density, granule size distribution, binder content and lubricant content. These powders were compacted at different pressures, and the microstructures of green and sintered compacts were then evaluated, and strength-limiting features were quantified. Comparisons were made on the basis of compaction curves, green strength, green density and microstructure quality at different pressures. Lowering the granule density reduced the number of granule relics and large intergranular pores. The presence of an internal lubricant improved particle packing and yielded compacts with higher green density and fewer large intergranular pores at comparable pressures. Spray dried powders with the externally applied plasticizer deformed at lower compaction pressures. This allowed easier knitting of particles across granule interfaces and elimination of large intergranular pores and persistent granule interfaces. Spherical (equiaxed) particles rearranged better at granule

  12. Optimization of the Büchi B-90 spray drying process using central composite design for preparation of solid dispersions.

    PubMed

    Gu, Bing; Linehan, Brian; Tseng, Yin-Chao

    2015-08-01

    A central composite design approach was applied to study the effect of polymer concentration, inlet temperature and air flow rate on the spray drying process of the Büchi B-90 nano spray dryer (B-90). Hypromellose acetate succinate-LF was used for the Design of Experiment (DoE) study. Statistically significant models to predict the yield, spray rate, and drying efficiency were generated from the study. The spray drying conditions were optimized according to the models to maximize the yield and efficiency of the process. The models were further validated using a poorly water-soluble investigational compound (BI064) from Boehringer Ingelheim Pharmaceuticals. The polymer/drug ratio ranged from 1/1 to 3/1w/w. The spray dried formulations were amorphous determined by differential scanning calorimetry and X-ray powder diffraction. The particle size of the spray dried formulations was 2-10 μm under polarized light microscopy. All the formulations were physically stable for at least 3h when suspended in an aqueous vehicle composed of 1% methyl cellulose. This study demonstrates that DoE is a useful tool to optimize the spray drying process, and the B-90 can be used to efficiently produce amorphous solid dispersions with a limited quantity of drug substance available during drug discovery stages.

  13. Spray drying of a poorly water-soluble drug nanosuspension for tablet preparation: formulation and process optimization with bioavailability evaluation.

    PubMed

    Sun, Wei; Ni, Rui; Zhang, Xin; Li, Luk Chiu; Mao, Shirui

    2015-06-01

    Spray drying experiments of an itraconazole nanosuspension were conducted to generate a dry nanocrystal powder which was subsequently formulated into a tablet formulation for direct compression. The nanosuspension was prepared by high pressure homogenization and characterized for particle-size distribution and surface morphology. A central composite statistical design approach was applied to identify the optimal drug-to-excipient ratio and spray drying temperature. It was demonstrated that the spray drying of a nanosuspension with a mannitol-to-drug mass ratio of 4.5 and at an inlet temperature of 120 °C resulted in a dry powder with the smallest increase in particle size as compared with that of the nanosuspension. X-ray diffraction results indicated that the crystalline structure of the drug was not altered during the spray-drying process. The tablet formulation was identified by determining the micromeritic properties such as flowability and compressibility of the powder mixtures composed of the spray dried nanocrystal powder and other commonly used direct compression excipients. The dissolution rate of the nanocrystal tablets was significantly enhanced and was found to be comparable to that of the marketed Sporanox®. No statistically significant difference in oral absorption between the nanocrystal tablets and Sporanox® capsules was found. In conclusion, the nanosuspension approach is feasible to improve the oral absorption of a BCS Class II drug in a tablet formulation and capable of achieving oral bioavailability equivalent to other well established oral absorption enhancement method.

  14. Critical processing parameters of carbon dioxide spray drying for the production of dried protein formulations: A study with myoglobin.

    PubMed

    Nuchuchua, O; Every, H A; Jiskoot, W

    2016-06-01

    The aim of this study was to gain fundamental insight into protein destabilization induced by supercritical CO2 spray drying processing parameters. Myoglobin was used as a model protein (5mg/ml with 50mg/ml trehalose in 10mM phosphate buffer, pH 6.2). The solution was exposed to sub- and supercritical CO2 conditions (65-130bar and 25-50°C), and CO2 spray drying under those conditions. The heme binding of myoglobin was determined by UV/Vis, fluorescence, and circular dichroism spectroscopy, while myoglobin aggregation was studied by using size-exclusion chromatography and flow imaging microscopy. It was found that pressure and temperature alone did not influence myoglobin's integrity. However, when pressurized CO2 was introduced into myoglobin solutions at any condition, the pH of the myoglobin formulation shifted to about 5 (measured after depressurization), resulting in heme binding destabilization and aggregation of myoglobin. When exposed to CO2, these degradation processes were enhanced by increasing temperature. Heme binding destabilization and myoglobin aggregation were also seen after CO2 spray drying, and to a greater extent. Moreover, the CO2 spray drying induced the partial loss of heme. In conclusion, pressurized CO2 destabilizes the myoglobin, leading to heme loss and protein aggregation upon spray drying.

  15. Spray drying of budesonide, formoterol fumarate and their composites-II. Statistical factorial design and in vitro deposition properties.

    PubMed

    Tajber, L; Corrigan, O I; Healy, A M

    2009-02-09

    The aim of this study was to investigate the effect of changing spray drying parameters on the production of a budesonide/formoterol fumarate 100:6 (w/w) composite. The systems were spray dried as solutions from 95% ethanol/5% water (v/v) using a Büchi 191-Mini Spray Dryer. A 2(5-1) factorial design study was undertaken to assess the consequence of altering spray drying processing variables on particle characteristics. The processing parameters that were studied were inlet temperature, spray drier airflow rate, pump rate, aspirator setting and feed concentration. Each batch of the resulting powder was characterised in terms of thermal and micromeritic properties as well as an in vitro deposition by twin impinger analysis. Overall, the parameter that had the greatest influence on each response investigated was production yield - airflow (higher airflow giving greater yields), median particle size - airflow (higher airflow giving smaller particle sizes) and Carr's compressibility index - feed concentration (lower feed concentration giving smaller Carr's indices). A six- to seven-fold difference in respirable fraction can be observed by changing the spray drying process parameters. The co-spray dried composite system which displayed best in vitro deposition characteristics, showed a 2.6-fold increase in respirable fraction in the twin impinger experiments and better dose uniformity compared with the physical mix of micronised powders.

  16. Preparation of a dispersible PEGylate nanostructured lipid carriers (NLC) loaded with 10-hydroxycamptothecin by spray-drying.

    PubMed

    Zhang, Xinxin; Pan, Weisan; Gan, Li; Zhu, Chunliu; Gan, Yong; Nie, Shufang

    2008-12-01

    Nanostructured lipid carriers (NLC) are based on mixture of solid lipids with spatially incompatible liquid lipids, which offer advantages of improving drug loading capacity and release properties. In the present study, hydroxycamptothecin (HCPT) loaded polyethylene glycol (PEG) modified NLC (PEG-NLC) was prepared by high pressure homogenize and spray drying method. PEG-NLC showed spherical particle with smooth surface in scanning electron microscopic (SEM) analysis. The crystallinity of lipid matrix within PEG-NLC was evaluated by powder X-ray diffraction and differential scanning calorimetry (DSC). The less ordered crystals or amorphous state of matrix were found in nanoparticles. A small, homogeneous particle size and high drug loading with fine entrapment efficiency of HCPT was obtained in PEG-NLC system. HCPT releasing from PEG-NLC showed a sustained release trend, and no significantly difference was found between two release curves of PEG-NLC before or after spray drying. After storage for 6 months, PEG-NLC powder after spray drying showed no significantly changes in particle size, drug loading and entrapment efficiency, crystal form and in vitro release. PEG modification statistically decreased the phagocytosis of NLC by RAW 264.7 cells, and spray drying process did not influence the cellular uptake of PEG-NLC. These results suggest that PEG-NLC prepared by spray drying is a stable and high-performance delivery system for HCPT.

  17. [Advances in the research of pathogenesis and treatment of severe smoke inhalation injury].

    PubMed

    Feng, Shengjuan; Jia, Chiyu; Liu, Zhen; Lyu, Xiaowu

    2016-02-01

    Among the fire victims, respiratory tract injury resulted from smoke inhalation is the major cause of death. Particulate substances in smoke, toxic and harmful gas, and chemical substances act together would rapidly induce the occurrence of dramatic pathophysiologic reaction in the respiratory tract, resulting in acute injury to the respiratory tract, thus inducing serious injury to it and acute respiratory distress syndrome, leading to death of the victims. In recent years, the pathophysiologic mechanism of severe smoke inhalation injury has been gradually clarified, thus appreciable advances in its treatment have been achieved. This paper is a brief review of above-mentioned aspects.

  18. Protective effects of oral microencapsulated Mycoplasma hyopneumoniae vaccine prepared by co-spray drying method.

    PubMed

    Lin, J H; Weng, C N; Liao, C W; Yeh, K S; Pan, M J

    2003-01-01

    The efficacy of Mycoplasma hyopneumoniae oral vaccine was investigated in microsphere dosage form. A co-spray drying process was used to apply an encapsulating material, Eudragit L30 D-55, to microspheres containing Mycoplasma hyopneumoniae antigens. The microspheres were generally effective (>93%) with protein release at pH 7.4, but almost none were released at pH 1.2, for 3 hr in an in vitro dissolution test. An SPF-swine model was used to evaluate the effectiveness of the microspheres as an oral vaccine, and the related immune responses. The serum's systemic IgG against M. hyopneumoniae was evoked by ELISA analysis, after a 2nd immunization of all pigs. The vaccinated groups' mean lesion score was significantly lower after the Mycoplasma hyopneumoniae challenge than that of the nonvaccinated/challenged groups (P<0.05). This study strongly suggests that the oral microspheres vaccine prepared by a co-spray drying method can provide effective protection against M. hyopneumoniae infection in pigs.

  19. Quality by Design approach to spray drying processing of crystalline nanosuspensions.

    PubMed

    Kumar, Sumit; Gokhale, Rajeev; Burgess, Diane J

    2014-04-10

    Quality by Design (QbD) principles were explored to understand spray drying process for the conversion of liquid nanosuspensions into solid nano-crystalline dry powders using indomethacin as a model drug. The effects of critical process variables: inlet temperature, flow and aspiration rates on critical quality attributes (CQAs): particle size, moisture content, percent yield and crystallinity were investigated employing a full factorial design. A central cubic design was employed to generate the response surface for particle size and percent yield. Multiple linear regression analysis and ANOVA were employed to identify and estimate the effect of critical parameters, establish their relationship with CQAs, create design space and model the spray drying process. Inlet temperature was identified as the only significant factor (p value <0.05) to affect dry powder particle size. Higher inlet temperatures caused drug surface melting and hence aggregation of the dried nano-crystalline powders. Aspiration and flow rates were identified as significant factors affecting yield (p value <0.05). Higher yields were obtained at higher aspiration and lower flow rates. All formulations had less than 3% (w/w) moisture content. Formulations dried at higher inlet temperatures had lower moisture compared to those dried at lower inlet temperatures.

  20. In situ cross-linking of stimuli-responsive hemicellulose microgels during spray drying.

    PubMed

    Zhao, Weifeng; Nugroho, Robertus Wahyu N; Odelius, Karin; Edlund, Ulrica; Zhao, Changsheng; Albertsson, Ann-Christine

    2015-02-25

    Chemical cross-linking during spray drying offers the potential for green fabrication of microgels with a rapid stimuli response and good blood compatibility and provides a platform for stimuli-responsive hemicellulose microgels (SRHMGs). The cross-linking reaction occurs rapidly in situ at elevated temperature during spray drying, enabling the production of microgels in a large scale within a few minutes. The SRHMGs with an average size range of ∼ 1-4 μm contain O-acetyl-galactoglucomannan as a matrix and poly(acrylic acid), aniline pentamer (AP), and iron as functional additives, which are responsive to external changes in pH, electrochemical stimuli, magnetic field, or dual-stimuli. The surface morphologies, chemical compositions, charge, pH, and mechanical properties of these smart microgels were evaluated using scanning electron microscopy, IR, zeta potential measurements, pH evaluation, and quantitative nanomechanical mapping, respectively. Different oxidation states were observed when AP was introduced, as confirmed by UV spectroscopy and cyclic voltammetry. Systematic blood compatibility evaluations revealed that the SRHMGs have good blood compatibility. This bottom-up strategy to synthesize SRHMGs enables a new route to the production of smart microgels for biomedical applications.

  1. Preparation of cellulose based microspheres by combining spray coagulating with spray drying.

    PubMed

    Wang, Qiao; Fu, Aiping; Li, Hongliang; Liu, Jingquan; Guo, Peizhi; Zhao, Xiu Song; Xia, Lin Hua

    2014-10-13

    Porous microspheres of regenerated cellulose with size in range of 1-2 μm and composite microspheres of chitosan coated cellulose with size of 1-3 μm were obtained through a two-step spray-assisted approach. The spray coagulating process must combine with a spray drying step to guarantee the formation of stable microspheres of cellulose. This approach exhibits the following two main virtues. First, the preparation was performed using aqueous solution of cellulose as precursor in the absence of organic solvent and surfactant; Second, neither crosslinking agent nor separated crosslinking process was required for formation of stable microspheres. Moreover, the spray drying step also provided us with the chance to encapsulate guests into the resultant cellulose microspheres. The potential application of the cellulose microspheres acting as drug delivery vector has been studied in two PBS (phosphate-buffered saline) solution with pH values at 4.0 and 7.4 to mimic the environments of stomach and intestine, respectively.

  2. Application of imaging based tools for the characterisation of hollow spray dried amorphous dispersion particles.

    PubMed

    Gamble, John F; Ferreira, Ana P; Tobyn, Mike; DiMemmo, Lynn; Martin, Kyle; Mathias, Neil; Schild, Richard; Vig, Balvinder; Baumann, John M; Parks, Stacy; Ashton, Mike

    2014-04-25

    The aim of this study was to investigate novel approaches to determine spray dried dispersion (SDD) specific particle characteristics through the use of imaging based technologies. The work demonstrates approaches that can be applied in order to access quantitative approximations for powder characteristics for hollow particles, such as SDD. Cryo-SEM has been used to measure the solid volume fraction and/or particle density of SDD particles. Application of this data to understand the impact of spray drying process conditions on SDD powder properties, and their impact on processability and final dosage form quality were investigated. The use of data from a Morphologi G3 image based particle characterisation system was also examined in order to explain both the propensity and extent of attrition within a series of SDD samples, and also demonstrate the use of light transmission data to assess the relative wall thickness of SDD particles. Such approaches demonstrate a means to access potentially useful information that can be linked to important particle characteristics for SDD materials which, in addition to the standard bulk powder measurements such as bulk density, may enable a better understanding of such materials and their impact on downstream processability and final dosage form acceptability.

  3. Influence of microencapsulation and spray drying on the viability of Lactobacillus and Bifidobacterium strains.

    PubMed

    Goderska, Kamila; Czarnecki, Zbigniew

    2008-01-01

    Improved production methods of starter cultures, which constitute the most important element of probiotic preparations, were investigated. The aim of the presented research was to analyse changes in the viability of Lactobacillus. acidophilus and Bifidobacterium bifidum after stabilization (spray drying, liophilization, fluidization drying) and storage in refrigerated conditions for 4 months. The highest numbers of live cells, up to the fourth month of storage in refrigerated conditions, of the order of 10(7) cfu/g preparation were recorded for the B. bifidum DSM 20239 bacteria in which the N-Tack starch for spray drying was applied. Fluidization drying of encapsulated bacteria allowed obtaining a preparation of the comparable number of live bacterial cells up to the fourth month of storage with those encapsulated bacteria, which were subjected to freeze-drying but the former process was much shorter. The highest survivability of the encapsulated L. acidophilus DSM 20079 and B. bifidum DSM 20239 cells subjected to freeze-drying was obtained using skimmed milk as the cryoprotective substance. Stabilization of bacteria by microencapsulation can give a product easy to store and apply to produce dried food composition.

  4. Enhancing graphene oxide reinforcing potential in composites by combined latex compounding and spray drying

    NASA Astrophysics Data System (ADS)

    Mao, Yingyan; Zhang, Shubai; Zhang, Dandan; Chan, Tung W.; Liu, Li

    2014-04-01

    A new strategy was developed to prepare graphene oxide/styrene-butadiene rubber (GO/SBR) composites with highly exfoliated GO sheets and strong interfaces. In particular, GO/SBR microparticles, in which exfoliated GO sheets (with a thickness of ˜1 nm and diameter of tens of nanometers) are trapped in a well-dispersed state throughout the SBR matrix, were made by a combined latex-compounding and spray-drying method. Subsequently, a chemical bridge between GO and rubber matrix through KH550 and Si69 was built during vulcanization, and the interfacial strength of the cured GO/SBR composite was remarkably improved. Due to the highly exfoliated structure and the strong interface, the GO/SBR composite exhibited 7.8 times higher modulus at 300% strain and 6.4 times higher tensile strength compared with cured pure SBR. The combined latex-compounding and spray-drying method presented here is feasible and water-mediated and has great potential for industrial applications.

  5. Spray Drying of Rhodomyrtus tomentosa (Ait.) Hassk. Flavonoids Extract: Optimization and Physicochemical, Morphological, and Antioxidant Properties.

    PubMed

    Wu, Pingping; Deng, Qian; Ma, Guangzhi; Li, Nianghui; Yin, Yanyan; Zhu, Baojun; Chen, Meiling; Huang, Ruqiang

    2014-01-01

    The optimal condition of spray drying purified flavonoids extract from R. tomentosa berries was studied by response surface methodology. The optimized condition for microencapsulation was of maltodextrin to gum Arabic ratio 1 : 1.3, total solid content 27.4%, glycerol monostearate content 0.25%, and core to coating material ratio 3 : 7, resulting in EE 91.75%. Prepared at the optimized condition, the flavonoids extract microcapsules (FEMs) were irregularly spherical particles with low moisture content (3.27%), high solubility (92.35%), and high bulk density (0.346 g/cm(3)). DPPH radical scavenging activity of FEMs was not decreased after spray drying (P > 0.05) and higher than those in citric acid and rutin at the same concentration. Moreover, FEMs effectively retarded the oxidation of fresh lard during the 10-day storage period compared with vitamin C, nonencapsulated flavonoids extract, and rutin. Therefore, FEMs produced at the optimized condition could be used as powder ingredients with antioxidant capacities.

  6. Spray Drying of Rhodomyrtus tomentosa (Ait.) Hassk. Flavonoids Extract: Optimization and Physicochemical, Morphological, and Antioxidant Properties

    PubMed Central

    Wu, Pingping; Ma, Guangzhi; Li, Nianghui; Yin, Yanyan; Zhu, Baojun; Chen, Meiling; Huang, Ruqiang

    2014-01-01

    The optimal condition of spray drying purified flavonoids extract from R. tomentosa berries was studied by response surface methodology. The optimized condition for microencapsulation was of maltodextrin to gum Arabic ratio 1 : 1.3, total solid content 27.4%, glycerol monostearate content 0.25%, and core to coating material ratio 3 : 7, resulting in EE 91.75%. Prepared at the optimized condition, the flavonoids extract microcapsules (FEMs) were irregularly spherical particles with low moisture content (3.27%), high solubility (92.35%), and high bulk density (0.346 g/cm3). DPPH radical scavenging activity of FEMs was not decreased after spray drying (P > 0.05) and higher than those in citric acid and rutin at the same concentration. Moreover, FEMs effectively retarded the oxidation of fresh lard during the 10-day storage period compared with vitamin C, nonencapsulated flavonoids extract, and rutin. Therefore, FEMs produced at the optimized condition could be used as powder ingredients with antioxidant capacities. PMID:26904629

  7. Protection of L. rhamnosus by spray-drying using two prebiotics colloids to enhance the viability.

    PubMed

    Avila-Reyes, Sandra V; Garcia-Suarez, Francisco J; Jiménez, María Teresa; San Martín-Gonzalez, María F; Bello-Perez, Luis A

    2014-02-15

    Protection of probiotics by substances considered as prebiotics can be an alternative to increase their viability in the large intestine. The objective of this study was to use two wall materials (native rice starch and inulin) without bonding agent to protect Lactobacillus rhamnosus during spray-drying and determine the viability of the microorganism under two storage conditions. For spray-drying conditions tested in this work the product yield with native rice starch (NRS) ranged between 65% and 74% whereas for inulin (IN) it ranged between 43% and 54%. In general, IN solutions exhibited higher outlet temperature than NRS dispersions. Capsules of IN had smaller particle size than those of NRS. Due to the higher hydrophilic nature of IN capsules as compared to NRS, IN capsules exhibited higher water activity than NRS capsules. Confocal microscopy showed marked differences between both wall materials, which could in turn cause differences in the release profile of encapsulated microorganisms. Agglomerates of NRS provided better protection to the microorganisms as evidenced by the lower reduction in viability when compared to IN, and this effect was corroborated by the stability study. It is possible to protect probiotics using both colloids, but differences in the viability and stability during storage were determined. The use of IN could prove beneficial in the encapsulation of probiotic strains since this carbohydrate is not hydrolyzed by human digestive enzymes and may act as prebiotic.

  8. Microencapsulation of Nigella sativa oleoresin by spray drying for food and nutraceutical applications.

    PubMed

    Edris, Amr E; Kalemba, Danuta; Adamiec, Janusz; Piątkowski, Marcin

    2016-08-01

    Oleoresin of Nigella sativa L. (Black cumin) was obtained from the seeds using hexane extraction at room temperature. The oleoresin was emulsified in an aqueous solution containing gum Arabic/maltodextrin (1:1 w/w) and then encapsulated in powder form by spray drying. The characteristics of the obtained powder including moisture content, bulk density, wettability, morphology, encapsulation efficiency were evaluated. The effect of the spray drying on the chemical composition of the volatile oil fraction of N. sativa oleoresin was also evaluated using gas chromatographic-mass spectroscopic analysis. Results indicated that the encapsulation efficiency of the whole oleoresin in the powder can range from 84.2±1.5% to 96.2±0.2% depending on the conditions of extracting the surface oil from the powder. On the other hand the encapsulation efficiency of the volatile oil fraction was 86.2% ±4.7. The formulated N. sativa L. oleoresin powder can be used in the fortification of processed food and nutraceuticals.

  9. Formulation and characterization of Turkish oregano microcapsules prepared by spray-drying technology.

    PubMed

    Baranauskaite, Juste; Ivanauskas, Liudas; Masteikova, Ruta; Kopustinskiene, Dalia; Baranauskas, Algirdas; Bernatoniene, Jurga

    2016-06-02

    The aim of this study was optimization of spray-drying process conditions for microencapsulation of Turkish oregano extract. Different concentrations of maltodextrin and gum arabic as encapsulating agents (wall material) as well as influence of selected processing variables were evaluated. The optimal conditions were maintained on the basis of the load of main bioactive compounds - ursolic, rosmarinic acids and carvacrol - in prepared microparticles after comparison of all significant response variables using desirability function. Physicomechanical properties of powders such as flowability, wettability, solubility, moisture content as well as product yield, encapsulation efficiency (EE), density, morphology and size distribution of prepared microparticles have been determined. The results demonstrated that the optimal conditions for spray-drying mixture consisted of two parts of wall material solution and one part of ethanolic oregano extract when the feed flow rate was 40 mL/min and air inlet temperature -170 °C. Optimal concentration of wall materials in solution was 20% while the ratio of maltodextrin and gum arabic was 8.74:1.26.

  10. In Situ Cross-Linking of Stimuli-Responsive Hemicellulose Microgels during Spray Drying

    PubMed Central

    2015-01-01

    Chemical cross-linking during spray drying offers the potential for green fabrication of microgels with a rapid stimuli response and good blood compatibility and provides a platform for stimuli-responsive hemicellulose microgels (SRHMGs). The cross-linking reaction occurs rapidly in situ at elevated temperature during spray drying, enabling the production of microgels in a large scale within a few minutes. The SRHMGs with an average size range of ∼1–4 μm contain O-acetyl-galactoglucomannan as a matrix and poly(acrylic acid), aniline pentamer (AP), and iron as functional additives, which are responsive to external changes in pH, electrochemical stimuli, magnetic field, or dual-stimuli. The surface morphologies, chemical compositions, charge, pH, and mechanical properties of these smart microgels were evaluated using scanning electron microscopy, IR, zeta potential measurements, pH evaluation, and quantitative nanomechanical mapping, respectively. Different oxidation states were observed when AP was introduced, as confirmed by UV spectroscopy and cyclic voltammetry. Systematic blood compatibility evaluations revealed that the SRHMGs have good blood compatibility. This bottom-up strategy to synthesize SRHMGs enables a new route to the production of smart microgels for biomedical applications. PMID:25630464

  11. Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique.

    PubMed

    Tran, Tuan Hiep; Poudel, Bijay Kumar; Marasini, Nirmal; Woo, Jong Soo; Choi, Han-Gon; Yong, Chul Soon; Kim, Jong Oh

    2013-01-01

    The purpose of this study was to develop a raloxifene-loaded solid dispersion with enhanced dissolution rate and bioavailability via spray-drying technique. Solid dispersions of raloxifene (RXF) were prepared with PVP K30 at weight ratios of 1:4, 1:6 and 1:8 using a spray-drying method, and characterized by differential scanning calorimetry, X-ray powder diffraction, scanning electron microscopy, and solubility and dissolution tests. The bioavailability of the solid dispersion in rats was also evaluated compared to those of RXF powder and commercial product. Results showed that the RXF-loaded solid dispersion was in amorphous form with increased solubility and dissolution rate. The absorption of RXF from solid dispersion resulted in approximately 2.6-fold enhanced bioavailability compared to pure drug. Moreover, RXF-loaded solid dispersion gave similar AUC, C(max) and T(max) values to the commercial product, suggesting that it was bioequivalent to the commercial product in rats. These findings suggest that an amorphous solid dispersion of RXF could be a viable option for enhancing the oral bioavailability of RXF.

  12. Nutritional Profile and Carbohydrate Characterization of Spray-Dried Lentil, Pea and Chickpea Ingredients.

    PubMed

    Tosh, Susan M; Farnworth, Edward R; Brummer, Yolanda; Duncan, Alison M; Wright, Amanda J; Boye, Joyce I; Marcotte, Michèle; Benali, Marzouk

    2013-07-25

    Although many consumers know that pulses are nutritious, long preparation times are frequently a barrier to consumption of lentils, dried peas and chickpeas. Therefore, a product has been developed which can be used as an ingredient in a wide variety of dishes without presoaking or precooking. Dried green peas, chickpeas or lentils were soaked, cooked, homogenized and spray-dried. Proximate analyses were conducted on the pulse powders and compared to an instant mashed potato product. Because the health benefits of pulses may be due in part to their carbohydrate content, a detailed carbohydrate analysis was carried out on the pulse powders. Pulse powders were higher in protein and total dietary fibre and lower in starch than potato flakes. After processing, the pulse powders maintained appreciable amounts of resistant starch (4.4%-5.2%). Total dietary fibre was higher in chickpeas and peas (26.2% and 27.1% respectively) than lentils (21.9%), whereas lentils had the highest protein content (22.7%). Pulse carbohydrates were rich in glucose, arabinose, galactose and uronic acids. Stachyose, a fermentable fibre, was the most abundant oligosaccharide, making up 1.5%-2.4% of the dried pulse powders. Spray-drying of cooked, homogenized pulses produces an easy to use ingredient with strong nutritional profile.

  13. Interfacial protein engineering for spray-dried emulsions - part I: effects on protein distribution and physical properties.

    PubMed

    Moisio, Timo; Damerau, Annelie; Lampi, Anna-Maija; Piironen, Vieno; Forssell, Pirkko; Partanen, Riitta

    2014-02-01

    Distribution of protein and oil in aqueous and spray-dried emulsions and the effect of protein cross-linking on emulsion properties and matrix-water interactions were investigated. Sodium caseinate and sunflower oil were used to make emulsions which were spray dried using maltodextrin as a wall material. 3% Na-caseinate concentration showed optimum emulsion and process stability as observed in CLSM images, droplet size data and in the amount of heptane-extractable oil from spray-dried emulsions. Transglutaminase cross-linking prior to emulsification slightly increased the amount of protein both on the oil droplet interface and on the particle surface as confirmed by analysis of continuous phase protein in the feed emulsion and by XPS measurements from the powder surface. DSC and water sorption measurements were used to study the physical state of the matrix. Glass transition occurred between RH 54% and 75% at room temperature and it was not affected by cross-linking.

  14. Melt extrusion vs. spray drying: The effect of processing methods on crystalline content of naproxen-povidone formulations.

    PubMed

    Haser, Abbe; Cao, Tu; Lubach, Joe; Listro, Tony; Acquarulo, Larry; Zhang, Feng

    2017-03-01

    Our hypothesis is that melt extrusion is a more suitable processing method than spray drying to prepare amorphous solid dispersions of drugs with a high crystallization tendency. Naproxen-povidone K25 was used as the model system in this study. Naproxen-povidone K25 solid dispersions at 30% and 60% drug loadings were characterized by modulated DSC, powder X-ray diffraction, FT-IR, and solid-state (13)C NMR to identify phase separation and drug recrystallization during processing and storage. At 30% drug loading, hydrogen bond (H-bond) sites of povidone K25 were not saturated and the glass transition (Tg) temperature of the formulation was higher. As a result, both melt-extruded and spray-dried materials were amorphous initially and remained so after storage at 40°C. At 60% drug loading, H-bond sites were saturated, and Tg was low. We were not able to prepare amorphous materials. The initial crystallinity of the formulations was 0.4%±0.2% and 5.6%±0.6%, and increased to 2.7%±0.3% and 21.6%±1.0% for melt-extruded and spray-dried materials, respectively. Spray-dried material was more susceptible to re-crystallization during processing, due to the high diffusivity of naproxen molecules in the formulation matrix and lack of kinetic stabilization from polymer solution. A larger number of crystalline nucleation sites and high surface area made the spray-dried material more susceptible to recrystallization during storage. This study demonstrated the unique advantages of melt extrusion over spray drying for the preparation of amorphous solid dispersions of naproxen at high drug level.

  15. Advances in metered dose inhaler technology: hardware development.

    PubMed

    Stein, Stephen W; Sheth, Poonam; Hodson, P David; Myrdal, Paul B

    2014-04-01

    Pressurized metered dose inhalers (MDIs) were first introduced in the 1950s and they are currently widely prescribed as portable systems to treat pulmonary conditions. MDIs consist of a formulation containing dissolved or suspended drug and hardware needed to contain the formulation and enable efficient and consistent dose delivery to the patient. The device hardware includes a canister that is appropriately sized to contain sufficient formulation for the required number of doses, a metering valve capable of delivering a consistent amount of drug with each dose delivered, an actuator mouthpiece that atomizes the formulation and serves as a conduit to deliver the aerosol to the patient, and often an indicating mechanism that provides information to the patient on the number of doses remaining. This review focuses on the current state-of-the-art of MDI hardware and includes discussion of enhancements made to the device's core subsystems. In addition, technologies that aid the correct use of MDIs will be discussed. These include spacers, valved holding chambers, and breath-actuated devices. Many of the improvements discussed in this article increase the ability of MDI systems to meet regulatory specifications. Innovations that enhance the functionality of MDIs continue to be balanced by the fact that a key advantage of MDI systems is their low cost per dose. The expansion of the health care market in developing countries and the increased focus on health care costs in many developed countries will ensure that MDIs remain a cost-effective crucial delivery system for treating pulmonary conditions for many years to come.

  16. Fourier transform infared spectroscopy investigation of protein conformation in spray-dried protein/trehalose powders.

    PubMed

    French, Donna L; Arakawa, Tsutomu; Li, Tiansheng

    2004-03-01

    Spray drying is a way to generate protein solids (powders), which is also true for lyophilization. Sugars are used to protect proteins from conformational changes and chemical degradations arising from drying processes and storage conditions such as the humidity. The influence of trehalose and humidity on the conformation and hydration of spray-dried recombinant human granolucyte colony stimulating factor (rhG-CSF) and recombinant consensus interferon-alpha (rConIFN) was investigated using Fourier transform IR spectroscopy. The spectral analysis of spray-dried powders in the amide I region demonstrated that trehalose stabilized the alpha-helical conformation of both rhG-CSF and rConIFN proteins. Exposure of the pure protein powders to 33% relative humidity (RH) resulted in the formation of beta sheets and loss of turns but no change in alpha-helical structure. Trehalose reduced the magnitude of the changes in beta sheets and turns. Exposure of the pure protein powders to 75% RH resulted in the loss of alpha-helical conformation with a corresponding increase in beta structures (beta sheets and turns). Trehalose did not protect proteins from the loss of alpha-helical structures, but it reduced the formation of antiparallel beta sheets. Hydrogen-deuterium exchange (H-D exchange) was used to further characterize these hydration-induced conformational changes. At 33% RH the percent exchange of the protein decreased with increasing trehalose content, indicating a greater protection of the protein from H-D exchange by a higher concentration of trehalose. Such protection correlates with decreased conformational changes of the protein by trehalose at this humidity. At 75% RH the degree of H-D exchange of the protein was insensitive to the powder composition in all powders. Surprisingly, the H-D exchange of trehalose was low at about 20-25%, which was nearly independent of the protein/trehalose ratio and humidity, indicating that the exchangeable protons on trehalose

  17. Survival of Beijerinckia sp. microencapsulated in carbohydrates by spray-drying.

    PubMed

    Boza, Y; Barbin, D; Scamparini, A R P

    2004-02-01

    The encapsulation of Beijerinckia sp. cell suspension in different wall materials using the spray drying technique was performed. Mat dextrin, dehydrated glucose syrups, gum acacia and modified starch materials were tested. Cell viability assays were carried out before and after drying and during storage of the products. The surface area and characteristics of the encapsulated powders were examined using BET adsorption of N(2) and scanning electron microscopy, respectively. The residual moisture content and water activity of the powders were also determined. The best results were obtained with the dehydrated glucose syrup, which resulted in products with the greatest per cent survival during the drying process and subsequent storage period. The products obtained with the dehydrated glucose syrup showed more uniform microcapsule surfaces at lower A(w) values and residual moisture content.

  18. Production of amorphous nanoparticles by supersonic spray-drying with a microfluidic nebulator

    NASA Astrophysics Data System (ADS)

    Amstad, Esther; Gopinadhan, Manesh; Holtze, Christian; Osuji, Chinedum O.; Brenner, Michael P.; Spaepen, Frans; Weitz, David A.

    2015-08-01

    Amorphous nanoparticles (a-NPs) have physicochemical properties distinctly different from those of the corresponding bulk crystals; for example, their solubility is much higher. However, many materials have a high propensity to crystallize and are difficult to formulate in an amorphous structure without stabilizers. We fabricated a microfluidic nebulator that can produce amorphous NPs from a wide range of materials, even including pure table salt (NaCl). By using supersonic air flow, the nebulator produces drops that are so small that they dry before crystal nuclei can form. The small size of the resulting spray-dried a-NPs limits the probability of crystal nucleation in any given particle during storage. The kinetic stability of the a-NPs—on the order of months—is advantageous for hydrophobic drug molecules.

  19. Manufacturing of solid dispersions of poorly water soluble drugs by spray drying: formulation and process considerations.

    PubMed

    Paudel, Amrit; Worku, Zelalem Ayenew; Meeus, Joke; Guns, Sandra; Van den Mooter, Guy

    2013-08-30

    Spray drying is an efficient technology for solid dispersion manufacturing since it allows extreme rapid solvent evaporation leading to fast transformation of an API-carrier solution to solid API-carrier particles. Solvent evaporation kinetics certainly contribute to formation of amorphous solid dispersions, but also other factors like the interplay between the API, carrier and solvent, the solution state of the API, formulation parameters (e.g. feed concentration or solvent type) and process parameters (e.g. drying gas flow rate or solution spray rate) will influence the final physical structure of the obtained solid dispersion particles. This review presents an overview of the interplay between manufacturing process, formulation parameters, physical structure, and performance of the solid dispersions with respect to stability and drug release characteristics.

  20. Self-dispersible nanocrystals of albendazole produced by high pressure homogenization and spray-drying.

    PubMed

    Paredes, Alejandro Javier; Llabot, Juan Manuel; Sánchez Bruni, Sergio; Allemandi, Daniel; Palma, Santiago Daniel

    2016-10-01

    Albendazole (ABZ) is a broad-spectrum antiparasitic drug used in the treatment of human or animal infections. Although ABZ has shown a high efficacy for repeated doses in monogastric mammals, its low aqueous solubility leads to erratic bioavailability. The aim of this work was to optimize a procedure in order to obtain ABZ self-dispersible nanocrystals (SDNC) by combining high pressure homogenization (HPH) and spray-drying (SD). The material thus obtained was characterized and the variables affecting both the HPH and SD processes were studied. As expected, the homogenizing pressure and number of cycles influenced the final particle size, while the stabilizer concentration had a strong impact on SD output and redispersion of powders upon contact with water. ABZ SDNC were successfully obtained with high process yield and redispersibility. The characteristic peaks of ABZ were clearly identified in the X-ray patterns of the processed samples. A noticeable increase in the dissolution rate was observed in the aqueous environment.

  1. Optimization of Sour Cherry Juice Spray Drying as
Affected by Carrier Material and Temperature

    PubMed Central

    Zorić, Zoran; Pedisić, Sandra; Dragović-Uzelac, Verica

    2016-01-01

    Summary Response surface methodology was applied for optimization of the sour cherry Marasca juice spray drying process with 20, 30 and 40% of carriers maltodextrin with dextrose equivalent (DE) value of 4–7 and 13–17 and gum arabic, at three drying temperatures: 150, 175 and 200 °C. Increase in carrier mass per volume ratio resulted in lower moisture content and powder hygroscopicity, higher bulk density, solubility and product yield. Higher temperatures decreased the moisture content and bulk density of powders. Temperature of 200 °C and 27% of maltodextrin with 4–7 DE were found to be the most suitable for production of sour cherry Marasca powder. PMID:28115901

  2. Physicochemical aspects involved in methotrexate release kinetics from biodegradable spray-dried chitosan microparticles

    NASA Astrophysics Data System (ADS)

    Mesquita, Philippe C.; Oliveira, Alice R.; Pedrosa, Matheus F. Fernandes; de Oliveira, Anselmo Gomes; da Silva-Júnior, Arnóbio Antônio

    2015-06-01

    Spray dried methotrexate (MTX) loaded chitosan microparticles were prepared using different drug/copolymer ratios (9%, 18%, 27% and 45% w/w). The physicochemical aspects were assessed in order to select particles that were able to induce a sustained drug release effect. Particles were successfully produced which exhibited desired physicochemical aspects such as spherical shape and high drug loading. XRD and FT-IR analysis demonstrated that drug is not bound to copolymer and is only homogeneously dispersed in an amorphous state into polymeric matrix. Even the particles with higher drug loading levels presented a sustained drug release profile, which were mathematically modeled using adjusted Higuchi model. The drug release occurred predominantly with drug dissolution and diffusion through swollen polymeric matrix, with the slowest release occurring with particles containing 9% of drug, demonstrating an interesting and promising drug delivery system for MTX.

  3. EVALUATION OF ALGINATE MICROSPHERES WITH METRONIDAZOLE OBTAINED BY THE SPRAY DRYING TECHNIQUE.

    PubMed

    Szekalska, Marta; Winnicka, Katarzyna; Czajkowska-Kośnik, Anna; Sosnowska, Katarzyna; Amelian, Aleksandra

    2015-01-01

    In the present study, nine formulations (F1-F9) of alginate microspheres with metronidazole were prepared by the spray drying technique with using different drug:polymer ratio (1:2, 1:1, 2:1) and different sodium alginate concentration (1, 2, 3%). The obtained microspheres were characterized for size, morphology, drug loading, (potential and swelling degree. Mucoadhesive properties were examined using texture analyzer and three different models of adhesive layers--gelatin discs, mucin gel and porcine vaginal mucosa. In vitro drug release, mathematical release profile and physical state of microspheres were also evaluated. The obtained results indicate that sodium alginate is a suitable polymer for developing mucoadhesive dosage forms of metronidazole. The optimal formulation F3 (drug:polymer ratio 1:2 and 1% alginate solution) was characterized by the highest metronidazole loading and sustained drug release. The results of this study indicate promising potential of ALG microspheres as alternative dosage forms for metronidazole delivery.

  4. Rheological and physical properties of spray-dried mucilage obtained from Hylocereus undatus cladodes.

    PubMed

    García-Cruz, E E; Rodríguez-Ramírez, J; Méndez Lagunas, L L; Medina-Torres, L

    2013-01-02

    This study examines the rheological behavior of reconstituted spray-dried mucilage isolated from the cladodes of pitahaya (Hylocereus undatus), the effects of concentration and its relationship with physical properties were analyzed in reconstituted solutions. Drying process optimization was carried out through the surface response method, utilizing a factorial 2(3) design with three central points, in order to evaluate yield and rheological properties. The reconstituted mucilage exhibited non-Newtonian shear-thinning behavior, which adequately fit the Cross model (R(2)>0.95). This dynamic response suggests a random coil configuration. The steady-shear viscosity and dynamic response are suitably correlated through the Cox-Merz rule, confirming the mucilage's stability of flow. Analysis of the physical properties of the mucilage (Tg, DTP, and particle morphology) explains the shear-thinning behavior.

  5. Preparation of polyaniline/sodium alanate hybrid using a spray-drying process

    NASA Astrophysics Data System (ADS)

    Moreira, B. R.; Passador, F. R.; Pessan, L. A.

    2014-05-01

    Nowadays, hydrogen is highly interesting as an energy source, in particular in the automotive field. In fact, hydrogen is attractive as a fuel because it prevents air pollution and greenhouse emissions. One of the main problems with the utilization of hydrogen as a fuel is its on-board storage. The purpouse of this work was to develop a new hybrid material consisting of a polyaniline matrix with sodium alanate (NaAlH4) using a spray-drying process. The polyaniline used for this experiment was synthesized by following a well-established method for the synthesis of the emeraldine base form of polyaniline using dodecylbenzenesulfonic acid as dopant. Micro particles of polyaniline/sodium alanate hybrids with 30 and 50 wt% of sodium alanate were prepared by using a spray-drying technique. Dilute solutions of polyaniline/sodium alanate were first prepared, 10g of the solid materials were mixed with 350 ml of toluene under stirring at room temperature for 24h and the solutions were dried using spray-dryer (Büchi, Switzerland) with 115°C of an inlet temperature. The hybrids were analyzed by differential scanning calorimetry, FT-IR and scanning electron microscopy (SEM). The addition of sodium alanate decreased the glass transition temperature of the hybrids when compared to neat polyaniline. FT-IR spectrum analysis was performed to identify the bonding environment of the synthesized material and was observed that simply physically mixture occurred between polyaniline and sodium alanate. The SEM images of the hybrids showed the formation of microspheres with sodium alanate dispersed in the polymer matrix.

  6. Relationship between surface concentration of L-leucine and bulk powder properties in spray dried formulations.

    PubMed

    Mangal, Sharad; Meiser, Felix; Tan, Geoffrey; Gengenbach, Thomas; Denman, John; Rowles, Matthew R; Larson, Ian; Morton, David A V

    2015-08-01

    The amino acid L-leucine has been demonstrated to act as a lubricant and improve the dispersibility of otherwise cohesive fine particles. It was hypothesized that optimum surface L-leucine concentration is necessary to achieve optimal surface and bulk powder properties. Polyvinylpyrrolidone was spray dried with different concentration of L-leucine and the change in surface composition of the formulations was determined using X-ray photoelectron spectroscopy (XPS) and time of flight-secondary ion mass spectrometry (ToF-SIMS). The formulations were also subjected to powder X-ray diffraction analysis in order to understand the relationship between surface concentration and solid-state properties of L-leucine. In addition, the morphology, surface energy and bulk cohesion of spray dried formulations were also assessed to understand the relation between surface L-leucine concentration and surface and bulk properties. The surface concentration of L-leucine increased with higher feed concentrations and plateaued at about 10% L-leucine. Higher surface L-leucine concentration also resulted in the formation of larger L-leucine crystals and not much change in crystal size was noted above 10% L-leucine. A change in surface morphology of particles from spherical to increasingly corrugated was also observed with increasing surface l-leucine concentration. Specific collapsed/folded over particles were only seen in formulations with 10% or higher l-leucine feed concentration suggesting a change in particle surface formation process. In addition, bulk cohesion also reduced and approached a minimum with 10% L-leucine concentration. Thus, the surface concentration of L-leucine governs particle formation and optimum surface L-leucine concentration results in optimum surface and bulk powder properties.

  7. Development and Characterization of Multifunctional Directly Compressible Co-processed Excipient by Spray Drying Method.

    PubMed

    Chauhan, Sohil I; Nathwani, Sandeep V; Soniwala, Moinuddin M; Chavda, Jayant R

    2016-08-01

    The present investigation was carried out to develop and characterize a multifunctional co-processed excipient for improving the compressibility of poorly compressible drugs. Etodolac was used as a model drug. Microcrystalline cellulose (MCC), lactose monohydrate (lactose), and StarCap 1500 (StarCap) were selected as components of the co-processed excipient. The spray drying method was used for co-processing of excipients. D-optimal mixture design was applied to optimize the proportion of component excipients. Statistical analysis of the D-optimal mixture design revealed that all response variables were significantly affected by the independent variables (p value < 0.05). Optimized composition was obtained from the desirability function. The optimized composition of the co-processed excipient was found to be 30% MCC, 25% lactose, and 45% StarCap. This optimized batch was evaluated for flow properties, compressibility parameters such as Kawakita's and Kuno's equation and Heckel's equation, and dilution potential. Evaluation parameters for flow properties (angle of repose, Carr's index, and Hausner's ratio) suggested excellent flow character. The parameters of Kawakita's and Kuno's equation and Heckel's equation suggested improvement in the compressibility of the model drug. Dilution potential was found to be 40%, and based on that, tablets of the model drug were formulated and evaluated for general evaluation parameters of tablets. All the parameters were found to be within the acceptance criteria which concluded that the multifunctional directly compressible co-processed excipient was prepared successfully that improved the compressibility of the poorly compressible model drug etodolac along with spray drying as an efficient method for the preparation of co-processed excipient.

  8. Preparation of polyaniline/sodium alanate hybrid using a spray-drying process

    SciTech Connect

    Moreira, B. R. E-mail: fabiopassador@gmail.com Passador, F. R. E-mail: fabiopassador@gmail.com Pessan, L. A. E-mail: fabiopassador@gmail.com

    2014-05-15

    Nowadays, hydrogen is highly interesting as an energy source, in particular in the automotive field. In fact, hydrogen is attractive as a fuel because it prevents air pollution and greenhouse emissions. One of the main problems with the utilization of hydrogen as a fuel is its on-board storage. The purpouse of this work was to develop a new hybrid material consisting of a polyaniline matrix with sodium alanate (NaAlH{sub 4}) using a spray-drying process. The polyaniline used for this experiment was synthesized by following a well-established method for the synthesis of the emeraldine base form of polyaniline using dodecylbenzenesulfonic acid as dopant. Micro particles of polyaniline/sodium alanate hybrids with 30 and 50 wt% of sodium alanate were prepared by using a spray-drying technique. Dilute solutions of polyaniline/sodium alanate were first prepared, 10g of the solid materials were mixed with 350 ml of toluene under stirring at room temperature for 24h and the solutions were dried using spray-dryer (Büchi, Switzerland) with 115°C of an inlet temperature. The hybrids were analyzed by differential scanning calorimetry, FT-IR and scanning electron microscopy (SEM). The addition of sodium alanate decreased the glass transition temperature of the hybrids when compared to neat polyaniline. FT-IR spectrum analysis was performed to identify the bonding environment of the synthesized material and was observed that simply physically mixture occurred between polyaniline and sodium alanate. The SEM images of the hybrids showed the formation of microspheres with sodium alanate dispersed in the polymer matrix.

  9. Development of spray-dried co-precipitate of amorphous celecoxib containing storage and compression stabilizers.

    PubMed

    Dhumal, Ravindra S; Shimpi, Shamkant L; Paradkar, Anant R

    2007-09-01

    The purpose of this study was to obtain an amorphous system with minimum unit operations that will prevent recrystallization of amorphous drugs since preparation, during processing (compression) and further storage. Amorphous celecoxib, solid dispersion (SD) of celecoxib with polyvinyl pyrrollidone (PVP) and co-precipitate with PVP and carrageenan (CAR) in different ratios were prepared by the spray drying technique and compressed into tablets. Saturation solubility and dissolution studies were performed to differentiate performance after processing. Differential scanning calorimetry and X-ray powder difraction revealed the amorphous form of celecoxib, whereas infrared spectroscopy revealed hydrogen bonding between celecoxib and PVP. The dissolution profile of the solid dispersion and co-precipitate improved compared to celecoxib and amorphous celecoxib. Amorphous celecoxib was not stable on storage whereas the solid dispersion and co-precipitate powders were stable for 3 months. Tablets of the solid dispersion of celecoxib with PVP and physical mixture with PVP and carrageenan showed better resistance to recrystallization than amorphous celecoxib during compression but recrystallized on storage. However, tablets of co-precipitate with PVP and carageenan showed no evidence of crystallinity during stability studies with comparable dissolution profiles. This extraordinary stability of spray-dried co-precipitate tablets may be attributed to the cushioning action provided by the viscoelastic polymer CAR and hydrogen bonding interaction between celecoxib and PVP. The present study demonstrates the synergistic effect of combining two types of stabilizers, PVP and CAR, on the stability of amorphous drug during compression and storage as compared to their effect when used alone.

  10. Encapsulation of mixtures of tuna oil, tributyrin and resveratrol in a spray dried powder formulation.

    PubMed

    Sanguansri, Luz; Day, Li; Shen, Zhiping; Fagan, Peter; Weerakkody, Rangika; Cheng, Li Jiang; Rusli, Jenny; Augustin, Mary Ann

    2013-12-01

    Spray dried emulsions are effective for carrying and stabilising combinations of fish oil and tributyrin, fish oil and resveratrol, or fish oil, tributyrin and resveratrol in one formulation. The encapsulation efficiencies were >99% for all three bioactives when a heated mixture of sodium caseinate: glucose: dried glucose syrup matrix (Encapsulant matrix 1) was used. When a heated sodium caseinate: glucose: processed starch matrix (Encapsulant matrix 2) was used, the encapsulation efficiencies were 90-92% for tributyrin and approximately 98% for resveratrol for all formulations but 79-91% for tuna oil where the efficiency was more formulation dependent. There was 84-86% remaining EPA, 85-87% remaining DHA, 85% remaining tributyrin and 94-96% remaining resveratrol after 18 months at 25 °C storage of the spray dried emulsions using Encapsulant matrix 1 across all formulations. In comparison, there was 83-87% remaining EPA and 84-89% remaining DHA, 80-82% remaining tributyrin, and 81-100% remaining resveratrol across all formulations with Encapsulant matrix 2. In vitro studies showed that on sequential exposure to simulated gastric and intestinal fluids, <5% tuna oil was found as triglycerides, but all the tributyrin had been lipolysed. The presence of diglycerides, monoglycerides and free fatty acids in the in vitro digests suggested that lipolysis of tuna oil had occurred. The type of matrix used for encapsulating the bioactives had little effect on the lipolysis of the oils but affected the amount of solvent extractable resveratrol. The ability of delivering mixtures of bioactives within one formulation was demonstrated.

  11. Synthesis of nanostructured magnetic photocatalyst by colloidal approach and spray-drying technique.

    PubMed

    Costa, A L; Ballarin, B; Spegni, A; Casoli, F; Gardini, D

    2012-12-15

    Nanostructured particles with a magnetic core and a photocatalytic shell are very interesting systems for their properties to be magnetically separable (and so reusable) in photocatalytic water depuration implant. Here, a robust, low time-consuming, easily scale up method to produce Fe(3)O(4)/SiO(2)/TiO(2) hierarchical nanostructures starting from commercial precursors (i.e. Fe(3)O(4), SiO(2)) by employing a colloidal approach (i.e. heterocoagulation) coupled with the spray-drying technique is presented. In particular, a self-assembled layer-by-layer methodology based on the coagulation of dissimilar colloidal particles was applied. First, a passive layer of silica (SiO(2), amorphous) was created on magnetite in order to avoid detrimental phenomena arising from the direct contact between magnetite and titania, then the deposition of titania onto silica-coated-magnetite was promoted. TiO(2), SiO(2) and Fe(3)O(4) nanosols were characterized in terms of zeta potential, optimized and a self-assembled layer-by-layer approach was followed in order to promote the heterocoagulation of silica onto magnetite surface and of titania onto silica coated magnetite. Once optimized the colloidal route, the mixture was then spray-dried to obtain a granulated powder with nano-scale reactivity, easier to handle and re-disperse in comparison to starting nanopowders with the same surface properties. The nanostructured particles have been characterized by different techniques such as SEM, TEM, XDR and their magnetic properties have been investigated. Moreover, preliminary photocatalytic texts have been performed.

  12. Ultrasonic atomization for spray drying: a versatile technique for the preparation of protein loaded biodegradable microspheres.

    PubMed

    Bittner, B; Kissel, T

    1999-01-01

    Bovine serum albumin (BDA) loaded microspheres with a spherical shape and smooth surface structure were successfully prepared from poly(lactide-co-glycolide) using an ultrasonic nozzle installed in a Niro laboratory spray dryer. Process and formulation parameters were investigated with respect to their influence on microsphere characteristics, such as particle size, loading capacity, and release properties. Preparation of microspheres in yields of more than 50% was achieved using an ultrasonic atomizer connected to a stream of carrier air. Microsphere characteristics could be modified by changing several technological parameters. An increased polymer concentration of the feed generated larger particles with a significantly reduced initial release of the protein. Moreover, microspheres with a smooth surface structure were obtained from the organic polymer solution with the highest viscosity. Microparticles with a low BSA loading showed a large central cavity surrounded by a thin polymer layer in scanning electron microspheres. A high protein loading led to an enlargement of the shell layer, or even to dense particles without any cavities. A continuous in vitro release pattern of BSA was obtained from the particles with low protein loading. Glass transition temperatures (Tg) of the microspheres before and after lyophilization did not differ from those of the BSA loaded particles prepared by spray drying with a rotary atomizer. Analysis of the polymer by gel permeation chromatography indicated that ultrasonication had no effect on polymer molecular weight. Molecular weight and polydispersity of the pure polymer, placebo microspheres prepared by spray drying, and placebo microspheres prepared using the ultrasonic nozzle were in the same range. In conclusion, ultrasonic atomization represents a versatile and reliable technique for the production of protein loaded biodegradable microspheres without inducing a degradation of the polymer matrix. Particle characteristics

  13. Microencapsulation of superoxide dismutase into biodegradable microparticles by spray-drying.

    PubMed

    Youan, Bi-Botti Célestin

    2004-01-01

    The aim of this work was to encapsulate superoxide dismutase (SOD) into biodegradable microparticles by spray-drying technique. The nature of the organic solvent to dissolve the polymer, the method of incorporation of the drug in the organic phase (with or without a surfactant, namely sucrose ester of HLB = 6), the surfactant/polymer ratio, and the nature of the biodegradable polyesters were investigated as formulation variables. The polyesters investigated as matrix were poly(epsilon-caprolactone) (PCL), poly(d, l, lactide-co-glycolide) (PLG-RG756), and poly(d, l-lactide) (PLA-R207) of respective molecular weight 78.2 kDa, 84.8 kDa, and 199.8 kDa. At surfactant/polymer ratio of 1/10, the SOD-retained enzymatic activities were higher (> 95%) for PLG-RG756 and PLA-R207 but relatively lower for the PCL (approximately 85%) probably due to the PCL relatively higher hydrophobicity. The obtained microparticles exhibited average volume mean diameter of 4-10 microm, the smaller for PCL and the larger for PLG-RG756 polymeric matrix. The in vitro release profile showed that SOD was completely (100%) released from PLA-R207 in 48 hr and from PLG-RG756 and PCL within 72 hr. These results showed that spray-drying with incorporation of surfactant such as sucrose ester may efficiently encapsulate SOD into biodegradable microparticles. Such formulations may improve the bioavailability of SOD and similar biopharmaceuticals.

  14. Advances in Inhalation Gas Dosimetry for Derivation of a Reference Concentration (RfC) and Use in Risk Assessment

    EPA Science Inventory

    This status report provides a review of advances in the state of the science for interspecies inhalation gas dosimetry related to extrathoracic (ET) or upper respiratory tract (URT), tracheobronchial (TB), pulmonary (PU), and extrarespiratory (systemic, SYS) effects.

  15. Sensory aroma characteristics of alcalase hydrolyzed rice bran protein concentrate as affected by spray drying and sugar addition.

    PubMed

    Arsa, Supeeraya; Theerakulkait, Chockchai

    2015-08-01

    The sensory aroma characteristics of alcalase hydrolyzed rice bran protein concentrate as affected by spray drying and sugar addition were investigated. Rice bran protein concentrate (RBPC) was hydrolyzed by alcalase. Sucrose, glucose or fructose was added to the liquid rice bran protein hydrolysate (LRBPH) and subsequently spray dried. The sensory aroma intensities of the hydrolysates were evaluated. Results showed that after spray drying, the rice bran protein concentrate powder (RBPC-P) had higher sweet and cocoa-like aroma intensities than RBPC (p ≤ 0.05) and hydrolyzed rice bran protein powder (HRBPP) had higher milk powder-like aroma intensities than LRBPH (p ≤ 0.05). The sweet, cocoa-like and milk powder-like aroma intensities in hydrolyzed rice bran protein powder with fructose addition (HRBPP-F) were significantly higher (p ≤ 0.05) than those of hydrolyzed rice bran protein powder with sucrose or glucose addition (HRBPP-S or HRBPP-G). HRBPP-F had the highest overall aroma liking score. These results also indicate that spray drying and sugar addition could improve the sensory aroma characteristics of alcalase hydrolyzed RBPC.

  16. Enhancement of solubility and antidiabetic effects of Repaglinide using spray drying technique in STZ-induced diabetic rats.

    PubMed

    Varshosaz, Jaleh; Minayian, Mohsen; Ahmadi, Mahdieh; Ghassami, Erfaneh

    2016-02-19

    The purpose of the study was to enhance the solubility of the poorly water-soluble drug, Repaglinide using spray drying based solid dispersion technique by different carriers including Eudragit E100, hydroxyl propyl cellulose Mw 80 000 and poly vinyl pyrollidone K30. Optimization of the best formulation was carried out according to drug solubility, release profile, particle size and angle of repose of the solid dispersions. The optimized sample was characterized using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). The morphology of the dispersions was studied by SEM. The blood glucose lowering effect of spray dried solid dispersions was studied in normal and streptozocin-induced diabetic rats. The results showed that Eudragit E100 in 1:3 ratio could enhance drug solubility by 100-fold. DSC studies indicated a marked change in melting point of the drug possibly due to strong hydrogen bonds between the drug and Eudragit, while FT-IR study did not show obvious interactions between them. According to XRPD results Repaglinide converted to an amorphous state in the spray dried dispersions. Spray dried Repaglinide reduced the blood glucose level significantly during the 8 h of obtaining blood samples in comparison with untreated drug (p < 0.05).

  17. Preparation and evaluation of glibenclamide-polyglycolized glycerides solid dispersions with silicon dioxide by spray drying technique.

    PubMed

    Chauhan, Bhaskar; Shimpi, Shyam; Paradkar, Anant

    2005-10-01

    Solid dispersions (SDs) of glibenclamide (GBM); a poorly water-soluble drug and polyglycolized glycerides (Gelucire with the aid of silicon dioxide (Aerosil 200); as an adsorbent, were prepared by spray drying technique. SDs and spray dried GBM in comparison with pure GBM and corresponding physical mixtures (PMs) were initially characterized and then subjected to ageing study up to 3 months. Initial characterization of SDs and spray dried GBM by DSC and XRPD showed that GBM was present in its amorphous form (AGBM). Improvement in the solubility and dissolution rate was observed for all samples. DRIFT spectroscopy revealed presence of hydrogen bonding in SDs. During ageing study, almost no decrease of in vitro drug dissolution was observed, over the period of 3 months as compare with freshly prepared SDs. Slight crystallinity in SDs was observed in the DSC and XRPD studies during ageing. Moreover in vivo study in Swiss Albino mice also justified the improvement in the therapeutic efficacy of amorphous GBM in SDs over pure GBM. Thus, present study demonstrated the high potential of spray drying technique for obtaining stable free flowing SDs of poorly water-soluble drugs using polyglycolized glycerides carriers with the aid of silicon dioxide as an adsorbent.

  18. Value-Added Processing of Peanut Skins: Antioxidant Capacity,Total Phenolics,and Procyanidin Content of Spray Dried Extracts

    Technology Transfer Automated Retrieval System (TEKTRAN)

    To explore a potential use for peanut skins as a functional food ingredient, milled skins were extracted with 70% ethanol, separated into a soluble extract and insoluble material by filtration, and spray dried with or without the addition of maltodextrin. Peanut skin extracts had high levels of proc...

  19. Value-Added Processing of Peanut Skins: Antioxidant Capacity, Total Phenolics, and Procyanidin Content of Spray Dried Extracts

    Technology Transfer Automated Retrieval System (TEKTRAN)

    To explore a potential use for peanut skins as a functional food ingredient, milled skins were extracted with 70% ethanol, separated into a soluble extract and insoluble material by filtration, and spray dried with or without the addition of maltodextrin. Peanut skin extracts had high levels of proc...

  20. [Effect of air humidity on traditional Chinese medicine extract of spray drying process and prediction of its powder stability].

    PubMed

    He, Yan; Xie, Yin; Zheng, Long-jin; Liu, Wei; Rao, Xiao-yong; Luo, Xiao-jian

    2015-02-01

    In order to solve the adhesion and the softening problems of traditional Chinese medicine extract during spray drying, a new method of adding dehumidified air into spray drying process was proposed, and the storage stability conditions of extract powder could be predicted. Kouyanqing extract was taken as model drug to investigate on the wet air (RH = 70%) and dry air conditions of spray drying. Under the dry air condition, the influence of the spray drying result with different air compression ratio and the spray-dried powder properties (extract powder recovery rate, adhesion percentage, water content, angle of repose, compression ratio, particle size and distribution) with 100, 110, 120, 130, 140 °C inlet temperature were studied. The hygroscopic investigation and Tg value with different moisture content of ideal powder were determined. The water activity-equilibrium moisture content (aw-EMC) and the equilibrium moisture content-Tg (EMC-Tg) relationships were fitted by GAB equation and Gordon-Taylor model respectively, and the state diagram of kouyanqing powder was obtained to guide the rational storage conditions. The study found that in the condition of dry air, the extract powder water content decreased with the increase of air compression ratio and the spray drying effect with air compression ratio of 100% was the best performance; in the condition of wet air, the extract powder with high water content and low yield, and the value were 4.26% and 16.73 °C, while, in the dry air condition the values were 2.43% and 24.86 °C with the same other instru- ment parameters. From the analysis of kouyanqing powder state diagram, in order to keep the stability, the critical water content of 3.42% and the critical water content of 0.188. As the water decreased Tg value of extract powder is the major problem of causing adhesion and softening during spray drying, it is meaningful to aid dehumidified air during the process.

  1. The effect of feed solids concentration and inlet temperature on the flavor of spray dried whey protein concentrate.

    PubMed

    Park, Curtis W; Bastian, Eric; Farkas, Brian; Drake, MaryAnne

    2014-01-01

    Previous research has demonstrated that unit operations in whey protein manufacture promote off-flavor production in whey protein. The objective of this study was to determine the effects of feed solids concentration in liquid retentate and spray drier inlet temperature on the flavor of dried whey protein concentrate (WPC). Cheddar cheese whey was manufactured, fat-separated, pasteurized, bleached (250 ppm hydrogen peroxide), and ultrafiltered (UF) to obtain WPC80 retentate (25% solids, wt/wt). The liquid retentate was then diluted with deionized water to the following solids concentrations: 25%, 18%, and 10%. Each of the treatments was then spray dried at the following temperatures: 180 °C, 200 °C, and 220 °C. The experiment was replicated 3 times. Flavor of the WPC80 was evaluated by sensory and instrumental analyses. Particle size and surface free fat were also analyzed. Both main effects (solids concentration and inlet temperature) and interactions were investigated. WPC80 spray dried at 10% feed solids concentration had increased surface free fat, increased intensities of overall aroma, cabbage and cardboard flavors and increased concentrations of pentanal, hexanal, heptanal, decanal, (E)2-decenal, DMTS, DMDS, and 2,4-decadienal (P < 0.05) compared to WPC80 spray dried at 25% feed solids. Product spray dried at lower inlet temperature also had increased surface free fat and increased intensity of cardboard flavor and increased concentrations of pentanal, (Z)4-heptenal, nonanal, decanal, 2,4-nonadienal, 2,4-decadienal, and 2- and 3-methyl butanal (P < 0.05) compared to product spray dried at higher inlet temperature. Particle size was higher for powders from increased feed solids concentration and increased inlet temperature (P < 0.05). An increase in feed solids concentration in the liquid retentate and inlet temperature within the parameters evaluated decreased off-flavor intensity in the resulting WPC80.

  2. Effect of Galacto-Oligosaccharides: Maltodextrin Matrices on the Recovery of Lactobacillus plantarum after Spray-Drying.

    PubMed

    Sosa, Natalia; Gerbino, Esteban; Golowczyc, Marina A; Schebor, Carolina; Gómez-Zavaglia, Andrea; Tymczyszyn, E Elizabeth

    2016-01-01

    In this work maltodextrins were added to commercial galacto-oligosaccharides (GOS) in a 1:1 ratio and their thermophysical characteristics were analyzed. GOS:MD solutions were then used as matrices during spray-drying of Lactobacillus plantarum CIDCA 83114. The obtained powders were equilibrated at different relative humidities (RH) and stored at 5 and 20°C for 12 weeks, or at 30°C for 6 weeks. The Tgs of GOS:MD matrices were about 20-30°C higher than those of GOS at RH within 11 and 52%. A linear relation between the spin-spin relaxation time (T2) and T-Tg parameter was observed for GOS:MD matrices equilibrated at 11, 22, 33, and 44% RH at 5, 20, and 30°C. Spray-drying of L. plantarum CIDCA 83114 in GOS:MD matrices allowed the recovery of 93% microorganisms. In contrast, only 64% microorganisms were recovered when no GOS were included in the dehydration medium. Survival of L. plantarum CIDCA 83114 during storage showed the best performance for bacteria stored at 5°C. In a further step, the slopes of the linear regressions provided information about the rate of microbial inactivation for each storage condition (k values). This information can be useful to calculate the shelf-life of spray-dried starters stored at different temperatures and RH. Using GOS:MD matrices as a dehydration medium enhanced the recovery of L. plantarum CIDCA 83114 after spray-drying. This strategy allowed for the first time the spray-drying stabilization of a potentially probiotic strain in the presence of GOS.

  3. Physicochemical properties and oral bioavailability of amorphous atorvastatin hemi-calcium using spray-drying and SAS process.

    PubMed

    Kim, Jeong-Soo; Kim, Min-Soo; Park, Hee Jun; Jin, Shun-Ji; Lee, Sibeum; Hwang, Sung-Joo

    2008-07-09

    The objective of the study was to prepare amorphous atorvastatin hemi-calcium using spray-drying and supercritical antisolvent (SAS) process and evaluate its physicochemical properties and oral bioavailability. Atorvastatin hemi-calcium trihydrate was transformed to anhydrous amorphous form by spray-drying and SAS process. With the SAS process, the mean particle size and the specific surface area of amorphous atorvastatin were drastically changed to 68.7+/-15.8nm, 120.35+/-1.40m2/g and 95.7+/-12.2nm, 79.78+/-0.93m2/g from an acetone solution and a tetrahydrofuran solution, respectively and appeared to be associated with better performance in apparent solubility, dissolution and pharmacokinetic studies, compared with unprocessed crystalline atorvastatin. Oral AUC0-8h values in SD rats for crystalline and amorphous atorvastatin were as follow: 1121.4+/-212.0ngh/mL for crystalline atorvastatin, 3249.5+/-406.4ngh/mL and 3016.1+/-200.3ngh/mL for amorphous atorvastatin from an acetone solution and a tetrahydrofuran solution with SAS process, 2227.8+/-274.5 and 2099.9+/-339.2ngh/mL for amorphous atorvastatin from acetone and tetrahydrofuran with spray-drying. The AUCs of all amorphous atorvastatin significantly increased (P<0.05) compared with crystalline atorvastatin, suggesting that the enhanced bioavailability was attributed to amorphous nature and particle size reduction. In addition, the SAS process exhibits better bioavailability than spray-drying because of particle size reduction with narrow particle size distribution. It was concluded that physicochemical properties and bioavailability of crystalline atorvastatin could be improved by physical modification such as particle size reduction and generation of amorphous state using spray-drying and SAS process. Further, SAS process was a powerful methodology for improving the physicochemical properties and bioavailability of atorvastatin.

  4. Comparative survival rates of human-derived probiotic Lactobacillus paracasei and L. salivarius strains during heat treatment and spray drying.

    PubMed

    Gardiner, G E; O'Sullivan, E; Kelly, J; Auty, M A; Fitzgerald, G F; Collins, J K; Ross, R P; Stanton, C

    2000-06-01

    Spray drying of skim milk was evaluated as a means of preserving Lactobacillus paracasei NFBC 338 and Lactobacillus salivarius UCC 118, which are human-derived strains with probiotic potential. Our initial experiments revealed that NFBC 338 is considerably more heat resistant in 20% (wt/vol) skim milk than UCC 118 is; the comparable decimal reduction times were 11.1 and 1.1 min, respectively, at 59 degrees C. An air outlet temperature of 80 to 85 degrees C was optimal for spray drying; these conditions resulted in powders with moisture contents of 4.1 to 4.2% and viable counts of 3.2 x 10(9) CFU/g for NFBC 338 and 5.2 x 10(7) CFU/g for UCC 118. Thus, L. paracasei NFBC 338 survived better than L. salivarius UCC 118 during spray drying; similar results were obtained when we used confocal scanning laser microscopy and LIVE/DEAD BacLight viability staining. In addition, confocal scanning laser microscopy revealed that the probiotic lactobacilli were located primarily in the powder particles. Although both spray-dried cultures appeared to be stressed, as shown by increased sensitivity to NaCl, bacteriocin production by UCC 118 was not affected by the process, nor was the activity of the bacteriocin peptide. The level of survival of NFBC 338 remained constant at approximately 1 x 10(9) CFU/g during 2 months of powder storage at 4 degrees C, while a decline in the level of survival of approximately 1 log (from 7.2 x 10(7) to 9.5 x 10(6) CFU/g) was observed for UCC 118 stored under the same conditions. However, survival of both Lactobacillus strains during powder storage was inversely related to the storage temperature. Our data demonstrate that spray drying may be a cost-effective way to produce large quantities of some probiotic cultures.

  5. Comparative Survival Rates of Human-Derived Probiotic Lactobacillus paracasei and L. salivarius Strains during Heat Treatment and Spray Drying

    PubMed Central

    Gardiner, G. E.; O'Sullivan, E.; Kelly, J.; Auty, M. A. E.; Fitzgerald, G. F.; Collins, J. K.; Ross, R. P.; Stanton, C.

    2000-01-01

    Spray drying of skim milk was evaluated as a means of preserving Lactobacillus paracasei NFBC 338 and Lactobacillus salivarius UCC 118, which are human-derived strains with probiotic potential. Our initial experiments revealed that NFBC 338 is considerably more heat resistant in 20% (wt/vol) skim milk than UCC 118 is; the comparable decimal reduction times were 11.1 and 1.1 min, respectively, at 59°C. An air outlet temperature of 80 to 85°C was optimal for spray drying; these conditions resulted in powders with moisture contents of 4.1 to 4.2% and viable counts of 3.2 × 109 CFU/g for NFBC 338 and 5.2 × 107 CFU/g for UCC 118. Thus, L. paracasei NFBC 338 survived better than L. salivarius UCC 118 during spray drying; similar results were obtained when we used confocal scanning laser microscopy and LIVE/DEAD BacLight viability staining. In addition, confocal scanning laser microscopy revealed that the probiotic lactobacilli were located primarily in the powder particles. Although both spray-dried cultures appeared to be stressed, as shown by increased sensitivity to NaCl, bacteriocin production by UCC 118 was not affected by the process, nor was the activity of the bacteriocin peptide. The level of survival of NFBC 338 remained constant at ∼1 × 109 CFU/g during 2 months of powder storage at 4°C, while a decline in the level of survival of approximately 1 log (from 7.2 × 107 to 9.5 × 106 CFU/g) was observed for UCC 118 stored under the same conditions. However, survival of both Lactobacillus strains during powder storage was inversely related to the storage temperature. Our data demonstrate that spray drying may be a cost-effective way to produce large quantities of some probiotic cultures. PMID:10831444

  6. Effect of Galacto-Oligosaccharides: Maltodextrin Matrices on the Recovery of Lactobacillus plantarum after Spray-Drying

    PubMed Central

    Sosa, Natalia; Gerbino, Esteban; Golowczyc, Marina A.; Schebor, Carolina; Gómez-Zavaglia, Andrea; Tymczyszyn, E. Elizabeth

    2016-01-01

    In this work maltodextrins were added to commercial galacto-oligosaccharides (GOS) in a 1:1 ratio and their thermophysical characteristics were analyzed. GOS:MD solutions were then used as matrices during spray-drying of Lactobacillus plantarum CIDCA 83114. The obtained powders were equilibrated at different relative humidities (RH) and stored at 5 and 20°C for 12 weeks, or at 30°C for 6 weeks. The Tgs of GOS:MD matrices were about 20–30°C higher than those of GOS at RH within 11 and 52%. A linear relation between the spin-spin relaxation time (T2) and T-Tg parameter was observed for GOS:MD matrices equilibrated at 11, 22, 33, and 44% RH at 5, 20, and 30°C. Spray-drying of L. plantarum CIDCA 83114 in GOS:MD matrices allowed the recovery of 93% microorganisms. In contrast, only 64% microorganisms were recovered when no GOS were included in the dehydration medium. Survival of L. plantarum CIDCA 83114 during storage showed the best performance for bacteria stored at 5°C. In a further step, the slopes of the linear regressions provided information about the rate of microbial inactivation for each storage condition (k values). This information can be useful to calculate the shelf-life of spray-dried starters stored at different temperatures and RH. Using GOS:MD matrices as a dehydration medium enhanced the recovery of L. plantarum CIDCA 83114 after spray-drying. This strategy allowed for the first time the spray-drying stabilization of a potentially probiotic strain in the presence of GOS. PMID:27199918

  7. The effect of acidification of liquid whey protein concentrate on the flavor of spray-dried powder.

    PubMed

    Park, Curtis W; Bastian, Eric; Farkas, Brian; Drake, MaryAnne

    2014-07-01

    Off-flavors in whey protein negatively influence consumer acceptance of whey protein ingredient applications. Clear acidic beverages are a common application of whey protein, and recent studies have demonstrated that beverage processing steps, including acidification, enhance off-flavor production from whey protein. The objective of this study was to determine the effect of preacidification of liquid ultrafiltered whey protein concentrate (WPC) before spray drying on flavor of dried WPC. Two experiments were performed to achieve the objective. In both experiments, Cheddar cheese whey was manufactured, fat-separated, pasteurized, bleached (250 mg/kg of hydrogen peroxide), and ultrafiltered (UF) to obtain liquid WPC that was 13% solids (wt/wt) and 80% protein on a solids basis. In experiment 1, the liquid retentate was then acidified using a blend of phosphoric and citric acids to the following pH values: no acidification (control; pH 6.5), pH 5.5, or pH 3.5. The UF permeate was used to normalize the protein concentration of each treatment. The retentates were then spray dried. In experiment 2, 150 μg/kg of deuterated hexanal (D₁₂-hexanal) was added to each treatment, followed by acidification and spray drying. Both experiments were replicated 3 times. Flavor properties of the spray-dried WPC were evaluated by sensory and instrumental analyses in experiment 1 and by instrumental analysis in experiment 2. Preacidification to pH 3.5 resulted in decreased cardboard flavor and aroma intensities and an increase in soapy flavor, with decreased concentrations of hexanal, heptanal, nonanal, decanal, dimethyl disulfide, and dimethyl trisulfide compared with spray drying at pH 6.5 or 5.5. Adjustment to pH 5.5 before spray drying increased cabbage flavor and increased concentrations of nonanal at evaluation pH values of 3.5 and 5.5 and dimethyl trisulfide at all evaluation pH values. In general, the flavor effects of preacidification were consistent regardless of the pH to

  8. STATUS REPORT: EVIDENCE BASED ADVANCES IN INHALATION DOSIMETRY FOR GASES WITH EFFECTS IN THE LOWER RESPIRATORY TRACT AND IN THE BODY

    EPA Science Inventory

    This report summarizes the status of specific inhalation dosimetry procedures for gases as outlined in U.S. EPA’s 1994 Methods for Derivation of Inhalation Reference Concentrations and Applications of Inhalation Dosimetry (U.S. EPA 1994) and reviews recent scientific advances in...

  9. Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique

    PubMed Central

    Tobar-Grande, Blanca; Godoy, Ricardo; Bustos, Paulina; von Plessing, Carlos; Fattal, Elias; Tsapis, Nicolas; Olave, Claudia; Gómez-Gaete, Carolina

    2013-01-01

    In this work, microparticles were prepared by spray-drying using albumin, chondroitin sulfate, and hyaluronic acid as excipients to create a controlled-release methylprednisolone system for use in inflammatory disorders such as arthritis. Scanning electron microscopy demonstrated that these microparticles were almost spherical, with development of surface wrinkling as the methylprednisolone load in the formulation was increased. The methylprednisolone load also had a direct influence on the mean diameter and zeta potential of the microparticles. Interactions between formulation excipients and the active drug were evaluated by x-ray diffraction, differential scanning calorimetry, and thermal gravimetric analysis, showing limited amounts of methylprednisolone in a crystalline state in the loaded microparticles. The encapsulation efficiency of methylprednisolone was approximately 89% in all formulations. The rate of methylprednisolone release from the microparticles depended on the initial drug load in the formulation. In vitro cytotoxic evaluation using THP-1 cells showed that none of the formulations prepared triggered an inflammatory response on release of interleukin-1β, nor did they affect cellular viability, except for the 9.1% methylprednisolone formulation, which was the maximum test concentration used. The microparticles developed in this study have characteristics amenable to a therapeutic role in inflammatory pathology, such as arthritis. PMID:23737670

  10. Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique.

    PubMed

    Tobar-Grande, Blanca; Godoy, Ricardo; Bustos, Paulina; von Plessing, Carlos; Fattal, Elias; Tsapis, Nicolas; Olave, Claudia; Gómez-Gaete, Carolina

    2013-01-01

    In this work, microparticles were prepared by spray-drying using albumin, chondroitin sulfate, and hyaluronic acid as excipients to create a controlled-release methylprednisolone system for use in inflammatory disorders such as arthritis. Scanning electron microscopy demonstrated that these microparticles were almost spherical, with development of surface wrinkling as the methylprednisolone load in the formulation was increased. The methylprednisolone load also had a direct influence on the mean diameter and zeta potential of the microparticles. Interactions between formulation excipients and the active drug were evaluated by x-ray diffraction, differential scanning calorimetry, and thermal gravimetric analysis, showing limited amounts of methylprednisolone in a crystalline state in the loaded microparticles. The encapsulation efficiency of methylprednisolone was approximately 89% in all formulations. The rate of methylprednisolone release from the microparticles depended on the initial drug load in the formulation. In vitro cytotoxic evaluation using THP-1 cells showed that none of the formulations prepared triggered an inflammatory response on release of interleukin-1β, nor did they affect cellular viability, except for the 9.1% methylprednisolone formulation, which was the maximum test concentration used. The microparticles developed in this study have characteristics amenable to a therapeutic role in inflammatory pathology, such as arthritis.

  11. Encapsulation of lemongrass oil with cyclodextrins by spray drying and its controlled release characteristics.

    PubMed

    Phunpee, Sarunya; Ruktanonchai, Uracha Rangsadthong; Yoshii, Hidefumi; Assabumrungrat, Suttichai; Soottitantawat, Apinan

    2017-04-01

    Inclusion of the two isomers of citral (E-citral and Z-citral), components of lemongrass oil, was investigated within the confines of various cyclodextrin (α-CD, β-CD and γ-CD) host molecules. Aqueous complex formation constants for E-citral with α-CD, β-CD and γ-CD were determined to be 123, 185, and 204 L/mol, respectively, whereas Z-citral exhibited stronger affinities (157, 206, and 253 L/mol, respectively). The binding trend γ-CD > β-CD > α-CD is a reflection of the more favorable geometrical accommodation of the citral isomers with increasing cavity size. Encapsulation of lemongrass oil within CDs was undertaken through shaking citral:CD (1:1, 1.5:1, and 2:1 molar ratio) mixtures followed by spray drying. Maximum citral retention occurred at a 1:1 molar ratio with β-CD and α-CD demonstrating the highest levels of total E-citral and Z-citral retention, respectively. Furthermore, the β-CD complex demonstrated the slowest release rate of all inclusion complex powders.

  12. Comparison of spray drying, electroblowing and electrospinning for preparation of Eudragit E and itraconazole solid dispersions.

    PubMed

    Sóti, Péter Lajos; Bocz, Katalin; Pataki, Hajnalka; Eke, Zsuzsanna; Farkas, Attila; Verreck, Geert; Kiss, Éva; Fekete, Pál; Vigh, Tamás; Wagner, István; Nagy, Zsombor K; Marosi, György

    2015-10-15

    Three solvent based methods: spray drying (SD), electrospinning (ES) and air-assisted electrospinning (electroblowing; EB) were used to prepare solid dispersions of itraconazole and Eudragit E. Samples with the same API/polymer ratios were prepared in order to make the three technologies comparable. The structure and morphology of solid dispersions were identified by scanning electron microscopy and solid phase analytical methods such as, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and Raman chemical mapping. Moreover, the residual organic solvents of the solid products were determined by static headspace-gas chromatography/mass spectroscopy measurements and the wettability of samples was characterized by contact angle measurement. The pharmaceutical performance of the three dispersion type, evaluated by dissolution tests, proved to be very similar. According to XRPD and DSC analyses, made after the production, all the solid dispersions were free of any API crystal clusters but about 10 wt% drug crystallinity was observed after three months of storage in the case of the SD samples in contrast to the samples produced by ES and EB in which the polymer matrix preserved the API in amorphous state.

  13. Characterization and performance assessment of solid dispersions prepared by hot melt extrusion and spray drying process.

    PubMed

    Agrawal, Anjali M; Dudhedia, Mayur S; Patel, Ashwinkumar D; Raikes, Michelle S

    2013-11-30

    The present study investigated effect of manufacturing methods such as hot melt extrusion (HME) and spray drying (SD) on physicochemical properties, manufacturability, physical stability and product performance of solid dispersion. Solid dispersions of compound X and PVP VA64 (1:2) when prepared by SD and HME process were amorphous by polarized light microscopy, powder X-ray diffractometry, and modulated differential scanning calorimetry analyses with a single glass transition temperature. Fourier transform infrared (FT-IR) and Raman spectroscopic analyses revealed similar molecular level interactions between compound X and PVP VA64 as evident by overlapping FT-IR and FT Raman spectra in SD and HME solid dispersions. The compactibility, tabletability, disintegration and dissolution performance were similar for solid dispersions prepared by both processing techniques. Differences in material properties such as surface area, morphological structure, powder densities, and flow characteristics were observed between SD and HME solid dispersion. The SD solid dispersion was physically less stable compared to HME solid dispersion under accelerated stability conditions. Findings from this study suggest that similar product performance could be obtained if the molecular properties of the solid dispersion processed by two different techniques are similar. However differences in material properties might affect the physical stability of the solid dispersions.

  14. Sodium and Lithium Storage Properties of Spray-Dried Molybdenum Disulfide-Graphene Hierarchical Microspheres

    PubMed Central

    Kalluri, Sujith; Seng, Kuok Hau; Guo, Zaiping; Du, Aijun; Konstantinov, Konstantin; Liu, Hua Kun; Dou, Shi Xue

    2015-01-01

    Developing nano/micro-structures which can effectively upgrade the intriguing properties of electrode materials for energy storage devices is always a key research topic. Ultrathin nanosheets were proved to be one of the potential nanostructures due to their high specific surface area, good active contact areas and porous channels. Herein, we report a unique hierarchical micro-spherical morphology of well-stacked and completely miscible molybdenum disulfide (MoS2) nanosheets and graphene sheets, were successfully synthesized via a simple and industrial scale spray-drying technique to take the advantages of both MoS2 and graphene in terms of their high practical capacity values and high electronic conductivity, respectively. Computational studies were performed to understand the interfacial behaviour of MoS2 and graphene, which proves high stability of the composite with high interfacial binding energy (−2.02 eV) among them. Further, the lithium and sodium storage properties have been tested and reveal excellent cyclic stability over 250 and 500 cycles, respectively, with the highest initial capacity values of 1300 mAh g−1 and 640 mAh g−1 at 0.1 A g−1. PMID:26173985

  15. Effects of spray-drying conditions on the chemical, physical, and sensory properties of cheese powder.

    PubMed

    Koca, Nurcan; Erbay, Zafer; Kaymak-Ertekin, Figen

    2015-05-01

    Dairy powders are produced to increase the shelf life of fresh dairy products and for use as flavoring agents. In this study, 24 cheese powders produced under 7 different conditions were used to investigate the effects of spray-drying parameters (e.g., inlet air temperature, atomization pressure, and outlet air temperature) on the quality of white cheese powder. Composition, color, physical properties, reconstitution, and sensory characteristics of white cheese powders were determined. The results revealed that the white cheese powders produced in this study had low moisture content ratios and water activity values. High outlet air temperatures caused browning and enhanced Maillard reactions. Additionally, high outlet air temperatures increased wettability and dispersibility and decreased the solubility of white cheese powders. Free fat content was positively correlated with inlet air temperature and negatively correlated with outlet air temperature and atomization pressure. Sensory analyses revealed that white cheese powder samples had acceptable sensory characteristics with the exception of the sample produced at an outlet air temperature of 100°C, which had high scores for scorched flavor and color and low scores for cheese flavor.

  16. Accelerated ketoprofen release from spray-dried polymeric particles: importance of phase transitions and excipient distribution.

    PubMed

    Gue, Emilie; Muschert, Susanne; Willart, Jean-Francois; Danede, Florence; Delcourt-Debruyne, Elisabeth; Descamps, Marc; Siepmann, Juergen

    2015-05-01

    HPMC-, PVPVA- and PVP-based microparticles loaded with 30% ketoprofen were prepared by spray drying suspensions or solutions in various water:ethanol blends. The inlet temperature, drying gas and feed flow rates were varied. The resulting differences in the ketoprofen release rates in 0.1 M HCl could be explained based on X-ray diffraction, mDSC, SEM and particle size analysis. Importantly, long term stable drug release could be provided, being much faster than: (i) drug release from a commercial reference product, (ii) the respective physical drug:polymer mixtures, as well as (iii) the dissolution of ketoprofen powder as received. In addition, highly supersaturated release media were obtained, which did not show any sign for re-crystallization during the observation period. Surprisingly, spraying suspensions resulted in larger microparticles exhibiting faster drug release compared to spraying solutions, which resulted in smaller particles exhibiting slower drug release. These effects could be explained based on the physico-chemical characteristics of the systems.

  17. Spray-drying microencapsulation of synergistic antioxidant mushroom extracts and their use as functional food ingredients.

    PubMed

    Ribeiro, Andreia; Ruphuy, Gabriela; Lopes, José Carlos; Dias, Madalena Maria; Barros, Lillian; Barreiro, Filomena; Ferreira, Isabel C F R

    2015-12-01

    In this work, hydroalcoholic extracts of two mushrooms species, Suillus luteus (L.: Fries) (Sl) and Coprinopsis atramentaria (Bull.) (Ca), were studied for their synergistic antioxidant effect and their viability as functional food ingredients tested by incorporation into a food matrix (cottage cheese). In a first step, the individual extracts and a combination of both, showing synergistic effects (Sl:Ca, 1:1), were microencapsulated by spray-drying using maltodextrin as the encapsulating material. The incorporation of free extracts resulted in products with a higher initial antioxidant activity (t0) but declining after 7 days (t7), which was associated with their degradation. However, the cottage cheese enriched with the microencapsulated extracts, that have revealed a lower activity at the initial time, showed an increase at t7. This improvement can be explained by an effective protection provided by the microspheres together with a sustained release. Analyses performed on the studied cottage cheese samples showed the maintenance of the nutritional properties and no colour modifications were noticed.

  18. Preparation and pharmaceutical characterization of amorphous cefdinir using spray-drying and SAS-process.

    PubMed

    Park, Junsung; Park, Hee Jun; Cho, Wonkyung; Cha, Kwang-Ho; Kang, Young-Shin; Hwang, Sung-Joo

    2010-08-30

    The aim of this study was to investigate the effects of micronization and amorphorization of cefdinir on solubility and dissolution rate. The amorphous samples were prepared by spray-drying (SD) and supercritical anti-solvent (SAS) process, respectively and their amorphous natures were confirmed by DSC, PXRD and FT-IR. Thermal gravimetric analysis was performed by TGA. SEM was used to investigate the morphology of particles and the processed particle had a spherical shape, while the unprocessed crystalline particle had a needle-like shape. The mean particle size and specific surface area were measured by dynamic light scattering (DLS) and BET, respectively. The DLS result showed that the SAS-processed particle was the smallest, followed by SD and the unprocessed cefdinir. The BET result was the same as DLS result in that the SAS-processed particle had the largest surface area. Therefore, the processed cefdinir, especially the SAS-processed particle, appeared to have enhanced apparent solubility, improved intrinsic dissolution rate and better drug release when compared with SD-processed and unprocessed crystalline cefdinir due not only to its amorphous nature, but also its reduced particle size. Conclusions were that the solubility and dissolution rate of crystalline cefdinir could be improved by physically modifying the particles using SD and SAS-process. Furthermore, SAS-process was a powerful methodology for improving the solubility and dissolution rate of cefdinir.

  19. In situ forming antibacterial dextran blend hydrogel for wound dressing: SAA technology vs. spray drying.

    PubMed

    De Cicco, Felicetta; Reverchon, Ernesto; Adami, Renata; Auriemma, Giulia; Russo, Paola; Calabrese, Elena C; Porta, Amalia; Aquino, Rita P; Del Gaudio, Pasquale

    2014-01-30

    This study focuses on designing microparticulate carriers based on high-mannuronic alginate and amidated pectin blend loaded with gentamicin sulphate able to move rapidly from dry to soft hydrogel. Supercritical assisted atomization was used to produce microparticles in form of dry powder and characteristics were compared with those obtained by spray-drying. Particles with very high encapsulation efficiency (approximately 100%) and small diameter (less than 2 μm) showed good flowability and high fluid uptake enabling wound site filling and limiting bacterial proliferation. Moisture transmission of the in situ formed hydrogel was about 95 g/m(2)h, ideal to avoid wound dehydration or occlusion phenomena. All formulations presented a burst effect, suitable to prevent infection spreading at the beginning of the therapy, followed by prolonged release (4-10 days) related to drug/polymers ratio. Antimicrobial tests showed stronger effect than pure GS over time (up-to 24 days) and the ability to degrade preformed biofilms, essential to properly treat infected wounds.

  20. Tailored Crumpling and Unfolding of Spray-Dried Pristine Graphene and Graphene Oxide Sheets.

    PubMed

    Parviz, Dorsa; Metzler, Shane D; Das, Sriya; Irin, Fahmida; Green, Micah J

    2015-06-10

    For the first time, pristine graphene can be controllably crumpled and unfolded. The mechanism for graphene is radically different than that observed for graphene oxide; a multifaced crumpled, dimpled particle morphology is seen for pristine graphene in contrast to the wrinkled, compressed surface of graphene oxide particles, showing that surface chemistry dictates nanosheet interactions during the crumpling process. The process demonstrated here utilizes a spray-drying technique to produce droplets of aqueous graphene dispersions and induce crumpling through rapid droplet evaporation. For the first time, the gradual dimensional transition of 2D graphene nanosheets to a 3D crumpled morphology in droplets is directly observed; this is imaged by a novel sample collection device inside the spray dryer itself. The degree of folding can be tailored by altering the capillary forces on the dispersed sheets during evaporation. It is also shown that the morphology of redispersed crumpled graphene powder can be controlled by solvent selection. This process is scalable, with the ability to rapidly process graphene dispersions into powders suitable for a variety of engineering applications.

  1. Preparation and recrystallization behavior of spray-dried co-amorphous naproxen-indomethacin.

    PubMed

    Beyer, Andreas; Radi, Lydia; Grohganz, Holger; Löbmann, Korbinian; Rades, Thomas; Leopold, Claudia S

    2016-07-01

    To improve the dissolution properties and the physical stability of amorphous active pharmaceutical ingredients, small molecule stabilizing agents may be added to prepare co-amorphous systems. The objective of the study was to investigate if spray-drying allows the preparation of co-amorphous drug-drug systems such as naproxen-indomethacin and to examine the influence of the process conditions on the resulting initial sample crystallinity and the recrystallization behavior of the drug(s). For this purpose, the process parameters inlet temperature and pump feed rate were varied according to a 2(2) factorial design and the obtained samples were analyzed with X-ray powder diffractometry and Fourier-transformed infrared spectroscopy. Evaluation of the data revealed that the preparation of fully amorphous samples could be achieved depending on the process conditions. The resulting recrystallization behavior of the samples, such as the total recrystallization rate, the individual recrystallization rates of naproxen and indomethacin as well as the polymorphic form of indomethacin that was formed were influenced by these process conditions. For initially amorphous samples, it was found that naproxen and indomethacin recrystallized almost simultaneously, which supports the theory of formation of drug-drug heterodimers in the co-amorphous phase.

  2. Spray Drying Tenofovir Loaded Mucoadhesive and pH-Sensitive Microspheres Intended for HIV Prevention

    PubMed Central

    Zhang, Tao; Zhang, Chi; Agrahari, Vivek; Murowchick, James B.; Oyler, Nathan A.; Youan, Bi-Botti C.

    2013-01-01

    Purpose To develop spray dried mucoadhesive and pH-sensitive microspheres (MS) based on polymethacrylate salt intended for vaginal delivery of tenofovir (a model HIV microbicide) and assess their critical biological responses. Methods The formulation variables and process parameters are screened and optimized using a 24-1 fractional factorial design. The MS are characterized for size, zeta potential, yield, encapsulation efficiency, Carr’s index, drug loading, in vitro release, cytotoxicity, inflammatory responses and mucoadhesion. Results The optimal MS formulation has an average size of 4.73 µm, Zeta potential of −26.3 mV, 68.9% yield, encapsulation efficiency of 88.7%, Carr’s index of 28.3 and drug loading of 2% (w/w). The MS formulation can release 90% of its payload in the presence of simulated human semen. At a concentration of 1 mg/ml, the MS are noncytotoxic to vaginal endocervical/epithelial cells and Lactobacillus crispatus when compared to control media. There is also no statistically significant level of inflammatory cytokine (IL1-α, IL-1β, IL-6, IL-8, and IP-10) release triggered by MS. The mucoadhesive property of MS formulation is 2-fold higher than that of 1% HEC gel formulation. Conclusion These data suggest the promise of using such MS as an alternative controlled microbicide delivery template by intravaginal route for HIV prevention. PMID:23274788

  3. The stability and degradation kinetics of Sulforaphene in microcapsules based on several biopolymers via spray drying.

    PubMed

    Tian, Guifang; Li, Yuan; Yuan, Qipeng; Cheng, Li; Kuang, Pengqun; Tang, Pingwah

    2015-05-20

    Sulforaphene (SFE) was extracted from the radish seeds and the purity of SFE extracted by our laboratory was 95%. It is well known that SFE can prevent cancers. It is also known that SFE is unstable to heat. To overcome the problem, SFE microcapsules using natural biopolymers were prepared by spray drying. The results indicated that SFE microcapsules using hydroxypropyl-β-cyclodextrin (HP-β-CD), maltodextrin (MD) and isolated soybean protein (SPI) as wall materials could effectively improve its stability against heat, especially SFE-loaded HP-β-CD and MD microcapsules. The amount of SFE in the microcapsules was found 20% higher than that of the non-encapsulated SFE under 90 °C in 168 h. Our finding suggested that the rate of degradation of the non-encapsulated and encapsulated SFE with HP-β-CD, MD and SPI followed the first-order kinetics. The speed of the degradation of the encapsulated SFE in biopolymers increased from SFE with HP-β-CD, to SFE with MD, and to SFE-SPI. The non-encapsulated SFE degrades fastest.

  4. Evaporation of multi-component mixtures and shell formation in spray dried droplets

    NASA Astrophysics Data System (ADS)

    Valente, Pedro; Duarte, Íris; Porfirio, Tiago; Temtem, Márcio

    2015-11-01

    Drug particles where the active pharmaceutical ingredient (APIs) is dispersed in a polymer matrix forming an amorphous solid dispersion (ASD) is a commonly used strategy to increase the solubility and dissolution rate of poorly water soluble APIs. However, the formation and stability of an amorphous solid dispersion depends on the polymer/API combination and process conditions to generate it. The focus of the present work is to further develop a numerical tool to predict the formation of ASDs by spray drying solutions of different polymer/API combinations. Specifically, the evaporation of a multi-component droplet is coupled with a diffusion law within the droplet that minimizes the Gibbs free energy of the polymer/API/solvents system, following the Flory-Huggins model. Prior to the shell formation, the evaporation of the solvents is modelled following the simplified approach proposed by Abramzon & Sirignano (1989) which accounts for the varying relative velocity between the droplet and the drying gas. After shell formation, the diffusion of the solvents across the porous shell starkly modifies the evaporative dynamics.

  5. Preparation and structural characterization of amorphous spray-dried dispersions of tenoxicam with enhanced dissolution.

    PubMed

    Patel, Jagdishwar R; Carlton, Robert A; Yuniatine, Fnu; Needham, Thomas E; Wu, Lianming; Vogt, Frederick G

    2012-02-01

    Tenoxicam is a poorly soluble nonsteroidal anti-inflammatory drug. In this work, the solubility of tenoxicam is enhanced using amorphous spray-dried dispersions (SDDs) prepared using two molar equivalents of l-arginine and optionally with 10%-50% (w/w) polyvinylpyrrolidone (PVP). When added to the dispersions, PVP is shown to improve physical properties and also assists in maintaining supersaturation in solution. The dispersions provide a twofold increase over equilibrium solubility at the same pH. The dispersions are characterized using electron microscopy, vibrational spectroscopy, diffuse-reflectance visible spectroscopy, and X-ray powder diffraction. The structures of the dispersions are probed using solid-state nuclear magnetic resonance (SSNMR) experiments applied to the (1) H, (13) C, and (15) N nuclei, including two-dimensional dipolar correlation experiments that detect molecular association and the formation of a glass solution between tenoxicam, l-arginine, and PVP. Other aspects of the amorphous structure, including hydrogen-bonding interactions and the ionization state of tenoxicam and l-arginine, are also explored using SSNMR methods. These methods are used to show that the SDDs contain an amorphous l-arginine salt of tenoxicam in a glass solution that also includes PVP when present. Finally, the dispersions show only a minor decrease in chemical stability during accelerated stability studies relative to a crystalline form of tenoxicam.

  6. Effects of spray-drying and storage on astaxanthin content of Haematococcus pluvialis biomass.

    PubMed

    Raposo, Maria Filomena J; Morais, Alcina M M B; Morais, Rui M S C

    2012-03-01

    The main objective of this study was to evaluate the stability of astaxanthin after drying and storage at different conditions during a 9-week period. Recovery of astaxanthin was evaluated by extracting pigments from the dried powders and analysing extracts by HPLC. The powders obtained were stored under different conditions of temperature and oxygen level and the effects on the degradation of astaxanthin were examined. Under the experimental conditions conducted in this study, the drying temperature that yielded the highest content of astaxanthin was 220°C, as the inlet, and 120°C, as the outlet temperature of the drying chamber. The best results were obtained for biomass dried at 180/110°C and stored at -21°C under nitrogen, with astaxanthin degradation lower than 10% after 9 weeks of storage. A reasonable preservation of astaxanthin can be achieved by conditions 180/80°C, -21°C nitrogen, 180/110°C, 21°C nitrogen, and 220/80°C, 21°C vacuum: the ratio of astaxanthin degradation is equal or inferior to 40%. In order to prevent astaxanthin degradation of Haematococcus pluvialis biomass, it is recommended the storage of the spray dried carotenized cells (180/110ºC) under nitrogen and -21°C.

  7. Microencapsulation of garlic oleoresin using maltodextrin as wall material by spray drying technology.

    PubMed

    Balasubramani, P; Palaniswamy, P T; Visvanathan, R; Thirupathi, V; Subbarayan, A; Prakash Maran, J

    2015-01-01

    Experiments were conducted on microencapsulation of garlic oleoresin by spray drying with garlic oleoresin concentration (10%, 20% and 30%) as core material, maltodextrin concentration (40%, 50% and 60%) as wall material and inlet temperature of drying air (180 °C, 200 °C and 220 °C) as process parameters. The process in-terms of encapsulation efficiency was optimised following response surface methodology and Pareto analysis of variance (ANOVA). Second order polynomial regression model showed good fit of the experimental data with high coefficient of determination (R(2)) along with predicted values. The relationships between the independent and dependent parameters were represented using response surface and contour plots. The optimum levels of process parameters, viz., garlic oleoresin concentration, maltodextrin concentration and inlet temperature of air drying were found to be 10%, 60% and 200 °C, respectively with the maximum encapsulation efficiency of 81.9% and desirability of 0.998. The microencapsulated garlic oleoresin powder obtained at optimized conditions was spherical with smooth surface as analysed through scanning electron microscopy.

  8. The physicochemical properties of a spray dried glutinous rice starch biopolymer.

    PubMed

    Laovachirasuwan, Pornpun; Peerapattana, Jomjai; Srijesdaruk, Voranuch; Chitropas, Padungkwan; Otsuka, Makoto

    2010-06-15

    Glutinous rice starch (GRS) is a biopolymer used widely in the food industry but not at all in the pharmaceutical industry. There are several ways to modify this biopolymer. Physical modification is simple and cheap because it requires no chemicals or biological agents. The aim of this study was to characterize the physicochemical properties of a spray dried glutinous rice starch (SGRS) produced from pregelatinized GRS. The surface morphology changed from an irregular to concave spherical shape as revealed by Scanning Electron Microscopy (SEM). SGRS was almost amorphous as determined by X-ray Diffraction (XRD) spectroscopy. The water molecules became linked through hydrogen bonds to the exposed hydroxyl group of amorphous SGRS as determined by Near Infrared (NIR) spectroscopy. Then, SGRS formed a colloid gel matrix with water and developed a highly viscous gelatinous form as determined using Differential Scanning Calorimetry (DSC) and a stress control type rheometer. In addition, SGRS can swell and produce a gelatinous surface barrier like a hydrophilic matrix biopolymer which controls drug release. Therefore, a novel application of SGRS is as a sustained release modifier for direct compression tablets in the pharmaceutical industry.

  9. Development of Orodispersible Tizanidine HCl Tablets Using Spray Dried Coprocessed Exipient Bases

    PubMed Central

    Masareddy, Rajashree; Kokate, A.; Shah, V.

    2011-01-01

    Tizanidine HCl is a centrally acting α-2 adrenergic agonist muscle relaxant with a slightly bitter taste having short half-life of 2.5 h. In the present study effect of co-processed excipient bases in formulation of orodispersible tizanidine HCl tablets by direct compression method was investigated. Co-processed excipient of microcrystalline cellulose with SSL-hydroxypropylcellulose was prepared using spray drier in 1:1, 1:2 and 1:3 ratio. Formulated tablets were evaluated for hardness, friability, in vitro disintegration time and in vitro drug release. Formulation F-3 prepared by addition of co-processed excipient base in ratio of 1:3 showed minimum disintegration time of 9.15±0.04 s and higher amount of drug release of 93.75% at the end of 15 min. Granules obtained by spray drying technique were found to be more spherical which improved its flow property and was supported by scanning electron microscope studies. Thermal studies indicated change in amorphous state, compatibility of drug in formulation was confirmed by fourier transform infrared studies. Analyses of drug release data indicated formulation followed first order kinetics. Inclusion of co-processed excipient base in formulation of orodispersible tablets enhanced disintegration significantly. PMID:22707822

  10. Modelling drug degradation in a spray dried polymer dispersion using a modified Arrhenius equation.

    PubMed

    Patterson, Adele; Ferreira, Ana P; Banks, Elizabeth; Skeene, Kirsty; Clarke, Graham; Nicholson, Sarah; Rawlinson-Malone, Clare

    2015-01-15

    The Pharmaceutical industry is increasingly utilizing amorphous technologies to overcome solubility challenges. A common approach is the use of drug in polymer dispersions to prevent recrystallization of the amorphous drug. Understanding the factors affecting chemical and physical degradation of the drug within these complex systems, e.g., temperature and relative humidity, is an important step in the selection of a lead formulation, and development of appropriate packaging/storage control strategies. The Arrhenius equation has been used as the basis of a number of models to predict the chemical stability of formulated product. In this work, we investigate the increase in chemical degradation seen for one particular spray dried dispersion formulation using hydroxypropyl methylcellulose acetate succinate (HPMC-AS). Samples, prepared using polymers with different substitution levels, were placed on storage for 6 months under a range of different temperature and relative humidity conditions and the degradant level monitored using high-performance liquid chromatography (HPLC). While the data clearly illustrates the impact of temperature and relative humidity on the degradant levels detected, it also highlighted that these terms do not account for all the variability in the data. An extension of the Arrhenius equation to include a term for the polymer chemistry, specifically the degree of succinoyl substitution on the polymer backbone, was shown to improve the fit of the model to the data.

  11. Effect of carrier type and spray drying on the physicochemical properties of powdered and reconstituted pomegranate juice (Punica Granatum L.).

    PubMed

    Yousefi, Shima; Emam-Djomeh, Zahra; Mousavi, S M

    2011-12-01

    Pomegranate juice was diluted to 12° Brix and carriers (maltodextrin, gum Arabic, waxy starch) were added with varying concentrations of cellulose before being reduced to powder by spray drying. All carrier concentrations improved dryer yield, with gum Arabic being the most effective. The bulk density of the powder decreased when higher carrier concentrations were used. As cellulose concentration increased in solution, the solubility of the final product decreased. The optical properties of the powder were affected by the type and concentration of the carrier; powders produced with gum Arabic showed the greatest color change. Adding a carrier increased the Tg of the powder and its storage stability. Variation in the anthocyanin may be related to the type of carrier agent and its behavior during spray drying.

  12. Preparation and evaluation of solid dispersion of atorvastatin calcium with Soluplus® by spray drying technique.

    PubMed

    Ha, Eun-Sol; Baek, In-hwan; Cho, Wonkyung; Hwang, Sung-Joo; Kim, Min-Soo

    2014-01-01

    The aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Several solid dispersion formulations of atorvastatin calcium with Soluplus® were prepared at various drug : carrier ratios by spray drying. Physicochemical analysis demonstrated that atorvastatin calcium is amorphous in each solid dispersion, and the 2 : 8 drug : carrier ratio provided the highest degree of sustained atorvastatin supersaturation. Pharmacokinetic analysis in rats revealed that the 2 : 8 dispersion significantly improved the oral bioavailability of atorvastatin. This study demonstrates that spray-dried Soluplus® solid dispersions can be an effective method for achieving higher atorvastatin plasma levels.

  13. Structural and oxidative stabilization of spray dried fish oil microencapsulates with gum arabic and sage polyphenols: Characterization and release kinetics.

    PubMed

    Binsi, P K; Nayak, Natasha; Sarkar, P C; Jeyakumari, A; Muhamed Ashraf, P; Ninan, George; Ravishankar, C N

    2017-03-15

    The synergistic efficacy of gum arabic and sage polyphenols in stabilising capsule wall and protecting fish oil encapsulates from heat induced disruption and oxidative deterioration during spray drying was assessed. The emulsions prepared with sodium caseinate as wall polymer, gum arabic as wall co-polymer and sage extract as wall stabiliser was spray dried using a single fluid nozzle. Fish oil encapsulates stabilised with gum arabic and sage extract (SOE) exhibited significantly higher encapsulation efficiency compared to encapsulates containing gum arabic alone (FOE). Scanning electron microscopic and atomic force microscopic images revealed uniform encapsulates with good sphericity and smooth surface for SOE, compared to FOE powder. In vitro oil release of microencapsulates indicated negligible oil release in buffered saline whereas more than 80% of the oil loaded in encapsulates were released in simulated GI fluids. The encapsulates containing sage extract showed a lower rate of lipid oxidation during storage.

  14. Influence of different combinations of wall materials on the microencapsulation of jussara pulp (Euterpe edulis) by spray drying.

    PubMed

    Santana, Audirene A; Cano-Higuita, Diana M; de Oliveira, Rafael A; Telis, Vânia R N

    2016-12-01

    The objective of this work was to study the spray drying of jussara pulp using ternary mixtures of gum Arabic (GA) and modified starch (MS) together with either whey protein concentrate (WPC) or soy protein isolate (SPI), as the carrier agents. Two experimental mixture designs and triangular response surfaces were used to evaluate the effects of the mixtures on the responses for powders formulated with GA:MS:WPC and GA:MS:SPI, respectively. The spray drying process was selected for each carrier agent mixture, aiming to maximum the process yield (PY), solubility (S), retention of total anthocyanins (RTA) and encapsulation efficiency (EE). It was shown that the ternary formulations showed higher PY, S and RTA than the pure and binary formulations, as well as good results for EE and a low moisture content, showing that the use of GA and MS together with either WPC or SPI provide better microencapsulation of the jussara pulp.

  15. Spray-dried powders containing tretinoin-loaded engineered lipid-core nanocapsules: development and photostability study.

    PubMed

    Marchiori, M C L; Ourique, A F; da Silva, C de B; Raffin, R P; Pohlmann, A R; Guterres, S S; Beck, R C R

    2012-03-01

    The influence of the spray-drying process on the ability of engineered lipid-core nanocapsules to protect tretinoin against UV degradation was evaluated. This approach represents a technological alternative to improve the microbiological stability, storage and transport properties of such formulations. Tretinoin-loaded lipid-core nanocapsules or tretinoin-loaded nanoemulsion were dispersed in lactose (10% w/v) and fed in the spray-drier to obtain a solid product (spray-dried powder containing tretinoin-loaded nanocapsules or nanoemulsion--SD-TTN-NCL or SD-TTN-NE, respectively). SD-TTN-NE showed a lower (p < or = 0.05) percentage of encapsulation (89 +/- 1%) compared to SD-TTN-NCL (94 +/- 2%). Redispersed SD-TTN-NCL and SD-TTN-NE showed z-average sizes of 204 +/- 2 nm and 251 +/- 9 nm, which were close to those of the original suspensions (220 +/- 3 nm and 239 +/- 14 nm, respectively). Similar percentage of photodegradation were determined for tretinoin loaded in nanocapsules (26.15 +/- 4.34%) or in the respective redispersed spray-dried powder (28.73 +/- 6.19 min) after 60 min of UVA radiation exposure (p > 0.05). Our experimental design showed for the first time that spray-dried lipid-core nanocapsules are able to protect tretinoin against UVA radiation, suggesting that the drying process did not alter the supramolecular structure of the lipid-core nanocapsules. Such powders are potential intermediate products for the development of nanomedicines containing tretinoin.

  16. Hydrogels containing redispersible spray-dried melatonin-loaded nanocapsules: a formulation for transdermal-controlled delivery

    NASA Astrophysics Data System (ADS)

    Hoffmeister, Cristiane RD; Durli, Taís L.; Schaffazick, Scheila R.; Raffin, Renata P.; Bender, Eduardo A.; Beck, Ruy CR; Pohlmann, Adriana R.; Guterres, Sílvia S.

    2012-05-01

    The aim of the present study was to develop a transdermal system for controlled delivery of melatonin combining three strategies: nanoencapsulation of melatonin, drying of melatonin-loaded nanocapsules, and incorporation of nanocapsules in a hydrophilic gel. Nanocapsules were prepared by interfacial deposition of the polymer and were spray-dried using water-soluble excipients. In vitro drug release profiles were evaluated by the dialysis bag method, and skin permeation studies were carried out using Franz cells with porcine skin as the membrane. The use of 10% ( w/ v) water-soluble excipients (lactose or maltodextrin) as spray-drying adjuvants furnished redispersible powders (redispersibility index approximately 1.0) suitable for incorporation into hydrogels. All formulations showed a better controlled in vitro release of melatonin compared with the melatonin solution. The best controlled release results were achieved with hydrogels prepared with dried nanocapsules (hydrogels > redispersed dried nanocapsules > nanocapsule suspension > melatonin solution). The skin permeation studies demonstrated a significant modulation of the transdermal melatonin permeation for hydrogels prepared with redispersible nanocapsules. In this way, the additive effect of the different approaches used in this study (nanoencapsulation, spray-drying, and preparation of semisolid dosage forms) allows not only the control of melatonin release, but also transdermal permeation.

  17. Agglomerated oral dosage forms of artemisinin/β-cyclodextrin spray-dried primary microparticles showing increased dissolution rate and bioavailability.

    PubMed

    Balducci, Anna Giulia; Magosso, Enrico; Colombo, Gaia; Sonvico, Fabio; Khan, Nurzalina Abdul Karim; Yuen, Kah Hay; Bettini, Ruggero; Colombo, Paolo; Rossi, Alessandra

    2013-09-01

    Artemisinin, a poorly water-soluble antimalarial drug, presents a low and erratic bioavailability upon oral administration. The aim of this work was to study an agglomerated powder dosage form for oral administration of artemisinin based on the artemisinin/β-cyclodextrin primary microparticles. These primary microparticles were prepared by spray-drying a water-methanol solution of artemisinin/β-cyclodextrin. β-Cyclodextrin in spray-dried microparticles increased artemisinin water apparent solubility approximately sixfold. The thermal analysis evidenced a reduction in the enthalpy value associated with drug melting, due to the decrease in drug crystallinity. The latter was also evidenced by powder X-ray diffraction analysis, while (13)C-NMR analysis indicated the partial complexation with β-cyclodextrin. Agglomerates obtained by sieve vibration of spray-dried artemisinin/β-cyclodextrin primary microparticles exhibited free flowing and close packing properties compared with the non-flowing microparticulate powder. The in vitro dissolution rate determination of artemisinin from the agglomerates showed that in 10 min about 70% of drug was released from the agglomerates, whereas less than 10% of artemisinin was dissolved from raw material powder. Oral administration of agglomerates in rats yielded higher artemisinin plasma levels compared to those of pure drug. In the case of the agglomerated powder, a 3.2-fold increase in drug fraction absorbed was obtained.

  18. Nanoparticles by spray drying using innovative new technology: the Büchi nano spray dryer B-90.

    PubMed

    Li, Xiang; Anton, Nicolas; Arpagaus, Cordin; Belleteix, Fabrice; Vandamme, Thierry F

    2010-10-15

    Spray drying technology is widely known and used to transform liquids (solutions, emulsions, suspension, slurries, pastes or even melts) into solid powders. Its main applications are found in the food, chemical and materials industries to enhance ingredient conservation, particle properties, powder handling and storage etc. However, spray drying can also be used for specific applications in the formulation of pharmaceuticals for drug delivery (e.g. particles for pulmonary delivery). Büchi is a reference in the development of spray drying technology, notably for laboratory scale devices. This study presents the Nano Spray Dryer B-90, a revolutionary new sprayer developed by Büchi, use of which can lower the size of the produced dried particles by an order of magnitude attaining submicron sizes. In this paper, results are presented with a panel of five representative polymeric wall materials (arabic gum, whey protein, polyvinyl alcohol, modified starch, and maltodextrin) and the potentials to encapsulate nano-emulsions, or to formulate nano-crystals (e.g. from furosemide) are also shown.

  19. Study on Enhanced Dissolution of Azilsartan-Loaded Solid Dispersion, Prepared by Combining Wet Milling and Spray-Drying Technologies.

    PubMed

    Lu, Tianshu; Sun, Yinghua; Ding, Dawei; Zhang, Qi; Fan, Rui; He, Zhonggui; Wang, Jing

    2017-02-01

    The purpose of this study was to develop a combination method of wet milling and spray-drying technologies to prepare the solid dispersion and improve the dissolution rate of poorly water-soluble drug candidates. Azilsartan (AZL) was selected as the model drug for its poor water solubility. In the study, AZL-loaded solid dispersion was prepared with polyethylene glycol 6000 (PEG6000) and hydroxypropyl cellulose with super low viscosity (HPC-SL) as stabilizers by using combination of wet grinding and spray-drying methods. The high AZL loading solid dispersion was then characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier transform infrared spectroscopy (FTIR). Besides, dissolution test was carried out by the paddle method and stability investigation was also conducted. As a result, the dissolution rate of the solid dispersion tablets was found to be greater than conventional tablets, but in close agreement with market tablets. Furthermore, the formulation was shown to be stable at 40 ± 2°C and 75 ± 5% for at least 6 months, owing to its decreased particle size, morphology, and its crystal form. It was concluded that the combination of wet milling and spray-drying approaches to prepare solid dispersion would be a prospective method to improve the dissolution rate of poorly water-soluble drugs.

  20. Impact of surfactants on the crystallization of aqueous suspensions of celecoxib amorphous solid dispersion spray dried particles.

    PubMed

    Chen, Jie; Ormes, James D; Higgins, John D; Taylor, Lynne S

    2015-02-02

    Amorphous solid dispersions are frequently prepared by spray drying. It is important that the resultant spray dried particles do not crystallize during formulation, storage, and upon administration. The goal of the current study was to evaluate the impact of surfactants on the crystallization of celecoxib amorphous solid dispersions (ASD), suspended in aqueous media. Solid dispersions of celecoxib with hydroxypropylmethylcellulose acetate succinate were manufactured by spray drying, and aqueous suspensions were prepared by adding the particles to acidified media containing various surfactants. Nucleation induction times were evaluated for celecoxib in the presence and absence of surfactants. The impact of the surfactants on drug and polymer leaching from the solid dispersion particles was also evaluated. Sodium dodecyl sulfate and Polysorbate 80 were found to promote crystallization from the ASD suspensions, while other surfactants including sodium taurocholate and Triton X100 were found to inhibit crystallization. The promotion or inhibition of crystallization was found to be related to the impact of the surfactant on the nucleation behavior of celecoxib, as well as the tendency to promote leaching of the drug from the ASD particle into the suspending medium. It was concluded that surfactant choice is critical to avoid failure of amorphous solid dispersions through crystallization of the drug.

  1. Spray-dried powders improve the controlled release of antifungal tioconazole-loaded polymeric nanocapsules compared to with lyophilized products.

    PubMed

    Ribeiro, Roseane Fagundes; Motta, Mariana Heldt; Härter, Andréia Pisching Garcia; Flores, Fernanda Cramer; Beck, Ruy Carlos Ruver; Schaffazick, Scheila Rezende; de Bona da Silva, Cristiane

    2016-02-01

    This work aimed to obtain solid formulations from polymeric nanocapsules and nanoemulsions containing tioconazole, a broad spectrum antifungal drug. Two dehydration methods were used: spray-drying and freeze drying, using lactose as adjuvant (10%, w/v). The liquid formulations had a mean particle size around 206 nm and 182 nm for nanocapsules and nanoemulsions, respectively, and an adequate polydispersity index. Tioconazole content was close to the theoretical amount (1.0 mg/mL). After drying, the content ranged between 98 and 102%with a mean nanometric size of the dried products after redispersion. Scanning electron microscopy showed that the particles are rounded, sphere-shaped for the dried products obtained by spray-drying, and shapeless and irregular shapes for those obtained by freeze-drying. In the microbiological evaluation, all dried products remained active against the yeast Candida albicans when compared to the original systems. The dried products obtained by spray-drying from nanocapsules presented better control of the tioconazole release when compared to the freeze-drying products.

  2. Low hygroscopic spray-dried powders with trans-glycosylated food additives enhance the solubility and oral bioavailability of ipriflavone.

    PubMed

    Fujimori, Miki; Kadota, Kazunori; Kato, Kouki; Seto, Yoshiki; Onoue, Satomi; Sato, Hideyuki; Ueda, Hiroshi; Tozuka, Yuichi

    2016-01-01

    The improvement in the solubility and dissolution rate may promote a superior absorption property towards the human body. The spray-dried powders (SDPs) of ipriflavone, which was used as a model hydrophobic flavone, with trans-glycosylated rutin (Rutin-G) showed the highest solubilizing effect of ipriflavone among three types of trans-glycosylated food additives. The SDPs of ipriflavone with Rutin-G have both a significant higher dissolution rate and solubility enhancement of ipriflavone. This spray-dried formulation of ipriflavone with Rutin-G exhibited a low hygroscopicity as a critical factor in product preservation. In addition, an improvement in the oral absorption of ipriflavone was achieved by means of preparing composite particles of ipriflavone/Rutin-G via spray drying, indicating a 4.3-fold increase in the area under the plasma concentration-time curve compared with that of untreated ipriflavone. These phenomena could be applicable to food ingredients involving hydrophobic flavones for producing healthy food with a high quality.

  3. Stability of microencapsulated B. lactis (BI 01) and L. acidophilus (LAC 4) by complex coacervation followed by spray drying.

    PubMed

    Oliveira, A C; Moretti, T S; Boschini, C; Baliero, J C C; Freitas, O; Favaro-Trindade, C S

    2007-11-01

    Microcapsules containing Bifidobacterium lactis (BI 01) and Lactobacillus acidophilus (LAC 4) were produced by complex coacervation using a casein/pectin complex as the wall material, followed by spray drying. The aim of this study was to evaluate the resistance of these microorganisms when submitted to the spray drying process, a shelf-life of 120 days at 7-37 degrees C and the in vitro tolerance after being submitted to acid pH (pH 1.0 and 3.0) solutions besides morphology of microcapsules. Microencapsulated microorganisms were shown to be more resistant to acid conditions than free ones. Microencapsulated L. acidophilus maintained its viability for a longer storage period at both temperatures. The microcapsules presented a spherical shape with no fissures. The process used and the wall material were efficient in protecting the microorganisms under study against the spray drying process and simulated gastric juice; however, microencapsulated B. lactis lost its viability before the end of the storage time.

  4. CNS activities of liquid and spray-dried extracts from Lippia alba-Verbenaceae (Brazilian false melissa).

    PubMed

    Zétola, M; De Lima, T C M; Sonaglio, D; González-Ortega, G; Limberger, R P; Petrovick, P R; Bassani, V L

    2002-10-01

    The CNS activity of Lippia alba liquid and spray-dried extracts, containing the non-volatile fraction from the leaves, was investigated. L. alba liquid extracts were prepared by percolation with EtOH 40, 60 or 80%. The liquid extracts, named ES(40%,) ES(60%) and ES(80%,) were concentrated, the ethanol eliminated and then tested in Swiss mice to evaluate its sedative and anticonvulsant effects. The animals received the extracts, orally, in doses corresponding to 200 mg of dry residue by kilogram of body weight. All mice were evaluated in the barbiturate-induced sleep test. Similarly, other groups of mice were submitted to convulsions induced by pentylenetetrazol (PTZ). The concentrated extract obtained from ES(80%) showed the most significant sedative and myorelaxant effects as well as the highest total flavonoid content (66 mg/100 g, expressed in apigenin). Two spray-dried powders, SDP(1) and SDP(2), were prepared from ES(80%) using as excipients, respectively, colloidal silicon dioxide (CSD) and CSD associated to beta-cyclodextrin. Only SDP(1) showed sedative profile similar to that presented by ES(80). In conclusion, we demonstrated that the non-volatile fraction of L. alba, extracted in ethanol 80% (v/v), presents sedative and myorelaxant effects and that, among the tested extracts, this presents the highest flavonoid content. We demonstrated also the technological feasibility of spray-dried extracts and the influence of the excipient on its sedative properties.

  5. Hydrogels containing redispersible spray-dried melatonin-loaded nanocapsules: a formulation for transdermal-controlled delivery

    PubMed Central

    2012-01-01

    The aim of the present study was to develop a transdermal system for controlled delivery of melatonin combining three strategies: nanoencapsulation of melatonin, drying of melatonin-loaded nanocapsules, and incorporation of nanocapsules in a hydrophilic gel. Nanocapsules were prepared by interfacial deposition of the polymer and were spray-dried using water-soluble excipients. In vitro drug release profiles were evaluated by the dialysis bag method, and skin permeation studies were carried out using Franz cells with porcine skin as the membrane. The use of 10% (w/v) water-soluble excipients (lactose or maltodextrin) as spray-drying adjuvants furnished redispersible powders (redispersibility index approximately 1.0) suitable for incorporation into hydrogels. All formulations showed a better controlled in vitro release of melatonin compared with the melatonin solution. The best controlled release results were achieved with hydrogels prepared with dried nanocapsules (hydrogels > redispersed dried nanocapsules > nanocapsule suspension > melatonin solution). The skin permeation studies demonstrated a significant modulation of the transdermal melatonin permeation for hydrogels prepared with redispersible nanocapsules. In this way, the additive effect of the different approaches used in this study (nanoencapsulation, spray-drying, and preparation of semisolid dosage forms) allows not only the control of melatonin release, but also transdermal permeation. PMID:22587614

  6. Cetirizine dihydrochloride loaded microparticles design using ionotropic cross-linked chitosan nanoparticles by spray-drying method.

    PubMed

    Li, Feng-Qian; Ji, Rui-Rui; Chen, Xu; You, Ben-Ming; Pan, Yong-Hua; Su, Jia-Can

    2010-12-01

    To control the release rate and mask the bitter taste, cetirizine dihydrochloride (CedH) was entrapped within chitosan nanoparticles (CS-NPs) using an ionotropic gelation process, followed by microencapsulation to produce CS matrix microparticles using a spray-drying method. The aqueous colloidal CS-NPs dispersions with a drug encapsulation efficiency (EE) of <15%, were then spray dried to produce a powdered nanoparticles-in-microparticles system with an EE of >70%. The resultant spherical CS microparticles had a smooth surface, were free of organic solvent residue and showed a diameter range of 0.5~5 μm. The in vitro drug release properties of CedH encapsulated microparticles showed an initial burst effect during the first 2 h. Drug release from the matrix CS microparticles could be retarded by the crosslinking agent pentasodium tripolyphosphate or the wall material. The technique of 'ionotropic gelation' combined with 'spray-drying' could be applicable for preparation of CS nanoparticlesin-microparticles drug delivery systems. CS-NPs based microparticles might provide a potential micro-carrier for oral administration of the freely water-soluble drug--CedH.

  7. Solubility enhancement of BCS Class II drug by solid phospholipid dispersions: Spray drying versus freeze-drying.

    PubMed

    Fong, Sophia Yui Kau; Ibisogly, Asiye; Bauer-Brandl, Annette

    2015-12-30

    The poor aqueous solubility of BCS Class II drugs represents a major challenge for oral dosage form development. Using celecoxib (CXB) as model drug, the current study adopted a novel solid phospholipid nanoparticle (SPLN) approach and compared the effect of two commonly used industrial manufacturing methods, spray- and freeze-drying, on the solubility and dissolution enhancement of CXB. CXB was formulated with Phospholipoid E80 (PL) and trehalose at different CXB:PL:trehalose ratios, of which 1:10:16 was the optimal formulation. Spherical amorphous SPLNs with average diameters <1μm were produced by spray-drying; while amorphous 'matrix'-like structures of solid PL dispersion with larger particle sizes were prepared by freeze-drying. Formulations from both methods significantly enhanced the dissolution rates, apparent solubility, and molecularly dissolved concentration of CXB in phosphate buffer (PBS, pH 6.5) and in biorelevant fasted state simulated intestinal fluid (FaSSIF, pH 6.5) (p<0.05). While similar dissolution rates were found, the spray-dried SPLNs had a larger enhancement in apparent solubility (29- to 132-fold) as well as molecular solubility (18-fold) of CXB at equilibrium (p<0.05). The strong capability of the spray-dried SPLNs to attain 'true' supersaturation state makes them a promising approach for bioavailability enhancement of poorly soluble drugs.

  8. Extracellular β-fructofuranosidase from Fusarium graminearum: stability of the spray-dried enzyme in the presence of different carbohydrates.

    PubMed

    Gonçalves, Heloísa Bressan; Jorge, João Atílio; Oliveira, Wanderley Pereira; Souza, Claudia Regina Fernandes; Guimarães, Luis Henrique Souza

    2013-01-01

    Microbial enzymes have been used for various biotechnological applications; however, enzyme stabilization remains a challenge for industries and needs to be considered. This study describes the effects of spray-drying conditions on the activity and stability of β-fructofuranosidase from Fusarium graminearum. The extracellular enzyme β-fructofuranosidase was spray dried in the presence of stabilizers, including starch (Capsul) (SC), microcrystalline cellulose (MC), trehalose (TR), lactose (LC) and β-cyclodextrin (CD). In the presence of TR (2% w/v), the enzymatic activity was fully retained. After 1 year of storage, 74% of the enzymatic activity was maintained with the CD stabilizer (10% w/v). The residual activity was maintained as high as 80% for 1 h at 70°C when MC, SC and CD (5% w/v) stabilizers were used. Spray drying with carbohydrates was effective in stabilizing the F. graminearum β-fructofuranosidase, improved enzymatic properties compared to the soluble enzyme and demonstrated a potential use in future biotechnology applications.

  9. Synthesis of Cr-doped CaTiSiO{sub 5} ceramic pigments by spray drying

    SciTech Connect

    Lyubenova, T. Stoyanova Matteucci, F.; Costa, A.L.; Dondi, M.; Ocana, M.

    2009-04-02

    Cr-doped CaTiSiO{sub 5} was synthesized by spray drying and conventional ceramic method in order to assess its potential as ceramic pigment. The evolution of the phase composition with thermal treatment was investigated by X-ray powder diffraction (XRPD) and thermal analyses (DTA-TGA-EGA). Powder morphology and particle size distribution were analyzed by scanning electron microscopy (SEM) and laser diffraction, respectively. The color efficiency of pigments was evaluated by optical spectroscopy (UV-vis-NIR) and colorimetric analysis (CIE Lab). Results proved that spray drying is an efficient procedure to prepare highly reactive pigment precursors. The spray-dried powders consist of hollow spherical particles with aggregate size in the 1-10 {mu}m range, developing a brown coloration. Optical spectra reveal the occurrence of Cr(III) and Cr(IV), both responsible for the brown color of this pigment. The former occupies the octahedral site of titanite, in substitution of Ti(IV), while the latter is located at the tetrahedral site, where replaces Si(IV)

  10. The effect of pigment matrix, temperature and amount of carrier on the yield and final color properties of spray dried purple corn (Zea mays L.) cob anthocyanin powders.

    PubMed

    Lao, Fei; Giusti, M Monica

    2017-07-15

    Spray drying is an economic technique to produce anthocyanin-based colorants. High pigments yields with minimum color degradation are desirable to maximize quality and profits. This study evaluated the impacts of purple corncob (PCC) anthocyanin extraction matrices (hot water, 40% ethanol, C18 purified), drying inlet temperature (130, 150, 170°C) and amount of carrier (2%, 5%, 10% maltodextrin) on the yields and quality of PCC anthocyanin powders. Monomeric and polymeric anthocyanins, color properties (CIELch, haze), and pigments composition before and after spray drying were determined. The yield and final color quality of spray dried PCC anthocyanins were affected (p<0.05) by all parameters evaluated. The pigment matrix, inlet temperature, and carrier amount had biggest impacts on product water solubility, pigments degradation and yield, respectively. The optimal combination of hot water extracts spray dried with 5% maltodextrin at 150°C gave the highest pigment yield (∼90%) with good solubility with the least color loss.

  11. Impact of different spray-drying conditions on the viability of wine Saccharomyces cerevisiae strains.

    PubMed

    Aponte, Maria; Troianiello, Gabriele Danilo; Di Capua, Marika; Romano, Raffaele; Blaiotta, Giuseppe

    2016-01-01

    Spray-drying (SD) is widely considered a suitable method to preserve microorganisms, but data regarding yeasts are still scanty. In this study, the effect of growing media, process variables and carriers over viability of a wild wine Saccharomyces (S.) cerevisiae LM52 was evaluated. For biomass production, the strain was grown (batch and fed-batch fermentation) in a synthetic, as well as in a beet sugar molasses based-medium. Drying of cells resuspended in several combinations of soluble starch and maltose was performed at different inlet and outlet temperatures. Under the best conditions-suspension in soluble starch plus maltose couplet to inlet and outlet temperatures of 110 and 55 °C, respectively-the loss of viability of S. cerevisiae LM52 was 0.8 ± 0.1 and 0.5 ± 0.2 Log c.f.u. g(-1) for synthetic and molasses-based medium, respectively. Similar results were obtained when S. cerevisiae strains Zymoflore F15 and EC1118, isolated from commercial active dry yeast (ADY), were tested. Moreover, powders retained a high vitality and showed good fermentation performances up to 6 month of storage, at both 4 and -20 °C. Finally, fermentation performances of different kinds of dried formulates (SD and ADY) compared with fresh cultures did not show significant differences. The procedure proposed allowed a small-scale production of yeast in continuous operation with relatively simple equipment, and may thus represent a rapid response-on-demand for the production of autochthonous yeasts for local wine-making.

  12. Preparation and characterization of fast dissolving flurbiprofen and esomeprazole solid dispersion using spray drying technique.

    PubMed

    Pradhan, Roshan; Tran, Tuan Hiep; Kim, Sung Yub; Woo, Kyu Bong; Choi, Yong Joo; Choi, Han-Gon; Yong, Chul Soon; Kim, Jong Oh

    2016-04-11

    We aimed to develop an immediate-release flurbiprofen (FLU) and esomeprazole (ESO) combination formulation with enhanced gastric aqueous solubility and dissolution rate. Aqueous solubility can be enhanced by formulating solid dispersions (SDs) with a polyvinylpyrrolidone (PVP)-K30 hydrophilic carrier, using spray-drying technique. Aqueous and gastric pH dissolution can be achieved by macro-environmental pH modulation using sodium bicarbonate (NaHCO3) and magnesium hydroxide (Mg(OH)2) as the alkaline buffer. FLU/ESO-loaded SDs (FLU/ESO-SDs) significantly improved aqueous solubility of both drugs, compared to each drug powder. Dissolution studies in gastric pH and water were compared with the microenvironmental pH modulated formulations. The optimized FLU/ESO-SD powder formulation consisted of FLU/ESO/PVP-K30/sodium carbonate (Na2CO3) in a weight ratio 1:0.22:1.5:0.3, filled in the inner capsule. The outer capsule consisted of NaHCO3 and Mg(OH)2, which created the macro-environmental pH modulation. Increased aqueous and gastric pH dissolution of FLU and ESO from the SD was attributed to the alkaline buffer effects and most importantly, to drug transformation from crystalline to amorphous SD powder, clearly revealed by scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffraction studies. Thus, the combined FLU and ESO SD powder can be effectively delivered as an immediate-release formulation using the macro-environmental pH modulation concept.

  13. Spray dried glyceryl monooleate-magnesium trisilicate dry powder as cubic phase precursor.

    PubMed

    Shah, Manish H; Biradar, Shailesh V; Paradkar, Anant R

    2006-10-12

    Glyceryl monooleate (GMO) is a polar amphiphilic lipid, which forms different sequential lyotropic liquid crystals upon hydration. GMO has been utilized for various delivery systems and routes of administrations. Owing to sticky and waxy nature of GMO, preparation of oral solid dosage form utilizing GMO is still a challenge for pharmaceutical researchers. Therefore, the objective of the present work was to fabricate dry powder precursors using GMO, which upon hydration in situ forms cubic phase and can be wisely used for fabrication of oral solid dosage forms. In addition to this, dry powder precursor was evaluated for drug loading, in vitro release behavior and in vivo performance of model drug diclofenac sodium (DiNa). The dry powder precursor was obtained by spray-drying GMO with DiNa using magnesium trisilicate (MTS) as adsorbent. The percent drug entrapment of various batches of powder precursor was in the range of 84-93% indicating high content uniformity. SEM and image analysis showed that as the amount of MTS in powder precursor was increased, the particle size decreased. Furthermore, the viscosity of powder precursor was function of amount of MTS. The rate of water uptake of powder precursor was higher due to uniform layer of GMO on the MTS surface, which led to faster transformation of lamellar phase into cubic phase. The polarizing light microscopy confirmed that cubic phase was formed upon hydration of powder precursor. The drug released from powder precursor was initially governed by the cubic phase formed and in later stage it depends upon dynamic swelling behavior of hexagonally packed cylindrical aggregates. The drug loaded powder precursor was found to have more effective and prolonged anti-inflammatory and analgesic activity as compared to pure drug. Thus the dry powder precursor of cubic phase was prepared in which drug release was entirely governed by the mesophases formed.

  14. Formulation Development, Process Optimization, and In Vitro Characterization of Spray-Dried Lansoprazole Enteric Microparticles

    PubMed Central

    Vora, Chintan; Patadia, Riddhish; Mittal, Karan; Mashru, Rajashree

    2016-01-01

    This research focuses on the development of enteric microparticles of lansoprazole in a single step by employing the spray drying technique and studies the effects of variegated formulation/process variables on entrapment efficiency and in vitro gastric resistance. Preliminary trials were undertaken to optimize the type of Eudragit and its various levels. Further trials included the incorporation of plasticizer triethyl citrate and combinations of other polymers with Eudragit S 100. Finally, various process parameters were varied to investigate their effects on microparticle properties. The results revealed Eudragit S 100 as the paramount polymer giving the highest gastric resistance in comparison to Eudragit L 100-55 and L 100 due to its higher pH threshold and its polymeric backbone. Incorporation of plasticizer not only influenced entrapment efficiency, but diminished gastric resistance severely. On the contrary, polymeric combinations reduced entrapment efficiency for both sodium alginate and glyceryl behenate, but significantly influenced gastric resistance for only sodium alginate and not for glyceryl behenate. The optimized process parameters were comprised of an inlet temperature of 150°C, atomizing air pressure of 2 kg/cm2, feed solution concentration of 6% w/w, feed solution spray rate of 3 ml/min, and aspirator volume of 90%. The SEM analysis revealed smooth and spherical shape morphologies. The DSC and PXRD study divulged the amorphous nature of the drug. Regarding stability, the product was found to be stable under 3 months of accelerated and long-term stability conditions as per ICH Q1A(R2) guidelines. Thus, the technique offers a simple means to generate polymeric enteric microparticles that are ready to formulate and can be directly filled into hard gelatin capsules. PMID:27222612

  15. High-volume use of self-cementing spray dry absorber material for structural applications

    NASA Astrophysics Data System (ADS)

    Riley, Charles E.

    Spray dry absorber (SDA) material, or spray dryer ash, is a byproduct of energy generation by coal combustion and sulfur emissions controls. Like any resource, it ought to be used to its fullest potential offsetting as many of the negative environmental impacts of coal combustion as possible throughout its lifecycle. Its cementitious and pozzolanic properties suggest it be used to augment or replace another energy and emissions intensive product: Portland cement. There is excellent potential for spray dryer ash to be used beneficially in structural applications, which will offset CO2 emissions due to Portland cement production, divert landfill waste by further utilizing a plentiful coal combustion by-product, and create more durable and sustainable structures. The research into beneficial use applications for SDA material is relatively undeveloped and the material is highly underutilized. This dissertation explored a specific self-cementing spray dryer ash for use as a binder in structural materials. Strength and stiffness properties of hydrated spray dryer ash mortars were improved by chemical activation with Portland cement and reinforcement with polymer fibers from automobile tire recycling. Portland cement at additions of five percent of the cementitious material was found to function effectively as an activating agent for spray dryer ash and had a significant impact on the hardened properties. The recycled polymer fibers improved the ductility and toughness of the material in all cases and increased the compressive strength of weak matrix materials like the pure hydrated ash. The resulting hardened materials exhibited useful properties that were sufficient to suggest that they be used in structural applications such as concrete, masonry block, or as a hydraulic cement binder. While the long-term performance characteristics remain to be investigated, from an embodied-energy and carbon emissions standpoint the material investigated here is far superior to

  16. Modification of electrostatic charge on inhaled carrier lactose particles by addition of fine particles.

    PubMed

    Bennett, F S; Carter, P A; Rowley, G; Dandiker, Y

    1999-01-01

    Triboelectrification affects particle adhesion and agglomeration and hence the formulation, manufacture, and use of dry powder inhaler (DPI) devices. Electrostatic charge measurement of two component mixes of spray-dried or crystalline lactose fine particles (< 10 microns) 0, 5, 10, 15, 20, and 30% w/w with spray-dried or crystalline lactose 63-90 microns, respectively, has been undertaken using a system incorporating pneumatic transport of the mixed powders to a stainless steel cyclone charging device. The magnitude of charge on the mixes was shown to decrease with increased fine particle content, and there was no significant difference in charge for each concentration between spray-dried and crystalline lactose. Both the variation of charge and powder adhesion to the cyclone surface increased with increase in fine particle content. The proportion of fine particles in carrier systems in DPIs may thus have an important role where triboelectrification is involved.

  17. Evaluation of the Microcentrifuge Dissolution Method as a Tool for Spray-Dried Dispersion.

    PubMed

    Wu, Benjamin; Li, Jinjiang; Wang, Yahong

    2016-03-01

    Although using spray-dried dispersions (SDDs) to improve the bioavailability of poorly water-soluble compounds has become a common practice in supporting the early phases of clinical studies, their performance evaluation, whether in solid dosage forms or alone, still presents significant challenges. A microcentrifuge dissolution method has been reported to quickly assess the dissolution performance of SDDs. While the microcentrifuge dissolution method has been used in the SDD community, there is still a need to understand the mechanisms about the molecular species present in supernatant after centrifugation, the molecular nature of active pharmaceutical ingredients (APIs), as well as the impact of experimental conditions. In this paper, we aim to assess the effect of API and polymer properties on the dissolution behavior of SDDs along with centrifuging parameters, and for this, two poorly water-soluble compounds (indomethacin and ketoconazole) and two commonly used polymers in the pharmaceutical industry (PVP and HPMC-AS) were chosen to prepare SDDs. A typical microcentrifuge dissolution procedure as reported in the publication (Curatolo et al., Pharm Res 26:1419-1431, 2009) was followed. In addition, after separation of the supernatant from precipitation, some of the samples were filtered through filters of various sizes to investigate the particulate nature (particle size) of the supernatant. Furthermore, the centrifuge speed was varied to study sedimentation of API, SDD, or polymer particles. The results indicated that for the SDDs of four drug-polymer pairs, microcentrifuge dissolution exhibited varied behaviors, depending on the polymer and the drug used. The SDDs of indomethacin with either PVP or HPMC-AS showed a reproducible dissolution with minimum variability even after filtration and subjecting to varied centrifugation speed, suggesting that the supernatant behaved solution-like. However, ketoconazole-PVP and ketoconazole-HPMC-AS SDDs displayed a

  18. Simple and scalable method for peptide inhalable powder production.

    PubMed

    Schoubben, Aurélie; Blasi, Paolo; Giovagnoli, Stefano; Ricci, Maurizio; Rossi, Carlo

    2010-01-31

    The aim of this work was to produce capreomycin dry powder and capreomycin loaded PLGA microparticles intended for tuberculosis inhalation therapy, using simple and scalable methods. Capreomycin physico-chemical characteristics have been modified by hydrophobic ion pairing with oleate. The powder suspension was processed by high pressure homogenization and spray-dried. Spray-drying was also used to prepare capreomycin oleate (CO) loaded PLGA microparticles. CO powder was suspended in the organic phase containing PLGA and the suspension was spray-dried. Particle dimensions were determined using photon correlation spectroscopy and Accusizer C770. Morphology was investigated by scanning electron microscopy (SEM) and capreomycin content by spectrophotometry. Capreomycin properties were modified to increase polymeric microparticle content and obtain respirable CO powder. High pressure homogenization allowed to reduce CO particle dimensions obtaining a population in the micrometric (6.18 microm) and one in the nanometric (approximately 317 nm) range. SEM pictures showed not perfectly spherical particles with a wrinkled surface, generally suitable for inhalation. PLGA particles were characterized by a high encapsulation efficiency (about 90%) and dimensions (approximately 6.69 microm) suitable for inhalation. Concluding, two different formulations were successfully developed for capreomycin pulmonary delivery. The hydrophobic ion pair strategy led to a noticeable drug content increase.

  19. High drug load, stable, manufacturable and bioavailable fenofibrate formulations in mesoporous silica: a comparison of spray drying versus solvent impregnation methods.

    PubMed

    Hong, Shiqi; Shen, Shoucang; Tan, David Cheng Thiam; Ng, Wai Kiong; Liu, Xueming; Chia, Leonard S O; Irwan, Anastasia W; Tan, Reginald; Nowak, Steven A; Marsh, Kennan; Gokhale, Rajeev

    2016-01-01

    Encapsulation of drugs in mesoporous silica using co-spray drying process has been recently explored as potential industrial method. However, the impact of spray drying on manufacturability, physiochemical stability and bioavailability in relation to conventional drug load processes are yet to be fully investigated. Using a 2(3) factorial design, this study aims to investigate the effect of drug-loading process (co-spray drying and solvent impregnation), mesoporous silica pore size (SBA-15, 6.5 nm and MCM-41, 2.5 nm) and percentage drug load (30% w/w and 50% w/w) on material properties, crystallinity, physicochemical stability, release profiles and bioavailability of fenofibrate (FEN) loaded into mesoporous silica. From the scanning electronic microscopy (SEM) images, powder X-ray diffraction and Differential scanning calorimetry measurements, it is indicated that the co-spray drying process was able to load up to 50% (w/w) FEN in amorphous form onto the mesoporous silica as compared to the 30% (w/w) for solvent impregnation. The in vitro dissolution rate of the co-spray dried formulations was also significantly (p = 0.044) better than solvent impregnated formulations at the same drug loading. Six-month accelerated stability test at 40 °C/75 RH in open dish indicated excellent physical and chemical stability of formulations prepared by both methods. The amorphous state of FEN and the enhanced dissolution profiles were well preserved, and very low levels of degradation were detected after storage. The dog data for the three selected co-spray-dried formulations revealed multiple fold increment in FEN bioavailability compared to the reference crystalline FEN. These results validate the viability of co-spray-dried mesoporous silica formulations with high amorphous drug load as potential drug delivery systems for poorly water soluble drugs.

  20. The effect of spray-drying parameters on the flavor of nonfat dry milk and milk protein concentrate 70.

    PubMed

    Park, Curtis W; Stout, Mark A; Drake, MaryAnne

    2016-12-01

    Unit operations during production influence the sensory properties of nonfat dry milk (NFDM) and milk protein concentrate (MPC). Off-flavors in dried dairy ingredients decrease consumer acceptance of ingredient applications. Previous work has shown that spray-drying parameters affect physical and sensory properties of whole milk powder and whey protein concentrate. The objective of this study was to determine the effect of inlet temperature and feed solids concentration on the flavor of NFDM and MPC 70% (MPC70). Condensed skim milk (50% solids) and condensed liquid MPC70 (32% solids) were produced using pilot-scale dairy processing equipment. The condensed products were then spray dried at either 160, 210, or 260°C inlet temperature and 30, 40, or 50% total solids for NFDM and 12, 22, or 32% for MPC70 in a randomized order. The entire experiment was replicated 3 times. Flavor of the NFDM and MPC70 was evaluated by sensory and instrumental volatile compound analyses. Surface free fat, particle size, and furosine were also analyzed. Both main effects (30, 40, and 50% solids and 160, 210, and 260°C inlet temperature) and interactions between solids concentration and inlet temperature were investigated. Interactions were not significant. In general, results were consistent for NFDM and MPC70. Increasing inlet temperature and feed solids concentration increased sweet aromatic flavor and decreased cardboard flavor and associated lipid oxidation products. Increases in furosine with increased inlet temperature and solids concentration indicated increased Maillard reactions during drying. Particle size increased and surface free fat decreased with increasing inlet temperature and solids concentration. These results demonstrate that increasing inlet temperatures and solids concentration during spray drying decrease off-flavor intensities in NFDM and MPC70 even though the heat treatment is greater compared with low temperature and low solids.

  1. Compaction of spray-dried ceramic powders: An experimental study of the factors that control green density

    SciTech Connect

    Readey, M.J.; Mahoney, F.M.

    1995-11-01

    The pressure-compaction response of a spray-dried, 94% alumina powder containing several percent of a polymeric binder was investigated as a function of die diameter and compact aspect ratio. The results show that the die fill density decreases markedly with decreasing die diameter and aspect ratio, while the final green density (at 120 MPa) decreases only slightly under the same conditions. These results suggest that the ratio of the initial compact dimensions to the size of the granules may be much more important than previously considered.

  2. Nano spray-dried sodium chloride and its effects on the microbiological and sensory characteristics of surface-salted cheese crackers.

    PubMed

    Moncada, Marvin; Astete, Carlos; Sabliov, Cristina; Olson, Douglas; Boeneke, Charles; Aryana, Kayanush J

    2015-09-01

    Reducing particle size of salt to approximately 1.5 µm would increase its surface area, leading to increased dissolution rate in saliva and more efficient transfer of ions to taste buds, and hence, perhaps, a saltier perception of foods. This has a potential for reducing the salt level in surface-salted foods. Our objective was to develop a salt using a nano spray-drying method, to use the developed nano spray-dried salt in surface-salted cheese cracker manufacture, and to evaluate the microbiological and sensory characteristics of cheese crackers. Sodium chloride solution (3% wt/wt) was sprayed through a nano spray dryer. Particle sizes were determined by dynamic light scattering, and particle shapes were observed by scanning electron microscopy. Approximately 80% of the salt particles produced by the nano spray dryer, when drying a 3% (wt/wt) salt solution, were between 500 and 1,900 nm. Cheese cracker treatments consisted of 3 different salt sizes: regular salt with an average particle size of 1,500 µm; a commercially available Microsized 95 Extra Fine Salt (Cargill Salt, Minneapolis, MN) with an average particle size of 15 µm; and nano spray-dried salt with an average particle size of 1.5 µm, manufactured in our laboratory and 3 different salt concentrations (1, 1.5, and 2% wt/wt). A balanced incomplete block design was used to conduct consumer analysis of cheese crackers with nano spray-dried salt (1, 1.5, and 2%), Microsized salt (1, 1.5, and 2%) and regular 2% (control, as used by industry) using 476 participants at 1wk and 4mo. At 4mo, nano spray-dried salt treatments (1, 1.5, and 2%) had significantly higher preferred saltiness scores than the control (regular 2%). Also, at 4mo, nano spray-dried salt (1.5 and 2%) had significantly more just-about-right saltiness scores than control (regular 2%). Consumers' purchase intent increased by 25% for the nano spray-dried salt at 1.5% after they were notified about the 25% reduction in sodium content of the

  3. Impact of extra virgin olive oil and ethylenediaminetetraacetic acid (EDTA) on the oxidative stability of fish oil emulsions and spray-dried microcapsules stabilized by sugar beet pectin.

    PubMed

    Polavarapu, Sudheera; Oliver, Christine M; Ajlouni, Said; Augustin, Mary Ann

    2012-01-11

    The influence of EDTA on lipid oxidation in sugar beet pectin-stabilized oil-in-water emulsions (pH 6, 15% oil, wet basis), prepared from fish oil (FO) and fish oil-extra virgin olive oil (FO-EVOO) (1:1 w/w), as well as the spray-dried microcapsules (50% oil, dry basis) prepared from these emulsions, was investigated. Under accelerated conditions (80 °C, 5 bar oxygen pressure) the oxidative stability was significantly (P < 0.05) higher for FO and FO-EVOO formulated with EDTA, in comparison to corresponding emulsions and spray-dried microcapsules formulated without EDTA. The EDTA effect was greater in emulsions than in spray-dried microcapsules, with the greatest protective effect obtained in FO-EVOO emulsions. EDTA enhanced the oxidative stability of the spray-dried microcapsules during ambient storage (~25 °C, a(w) = 0.5), as demonstrated by their lower concentration of headspace volatile oxidation products, propanal and hexanal. These results show that the addition of EDTA is an effective strategy to maximize the oxidative stability of both FO emulsions and spray-dried microcapsules in which sugar beet pectin is used as the encapsulant material.

  4. Storage stability of Anagrapha falcifera nucleopolyhedrovirus in spray-dried formulations.

    PubMed

    Tamez-Guerra, Patricia; McGuire, Michael R; Behle, Robert W; Shasha, Baruch S; Pingel, Randall L

    2002-01-01

    A multiply embedded nucleopolyhedrovirus isolated from Anagrapha falcifera (Kirby) (AfMNPV) can lose insecticidal activity during months of dry storage in ambient room conditions. We tested the spray-dried AfMNPV formulations after storage for up to 1 year at room temperatures for insecticidal activity against neonate Trichoplusia ni (Hübner). Experimental formulations were made using combinations of corn flours, lignin, and sucrose, and were selected based on previous work which demonstrated that these formulations resisted solar degradation in field experiments. Twelve experimental formulations (organized in three groups of four formulations) compared the effect of (1) the ratio of formulation ingredients (lignin and corn flour) to virus concentration, (2) different sources of lignin, or (3) different corn flours and sugar. Based on a single-dose plant assay with these 12 formulations, none of the formulations lost significant activity due to the drying process, when compared with the unformulated wet AfMNPV. Samples of the 12 dried formulations were stored at room (22+/-3 degrees C) and refrigerated (4 degrees C) temperatures. Insecticidal activity (LC(50)) was determined with a dosage-response assay for neonates fed on treated cotton-leaf disks. After 6 (or 9) and 12 months storage, refrigerated samples maintained insecticidal activity better than corresponding samples stored at room temperatures with LC(50)s that averaged 2.0 x 10(6) polyhedral inclusion bodies per milliliter (pibs/ml) for refrigerated samples and 5.4 x 10(6) pibs/ml for samples stored at room temperatures. Compared with unformulated stock virus stored frozen, six formulations stored at room temperature and 10 formulations stored in the refrigerator did not lose significant insecticidal activity after 1 year based on overlapping 90% confidence intervals. Changing the ratio of virus to formulation ingredients did not provide a clear trend over the range of concentrations tested, and may be

  5. Spray-dried plasma attenuates inflammation and improves pregnancy rate of mated female mice.

    PubMed

    Song, M; Liu, Y; Lee, J J; Che, T M; Soares-Almeida, J A; Chun, J L; Campbell, J M; Polo, J; Crenshaw, J D; Seo, S W; Pettigrew, J E

    2015-01-01

    Three studies were conducted to test the hypothesis that dietary spray-dried plasma (SDP) might improve pregnancy rate by ameliorating inflammation, using mice in an experimental model that produces a low pregnancy rate. Mated female mice (C57BL/6 strain) were purchased and shipped from a vendor (Bar Harbor, ME) to the university facility (Urbana, IL) on the day the vaginal plug was found (gestation day [GD] 1), arriving at the laboratory on GD 3 after 2 d transport by air and ground. Mice (Exp. 1: n = 250, 16.0 ± 1.2 g BW; Exp. 2: n = 202, 16.2 ± 1.2 g BW; Exp. 3: n = 156, 16.4 ± 1.1 g BW) were housed in individual cages and randomly assigned to dietary treatments (Exp. 1: 0 [CON] and 8% SDP in the diet, ≥ 90 mice/diet; Exp. 2: 0, 1, 2, 4, and 8% SDP in the diet, ≥ 40 mice/diet; Exp. 3: 0, 1, and 8% SDP in the diet, 48 mice/diet) fed from arrival. In Exp. 1 and 2, pregnancy of each mouse was determined on GD 17 based on BW, shape of abdomen, and inspection postmortem, and maternal growth performance from GD 3 to 17 was measured. On GD 19, pregnant mice in Exp. 2 were euthanized to measure number of fetuses and fetal and placental weights. Pregnancy rates in CON were low in both Exp. 1 (11%) and Exp. 2 (7%). The SDP consistently and markedly increased (P < 0.05) pregnancy rates in both Exp. 1 (49%) and Exp. 2 (35-43%) compared with the CON. In Exp. 3, 12 randomly selected mice were euthanized immediately after they arrived as an initial group. From GD 4 to 7, randomly selected mice were also euthanized each day (12 mice/diet). After euthanasia, the abdominal cavity was opened to check pregnancy by uterine inspection and to collect blood and uterus samples for immune measurements. The SDP increased (P < 0.05; 40 vs. 15%) pregnancy rate compared with the CON. Concentrations of indicators of inflammation and stress (uterine TNF-α and IFN-γ, and serum TNF-α, C-reactive protein, and cortisol) were greatest (P < 0.05) and an anti-inflammatory cytokine (TGF-β1

  6. Spray drying method for large-scale and high-performance silicon negative electrodes in Li-ion batteries.

    PubMed

    Jung, Dae Soo; Hwang, Tae Hoon; Park, Seung Bin; Choi, Jang Wook

    2013-05-08

    Nanostructured silicon electrodes have shown great potential as lithium ion battery anodes because they can address capacity fading mechanisms originating from large volume changes of silicon alloys while delivering extraordinarily large gravimetric capacities. Nonetheless, synthesis of well-defined silicon nanostructures in an industrially adaptable scale still remains as a challenge. Herein, we adopt an industrially established spray drying process to enable scalable synthesis of silicon-carbon composite particles in which silicon nanoparticles are embedded in porous carbon particles. The void space existing in the porous carbon accommodates the volume expansion of silicon and thus addresses the chronic fading mechanisms of silicon anodes. The composite electrodes exhibit excellent electrochemical performance, such as 1956 mAh/g at 0.05C rate and 91% capacity retention after 150 cycles. Moreover, the spray drying method requires only 2 s for the formation of each particle and allows a production capability of ~10 g/h even with an ultrasonic-based lab-scale equipment. This investigation suggests that established industrial processes could be adaptable to the production of battery active materials that require sophisticated nanostructures as well as large quantity syntheses.

  7. A novel spray-dried nanoparticles-in-microparticles system for formulating scopolamine hydrobromide into orally disintegrating tablets.

    PubMed

    Li, Feng-Qian; Yan, Cheng; Bi, Juan; Lv, Wei-Lin; Ji, Rui-Rui; Chen, Xu; Su, Jia-Can; Hu, Jin-Hong

    2011-01-01

    Scopolamine hydrobromide (SH)-loaded microparticles were prepared from a colloidal fluid containing ionotropic-gelated chitosan nanoparticles using a spray-drying method. The spray-dried microparticles were then formulated into orally disintegrating tablets (ODTs) using a wet granulation tablet formation process. A drug entrapment efficiency of about 90% (w/w) and loading capacity of 20% (w/w) were achieved for the microparticles, which ranged from 2 μm to 8 μm in diameter. Results of disintegration tests showed that the formulated ODTs could be completely dissolved within 45 seconds. Drug dissolution profiles suggested that SH is released more slowly from tablets made using the microencapsulation process compared with tablets containing SH that is free or in the form of nanoparticles. The time it took for 90% of the drug to be released increased significantly from 3 minutes for conventional ODTs to 90 minutes for ODTs with crosslinked microparticles. Compared with ODTs made with noncrosslinked microparticles, it was thus possible to achieve an even lower drug release rate using tablets with appropriate chitosan crosslinking. Results obtained indicate that the development of new ODTs designed with crosslinked microparticles might be a rational way to overcome the unwanted taste of conventional ODTs and the side effects related to SH's intrinsic characteristics.

  8. Pharmaceutical development of an oral tablet formulation containing a spray dried amorphous solid dispersion of docetaxel or paclitaxel.

    PubMed

    Sawicki, Emilia; Beijnen, Jos H; Schellens, Jan H M; Nuijen, Bastiaan

    2016-09-25

    Previously, it was shown in Phase I clinical trials that solubility-limited oral absorption of docetaxel and paclitaxel can be drastically improved with a freeze dried solid dispersion (fdSD). These formulations, however, are unfavorable for further clinical research because of limitations in amorphicity of SD and scalability of the production process. To resolve this, a spray drying method for an SD (spSD) containing docetaxel or paclitaxel and subsequently drug products were developed. Highest saturation solubility (Smax), precipitation onset time (Tprecip), amorphicity, purity, residual solvents, yield/efficiency and powder flow of spSDs were studied. Drug products were monitored for purity/content and dissolution during 24 months at +15-25°C. Docetaxel spSD Smax was equal to that of fdSD but Tprecip was 3 times longer. Paclitaxel spSD Smax was 30% increased but Tprecip was equal to fdSD. spSDs were fully amorphous, >99% pure, <5% residual solvents, mean batch yield was 100g and 84%. spSDs had poor powder flow characteristics, which could not be resolved by changing settings, but by using 75% lactose as diluent. The drug product was a tablet with docetaxel or paclitaxel spSD and was stable for at least 24 months. Spray drying is feasible for the production of SD of docetaxel or paclitaxel for upcoming clinical trials.

  9. Technological Characterization and Stability of Ilex paraguariensis St. Hil. Aquifoliaceae (Maté) Spray-Dried Powder

    PubMed Central

    Yatsu, Francini K.J.; Borghetti, Greice S.

    2011-01-01

    Abstract The present work was designed to produce an Ilex paraguariensis spray-dried powder (SDP), in semi-industrial scale, in order to characterize its technological and chemical properties as well as to evaluate the thermal stability and photostability of the main polyphenol constituents. The yield of the spray-drying process was satisfactory (67%). The resulting SDP showed to be a material presenting spherical particles with a mean size of 19.6 μm, smooth surface, and good flow properties. The four polyphenol compounds previously reported for the species—neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, and rutin—were identified. Regarding the photostability test, the polyphenols present in the SDP proved to be stable against ultraviolet C radiation for 48 hours, independently of the packaging material. In the thermal stability test, the polyphenols were demonstrated to be hygroscopic and responsive to temperature (40°C) under an atmosphere of high relative humidity (75%) for 4 months, especially when the SDP was conditioned in permeable flasks. These findings demonstrate that heat and residual moisture content play an important role in the stability of the polyphenols and reinforce the relevance of conditioning SDP in humid tight packages under low temperatures. PMID:21370969

  10. Spray-dried powders enhance vaginal siRNA delivery by potentially modulating the mucus molecular sieve structure

    PubMed Central

    Wu, Na; Zhang, Xinxin; Li, Feifei; Zhang, Tao; Gan, Yong; Li, Juan

    2015-01-01

    Vaginal small interfering RNA (siRNA) delivery provides a promising strategy for the prevention and treatment of vaginal diseases. However, the densely cross-linked mucus layer on the vaginal wall severely restricts nanoparticle-mediated siRNA delivery to the vaginal epithelium. In order to overcome this barrier and enhance vaginal mucus penetration, we prepared spray-dried powders containing siRNA-loaded nanoparticles. Powders with Pluronic F127 (F127), hydroxypropyl methyl cellulose (HPMC), and mannitol as carriers were obtained using an ultrasound-assisted spray-drying technique. Highly dispersed dry powders with diameters of 5–15 μm were produced. These powders showed effective siRNA protection and sustained release. The mucus-penetrating properties of the powders differed depending on their compositions. They exhibited different potential of opening mesh size of molecular sieve in simulated vaginal mucus system. A powder formulation with 0.6% F127 and 0.1% HPMC produced the maximum increase in the pore size of the model gel used to simulate vaginal mucus by rapidly extracting water from the gel and interacting with the gel; the resulting modulation of the molecular sieve effect achieved a 17.8-fold improvement of siRNA delivery in vaginal tract and effective siRNA delivery to the epithelium. This study suggests that powder formulations with optimized compositions have the potential to alter the steric barrier posed by mucus and hold promise for effective vaginal siRNA delivery. PMID:26347257

  11. Cellular injuries of spray-dried Lactobacillus spp. isolated from kefir and their impact on probiotic properties.

    PubMed

    Golowczyc, Marina A; Silva, Joana; Teixeira, Paula; De Antoni, Graciela L; Abraham, Analía G

    2011-01-05

    The injuries caused by spray drying (SD) of three potential probiotic lactobacilli isolated from kefir grains and the impact on some probiotic properties, were evaluated. Results demonstrated that Lactobacillus plantarum 83114 and L. kefir 8321 showed a slight reduction of viability (0.11 and 0.29 log CFU/ml respectively) after SD process, and L. kefir 8348 was found to be more sensitive to the process with a reduction in viability of 0.70 log CFU/ml. Neither membrane damage, evaluated by increased sensitivity to NaCl, lysozyme, bile salt and penicillin G, nor changes in acidifying activity in MRS and milk by lactobacilli were detected after SD. L. plantarum 83114 and L. kefir 8321 after SD did not lose their capacity to adhere to intestinal cells. Nevertheless, L. kefir 8348 showed a significant loss of adhesion capacity after SD. In addition, rehydrated spray-dried L. kefir 8321 retained the ability to protect against Salmonella invasion of intestinal cells. This effect was observed when L. kefir is co-incubated with Salmonella before invasion assay. This work shows that the membrane integrity evaluated by indirect methods and some probiotic properties of lactobacilli isolated from kefir did not change significantly after SD, and these powders could be used in functional foods applications.

  12. Structural, functional and in vitro digestion characteristics of spray dried fish roe powder stabilised with gum arabic.

    PubMed

    Binsi, P K; Natasha, Nayak; Sarkar, P C; Muhamed Ashraf, P; George, Ninan; Ravishankar, C N

    2017-04-15

    Fish roes are considered as nutritionally valuable for their high content of essential fatty acids and amino acids. However, roe lipids undergo considerable extent of oxidation during processing and storage, imparting objectionable bitter taste and rancid flavour to roe products. Hence, the objective of the study was to reconstitute the roe mass and microencapsulate lipid fraction, so that small oil droplets are entrapped within a dry matrix of roe proteins during spray drying. Prior to spray drying, the emulsion was stabilised with gum arabic as it also act as a co-wall polymer. The microscopic images indicated presence of larger aggregates in unstabilised powder (RC) compared to well-separated particles in stabilised powder (RG). Incorporation of gum arabic retarded rancidity development during storage. In vitro digestive pattern of roe powder indicated higher amount of oil release in RG. These observations highlight the potential of converting the soft textured carp roe mass into stable fish roe powder with superior storage stability and functionality.

  13. Evaluation of folic acid release from spray dried powder particles of pectin-whey protein nano-capsules.

    PubMed

    Assadpour, Elham; Jafari, Seid-Mahdi; Maghsoudlou, Yahya

    2017-02-01

    Our main goal was to evaluate release kinetics of nano-encapsulated folic acid within a double W1/O/W2 emulsion. First, W1/O nano-emulsions loaded with folic acid were prepared and re-emulsified into an aqueous phase (W2) containing single whey protein concentrate (WPC) layer or double layer complex of WPC-pectin to form W1/O/W2 emulsions. Final double emulsions were spray dried and their microstructure was analyzed in terms of scanning electron microscopy (SEM), and Fourier Transform Infrared spectroscopy (FTIR). Also the release trends of folic acid were determined and fitted with experimental models of zero and first order, Higuchi, and Hixson-Crowell. It was revealed that folic acid nano-capsules made with Span as the surfactant had the lowest release rate in acidic conditions (pH=4) and highest release in the alkaline conditions (pH=11). The best model fitting for folic acid release data was observed for single layer WPC encapsulated powders with the highest R(2). Our FTIR data showed there was no chemical interaction between WPC and pectin in double layered capsules and based on SEM results, single WPC layered capsules resulted in smooth and uniform particles which by incorporating pectin, some wrinkles and shrinkage were found in the surface of spray dried powder particles.

  14. Spray-dried powders enhance vaginal siRNA delivery by potentially modulating the mucus molecular sieve structure.

    PubMed

    Wu, Na; Zhang, Xinxin; Li, Feifei; Zhang, Tao; Gan, Yong; Li, Juan

    2015-01-01

    Vaginal small interfering RNA (siRNA) delivery provides a promising strategy for the prevention and treatment of vaginal diseases. However, the densely cross-linked mucus layer on the vaginal wall severely restricts nanoparticle-mediated siRNA delivery to the vaginal epithelium. In order to overcome this barrier and enhance vaginal mucus penetration, we prepared spray-dried powders containing siRNA-loaded nanoparticles. Powders with Pluronic F127 (F127), hydroxypropyl methyl cellulose (HPMC), and mannitol as carriers were obtained using an ultrasound-assisted spray-drying technique. Highly dispersed dry powders with diameters of 5-15 μm were produced. These powders showed effective siRNA protection and sustained release. The mucus-penetrating properties of the powders differed depending on their compositions. They exhibited different potential of opening mesh size of molecular sieve in simulated vaginal mucus system. A powder formulation with 0.6% F127 and 0.1% HPMC produced the maximum increase in the pore size of the model gel used to simulate vaginal mucus by rapidly extracting water from the gel and interacting with the gel; the resulting modulation of the molecular sieve effect achieved a 17.8-fold improvement of siRNA delivery in vaginal tract and effective siRNA delivery to the epithelium. This study suggests that powder formulations with optimized compositions have the potential to alter the steric barrier posed by mucus and hold promise for effective vaginal siRNA delivery.

  15. Application of spray-drying and electrospraying/electospinning for poorly water-soluble drugs: a particle engineering approach.

    PubMed

    Bohr, Adam; Boetker, Johan P; Rades, Thomas; Rantanen, Jukka; Yang, Mingshi

    2014-01-01

    Solid dispersions have been widely studied as an attractive formulation strategy for the increasingly prevalent poorly water-soluble drug compounds, including herbal medicines, often leading to improvements in drug dissolution rate and bioavailability. However, several challenges are encountered with solid dispersions, for instance regarding their physical stability, and the full potential of these formulations has yet to be reached. Solid dispersions have mainly been used to produce immediate release systems using water-soluble polymers but an extended release system may provide equal or better performance due to enhancement in the pharmacokinetics and low variability in plasma concentration. Progress in processing technologies and particle engineering provides new opportunities to prepare particle-based solid dispersions with control of physical characteristics and tailored drug release kinetics. Spray-drying and electrospraying are both technologies that allow production and continuous manufacturing of particle-based amorphous solid dispersions in a single step process and electrospinning further allows the production of fiber based systems. This review presents the use of spray drying and electrospraying/electrospinning as techniques for preparing particle-based solid dispersions, describes the particle formation processes via numerical and experimental models and discusses particle engineering using these techniques. Examples are given on the applications of these techniques for preparing solid dispersions and the challenges associated with the techniques such as stability, preparation of final dosage form and scale-up are also discussed.

  16. A study of a new co-processed dry binder based on spray-dried lactose and microcrystalline cellulose.

    PubMed

    Mužíková, Jitka; Sináglová, Pavla

    2013-06-01

    The paper studies the compressibility and disintegration time of tablets from the co-processed dry binder DisintequikTM MCC in combination with two lubricants at two concentrations in dependence on compression force. It also compares identical parameters in the physical mixtures of the spray-dried lactose Flowlac® 100 and the microcrystalline cellulose Microcel® MC-102 in the ratios of 9 : 1, 8 : 2 and 7 : 3, again in combination with two lubricants of two concentrations at one compression force. The lubricants employed are magnesium stearate and poloxamer 407 in concentrations of 1% and 2%. Compressibility is evaluated by means of energy balance of compression and tensile strength of tablets. DisintequikTM MCC shows higher values of total energy of compression due to higher values of the energy accumulated by the tablet, higher plasticity, higher strength and a longer disintegration time of tablets than the physical mixture of spray-dried lactose and microcrystalline cellulose of a corresponding content. .

  17. Microencapsulation of Lactobacillus acidophilus NCIMB 701748 in matrices containing soluble fibre by spray drying: Technological characterization, storage stability and survival after in vitro digestion☆

    PubMed Central

    Yonekura, Lina; Sun, Han; Soukoulis, Christos; Fisk, Ian

    2014-01-01

    We evaluated sodium alginate, chitosan and hydroxypropyl methylcellulose (HPMC) as co-encapsulants for spray dried Lactobacillus acidophilus NCIMB 701748 by assessing their impact on cell viability and physicochemical properties of the dried powders, viability over 35 days of storage at 25 °C and survival after simulated digestion. Fibres were added to a control carrier medium containing whey protein concentrate, d-glucose and maltodextrin. Sodium alginate and HPMC did not affect cell viability but chitosan reduced viable counts in spray dried powders, as compared to the control. Although chitosan caused large losses of viability during spray-drying, these losses were counteracted by the excellent storage stability compared to control, sodium alginate and HPMC, and the overall effect became positive after the 35-day storage. Chitosan also improved survival rates in simulated GI conditions, however no single fibre could improve L. acidophilus NCIMB 701748 viability in all steps from production through storage and digestion. PMID:24748900

  18. Preparation of ultra-fine powders from polysaccharide-coated solid lipid nanoparticles and nanostructured lipid carriers by innovative nano spray drying technology.

    PubMed

    Wang, Taoran; Hu, Qiaobin; Zhou, Mingyong; Xue, Jingyi; Luo, Yangchao

    2016-09-10

    In this study, five polysaccharides were applied as natural polymeric coating materials to prepare solid lipid nanoparticles (SLN) and nanostructure lipid carriers (NLC), and then the obtained lipid colloidal particles were transformed to solid powders by the innovative nano spray drying technology. The feasibility and suitability of this new technology to generate ultra-fine lipid powder particles were evaluated and the formulation was optimized. The spray dried SLN powder exhibited the aggregated and irregular shape and dimension, but small, uniform, well-separated spherical powder particles of was obtained from NLC. The optimal formulation of NLC was prepared by a 20-30% oleic acid content with carrageenan or pectin as coating material. Therefore, nano spray drying technology has a potential application to produce uniform, spherical, and sub-microscale lipid powder particles when the formulation of lipid delivery system is appropriately designed.

  19. Fortification of dark chocolate with spray dried black mulberry (Morus nigra) waste extract encapsulated in chitosan-coated liposomes and bioaccessability studies.

    PubMed

    Gültekin-Özgüven, Mine; Karadağ, Ayşe; Duman, Şeyma; Özkal, Burak; Özçelik, Beraat

    2016-06-15

    Fine-disperse anionic liposomes containing black mulberry (Morus nigra) extract (BME) were prepared by high pressure homogenization at 25,000 psi. Primary liposomes were coated with cationic chitosan (0.4, w/v%) using the layer-by-layer depositing method and mixed with maltodextrin (MD) (20, w/v%) prior to spray drying. After that, spray dried liposomal powders containing BME were added to chocolates with alkalization degrees (pH 4.5, 6, 7.5) at conching temperatures of 40 °C, 60 °C, and 80 °C. The results showed that, compared to spray dried extract, chitosan coated liposomal powders provided better protection of anthocyanin content in both increased temperature and pH. In addition, encapsulation in liposomes enhanced in vitro bioaccessability of anthocyanins. Chocolate was fortified with encapsulated anthocyanins maximum 76.8% depending on conching temperature and pH.

  20. Microencapsulation of Lactobacillus acidophilus NCIMB 701748 in matrices containing soluble fibre by spray drying: Technological characterization, storage stability and survival after in vitro digestion.

    PubMed

    Yonekura, Lina; Sun, Han; Soukoulis, Christos; Fisk, Ian

    2014-01-01

    We evaluated sodium alginate, chitosan and hydroxypropyl methylcellulose (HPMC) as co-encapsulants for spray dried Lactobacillus acidophilus NCIMB 701748 by assessing their impact on cell viability and physicochemical properties of the dried powders, viability over 35 days of storage at 25 °C and survival after simulated digestion. Fibres were added to a control carrier medium containing whey protein concentrate, d-glucose and maltodextrin. Sodium alginate and HPMC did not affect cell viability but chitosan reduced viable counts in spray dried powders, as compared to the control. Although chitosan caused large losses of viability during spray-drying, these losses were counteracted by the excellent storage stability compared to control, sodium alginate and HPMC, and the overall effect became positive after the 35-day storage. Chitosan also improved survival rates in simulated GI conditions, however no single fibre could improve L. acidophilus NCIMB 701748 viability in all steps from production through storage and digestion.

  1. Kilogram-scale production of SnO(2) yolk-shell powders by a spray-drying process using dextrin as carbon source and drying additive.

    PubMed

    Choi, Seung Ho; Kang, Yun Chan

    2014-05-05

    A simple and general method for the large-scale production of yolk-shell powders with various compositions by a spray-drying process is reported. Metal salt/dextrin composite powders with a spherical and dense structure were obtained by spray drying and transformed into yolk-shell powders by simple combustion in air. Dextrin plays a key role in the preparation of precursor powders for fabricating yolk-shell powders by spray drying. Droplets containing metal salts and dextrin show good drying characteristics even in a severe environment of high humidity. Sucrose, glucose, and polyvinylpyrrolidone are widely used as carbon sources in the preparation of metal oxide/carbon composite powders; however, they are not appropriate for large-scale spray-drying processes because of their caramelization properties and adherence to the surface of the spray dryer. SnO2 yolk-shell powders were studied as the first target material in the spray-drying process. Combustion of tin oxalate/dextrin composite powders at 600 °C in air produced single-shelled SnO2 yolk-shell powders with the configuration SnO2 @void@SnO2 . The SnO2 yolk-shell powders prepared by the simple spray-drying process showed superior electrochemical properties, even at high current densities. The discharge capacities of the SnO2 yolk-shell powders at a current density of 2000 mA g(-1) were 645 and 570 mA h g(-1) for the second and 100th cycles, respectively; the corresponding capacity retention measured for the second cycle was 88 %.

  2. Effects of ionic and nonionic surfactants on milk shell wettability during co-spray-drying of whole milk particles.

    PubMed

    Lallbeeharry, P; Tian, Y; Fu, N; Wu, W D; Woo, M W; Selomulya, C; Chen, X D

    2014-09-01

    Mixing surfactants with whole milk feed before spray drying could be a commercially favorable approach to produce instant whole milk powders in a single step. Pure whole milk powders obtained directly from spray drying often have a high surface fat coverage (up to 98%), rendering them less stable during storage and less wettable upon reconstitution. Dairy industries often coat these powders with lecithin, a food-grade surfactant, in a secondary fluidized-bed drying stage to produce instant powders. This study investigated the changes in wetting behavior on the surface of a whole milk particle caused by the addition of surfactants before drying. Fresh whole milk was mixed with 0.1% (wt/wt) Tween 80 or 1% (wt/wt) lecithin (total solids), and the wetting behavior of the shell formed by each sample was captured using a single-droplet drying device at intermediate drying stages as the shell was forming. The addition of surfactants improved shell wettability from the beginning of shell formation, producing more wettable milk particles after drying. The increase in surfactant loading by 10 times reduced the wetting time from around 30s to <5s. At the same loading of 1% (wt/wt; total solids), milk particles with Tween 80 were much more wettable than those with lecithin (<5s compared with >30s). We proposed that Tween 80 could adsorb at the oil-water interface of fat globules, making the surface fat more wettable, whereas lecithin tends to combine with milk proteins to form a complex, which then competes for the air-water surface with fat globules. Spray-drying experiments confirmed the greatly improved wettability of whole milk powders by the addition of either 0.1% (wt/wt) Tween 80 or 1% (wt/wt) lecithin; wetting time was reduced from 35±4s to <15s. To the best of our knowledge, this is the first time that a dynamic droplet drying system has been used to elucidate the complex interactions between ionic or nonionic surfactants and milk components (both proteins and fat

  3. Chemical composition and biological value of spray dried porcine blood by-products and bone protein hydrolysate for young chickens.

    PubMed

    Jamroz, D; Wiliczkiewicz, A; Orda, J; Skorupińska, J; Słupczyńska, M; Kuryszko, J

    2011-10-01

    The chemical composition of spray dried porcine blood by-products is characterised by wide variation in crude protein contents. In spray dried porcine blood plasma (SDBP) it varied between 670-780 g/kg, in spray dried blood cells (SDBC) between 830-930 g/kg, and in bone protein hydrolysate (BPH) in a range of 740-780 g/kg. Compared with fish meal, these feeds are poor in Met and Lys. Moreover, in BPH deep deficits of Met, Cys, Thr and other amino acids were found. The experiment comprised 7 dietary treatments: SDBP, SDBC, and BPH, each at an inclusion rate of 20 or 40 g/kg diet, plus a control. The addition of 20 or 40 g/kg of the analysed meals into feeds for very young chickens (1-28 d post hatch) significantly decreased the body weight (BW) of birds. Only the treatments with 40 g/kg of SDBP and SDBC showed no significant difference in BW as compared with the control. There were no significant differences between treatments and type of meal for feed intake, haematocrit and haemoglobin concentrations in blood. Addition of bone protein and blood cell meals to feed decreased the IgG concentration in blood and caused shortening of the femur and tibia bones. However, changes in the mineral composition of bones were not significantly affected by the type of meal used. The blood by-products, which are rich in microelements, improved retention of Ca and Cu only. In comparison to control chickens, significantly better accretion of these minerals was found in treatments containing 20 g/kg of SDBP or 40 g/kg of SDBC. Great variability in apparent ileal amino acid digestibility in chickens was determined. In this respect, some significant differences related to the type of meal fed were confirmed for Asp, Pro, Val, Tyr and His. In general, the apparent ileal digestibility of amino acids was about 2-3 percentage units better in chickens fed on diets containing the animal by products than in control birds.

  4. Effect of drying parameters on physiochemical and sensory properties of fruit powders processed by PGSS-, Vacuum- and Spray-drying.

    PubMed

    Feguš, Urban; Žigon, Uroš; Petermann, Marcus; Knez, Željko

    2015-01-01

    Aim of this experimental work was to investigate the possibility of producing fruit powders without employing drying aid and to investigate the effect of drying temperatures on the final powder characteristics. Raw fruit materials (banana puree, strawberry puree and blueberry concentrate) were processed using three different drying techniques each operating at a different temperature conditions: vacuum-drying (-27-17 °C), Spray-drying (130-160 °C) and PGSS-drying (112-152 °C). Moisture content, total colour difference, antioxidant activity and sensory characteristics of the processed fruit powders were analysed. The results obtained from the experimental work indicate that investigated fruit powders without or with minimal addition of maltodextrin can be produced. Additionally, it was observed that an increase in process temperature results in a higher loss of colour, antioxidant activity and intensity of the flavour profile.

  5. Optimization of Microencapsulation of Fish Oil with Gum Arabic/Casein/Beta-Cyclodextrin Mixtures by Spray Drying.

    PubMed

    Li, Junjie; Xiong, Shanbai; Wang, Fang; Regenstein, Joe M; Liu, Ru

    2015-07-01

    Fish oil was encapsulated with gum arabic/casein/beta-cyclodextrin mixtures using spray drying. The processing parameters (solids concentration of the barrier solutions, ratio of oil to barrier materials, emulsifying temperature, and air inlet temperature) were optimized based on emulsion viscosity, emulsion stability, encapsulation efficiency, and yield. A suitable viscosity and high emulsion stability could increase encapsulation efficiency and yield. Encapsulation efficiency and yield were significantly affected by all the 4 parameters. Based on the results of orthogonal experiments, encapsulation efficiency and yield reached a maximum of 79.6% and 55.6%, respectively, at the optimal condition: solids concentration of 35%, ratios of oil to barrier materials of 3:7, emulsifying temperature of 55 °C, and air inlet temperature of 220 °C. Scanning electron microscopy analysis showed that fish oil microcapsules were nearly spherical with a smooth surface with droplet size ranging from 1 to 10 μm.

  6. Flavor retention of peppermint (Mentha piperita L.) essential oil spray-dried in modified starches during encapsulation and storage.

    PubMed

    Baranauskiene, Renata; Bylaite, Egle; Zukauskaite, Jurate; Venskutonis, Rimantas P

    2007-04-18

    The effect of different commercial modified food starch carrier materials on the flavor retention of the essential oil (EO) of peppermint (Mentha piperita L.) during spray drying and storage was evaluated. The obtained results revealed that the emulsification and encapsulation efficiencies of peppermint EO were higher for all n-octenyl succinic anhydride (OSAN)-modified starches as compared to those of hydrolyzed starches (dextrins). The compositions of pure, emulsified, and encapsulated peppermint EOs in different matrices were quite similar; however, some changes in the percentages of some individual compounds were observed. Larger differences in the compositions of surface oils from various encapsulation products were obtained. Flavor components were released at different rates by each of the encapsulated products. The aroma binding capacity of different modified starch matrices to lock EO droplets depends on the water activity, and the leakage of aromas from encapsulated powder products during storage increased with increasing water activity.

  7. Submicron polymeric particles prepared by vibrational spray-drying: Semisolid formulation and skin penetration/permeation studies.

    PubMed

    Beber, T C; Andrade, D F; Kann, B; Fontana, M C; Coradini, K; Windbergs, M; Beck, R C R

    2014-11-01

    Topical glucocorticoids (TG) such as dexamethasone (DEX) have been used for decades for the treatment of skin diseases. However, TG present well-documented side effects and their delivery to the skin is often insufficient. Therefore, many efforts have been undergone to improve the amount of drug delivered to the skin and to reduce side effects at the same time. In this work, the feasibility of DEX-submicron polymeric particles (SP) prepared by vibrational spray-drying as an approach to overcome the challenges associated with the topical administration of this drug class was evaluated. DEX was homogeneously dispersed in the SP matrix, according to confocal Raman microscopy analysis. Drug-loaded SP were incorporated into the oil phase of oil-in-water emulsions (creams). The formulation containing polymeric submicron particles (C-SP) showed controlled drug release kinetics and a significant drug accumulation in skin compared to formulations containing non-polymeric particles or free drug. DEX accumulation in the stratum corneum was evaluated by tape stripping and a depot effect over time was observed for C-SP, while the formulation containing the free drug showed a decrease over time. Similarly, C-SP presented higher drug retention in epidermis and dermis in skin penetration studies performed on pig skin in Franz diffusion cells, while drug permeation into the receptor compartment was negligible. It was demonstrated, for the first time, the advantageous application of submicron polymeric particles obtained by vibrational spray-drying in semisolid formulations for cutaneous administration to overcome challenges related to the therapy with TG such as DEX.

  8. Preparation and Characterization of the Solid Spherical HMX/F2602 by the Suspension Spray-Drying Method

    NASA Astrophysics Data System (ADS)

    Ji, Wei; Li, Xiaodong; Wang, Jingyu; Ye, Baoyun; Wang, Cailing

    2016-10-01

    Solid spherical octahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine/fluororubber2602 (HMX/F2602) was prepared by the suspension spray-drying method as follows: firstly, thinning octahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine (HMX) was obtained by a solvent-anti-solvent method. Secondly, thinning HMX suspended in ethyl acetate solvent in a solution of a binder-F2602-was made into a suspension. Finally, the samples were prepared by spray drying. The samples were characterized by scanning electron microscopy (SEM), X-ray photoelectron spectrometry (XPS), X-ray diffraction (XRD), and Fourier transform infrared (FTIR), and its thermal stability as well as mechanical and spark sensitivities were measured. The results of SEM showed that the grain of HMX/F2602 was solid spherical and the particle distribution was homogeneous. The results of XPS indicated that F2602 can be successfully coated on the surface of HMX crystals. Compared to raw HMX, th characteristic drop height was increased from 19.60 to 40.37 cm, an increase of 79.10%. The friction sensitivities of HMX reduced from 100 to 28% and the spark sensitivity of HMX/F2602 increased. The critical explosion temperatures of raw HMX and HMX/F2602 were 275.43 and 274.30°C, respectively. The amount of gas evolution of raw HMX and HMX/F2602 was 0.15 and 0.12 ml.(5 g)-1, respectively. The results of DSC and vacuum stability tests (VSTs) indicate that the thermal stability of HMX/F2602 was equal to that of raw HMX and HMX and F2602 had good compatibility.

  9. Influence of spray drying and dispersing agent on surface and dissolution properties of griseofulvin micro and nanocrystals.

    PubMed

    Shah, Dhaval A; Patel, Manan; Murdande, Sharad B; Dave, Rutesh H

    2016-11-01

    The purpose for the current research is to compare and evaluate physiochemical properties of spray-dried (SD) microcrystals (MCs), nanocrystals (NCs), and nanocrystals with a dispersion agent (NCm) from a poorly soluble compound. The characterization was carried out by performing size and surface analysis, interfacial tension (at particle moisture interface), and in-vitro drug dissolution rate experiments. Nanosuspensions were prepared by media milling and were spray-dried. The SD powders that were obtained were characterized morphologically using scanning electron microscopy (SEM), polarized light microscopy (PLM), and Flowchem. Solid-state characterization was performed using X-ray powder diffraction (XRPD), Fourier transfer infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC) for the identification of the crystalline nature of all the SD powders. The powders were characterized for their redispersion tendency in the water and in pH 1.2. Significant differences in redispersion were noted for both the NCs in both dissolution media. The interfacial tension for particle moisture interface was determined by applying the BET (Braunauer-Emmett-Teller) equation to the vapor sorption data. No significant reduction in the interfacial tension was observed between MCs and NCs; however, a significant reduction in the interfacial tension was observed for NCm at both 25 °C and 35 °C temperatures. The difference in interfacial tension and redispersion behavior can be attributed to a difference in the wetting tendency for all the SD powders. The dissolution studies were carried out under sink and under non-sink conditions. The non-sink dissolution approach was found suitable for quantification of the dissolution rate enhancement, and also for providing the rank order to the SD formulations.

  10. Aerodynamic properties, solubility and in vitro antibacterial efficacy of dry powders prepared by spray drying: Clarithromycin versus its hydrochloride salt.

    PubMed

    Manniello, Michele Dario; Del Gaudio, Pasquale; Porta, Amalia; Aquino, Rita Patrizia; Russo, Paola

    2016-07-01

    Antibiotic therapy for a direct administration to the lung in cystic fibrosis patients has to provide suitable availability, possibly in the lower respiratory tract, characterized by the presence of thick secretions. One of the crucial steps in the therapeutic management of the respiratory disease could be the drug solubilization directly in this site of action. The aim of the study was to prepare respirable powders of clarithromycin, while improving drug aqueous solubility. With this aim, several batches of micronized particles were prepared by spray drying different feed solutions, varying the solvent composition (water/isopropyl alcohol ratio), the drug concentration and pH of the liquid feeds. Particle size distribution of raw materials and engineered particles was determined using a light-scattering laser granulometer while particle morphology was assessed by scanning electron microscopy. The in vitro deposition of the micronized clarithromycin powders was evaluated by means of a Single-Stage Glass Impinger using the RS01 model7 by Plastiape® as device for the aerosolization. Solubility measurements of raw and spray-dried (SD) drug were carried out at 37°C in phosphate buffer (0.05M, pH 6.8). Results indicate that morphology and aerodynamic properties of SD particles were strongly influenced by organic solvent concentration and pH of the liquid feeds processed, both modifying drug solubility. Spherical particles and crystals were obtained at higher pH and lower organic solvent content, while wrinkled particles with very interesting aerodynamic properties and higher drug solubility were obtained at lower pH values. Thanks to a fine tuning of the process parameters and liquid feed composition, we produced SD powders with good aerodynamic properties, without using any excipients. Furthermore, SD powders of clarithromycin hydrochloric salt showed higher activity against Pseudomonas aeruginosa growth, compared to clarithromycin raw material.

  11. Inhibition of the spontaneous polymorphic transition of pyrazinamide γ form at room temperature by co-spray drying with 1,3-dimethylurea.

    PubMed

    Baaklini, G; Dupray, V; Coquerel, G

    2015-02-01

    The present study focuses on the ability of excipients to induce the crystallization of a specific polymorphic form of pyrazinamide (PZA) and more interestingly, to block the irreversible solid-solid transition of the metastable forms of the PZA to the stable form at room temperature. We outline an experimental protocol for the production of a structurally pure γ form of PZA by means of spray drying. Without any particular treatment, phase transition to δ form was detected after 14 days of storage under ambient conditions. In order to prevent this irreversible phase transition, different excipients were co-spray dried with PZA. By co-spray drying 5% in mass of 1,3-dimethylurea (DMU) with PZA, we noticed its ability in preventing phase transitions and thus to maintain PZA under its γ form up to 12 months of storage at room temperature. Raman spectroscopy evidenced how DMU crystals surround particles of γ PZA which suggest that DMU might interact with the surface of PZA particles, thus blocking the phase transition. On the other hand, the co-spray drying of PZA with the polymerpolyvinylpyrrolidone (PVP) resulted in the crystallization of δ form of PZA. The physical mixture was intact over 12 months of storage at room temperature.

  12. The influence of lysozyme on mannitol polymorphism in freeze-dried and spray-dried formulations depends on the selection of the drying process.

    PubMed

    Grohganz, Holger; Lee, Yan-Ying; Rantanen, Jukka; Yang, Mingshi

    2013-04-15

    Freeze-drying and spray-drying are often applied drying techniques for biopharmaceutical formulations. The formation of different solid forms upon drying is often dependent on the complex interplay between excipient selection and process parameters. The purpose of this study was to investigate the influence of the chosen drying method on the solid state form. Mannitol-lysozyme solutions of 20mg/mL, with the amount of lysozyme varying between 2.5% and 50% (w/w) of total solid content, were freeze-dried and spray-dried, respectively. The resulting solid state of mannitol was analysed by near-infrared spectroscopy in combination with multivariate analysis and further, results were verified with X-ray powder diffraction. It was seen that the prevalence of the mannitol polymorphic form shifted from β-mannitol to δ-mannitol with increasing protein concentration in freeze-dried formulations. In spray-dried formulations an increase in protein concentration resulted in a shift from β-mannitol to α-mannitol. An increase in final drying temperature of the freeze-drying process towards the temperature of the spray-drying process did not lead to significant changes. It can thus be concluded that it is the drying process in itself, rather than the temperature, that leads to the observed solid state changes.

  13. Method of creating starch-like ultra-fine rice flour and effect of spray drying on formation of free fatty acid.

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Rice flour from long, medium, and short grain cultivars were processed by passing a 32% rice flour slurry through a microfluidizer at 100 MPa, and spray dryer at three different outlet temperatures, OT (50°C, 80°C, and 115°C). Spray drying conditions were controlled by the flow-rate of the slurry ...

  14. Application of a novel 3-fluid nozzle spray drying process for the microencapsulation of therapeutic agents using incompatible drug-polymer solutions.

    PubMed

    Sunderland, Tara; Kelly, John G; Ramtoola, Zebunnissa

    2015-04-01

    The aim of this study was to evaluate a novel 3-fluid concentric nozzle (3-N) spray drying process for the microencapsulation of omeprazole sodium (OME) using Eudragit L100 (EL100). Feed solutions containing OME and/or EL100 in ethanol were assessed visually for OME stability. Addition of OME solution to EL100 solution resulted in precipitation of OME followed by degradation of OME reflected by a colour change from colourless to purple and brown. This was related to the low pH of 2.8 of the EL100 solution at which OME is unstable. Precipitation and progressive discoloration of the 2-fluid nozzle (2-N) feed solution was observed over the spray drying time course. In contrast, 3-N solutions of EL100 or OME in ethanol were stable over the spray drying period. Microparticles prepared using either nozzle showed similar characteristics and outer morphology however the internal morphology was different. DSC showed a homogenous matrix of drug and polymer for 2-N microparticles while 3-N microparticles had defined drug and polymer regions distributed as core and coat. The results of this study demonstrate that the novel 3-N spray drying process can allow the microencapsulation of a drug using an incompatible polymer and maintain the drug and polymer in separate regions of the microparticles.

  15. Comparative studies on exenatide-loaded poly (D,L-lactic-co-glycolic acid) microparticles prepared by a novel ultra-fine particle processing system and spray drying.

    PubMed

    Zhu, Chune; Huang, Ying; Zhang, Xiaoying; Mei, Liling; Pan, Xin; Li, Ge; Wu, Chuanbin

    2015-08-01

    The purpose of this study was to compare the properties of exenatide-loaded poly (D,L-lactic-co-glycolic acid) microparticles (Ex-PLGA-MPs) prepared by a novel ultra-fine particle processing system (UPPS) and spray drying. UPPS is a proprietary technology developed by our group based on the disk rotation principle. Characteristics of the MPs including morphology, particle size distribution, drug content, encapsulation efficiency and in vitro release were comparatively studied. Cytotoxicity of the MPs was examined on A549 cells and the pharmacodynamics was investigated in vivo in type 2 diabetes Sprague-Dawley (SD) rats. Ex-PLGA-MPs prepared by UPPS showed larger particle size, denser surface, greater encapsulation efficiency, less initial burst release, and stable sustained release for more than one month in vitro as compared with the spray drying MPs. Meanwhile, the UPPS MPs effectively controlled the body growth rate and blood glucose in diabetes rats for at least three weeks after a single injection, while the spray drying MPs showed effective control period of about two weeks. UPPS technology was demonstrated to manufacture Ex-PLGA-MPs as a potential sustained release protein/polypeptide delivery system, which is an alternative method for the most commonly used spray drying. This comparative research provides a new guidance for microparticle preparation technology.

  16. An advanced protocol-driven transition from parenteral prostanoids to inhaled trepostinil in pulmonary arterial hypertension

    PubMed Central

    Agarwal, Manyoo; Rischard, Franz; De Marco, Teresa

    2016-01-01

    Abstract Patients with pulmonary arterial hypertension (PAH) often require parenteral prostanoids to improve symptoms and signs of PAH. Complications of parenteral prostanoids—such as catheter-related infections and intolerable adverse effects—may develop, prompting transition to inhaled prostanoids. We report a prospective, protocol-driven transition from parenteral prostanoids to inhaled prostanoids with monitoring of exercise gas exchange and acute hemodynamics. Three PAH centers recruited patients transitioning from parenteral prostanoids to inhaled trepostinil. Rigid inclusion criteria were used, including parenteral prostanoid dose < 30 ng/kg/min, New York Heart Association functional class (FC) < 3, and pulmonary vascular resistance (PVR) < 6 Wood units. Of the 9 patients meeting initial inclusion criteria, 3 were excluded. In the remaining patients, the parenteral prostanoid was reduced and the inhaled prostanoid was increased over 24–36 hours with continuous hemodynamic monitoring. Exercise capacity and FC were measured at baseline and weeks 1, 4, and 12. All patients were successfully weaned from parenteral prostanoids. An acute PVR decrease was seen with most inhaled prostanoid doses, but PVR varied throughout the transition. Patients tolerated inhaled prostanoids for 9–12 breaths 4 times a day with no treatment-limiting adverse events. At week 12, FC was unchanged, and all patients continued to receive inhaled prostanoids without serious adverse events or additional PAH therapy. In 5 of 6 patients, 6-minute walk distance and peak V˙O2 were within 10% of baseline. Using a strict transition protocol and rigid patient selection criteria, the parenteral prostanoid to inhaled prostanoid transition appeared safe and well tolerated and did not result in clinical deterioration over 12 weeks. Hemodynamic variability noted acutely during transition in our study did not adversely affect successful transition. (Trial registration: Clinical

  17. Development and Characterization of Sodium Hyaluronate Microparticle-Based Sustained Release Formulation of Recombinant Human Growth Hormone Prepared by Spray-Drying.

    PubMed

    Kim, Sun J; Kim, Chan W

    2016-02-01

    The purpose of this study was to develop and characterize a sodium hyaluronate microparticle-based sustained release formulation of recombinant human growth hormone (SR-rhGH) prepared by spray-drying. Compared to freeze-drying, spray-dried SR-rhGH showed not only prolonged release profiles but also better particle property and injectability. The results of size-exclusion high-performance liquid chromatography showed that no aggregate was detected, and dimer was just about 2% and also did not increase with increase of inlet temperature up to 150 °C. Meanwhile, the results of reversed-phase high-performance liquid chromatography revealed that related proteins increased slightly from 4.6% at 100 °C to 6.3% at 150 °C. Thermal mapping test proved that product temperature did not become high to cause protein degradation during spray-drying because thermal energy was used for the evaporation of surface moisture of droplets. The structural characterization by peptide mapping, sodium dodecyl sulfate-polyacrylamide gel electrophoresis, and circular dichroism revealed that the primary, secondary, and tertiary structures of rhGH in SR-rhGH were highly comparable to those of reference somatropin materials. The biological characterization by rat weight gain and cell proliferation assays provided that bioactivity of SR-rhGH was equivalent to that of native hGH. These data establish that spray-dried SR-rhGH is highly stable by preserving intact rhGH and hyaluronate microparticle-based formulation by spray-drying can be an alternative delivery system for proteins.

  18. Spray-dried solid dispersions containing ferulic acid: comparative analysis of three carriers, in vitro dissolution, antioxidant potential and in vivo anti-platelet effect.

    PubMed

    Nadal, Jessica Mendes; Gomes, Mona Lisa Simionatto; Borsato, Débora Maria; Almeida, Martinha Antunes; Barboza, Fernanda Malaquias; Zawadzki, Sônia Faria; Farago, Paulo Vitor; Zanin, Sandra Maria Warumby

    2016-11-01

    This article aimed to improve the relative solubility and dissolution rate of ferulic acid (FA) by the use of spray-dried solid dispersions (SDs) in order to ensure its in vitro antioxidant potential and to enhance its in vivo anti-platelet effect. These SDs were prepared by spray-drying at 10 and 20% of drug concentration using polyvinylpyrrolidone K30 (PVP-K30), polyethylene glycol 6000 (PEG 6000) and poloxamer-188 (PLX-188) as carriers. SDs and physical mixtures (PM) were characterized by SEM, XRPD, FTIR spectroscopy and TGA analysis. Spray-dried SDs containing FA were successfully obtained. Relative solubility of FA was improved with increasing carrier concentration. PVP-K30 and PEG 6000 formulations showed suitable drug content values close to 100%, whereas PLX-188 presented mean values between 70 and 90%. Agglomerates were observed depending on the carrier used. XRPD patterns and thermograms indicated that spray-drying led to drug amorphization and provided appropriate thermal stability, respectively. FTIR spectra demonstrated no remarkable interaction between carrier and drug for PEG 6000 and PLX-188 SDs. PVP-K30 formulations had changes in FTIR spectra, which denoted intermolecular O-H•••O = C bonds. Spray-dried SDs played an important role in enhancing dissolution rate of FA when compared to pure drug. The free radical-scavenging assay confirmed that the antioxidant activity of PEG 6000 10% SDs was kept. This formulation also provided a statistically increased in vivo anti-platelet effect compared to pure drug. In summary, these formulations enhanced relative solubility and dissolution rate of FA and chosen formulation demonstrated suitable in vitro antioxidant activity and improved in vivo anti-platelet effect.

  19. Inhaled sodium cromoglycate to treat cough in advanced lung cancer patients.

    PubMed

    Moroni, M; Porta, C; Gualtieri, G; Nastasi, G; Tinelli, C

    1996-07-01

    C-fibres probably represent the common final pathway in both ACE inhibitors and neoplastic cough. A recent report demonstrated that inhaled sodium cromoglycate is an effective treatment for ACE inhibitors' cough; this effect might be due to the suppression of afferent unmyelinated C-fibres. We tested the hypothesis that inhaled sodium cromoglycate might also be effective in lung cancer patients who presented with irritative neoplastic cough. Twenty non-small-cell lung cancer (NSCLC) patients complaining of cough resistant to conventional treatment were randomised to receive, in a double-blind trial, either inhaled sodium cromoglycate or placebo. Patients recorded cough severity daily, before and during treatment, on a 0 to 4 scale. The efficacy of treatment was tested with the Mann-Whitney U-test for non-parametric measures, comparing the intergroup differences in the measures of summary of symptom scores calculated in each patient before and after treatment. We report that inhaled sodium cromoglycate can reduce cough, also in NSCLC patients and that such reduction, observed in all patients treated, is statistically significant (P < 0.001). Inhaled sodium cromoglycate appears to be a cost-effective and safe treatment for lung cancer-related cough.

  20. Inhaled sodium cromoglycate to treat cough in advanced lung cancer patients.

    PubMed Central

    Moroni, M.; Porta, C.; Gualtieri, G.; Nastasi, G.; Tinelli, C.

    1996-01-01

    C-fibres probably represent the common final pathway in both ACE inhibitors and neoplastic cough. A recent report demonstrated that inhaled sodium cromoglycate is an effective treatment for ACE inhibitors' cough; this effect might be due to the suppression of afferent unmyelinated C-fibres. We tested the hypothesis that inhaled sodium cromoglycate might also be effective in lung cancer patients who presented with irritative neoplastic cough. Twenty non-small-cell lung cancer (NSCLC) patients complaining of cough resistant to conventional treatment were randomised to receive, in a double-blind trial, either inhaled sodium cromoglycate or placebo. Patients recorded cough severity daily, before and during treatment, on a 0 to 4 scale. The efficacy of treatment was tested with the Mann-Whitney U-test for non-parametric measures, comparing the intergroup differences in the measures of summary of symptom scores calculated in each patient before and after treatment. We report that inhaled sodium cromoglycate can reduce cough, also in NSCLC patients and that such reduction, observed in all patients treated, is statistically significant (P < 0.001). Inhaled sodium cromoglycate appears to be a cost-effective and safe treatment for lung cancer-related cough. PMID:8688342

  1. Dry Powder Inhalers: A Focus on Advancements in Novel Drug Delivery Systems

    PubMed Central

    2016-01-01

    Administration of drug molecules by inhalation route for treatment of respiratory diseases has the ability to deliver drugs, hormones, nucleic acids, steroids, proteins, and peptides, particularly to the site of action, improving the efficacy of the treatment and consequently lessening adverse effects of the treatment. Numerous inhalation delivery systems have been developed and studied to treat respiratory diseases such as asthma, COPD, and other pulmonary infections. The progress of disciplines such as biomaterials science, nanotechnology, particle engineering, molecular biology, and cell biology permits further improvement of the treatment capability. The present review analyzes modern therapeutic approaches of inhaled drugs with special emphasis on novel drug delivery system for treatment of various respiratory diseases. PMID:27867663

  2. Inhaled Steroids

    MedlinePlus

    ... Medications Long-Term Control Medications Inhaled Steroids Inhaled Steroids Make an Appointment Ask a Question Refer Patient ... more about steroids? What are some common inhaled steroids? Common inhaled steroids include: Asmanex ® (mometasone) Alvesco ® (ciclesonide) ...

  3. Design and formulation of nano-sized spray dried efavirenz-part I: influence of formulation parameters

    NASA Astrophysics Data System (ADS)

    Katata, Lebogang; Tshweu, Lesego; Naidoo, Saloshnee; Kalombo, Lonji; Swai, Hulda

    2012-11-01

    Efavirenz (EFV) is one of the first-line antiretroviral drugs recommended by the World Health Organisation for treating HIV. It is a hydrophobic drug that suffers from low aqueous solubility (4 μg/mL), which leads to a limited oral absorption and low bioavailability. In order to improve its oral bioavailability, nano-sized polymeric delivery systems are suggested. Spray dried polycaprolactone-efavirenz (PCL-EFV) nanoparticles were prepared by the double emulsion method. The Taguchi method, a statistical design with an L8 orthogonal array, was implemented to optimise the formulation parameters of PCL-EFV nanoparticles. The types of sugar (lactose or trehalose), surfactant concentration and solvent (dichloromethane and ethyl acetate) were chosen as significant parameters affecting the particle size and polydispersity index (PDI). Small nanoparticles with an average particle size of less than 254 ± 0.95 nm in the case of ethyl acetate as organic solvent were obtained as compared to more than 360 ± 19.96 nm for dichloromethane. In this study, the type of solvent and sugar were the most influencing parameters of the particle size and PDI. Taguchi method proved to be a quick, valuable tool in optimising the particle size and PDI of PCL-EFV nanoparticles. The optimised experimental values for the nanoparticle size and PDI were 217 ± 2.48 nm and 0.093 ± 0.02.

  4. Electrochemical properties of MnS-C and MnO-C composite powders prepared via spray drying process

    NASA Astrophysics Data System (ADS)

    Jeon, Kyung Min; Cho, Jung Sang; Kang, Yun Chan

    2015-11-01

    Spherical micron-sized MnS-C and MnO-C composite powders are successfully prepared by post-treating the spray-dried precursor powders. Dextrin, which is used as the carbon source material, plays a key role in the preparation of the composite powders with regular morphologies; the bare MnS and MnO powders prepared from the spray solution without dextrin have irregular morphologies. The MnS-C composite powders prepared from the spray solution containing 17 g L-1 of dextrin have mixed crystal structures of α- and γ-MnS phases. These powders exhibit superior electrochemical properties compared with those of their MnS and MnO-C counterparts. For example, at a current density of 0.5 A g-1, the MnO-C powders have a 100th-cycle discharge capacity of 321 mA h g-1; the corresponding discharge capacities of the MnS powders prepared from spray solutions containing 0, 17, and 50 g L-1 of dextrin are 501, 786, and 636 mA h g-1, respectively.

  5. Characterization of naproxen-loaded solid SMEDDSs prepared by spray drying: the effect of the polysaccharide carrier and naproxen concentration.

    PubMed

    Čerpnjak, Katja; Zvonar, Alenka; Vrečer, Franc; Gašperlin, Mirjana

    2015-05-15

    The purpose of this study was to prepare solid SMEDDS (sSMEDDS) particles produced by spray-drying using maltodextrin (MD), hypromellose (HPMC), and a combination of the two as a solid carrier. Naproxen (NPX) as the model drug was dissolved (at 6% concentration) or partially suspended (at 18% concentration) in a liquid SMEDDS composed of Miglyol(®) 812, Peceol™, Gelucire(®) 44/14, and Solutol(®) HS 15. Among the sSMEDDSs tested, the MD-based sSMEDDSs (with a granular, smooth-surfaced, microspherical appearance) preserved the self-microemulsifying properties of liquid SMEDDSs and exhibited dissolution profiles similar to those of liquid SMEDDSs, irrespective of the concentration of NPX. In contrast, HPMC-based sSMEDDSs (irregular-shaped microparticles) exhibited slightly prolonged release times due to the polymeric nature of the carrier. Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), and Raman mapping analysis confirmed molecularly dissolved NPX (at 6% of drug loading), whereas at 18% NPX loading drug is partially molecularly dissolved and partially in the crystalline state.

  6. Novel Spray Dried Glycerol 2-Phosphate Cross-Linked Chitosan Microparticulate Vaginal Delivery System—Development, Characterization and Cytotoxicity Studies

    PubMed Central

    Szymańska, Emilia; Szekalska, Marta; Czarnomysy, Robert; Lavrič, Zoran; Srčič, Stane; Miltyk, Wojciech; Winnicka, Katarzyna

    2016-01-01

    Chitosan microparticulate delivery systems containing clotrimazole were prepared by a spray drying technique using glycerol 2-phosphate as an ion cross-linker. The impact of a cross-linking ratio on microparticle characteristics was evaluated. Drug-free and drug-loaded unmodified or ion cross-linked chitosan microparticles were examined for the in vitro cytotoxicity in VK2/E6E7 human vaginal epithelial cells. The presence of glycerol 2-phosphate influenced drug loading and encapsulation efficacy in chitosan microparticles. By increasing the cross-linking ratio, the microparticles with lower diameter, moisture content and smoother surface were observed. Mucoadhesive studies displayed that all formulations possessed mucoadhesive properties. The in vitro release profile of clotrimazole was found to alter considerably by changing the glycerol 2-phosphate/chitosan ratio. Results from cytotoxicity studies showed occurrence of apoptotic cells in the presence of chitosan and ion cross-linked chitosan microparticles, followed by a loss of membrane potential suggesting that cell death might go through the mitochondrial apoptotic pathway. PMID:27690062

  7. Application of X-ray microtomography for the characterisation of hollow polymer-stabilised spray dried amorphous dispersion particles.

    PubMed

    Gamble, John F; Terada, Masako; Holzner, Christian; Lavery, Leah; Nicholson, Sarah J; Timmins, Peter; Tobyn, Mike

    2016-08-20

    The aim of this study was to investigate the capability of X-ray microtomography to obtain information relating to powder characteristics such as wall thickness and solid volume fraction for hollow, polymer-stabilised spray dried dispersion (SDD) particles. SDDs of varying particle properties, with respect to shell wall thickness and degree of particle collapse, were utilised to assess the capability of the approach. The results demonstrate that the approach can provide insight into the morphological characteristics of these hollow particles, and thereby a means to understand/predict the processability and performance characteristics of the bulk material. Quantitative assessments of particle wall thickness, particle/void volume and thereby solid volume fraction were also demonstrated to be achievable. The analysis was also shown to be able to qualitatively assess the impact of the drying rate on the morphological nature of the particle surfaces, thus providing further insight into the final particle shape. The approach demonstrated a practical means to access potentially important particle characteristics for SDD materials which, in addition to the standard bulk powder measurements such as particle size and bulk density, may enable a better understanding of such materials, and their impact on downstream processability and dosage form performance.

  8. Formulation and process design for a solid dosage form containing a spray-dried amorphous dispersion of ibipinabant.

    PubMed

    Leane, Michael M; Sinclair, Wayne; Qian, Feng; Haddadin, Raja; Brown, Alan; Tobyn, Mike; Dennis, Andrew B

    2013-01-01

    Amorphous forms of poorly soluble drugs are more frequently being incorporated into solid dispersions for administration and extensive research has led to a reasonable understanding of how these dispersions, although still kinetically unstable, improve stability relative to the pure amorphous form. There remains however a paucity of literature describing the effects on such solid dispersions of subsequent processing into solid dosage forms such as tablets. This paper addresses this area by looking at the effects of the addition of common excipients and different manufacturing routes on the stability of a spray-dried dispersion (SDD) of the cannabinoid CB-1 antagonist, ibipinabant. A marked difference in physical stability of tablets was seen with the different fillers with microcrystalline cellulose (MCC) giving the best stability profile. It was found that minimising the number of compression steps led to improved formulation stability with a direct compression process giving the best results. Increased levels of crystallinity were seen in coated tablets most likely due to the exposure of the amorphous matrix to moisture and heat during the coating process. DSIMS analysis of the SDD particles indicated increased levels of polymer on the surface.

  9. Matrix Effect on the Spray Drying Nanoencapsulation of Lippia sidoides Essential Oil in Chitosan-Native Gum Blends.

    PubMed

    Paula, Haroldo C B; Oliveira, Erick F; Carneiro, Maria J M; de Paula, Regina C M

    2017-03-01

    Essential oils have many applications in the pharmaceutical, chemical, and food fields, however, their use is limited to the fact that they are very labile, requiring their a priori encapsulation, aiming to preserve their properties.This work reports on the preparation of chitosan-gum nanoparticles loaded with thymol containing Lippia sidoides essential oil, using exudates of Anacardium Occidentale (cashew gum), Sterculia striata (chichá gum), and Anadenanthera macrocarpa trees (angico gum). Nanoparticles were produced by spray drying an emulsion of L. sidoides essential oil and aqueous solution of gums with different chitosan : gum ratios. Samples were characterized by FTIR and UV/VIS spectroscopy, particle size, volume distribution, and zeta potential. The FTIR spectrum showed the main signals of chitosan and the gums. Data obtained revealed that the samples had sizes in the nano range, varying from 17 nm to 800 nm. The zeta potential varied from + 30 mV to - 40 mV. Nanoparticle loading values varied from 6.7 % to 15.6 %, with an average encapsulating efficiency of 62 %, where the samples with high ratios of cashew gum and chichá gum presented high oil loading values. The data revealed that both the chitosan : gum ratio and polysaccharide characteristics play major roles in nanoencapsulation processes.

  10. Nano Spray Drying Technique as a Novel Approach To Formulate Stable Econazole Nitrate Nanosuspension Formulations for Ocular Use.

    PubMed

    Maged, Amr; Mahmoud, Azza A; Ghorab, Mahmoud M

    2016-09-06

    The effect of using methyl-β-cyclodextrin and hydroxypropyl-β-cyclodextrin as carriers for econazole nitrate nanoparticles prepared by nano spray dryer was explored in this work. Stabilizers, namely, poly(ethylene oxide), polyvinylpyrrolidone k30, poloxamer 407, Tween 80, and Cremophor EL, were used. The nano spray dried formulations revealed almost spherical particles with an average particle size values ranging from 121 to 1565 nm and zeta potential values ranging from -0.8 to -2.5 mV. The yield values for the obtained formulations reached 80%. The presence of the drug in the amorphous state within the nanosuspension matrix system significantly improved drug release compared to that for pure drug. Combination of hydroxypropyl-β-cyclodextrin with Tween 80 achieved an important role for preserving the econazole nanosuspension from aggregation during storage for one year at room temperature as well as improving drug release from the nanosuspension. This selected formulation was suspended in chitosan HCl to increase drug release and bioavailability. The in vivo evaluation on albino rabbit's eyes demonstrated distinctly superior bioavailability of the selected formulation suspended in chitosan compared to its counterpart formulation suspended in buffer and crude drug suspension due to its mucoadhesive properties and nanosize. The nano spray dryer could serve as a one step technique toward formulating stable and effective nanosuspensions.

  11. Improved stability and controlled release of CLA with spray-dried microcapsules of OSA-modified starch and xanthan gum.

    PubMed

    He, Huizi; Hong, Yan; Gu, Zhengbiao; Liu, Guodong; Cheng, Li; Li, Zhaofeng

    2016-08-20

    The objective of this investigation was to improve the stability of CLA and to allow for its controlled release by encapsulating it with combinations of octenyl-succinic anhydride (OSA) starch and xanthan gum (XG) in three ratios (OSA/XG: 60/1, 80/1, and 100/1, w/w). The wall material was examined using FTIR and TGA. The microcapsules were characterized by laser particle size analysis (LPS) and SEM. Oxidation of the microcapsules was monitored by headspace method. The results revealed that microcapsules created with an OSA/XG ratio of 60/1 provided superior protection to CLA against oxidation. When CLA-microcapsules were subjected to conditions simulating those in the human gastrointestinal system, 12.1%-50.1% of the CLA was released. CLA encapsulation in spray-dried microcapsules of OSA/XG appears to be an effective technique that provides good protection against oxidation and could be useful in the targeted delivery of functional lipids or other bioactive components to the small intestine.

  12. Optimizing spray drying conditions of sour cherry juice based on physicochemical properties, using response surface methodology (RSM).

    PubMed

    Moghaddam, Arasb Dabbagh; Pero, Milad; Askari, Gholam Reza

    2017-01-01

    In this study, the effects of main spray drying conditions such as inlet air temperature (100-140 °C), maltodextrin concentration (MDC: 30-60%), and aspiration rate (AR) (30-50%) on the physicochemical properties of sour cherry powder such as moisture content (MC), hygroscopicity, water solubility index (WSI), and bulk density were investigated. This investigation was carried out by employing response surface methodology and the process conditions were optimized by using this technique. The MC of the powder was negatively related to the linear effect of the MDC and inlet air temperature (IT) and directly related to the AR. Hygroscopicity of the powder was significantly influenced by the MDC. By increasing MDC in the juice, the hygroscopicity of the powder was decreased. MDC and inlet temperature had a positive effect, but the AR had a negative effect on the WSI of powder. MDC and inlet temperature negatively affected the bulk density of powder. By increasing these two variables, the bulk density of powder was decreased. The optimization procedure revealed that the following conditions resulted in a powder with the maximum solubility and minimum hygroscopicity: MDC = 60%, IT = 134 °C, and AR = 30% with a desirability of 0.875.

  13. Spray-dried structured lipid containing long-chain polyunsaturated fatty acids for use in infant formulas.

    PubMed

    Nagachinta, Supakana; Akoh, Casimir C

    2013-10-01

    Human milk fat (HMF) analogs are structured lipids (SLs) modified to have palmitic acid content at the sn-2 position of the triacylglycerol (TAG) and fatty acid composition comparable to HMF. Some of these SLs are also designed to incorporate long-chain polyunsaturated fatty acids (LCPUFAs) because of their important role in infant development. In this study, Maillard reaction products (MRPs), obtained from heated whey protein isolates and corn syrup solids (CSS) solution, were used as encapsulants for microencapsulation of 2 enzymatically synthesized SLs for infant formula applications. The encapsulated SL powders were obtained through spray-drying and evaluated in terms of their microencapsulation efficiency, chemical and physical properties, oxidative stability, and dispersibility. The microencapsulation efficiency of the SLs was 90%. Dispersibility test using particle size measurement demonstrated that these powders dispersed quickly into a homogeneous suspension. The encapsulated SL powders had low peroxide and thiobarbituric acid-reactive substances values. Lower oxidative stability was obtained in the powder containing SL with a higher degree of unsaturation and a lower concentration of tocopherols. The results demonstrated that the degree of fatty acid unsaturation and concentration of endogenous antioxidant in starting oils influenced the oxidative stability of the encapsulated SLs.

  14. Influence of sub-lethal stresses on the survival of lactic acid bacteria after spray-drying in orange juice.

    PubMed

    Barbosa, J; Borges, S; Teixeira, P

    2015-12-01

    The demand for new functional non-dairy based products makes the production of a probiotic orange juice powder an encouraging challenge. However, during drying process and storage, loss of viability of the dried probiotic cultures can occur, since the cells are exposed to various stresses. The influence of sub-lethal conditions of temperature, acidic pH and hydrogen peroxide on the viability of Pediococcus acidilactici HA-6111-2 and Lactobacillus plantarum 299v during spray drying in orange juice and subsequent storage under different conditions was investigated. At the end of storage, the survival of both microorganisms through simulated gastro-intestinal tract (GIT) conditions was also determined. The viability of cells previously exposed to each stress was not affected by the drying process. However, during 180 days of storage at room temperature, unlike P. acidilactici HA-6111-2, survival of L. plantarum 299v was enhanced by prior exposure to sub-lethal conditions. Previous exposure to sub-lethal stresses of each microorganism did not improve their viability after passage through simulated GIT. Nevertheless, as cellular inactivation during 180 days of storage was low, both microorganisms were present in numbers of ca. 10(7) cfu/mL at the end of GIT. This is an indication that both bacteria are good candidates for use in the development of an orange juice powder with functional characteristics.

  15. Highly Attrition Resistant Zinc Oxide-Based Sorbents for H2S Removal by Spray Drying Technique

    SciTech Connect

    Ryu, C.K.; Lee, J.B.; Ahn, D.H.; Kim, J.J.; Yi, C.K.

    2002-09-19

    Primary issues for the fluidized-bed/transport reactor process are high attrition resistant sorbent, its high sorption capacity and regenerability, durability, and cost. The overall objective of this project is the development of a superior attrition resistant zinc oxide-based sorbent for hot gas cleanup in integrated coal gasification combined cycle (IGCC). Sorbents applicable to a fluidized-bed hot gas desulfurization process must have a high attrition resistance to withstand the fast solid circulation between a desulfurizer and a regenerator, fast kinetic reactions, and high sulfur sorption capacity. The oxidative regeneration of zinc-based sorbent usually initiated at greater than 600 C with highly exothermic nature causing deactivation of sorbent as well as complication of sulfidation process by side reaction. Focusing on solving the sorbent attrition and regenerability of zinc oxide-based sorbent, we have adapted multi-binder matrices and direct incorporation of regeneration promoter. The sorbent forming was done with a spray drying technique that is easily scalable to commercial quantity.

  16. Assessment of Antioxidant Activity of Spray Dried Extracts of Psidium guajava Leaves by DPPH and Chemiluminescence Inhibition in Human Neutrophils

    PubMed Central

    Fernandes, M. R. V.; Azzolini, A. E. C. S.; Martinez, M. L. L.; Souza, C. R. F.; Lucisano-Valim, Y. M.; Oliveira, W. P.

    2014-01-01

    This work evaluated the physicochemical properties and antioxidant activity of spray dried extracts (SDE) from Psidium guajava L. leaves. Different drying carriers, namely, maltodextrin, colloidal silicon dioxide, Arabic gum, and β-cyclodextrin at concentrations of 40 and 80% relative to solids content, were added to drying composition. SDE were characterized through determination of the total phenolic, tannins, and flavonoid content. Antioxidant potential of the SDE was assessed by two assays: cellular test that measures the luminol-enhanced chemiluminescence (LumCL) produced by neutrophils stimulated with phorbol myristate acetate (PMA) and the DPPH radical scavenging (DPPH∗ method). In both assays the antioxidant activity of the SDE occurred in a concentration-dependent manner and showed no toxicity to the cells. Using the CLlum method, the IC50 ranged from 5.42 to 6.50 µg/mL. The IC50 of the SDE ranged from 7.96 to 8.11 µg/mL using the DPPH• method. Psidium guajava SDE presented significant antioxidant activity; thus they show high potential as an active phytopharmaceutical ingredient. Our findings in human neutrophils are pharmacologically relevant since they indicate that P. guajava SDE is a potential antioxidant and anti-inflammatory agent in human cells. PMID:24822200

  17. Quality evaluation of peony seed oil spray-dried in different combinations of wall materials during encapsulation and storage.

    PubMed

    Shi, Yan; Wang, Shu-Jie; Tu, Zong-Cai; Wang, Hui; Li, Ru-Yi; Zhang, Lu; Huang, Tao; Su, Ting; Li, Cui

    2016-06-01

    This study aimed at evaluating the performance of peony seed oil microencapsulated by spray drying during encapsulation and storage. Four different combinations of gum arabic (GA), corn syrup (CS), whey protein concentrate (WPC) and sodium caseinate (CAS) were used to encapsulate peony seed oil. The best encapsulation efficiency was obtained for CAS/CS followed by the CAS/GA/CS combination with the encapsulation ratio of 93.71 and 92.80 %, respectively, while the lowest encapsulation efficiency was obtained for WPC/GA/CS (85.96 %). Scanning electron microscopy and confocal laser scanning microscopy revealed that the particles were spherical in shape and did not exhibit apparent cracks or fissures, and gum arabic was uniformly distributed across the wall of the microcapsules. Oxidative stability study indicated that the CAS/GA/CS combination presented the best protection against lipid oxidation and the smallest loss of polyunsaturated fatty acid content among all of the formulas as measured by gas chromatography. Therefore, CAS/GA/CS could be promising materials encapsulate peony seed oil with high encapsulation efficiency and minimal lipid oxidation.

  18. Functional and antioxidant properties of hydrolysates of sardine (S. pilchardus) and horse mackerel (T. mediterraneus) for the microencapsulation of fish oil by spray-drying.

    PubMed

    Morales-Medina, R; Tamm, F; Guadix, A M; Guadix, E M; Drusch, S

    2016-03-01

    The functionality of fish protein hydrolysates (FPH) for the microencapsulation of fish oil was investigated. Muscle protein from sardine (Sardina pilchardus) and horse mackerel (Trachurus mediterraneus) was hydrolysed using Alcalase or trypsin. Physically stable emulsions suitable for spray-drying were obtained when using FPH with a degree of hydrolysis of 5%. Microencapsulation efficiency amounted to 98±0.1% and oxidative stability of the encapsulated oil over a period of twelve weeks was in a similar range as it is reported for other matrix systems. Therefore, the suitability of FPH for use in spray-dried emulsions has been shown for the first time. Since no clear correlation between the antioxidative activity of the FPH and the course of lipid oxidation could be established future research is required to more specifically characterise the molecular structure of the peptides and its impact on protein alteration and role in lipid oxidation.

  19. Survivability of porcine epidemic diarrhea virus (PEDV) in bovine plasma submitted to spray drying processing and held at different time by temperature storage conditions.

    PubMed

    Pujols, Joan; Segalés, Joaquim

    2014-12-05

    Bovine plasma was inoculated with porcine epidemic diarrhea virus (PEDV) at an average final titer of 4.2 log10 TCID50/mL to determine the effect of spray drying on viral inactivation. Using a laboratory scale drier, inoculated plasma was spray dried at 200 °C inlet temperature and either 70 or 80 °C throughout substance. Both liquid and dried samples were subjected to three passages on VERO cell monolayers to determine PEDV infectivity. Results indicated liquid samples contained infective virus, but none of the spray dried samples were infectious. Also, survivability of PEDV inoculated on spray dried bovine plasma (SDBP) and stored at 4, 12 or 22 °C was determined for 7, 14 and 21 days. Commercial SDBP powder was inoculated with PEDV to an average final titer of 2.8 log10 TCID50/g. Five samples per time and temperature conditions were subjected to three passages on VERO cell monolayers to determine PEDV infectivity. The virus was non-infectious for all samples stored at 22 °C at 7, 14 and 21 days. PEDV was infective in 1 out of 5 samples stored at 12 °C at 7 days, but none of the samples stored for 14 and 21 days were infectious in cell culture. For samples stored at 4 °C, 4 out of 5 samples were infectious at 7 days, 1 out of 5 samples were infectious at 14 days, but none were infectious at 21 days. In summary, PEDV was not infectious on cell culture within 7 days when stored at room temperature and within 21 days when stored at refrigerated temperature.

  20. Determination of residual acetone and acetone related impurities in drug product intermediates prepared as Spray Dried Dispersions (SDD) using gas chromatography with headspace autosampling (GCHS).

    PubMed

    Quirk, Emma; Doggett, Adrian; Bretnall, Alison

    2014-08-05

    Spray Dried Dispersions (SDD) are uniform mixtures of a specific ratio of amorphous active pharmaceutical ingredient (API) and polymer prepared via a spray drying process. Volatile solvents are employed during spray drying to facilitate the formation of the SDD material. Following manufacture, analytical methodology is required to determine residual levels of the spray drying solvent and its associated impurities. Due to the high level of polymer in the SDD samples, direct liquid injection with Gas Chromatography (GC) is not a viable option for analysis. This work describes the development and validation of an analytical approach to determine residual levels of acetone and acetone related impurities, mesityl oxide (MO) and diacetone alcohol (DAA), in drug product intermediates prepared as SDDs using GC with headspace (HS) autosampling. The method development for these analytes presented a number of analytical challenges which had to be overcome before the levels of the volatiles of interest could be accurately quantified. GCHS could be used after two critical factors were implemented; (1) calculation and application of conversion factors to 'correct' for the reactions occurring between acetone, MO and DAA during generation of the headspace volume for analysis, and the addition of an equivalent amount of polymer into all reference solutions used for quantitation to ensure comparability between the headspace volumes generated for both samples and external standards. This work describes the method development and optimisation of the standard preparation, the headspace autosampler operating parameters and the chromatographic conditions, together with a summary of the validation of the methodology. The approach has been demonstrated to be robust and suitable to accurately determine levels of acetone, MO and DAA in SDD materials over the linear concentration range 0.008-0.4μL/mL, with minimum quantitation limits of 20ppm for acetone and MO, and 80ppm for DAA.

  1. Phytase production by Rhizopus microsporus var. microsporus biofilm: characterization of enzymatic activity after spray drying in presence of carbohydrates and nonconventional adjuvants.

    PubMed

    Sato, Vanessa Sayuri; Jorge, João Atílio; Oliveira, Wanderley Pereira; Souza, Claudia Regina Fernandez; Guimarães, Luis Henrique Souza

    2014-02-28

    Microbial phytases are enzymes with biotechnological interest for the feed industry. In this article, the effect of spray-drying conditions on the stability and activity of extracellular phytase produced by R. microsporus var. microsporus biofilm is described. The phytase was spray-dried in the presence of starch, corn meal (>150 μm), soy bean meal (SB), corn meal (<150 μm) (CM), and maltodextrin as drying adjuvants. The residual enzyme activity after drying ranged from 10.7% to 60.4%, with SB and CM standing out as stabilizing agents. Water concentration and residual enzyme activity were determined in obtained powders as a function of the drying condition. When exposed to different pH values, the SB and CM products were stable, with residual activity above 50% in the pH range from 4.5 to 8.5 for 60 min. The use of CM as drying adjuvant promoted the best retention of enzymatic activity compared with SB. Spray drying of the R. microsporus var. microsporus phytase using different drying adjuvants showed interesting results, being quite feasible with regards their biotechnological applications, especially for poultry diets.

  2. Influence of Excipients and Spray Drying on the Physical and Chemical Properties of Nutraceutical Capsules Containing Phytochemicals from Black Bean Extract.

    PubMed

    Guajardo-Flores, Daniel; Rempel, Curtis; Gutiérrez-Uribe, Janet A; Serna-Saldívar, Sergio O

    2015-12-03

    Black beans (Phaseolus vulgaris L.) are a rich source of flavonoids and saponins with proven health benefits. Spray dried black bean extract powders were used in different formulations for the production of nutraceutical capsules with reduced batch-to-batch weight variability. Factorial designs were used to find an adequate maltodextrin-extract ratio for the spray-drying process to produce black bean extract powders. Several flowability properties were used to determine composite flow index of produced powders. Powder containing 6% maltodextrin had the highest yield (78.6%) and the best recovery of flavonoids and saponins (>56% and >73%, respectively). The new complexes formed by the interaction of black bean powder with maltodextrin, microcrystalline cellulose 50 and starch exhibited not only bigger particles, but also a rougher structure than using only maltodextrin and starch as excipients. A drying process prior to capsule production improved powder flowability, increasing capsule weight and reducing variability. The formulation containing 25.0% of maltodextrin, 24.1% of microcrystalline cellulose 50, 50% of starch and 0.9% of magnesium stearate produced capsules with less than 2.5% weight variability. The spray drying technique is a feasible technique to produce good flow extract powders containing valuable phytochemicals and low cost excipients to reduce the end-product variability.

  3. An investigation into the effect of spray drying temperature and atomizing conditions on miscibility, physical stability, and performance of naproxen-PVP K 25 solid dispersions.

    PubMed

    Paudel, Amrit; Loyson, Yves; Van den Mooter, Guy

    2013-04-01

    The present study investigates the effect of changing spray drying temperature (40°C-120°C) and/or atomizing airflow rate (AR; 5-15 L/min) on the phase structure, physical stability, and performance of spray-dried naproxen-polyvinylpyrrolidone (PVP) K 25 amorphous solid dispersions. The modulated differential scanning calorimetry, attenuated total internal reflectance-Fourier transform infrared, and powder X-ray diffractometry (pXRD) studies revealed that higher inlet temperature (IT) or atomization airflow leads to the formation of amorphous-phase-separated dispersions with higher strongly H-bonded and free PVP fractions, whereas that prepared with the lowest IT was more homogeneous. The dispersion prepared with the lowest atomization AR showed trace crystallinity. Upon exposure to 75% relative humidity (RH) for 3 weeks, the phase-separated dispersions generated by spray drying at higher temperature or higher atomization airflow retained relatively higher amorphous drug fraction compared with those prepared at slow evaporation conditions. The humidity-controlled pXRD analysis at 98% RH showed that the dispersion prepared with highest atomization AR displayed the slowest kinetics of recrystallization. The molecular-level changes occurring during recrystallization at 98% RH was elucidated by spectroscopic monitoring at the same humidity. The rate and extent of the drug dissolution was the highest for dispersions prepared at the highest atomizing AR and the lowest for that prepared with the slowest atomizing condition.

  4. Spray dried microspheres based on chitosan: A promising new carrier for intranasal administration of polymeric antigen BLSOmp31 for prevention of ovine brucellosis.

    PubMed

    Díaz, Alejandra Graciela; Quinteros, Daniela Alejandra; Llabot, Juan Manuel; Palma, Santiago Daniel; Allemandi, Daniel Alberto; Ghersi, Giselle; Zylberman, Vanesa; Goldbaum, Fernando Alberto; Estein, Silvia Marcela

    2016-05-01

    Previous studies have demonstrated that parenteral immunization with polymeric antigen BLSOmp31 induced a strong immune response and conferred protection against Brucella ovis in rams. This work describes the development of a novel formulation strategy for the delivery of BLSOmp31 in the nasal mucosa. Chitosan microparticles were prepared by spray-drying technology processes and recombinant chimera BLSOmp31 was loaded by passive adsorption onto chitosan microspheres, which were characterized by means of the evaluation of size, zeta potential, morphology, and loading and release rate of BLSOmp31. The mucoadhesive properties of microspheres were evaluated by studying the interaction between microparticles and mucin. The antigen BLSOmp31 integrity was investigated by SDS-PAGE. The yield of production of spray-drying process was 68.95%. Microspheres had a good sphericity, 1-10 μm of particle size and had a positive charge. The loading capacity was found to be 45.19%. The initial fast release of BLSOmp31 from chitosan microparticles was 60%. The BLSOmp31 integrity was not affected by passive adsorption (ionic interaction). The amount of mucin adsorbed on the surface of CMs-BLSOmp31 was lower than on the surface of blank CMs at neutral pH. In vivo studies were carried out in rams. Intranasal immunization induced systemic and local antibodies. In conclusion, the use of BLSOmp31-loaded chitosan spray-drying microspheres offers a promising way for nasal mucosal vaccination in sheep against brucellosis.

  5. Advances in Inhalation Dosimetry Models and Methods for Occupational Risk Assessment and Exposure Limit Derivation

    PubMed Central

    Kuempel, Eileen D.; Sweeney, Lisa M.; Morris, John B.; Jarabek, Annie M.

    2015-01-01

    The purpose of this article is to provide an overview and practical guide to occupational health professionals concerning the derivation and use of dose estimates in risk assessment for development of occupational exposure limits (OELs) for inhaled substances. Dosimetry is the study and practice of measuring or estimating the internal dose of a substance in individuals or a population. Dosimetry thus provides an essential link to understanding the relationship between an external exposure and a biological response. Use of dosimetry principles and tools can improve the accuracy of risk assessment, and reduce the uncertainty, by providing reliable estimates of the internal dose at the target tissue. This is accomplished through specific measurement data or predictive models, when available, or the use of basic dosimetry principles for broad classes of materials. Accurate dose estimation is essential not only for dose-response assessment, but also for interspecies extrapolation and for risk characterization at given exposures. Inhalation dosimetry is the focus of this paper since it is a major route of exposure in the workplace. Practical examples of dose estimation and OEL derivation are provided for inhaled gases and particulates. PMID:26551218

  6. A comparison of spray drying and milling in the production of amorphous dispersions of sulfathiazole/polyvinylpyrrolidone and sulfadimidine/polyvinylpyrrolidone.

    PubMed

    Caron, Vincent; Tajber, Lidia; Corrigan, Owen I; Healy, Anne Marie

    2011-04-04

    Formulations containing amorphous active pharmaceutical ingredients (APIs) present great potential to overcome problems of limited bioavailability of poorly soluble APIs. In this paper, we directly compare for the first time spray drying and milling as methods to produce amorphous dispersions for two binary systems (poorly soluble API)/excipient: sulfathiazole (STZ)/polyvinylpyrrolidone (PVP) and sulfadimidine (SDM)/PVP. The coprocessed mixtures were characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and intrinsic dissolution tests. PXRD and DSC confirmed that homogeneous glassy solutions (mixture with a single glass transition) of STZ/PVP were obtained for 0.05 ≤ X(PVP) (PVP weight fraction) < 1 by spray drying and for 0.6 ≤ X(PVP) < 1 by milling (at 400 rpm), and homogeneous glassy solutions of SDM/PVP were obtained for 0 < X(PVP) < 1 by spray drying and for 0.7 ≤ X(PVP) < 1 by milling. For these amorphous composites, the value of T(g) for a particular API/PVP ratio did not depend on the processing technique used. Variation of T(g) versus concentration of PVP was monotonic for all the systems and matched values predicted by the Gordon-Taylor equation indicating that there are no strong interactions between the drugs and PVP. The fact that amorphous SDM can be obtained on spray drying but not amorphous STZ could not be anticipated from the thermodynamic driving force of crystallization, but may be due to the lower molecular mobility of amorphous SDM compared to amorphous STZ. The solubility of the crystalline APIs in PVP was determined and the activities of the two APIs were fitted to the Flory-Huggins model. Comparable values of the Flory-Huggins interaction parameter (χ) were determined for the two systems (χ = -1.8 for SDM, χ = -1.5 for STZ) indicating that the two APIs have similar miscibility with PVP. Zones of stability and instability of the amorphous dispersions

  7. Solid dispersion particles of amorphous indomethacin with fine porous silica particles by using spray-drying method.

    PubMed

    Takeuchi, Hirofumi; Nagira, Shinsuke; Yamamoto, Hiromitsu; Kawashima, Yoshiaki

    2005-04-11

    The solid dispersion particles of indomethacin (IMC) were prepared with different types of silica, non-porous (Aerosil 200) or porous silica (Sylysia 350) by using spray-drying method. Powder X-ray diffraction analysis showed that IMC in solid dispersion particles is in amorphous state irrespective of the type of silica formulated. In DSC analysis, the melting peak of IMC in solid dispersion particles with Sylysia 350 shifted to lower temperature than that in solid dispersion particles with Aerosil 200 although the peak of each solid dispersion particles was much smaller than that of original IMC crystals. Dissolution property of IMC was remarkably improved by formulating the silica particles to the solid dispersion particles. In comparing the effect of the type of the silica particles, the dissolution rate of solid dispersion particles with Sylysia 350 was faster than that with Aerosil 200. The formulation amount of IMC did not affect on the amorphous state of IMC in the resultant solid dispersion particles in powder X-ray diffraction patterns. However, the area of the melting peak of IMC in the solid dispersion particles increased and an exothermic peak owing to recrystallization was observed with increasing the IMC content in the DSC patterns. The dissolution rate of IMC from the solid dispersion particles with Sylysia 350 was faster than that of Aerosil 200 irrespective of IMC content. In stability test, amorphous IMC in the solid dispersion particles with each silica particles did not crystallize under storing at severe storage conditions (40 degrees C, 75% RH) for 2 months, while amorphous IMC without silica easily crystallized under same conditions.

  8. A new approach to prepare well-dispersed CaF(2) nanoparticles by spray drying technique.

    PubMed

    Sun, Limin; Chow, Laurence C; Bonevich, John E; Wang, Tongxin; Mitchell, James W

    2011-08-01

    Previously, nano-sized calcium fluoride (CaF₂) particles were prepared using a spray drying method by simultaneously feeding Ca(OH)₂ and NH₄F solutions to a two-liquid nozzle. The aim of the present study was to prepare better-dispersed nano-CaF₂ particles by co-forming a soluble salt, sodium chloride (NaCl). NaCl of various concentrations were added to the NH(4) F solution, leading to formation of (CaF₂ +NaCl) composites with CaF₂ /NaCl molar ratios of 4/1, 4/4, and 4/16. Pure nano-CaF₂ was also prepared as the control. Powder X-ray diffraction analysis showed that the products contained crystalline CaF₂ and NaCl. Scanning electron microscopy examinations showed that both the CaF₂ /NaCl composite and pure CaF₂ particles were about (50-800) nm in size and consisted of primary CaF₂ particles of < 50 nm in size. BET surface area measurements showed similar primary particle sizes for all samples. Dynamic light scattering measurements showed that the washed (CaF₂+NaCl) particles were much smaller than the pure CaF₂ as the dissolution of NaCl "freed" most of the primary CaF₂ particles, leading to a greater degree of particle dispersion. The well-dispersed nano-CaF₂ may be expected to be a more effective anticaries agent than NaF by providing longer lasting elevations of fluoride concentrations in oral fluids.

  9. Nanoencapsulation of water-soluble drug, lamivudine, using a double emulsion spray-drying technique for improving HIV treatment

    NASA Astrophysics Data System (ADS)

    Tshweu, Lesego; Katata, Lebogang; Kalombo, Lonji; Swai, Hulda

    2013-11-01

    Current treatments available for human immunodeficiency virus, namely antiretrovirals, do not completely eradicate the virus from the body, leading to life-time commitment. Many antiretrovirals suffer drawbacks from toxicity and unpleasant side effects, causing patience non-compliance. To minimize challenges associated with the antiretrovirals, biodegradable nanoparticles used as drug delivery systems hold tremendous potential to enhance patience compliance. The main objective of this work was to load lamivudine (LAM) into poly(epsilon-caprolactone) (PCL) nanoparticles. LAM is a hydrophilic drug with low plasma half-life of 5-7 h and several unpleasant side effects. LAM was nanoencapsulated into PCL polymer via the double emulsion spray-drying method. Formulation parameters such as the effect of solvent, excipient and drug concentration were optimized for the synthesis of the nanoparticles. Spherical nanoparticles with an average size of 215 ± 3 nm and polydispersity index (PDI) of 0.227 ± 0.01 were obtained, when ethyl acetate and lactose were used in the preparation. However, dichloromethane presented sizes larger than 454 ± 11 nm with PDI of more than 0.4 ± 0.05, irrespective of whether lactose or trehalose was used in the preparation. Some of the nanoparticles prepared with trehalose resulted in crystal formation. UV spectroscopy showed encapsulation efficiency ranging from 68 ± 4 to 78 ± 4 % for LAM depending on the starting drug concentration. Fourier transform infrared spectroscopy and X-ray diffraction confirmed the possibility of preparing amorphous PCL nanoparticles containing LAM. Drug release extended for 4 days in pH 1.3, pH 4.5 and pH 6.8. These results indicated that LAM-loaded PCL nanoparticles show promise for controlled delivery.

  10. Viability, Acid and Bile Tolerance of Spray Dried Probiotic Bacteria and Some Commercial Probiotic Supplement Products Kept at Room Temperature.

    PubMed

    Dianawati, Dianawati; Mishra, Vijay; Shah, Nagendra P

    2016-06-01

    Production of probiotic food supplements that are shelf-stable at room temperature has been developed for consumer's convenience, but information on the stability in acid and bile environment is still scarce. Viability and acid and bile tolerance of microencapsulated Bifidobacterium spp. and Lactobacillus acidophilus and 4 commercial probiotic supplements were evaluated. Bifidobacterium and L. acidophilus were encapsulated with casein-based emulsion using spray drying. Water activity (aw ) of the microspheres containing Bifidobacterium or L. acidophilus (SD GM product) was adjusted to 0.07 followed by storage at 25 °C for 10 wk. Encapsulated Bifidobacterium spp. and Lactobacillus acidophilus and 4 commercial probiotic supplement products (AL, GH, RE, and BM) were tested. Since commercial probiotic products contained mixed bacteria, selective media MRS-LP (containing L-cysteine and Na-propionate) and MRS-clindamycin agar were used to grow Bifidobacterium spp. or L. acidophilus, respectively, and to inhibit the growth of other strains. The results showed that aw had a strong negative correlation with the viability of dehydrated probiotics of the 6 products. Viable counts of Bifidobacterium spp. and L. acidophilus of SD GM, AL, and GH were between 8.3 and 9.2 log CFU/g, whereas that of BM and RE were between 6.7 and 7.3 log CFU/g. Bifidobacterium in SD GM, in AL, and in GH products and L. acidophilus in SD GM, in AL, and in BM products demonstrated high tolerance to acid. Most of dehydrated probiotic bacteria were able to survive in bile environment except L. acidophilus in RE product. Exposure to gastric juice influenced bacterial survivability in subsequent bile environment.

  11. Microencapsulation of Lactobacillus acidophilus La-5 by spray-drying using sweet whey and skim milk as encapsulating materials.

    PubMed

    Maciel, G M; Chaves, K S; Grosso, C R F; Gigante, M L

    2014-01-01

    The aim of this study was to evaluate the effect of encapsulating material on encapsulation yield, resistance to passage through simulated gastrointestinal conditions, and viability of Lactobacillus acidophilus La-5 during storage. Microparticles were produced from reconstituted sweet whey or skim milk (30% total solids) inoculated with a suspension of L. acidophilus La-5 (1% vol/vol) and subjected to spray-drying at inlet and outlet temperatures of 180°C and 85 to 95°C, respectively. The samples were packed, vacuum-sealed, and stored at 4°C and 25°C. Encapsulation yield, moisture content, and resistance of microencapsulated L. acidophilus La-5 compared with free cells (control) during exposure to in vitro gastrointestinal conditions (pH 2.0 and 7.0) were evaluated. Viability was assessed after 0, 7, 15, 30, 45, 60, and 90d of storage. The experiments were repeated 3 times and data were analyzed by ANOVA and Tukey test for the comparison between means. The encapsulating material did not significantly affect encapsulation yield, average diameter, or moisture of the particles, which averaged 76.58±4.72%, 12.94±0.78μm, and 4.53±0.32%, respectively. Both microparticle types were effective in protecting the probiotic during gastrointestinal simulation, and the skim milk microparticles favored an increase in viability of L. acidophilus La-5. Regardless of the encapsulating material and temperature of storage, viability of the microencapsulated L. acidophilus La-5 decreased on average 0.43 log cfu/g at the end of 90d of storage, remaining higher than 10(6)cfu/g.

  12. Spray-dried animal plasma prevents the effects of Staphylococcus aureus enterotoxin B on intestinal barrier function in weaned rats.

    PubMed

    Pérez-Bosque, Anna; Amat, Concepció; Polo, Javier; Campbell, Joy M; Crenshaw, Joe; Russell, Louis; Moretó, Miquel

    2006-11-01

    In this study, we investigated intestinal barrier function during inflammation as well as the effects of dietary supplementation with porcine spray-dried animal plasma (SDAP) proteins and porcine immunoglobulin concentrate (IC). Wistar Lewis rats were fed from d 21 (weaning) until d 34 or 35 either a control diet or a diet containing SDAP or IC. On d 30 and d 33, rats received an intraperitoneal dose of Staphylococcus aureus enterotoxin B (SEB; 0.5 mg/kg body wt; groups SEB, SEB-SDAP, and SEB-IC). SEB reduced the potential difference across the jejunum by 60%, the short-circuit current by 70%, and Na-K-ATPase activity in intestinal mucosa (all P < 0.05). The fluxes of dextran flux (4 kDa) and horseradish peroxidase (HRP, 40 kDa) across the intestinal wall also increased in SEB-treated rats (P < 0.01, P = 0.068, respectively). SEB also increased HRP flux across the paracellular space (P < 0.05). Moreover, SEB-treated rats had a reduced expression of tight junction proteins, such as ZO-1 (10% reduction; P < 0.05) and beta-catenin (20% reduction; P < 0.05). Dietary supplementation with SDAP or IC prevented dextran (P < 0.05) and HRP (P < 0.05) paracellular flux across the intestinal epithelium. SDAP supplementation also prevented SEB effects on Na-K-ATPase activity (P < 0.05). In our model of SEB-induced intestinal inflammation, the increased permeability across the intestinal mucosa was due to the lower expression of tight junction proteins, an effect that can be prevented by both SDAP and IC supplementation.

  13. Inhalation toxicity of (1→3)-β-D glucan: recent advances

    PubMed Central

    Fogelmark, Birgitta; Sjöstrand, Margareta; Williams, David; Rylander, Ragnar

    1997-01-01

    To investigate the effects of (1→3)-β-D-glucan after inhalation, animals were exposed to different forms of glucan and the number of lung lavage cells was determined 24 h after exposure. None of the different forms assayed caused any increase in cell numbers. In animals exposed to endotoxin, all types of cells were increased after 24 h. A simultaneous exposure to curdlan reduced this increase in a dose-related fashion. The results suggest that (1→3)-β-D-glucan-related acute injury to the lung is induced by mechanisms other than those induced by inflammagenic agents such as endotoxin. PMID:18472855

  14. Advances in asthma and COPD management: delivering CFC-free inhaled therapy using Modulite technology.

    PubMed

    Acerbi, D; Brambilla, G; Kottakis, I

    2007-01-01

    Inhaled corticosteroids (ICS) and long-acting beta-agonists (LABA) are currently used in the management of asthma and chronic obstructive pulmonary disease (COPD). Localized targeted delivery of these drugs into the lungs is achieved by means of two types of inhalation devices; pressurized metered-dose inhalers (pMDIs) and dry powder-inhalers (DPIs). For environmental reasons, the chlorofluorocarbon (CFC) propellants used in pMDIs are now being replaced by ozone friendly hydrofluoroalkanes (HFAs). These new generation HFA-based pMDIs, developed to provide effective lung deposition of the active moiety, have a favorable safety and tolerability profile. However, HFA-based re-formulation of LABAs and ICS for pMDIs presents particular technical difficulties, especially in terms of ensuring dose content uniformity. This review focuses on the technology and clinical efficacy of the HFA solution pMDIs using Modulite platform technology (Chiesi Farmaceutici S.p.A). Modulite technology allows the development of HFA solution formulations that can mimic the established CFC-based drug formulations on a microgram to microgram basis and provides formulations with novel particle size distributions that improve on existing delivery systems; by manipulation of aerosol clouds and particle size, the delivery of HFA-formulated drugs can be optimized to either achieve fine particle fractions and deposition patterns similar to established CFC-based drug formulations, thus facilitating the transition to new environment-friendly pMDIs in the clinical setting, or achieve finer drug particles able to penetrate deeper into the bronchi for targeted drug delivery as medical need may dictate. Long-term, multiple-dose clinical studies of Modulite formulations of beclomethasone dipropionate (BDP), budesonide and formoterol have been demonstrated to be therapeutically equivalent to their respective previously established CFC or DPI formulations. As a result, a number of Modulite pMDIs have either

  15. [Inhaled therapy in asthma].

    PubMed

    Plaza Moral, Vicente; Giner Donaire, Jordi

    2016-04-01

    Because of its advantages, inhaled administration of aerosolized drugs is the administration route of choice for the treatment of asthma and COPD. Numerous technological advances in the devices used in inhaled therapy in recent decades have boosted the appearance of multiple inhalers and aerosolized drugs. However, this variety also requires that the prescribing physician is aware of their characteristics. The main objective of the present review is to summarize the current state of knowledge on inhalers and inhaled drugs commonly used in the treatment of asthma. The review ranges from theoretical aspects (fundamentals and available devices and drugs) to practical and relevant aspects for asthma care in the clinical setting (therapeutic strategies, education, and adherence to inhalers).

  16. Particle engineering techniques for inhaled biopharmaceuticals.

    PubMed

    Shoyele, Sunday A; Cawthorne, Simon

    2006-10-31

    Formulation of biopharmaceuticals for pulmonary delivery is faced with the challenge of producing particles with the optimal properties for deep lung deposition without altering the native conformation of these molecules. Traditional techniques such as milling are continuously being improved while newer and more advanced techniques such as spray drying, spray freeze drying and supercritical fluid technology are being developed so as to optimize pulmonary delivery of biopharmaceuticals. While some of these techniques are quite promising, some are harsh and impracticable. Method scale up, cost-effectiveness and safety issues are important factors to be considered in the choice of a technique. This paper reviews the presently developed techniques for particle engineering biopharmaceuticals.

  17. Effect of spray-dried bovine serum on intake, health, and growth of broilers housed in different environments.

    PubMed

    Campbell, J M; Quigley, J D; Russell, L E; Kidd, M T

    2003-11-01

    Three experiments utilizing broilers were conducted in different environments to evaluate the effects of Innavax (INX; spray-dried serum) administered in drinking water on broiler performance. In Exp. 1 (1 to 42 d), 252 Ross x Cobb male broilers were assigned randomly to one of six treatments consisting of tap water mixed with 0, 0.25, 0.50, 0.75, 1.0, or 1.25% (wt/wt) INX. Broilers (six broilers per pen; seven pens per treatment) were housed in Petersime battery cages (raised wire flooring) in temperature-controlled rooms. Average daily gain, and feed and water intake (as-fed) were not affected (P > 0.05) by experimental treatments. Feed efficiency tended to improve linearly (P = 0.076) from d 0 to 7 with increasing levels of INX, but was unaffected (P > 0.05) during the remaining periods. In Exp. 2 and 3, 800 Ross x Ross 308 male broilers (400 broilers in each trial; 10 broilers per pen; 10 pens per treatment) in two 21-d experiments were assigned randomly to one of four treatments consisting of tap water mixed with 0, 0.45, 0.90, or 1.35% (wt/wt) INX. Broilers were housed in floor pens containing clean (Exp. 2) or used (Exp. 3) litter. In Exp. 2, intake, ADG, and feed efficiency were linearly improved (P < 0.05) during the first week with increasing levels of INX. During the second week (d 8 to 14), ADG, water intake, and feed efficiency were linearly improved (P < 0.05) with increasing levels of INX. In the third week (d 15 to 21), ADG and feed and water intake were not affected (P > 0.10) by level of INX. Overall (d 0 to 21), ADG, intake, and feed efficiency were linearly improved (P < 0.05) with INX. In Exp. 3, ADG, water intake, and feed efficiency were linearly improved (P < 0.05) during each period. Feed intake was not affected (P > 0.05) by experimental treatment during d 0 to 7, but was linearly increased (P < 0.05) from d 8 to 14 and 15 to 21. The greatest growth response of broilers to INX was observed when broilers were housed in floor pens with used

  18. Compressional behavior of a mixture of granules containing high load of Phyllanthus niruri spray-dried extract and granules of adjuvants: comparison between eccentric and rotary tablet machines.

    PubMed

    Spaniol, Bárbara; Bica, Vinicius Claudino; Ruppenthal, Lisias Rafael; Volpato, Maria Ramos; Petrovick, Pedro Ros

    2009-01-01

    The purpose of this paper was to evaluate the compressional behavior of granules containing high load of a Phyllanthus niruri spray-dried extract in eccentric (ETM) and rotary (RTM) tablet presses. Tablets were constituted by spray-dried extract granules (SDEG, 92%), excipient granules (EXCG, 7.92%), and magnesium stearate (0.08%). SDEG was obtained by dry granulation and EXCG, composed of microcrystalline cellulose (62.9%) and sodium starch glycolate (37.1%), by wet granulation. Particle size distribution was fixed between 0.250 and 0.850 mm. Tablets did not evidence any mechanical failures, such as lamination or capping, or anomalous weight variation in either tablet machine types. Upper and lower tablet surface photomicrographs from ETM and RTM tablets showed differences in porosity and texture. Different RTM speeds suggested the visco-plastic behavior of the formulation, since, by slowing down rotation speeds, the tensile strength of the tablets increased significantly, but the porosity and disintegration time were not affected. Tablets produced in RTM showed lower friability and porosity than ETM tablets, which did not reflect on higher tensile strength. The EXCG distribution at upper and lower surfaces from ETM and RTM tablets was quantified by image analysis and evaluated through statistical methods. Spray-dried extract release was not influenced by the type of equipment or operational conditions to which the compacts were submitted. Construction and operation differences between both tablet presses influenced the final product, since tablets with similar tensile strength, made by distinct tablet machines, exhibited different quality parameters.

  19. Spray drying of drug-swellable dispersant suspensions for preparation of fast-dissolving, high drug-loaded, surfactant-free nanocomposites.

    PubMed

    Azad, Mohammad; Arteaga, Colby; Abdelmalek, Beshoy; Davé, Rajesh; Bilgili, Ecevit

    2015-01-01

    Bioavailability of a poorly soluble drug can be improved by preparing a drug nanosuspension and subsequently drying it into nanocomposite microparticles (NCMPs). Unfortunately, drug nanoparticles aggregate during milling and drying, causing incomplete recovery and slow dissolution. The aim of this study is to investigate the impact of various classes of dispersants on drug dissolution from drug NCMPs, with the ultimate goal of enhancing the bioavailability of poorly water-soluble drugs via high drug nanoparticle loaded, surfactant-free NCMPs. Precursor suspensions of griseofulvin (GF, model drug) nanoparticles in the presence of various dispersants were prepared via wet stirred media milling and spray dried to form the NCMPs. Hydroxypropyl cellulose (HPC, polymer) alone and with sodium dodecyl sulfate (SDS, surfactant) was used as a base-line stabilizer/dispersant during milling. Two swellable crosslinked polymers, croscarmellose sodium (CCS) and sodium starch glycolate (SSG), and a conventional soluble matrix former, Mannitol, were used in addition to HPC. Besides being used as-received, CCS was also wet co-milled with GF for two different durations to examine the impact of CCS particle size. Laser diffraction, scanning electron microscopy, powder X-ray diffraction (XRD), UV spectroscopy, NCMP redispersion and dissolution tests were used for characterization. The results show that incorporation of CCS/SSG, preferably wet-milled to a wide particle size distribution, into the spray-dried NCMPs resulted in fast release and dispersion of drug nanoparticle clusters. The swellable dispersants were superior to Mannitol in dissolution enhancement, and could achieve fast release comparable to SDS, demonstrating the feasibility of spray drying to prepare high drug-loaded, surfactant-free nanocomposites.

  20. Effect of salmon protein hydrolysate and spray-dried plasma protein on growth performance of weanling pigs.

    PubMed

    Tucker, J L; Naranjo, V D; Bidner, T D; Southern, L L

    2011-05-01

    Two experiments, each consisting of 2 trials, were conducted to determine the effect of salmon protein hydrolysate (SPH) and spray-dried plasma protein (SDPP) fed during the first week postweaning and their subsequent effect on the growth performance of weanling pigs. Pigs were fed in a 3-phase feeding program with durations of 7 d for phase 1 in both Exp. 1 and 2; 14 or 15 d for phase 2 in Exp. 1 and 2, respectively; and 7 or 8 d for phase 3 in Exp. 1 and 2, respectively. Dietary treatments were fed only during phase 1, whereas the same diet was fed to all pigs in phases 2 and 3. Pigs were blocked by initial BW and sex, and littermates were balanced across treatments. Data from the 2 trials within each experiment were combined and analyzed together; no treatment × trial interactions (P > 0.10) were observed. In Exp. 1, a total of 324 weanling pigs (10 replications of 5 or 6 pigs per pen) with an average initial BW of 6.4 ± 1.3 kg were assigned to 1) a control diet with no SPH or SDPP, 2) 1.5% SPH, 3) 3.0% SPH, 4) 1.5% SDPP, 5) 3.0% SDPP, or 6) 1.5% SPH + 1.5% SDPP. Experiment 2 was similar to Exp. 1, but red blood cells were removed from all diets to reduce diet complexity. In Exp. 2, weanling pigs (n = 320, 14 replications of 5 or 6 pigs per pen) with an average initial BW of 5.4 ± 1.2 kg were assigned to 1) a control diet with no SPH or SDPP, 2) 1.5% SPH, 3) 1.5% SDPP, or 4) 1.5% SPH + 1.5% SDPP. Three batches of SPH were used, and each batch was analyzed for AA composition. In Exp. 1, the inclusion of SDPP or SPH during phase 1 did not affect (P > 0.10) ADG, ADFI, or G:F compared with those of pigs fed the control diet. No carryover effects on growth performance were observed in any of the subsequent phases. Overall, G:F was greater (P = 0.08) in pigs fed the 1.5% diets compared with those fed the 3.0% diets. In Exp. 2, no differences (P > 0.10) were observed in ADG, ADFI, or G:F among pigs fed the SPH or SDPP diets compared with those of pigs fed the

  1. Oxidative stability of a heme iron-fortified bakery product: Effectiveness of ascorbyl palmitate and co-spray-drying of heme iron with calcium caseinate.

    PubMed

    Alemán, Mercedes; Bou, Ricard; Tres, Alba; Polo, Javier; Codony, Rafael; Guardiola, Francesc

    2016-04-01

    Fortification of food products with iron is a common strategy to prevent or overcome iron deficiency. However, any form of iron is a pro-oxidant and its addition will cause off-flavours and reduce a product's shelf life. A highly bioavailable heme iron ingredient was selected to fortify a chocolate cream used to fill sandwich-type cookies. Two different strategies were assessed for avoiding the heme iron catalytic effect on lipid oxidation: ascorbyl palmitate addition and co-spray-drying of heme iron with calcium caseinate. Oxidation development and sensory acceptability were monitored in the cookies over one-year of storage at room temperature in the dark. The addition of ascorbyl palmitate provided protection against oxidation and loss of tocopherols and tocotrienols during the preparation of cookies. In general, ascorbyl palmitate, either alone or in combination with the co-spray-dried heme iron, prevented primary oxidation and hexanal formation during storage. The combination of both strategies resulted in cookies that were acceptable from a sensory point of view after 1year of storage.

  2. Applying Nanoscale Kirkendall Diffusion for Template-Free, Kilogram-Scale Production of SnO2 Hollow Nanospheres via Spray Drying System

    NASA Astrophysics Data System (ADS)

    Cho, Jung Sang; Ju, Hyeon Seok; Kang, Yun Chan

    2016-04-01

    A commercially applicable and simple process for the preparation of aggregation-free metal oxide hollow nanospheres is developed by applying nanoscale Kirkendall diffusion to a large-scale spray drying process. The precursor powders prepared by spray drying are transformed into homogeneous metal oxide hollow nanospheres through a simple post-treatment process. Aggregation-free SnO2 hollow nanospheres are selected as the first target material for lithium ion storage applications. Amorphous carbon microspheres with uniformly dispersed Sn metal nanopowder are prepared in the first step of the post-treatment process under a reducing atmosphere. The post-treatment of the Sn-C composite powder at 500 °C under an air atmosphere produces carbon- and aggregation-free SnO2 hollow nanospheres through nanoscale Kirkendall diffusion. The hollow and filled SnO2 nanopowders exhibit different cycling performances, with their discharge capacities after 300 cycles being 643 and 280 mA h g‑1, respectively, at a current density of 2 A g‑1. The SnO2 hollow nanospheres with high structural stability exhibit superior cycling and rate performances for lithium ion storage compared to the filled ones.

  3. The influence of spray-drying parameters on phase behavior, drug distribution, and in vitro release of injectable microspheres for sustained release.

    PubMed

    Meeus, Joke; Lenaerts, Maité; Scurr, David J; Amssoms, Katie; Davies, Martyn C; Roberts, Clive J; Van Den Mooter, Guy

    2015-04-01

    For ternary solid dispersions, it is indispensable to characterize their structure, phase behavior, and the spatial distribution of the dispersed drug as this might influence the release profile and/or stability of these formulations. This study shows how formulation (feed concentration) and process (feed rate, inlet air temperature, and atomizing air pressure) parameters can influence the characteristics of ternary spray-dried solid dispersions. The microspheres considered here consist of a poly(lactic-co-glycolic acid) (PLGA) surface layer and an underlying polyvinylpyrrolidone (PVP) phase. A poorly soluble active pharmaceutical ingredient (API) was molecularly dispersed in this matrix. Differences were observed in component miscibility, phase heterogeneity, particle size, morphology, as well as API surface coverage for selected spray-drying parameters. Observed differences are likely because of changes in the droplet generation, evaporation, and thus particle formation processes. However, varying particle characteristics did not influence the drug release of the formulations studied, indicating the robustness of this approach to produce particles of consistent drug release characteristics. This is likely because of the fact that the release is dominated by diffusion from the PVP layer through pores in the PLGA surface layer and that observed differences in the latter have no influence on the release.

  4. Preparation and Analysis of Co-precipitated, Biodegradable Poly-(Lactide-co-Glycolide) and Polyethylene Glycol Microspheres Prepared by Spray Drying

    NASA Astrophysics Data System (ADS)

    Javiya, Curie

    Biodegradable poly-(d,l-lactide-co-glycolide) (PLGA) based microspheres are commonly used for numerous clinical applications. PEG is a widely used polymer due to its hydrophilic, biocompatible, and nontoxic nature. In this study, different blends of PLGA/PEG microspheres were prepared using a spray drying technique. The microspheres were spherical with maximum yield found to be 60.3% and average particle size in the range of 2.4 to 3.1 microm. Under the spray drying processing conditions, the polymers showed full miscibility slightly below 15% w/w and partial miscibility up to 20% w/w of PEG in the blended microspheres. At higher temperatures, PLGA and PEG were miscible in all proportions used for the blended microspheres. Blending 10% w/w PEG in PLGA membranes showed significant reduction in attachment of macrophages compared to PLGA membranes. The in-vitro response of macrophage towards the miscible blends of PLGA/PEG microspheres was further characterized. Results showed some reduction in macrophage viability and activation, however, significant effects with PLGA/PEG microspheres were not observed.

  5. Effective Lactobacillus plantarum and Bifidobacterium infantis encapsulation with chia seed (Salvia hispanica L.) and flaxseed (Linum usitatissimum L.) mucilage and soluble protein by spray drying.

    PubMed

    Bustamante, Mariela; Oomah, B Dave; Rubilar, Mónica; Shene, Carolina

    2017-02-01

    Mucilage (M) and soluble protein (SP) extracted from chia seed and flaxseed were used as encapsulating material for two probiotic bacteria: Bifidobacterium infantis and Lactobacillus plantarum by spray drying. Probiotic survival and viability after spray drying and during storage were evaluated. B. infantis and L. plantarum displayed high survival (⩾98%) after encapsulation with mixtures of maltodextrin (MD) combined with M and SP from flaxseed (MD:FM:FSP - 7.5:0.2:7.5%, w/w/w) and chia seed (MD:CM:CSP - 7.5:0.6:7.5%, w/w/w), respectively. These ternary blends protected the probiotics and enhanced their resistance to simulated gastric juice and bile solution. Probiotics encapsulated with the ternary blends incorporated in instant juice powder exhibited high viability (>9Log10CFU/g) after 45days refrigerated storage. Encapsulation with the ternary blends reduced particle size of the probiotic powders thereby offering additional functional benefits. Our results reveal that chia seed and flaxseed are excellent sources of probiotic encapsulating agents.

  6. Effects of Spray-Drying Parameters on In Vitro Functional Properties of Camu-Camu (Myrciaria dubia Mc. Vaugh): A Typical Amazonian Fruit.

    PubMed

    Fujita, Alice; Souza, Volnei Brito; Daza, Luis Daniel; Fávaro-Trindade, Carmen Silvia; Granato, Daniel; Genovese, Maria Inés

    2017-03-22

    Camu-camu (Myrciaria dubia) fruit is a rich source of bioactive compounds but its shelf life is rather short. Therefore, this study was aimed to evaluate the effect of inlet air temperature (T) and concentration (C) of maltodextrin and arabic gum on the spray-drying process of commercial camu-camu pulps (São Paulo and Manaus). Moisture, solubility, total phenolics (TP), ascorbic acid (AA), and proanthocyanidins (PAC) contents, and in vitro antioxidant capacity of the powders (FRAP, DPPH, Folin-Ciocalteu's reducing capacity were measured). Arabic gum resulted in better yields (22% to 30%), powder solubility (84% to 90%), and lower losses of analyzed compounds than the powders manufactured with maltodextrin. Overall, inlet air temperature had a lower impact on the responses studied than the concentration of carrier agents. Polynomial equations were generated for AA (R(2) = 0.993), TP (R(2) = 0.735), PAC (R(2) = 0.946), and for the antioxidant capacity assays (0.867 ≤ R(2 ) ≤ 0.963). In addition, principal component analysis showed that the lowest concentration of carrier agents (6%) in spray drying resulted in the lowest losses of bioactive compounds and, consequently, the highest antioxidant capacity.

  7. Spray-drying process preserves the protective capacity of a breast milk-derived Bifidobacterium lactis strain on acute and chronic colitis in mice.

    PubMed

    Burns, Patricia; Alard, Jeanne; Hrdỳ, Jiri; Boutillier, Denise; Páez, Roxana; Reinheimer, Jorge; Pot, Bruno; Vinderola, Gabriel; Grangette, Corinne

    2017-02-24

    Gut microbiota dysbiosis plays a central role in the development and perpetuation of chronic inflammation in inflammatory bowel disease (IBD) and therefore is key target for interventions with high quality and functional probiotics. The local production of stable probiotic formulations at limited cost is considered an advantage as it reduces transportation cost and time, thereby increasing the effective period at the consumer side. In the present study, we compared the anti-inflammatory capacities of the Bifidobacterium animalis subsp. lactis (B. lactis) INL1, a probiotic strain isolated in Argentina from human breast milk, with the commercial strain B. animalis subsp. lactis BB12. The impact of spray-drying, a low-cost alternative of bacterial dehydration, on the functionality of both bifidobacteria was also investigated. We showed for both bacteria that the spray-drying process did not impact on bacterial survival nor on their protective capacities against acute and chronic colitis in mice, opening future perspectives for the use of strain INL1 in populations with IBD.

  8. Applying Nanoscale Kirkendall Diffusion for Template-Free, Kilogram-Scale Production of SnO2 Hollow Nanospheres via Spray Drying System

    PubMed Central

    Cho, Jung Sang; Ju, Hyeon Seok; Kang, Yun Chan

    2016-01-01

    A commercially applicable and simple process for the preparation of aggregation-free metal oxide hollow nanospheres is developed by applying nanoscale Kirkendall diffusion to a large-scale spray drying process. The precursor powders prepared by spray drying are transformed into homogeneous metal oxide hollow nanospheres through a simple post-treatment process. Aggregation-free SnO2 hollow nanospheres are selected as the first target material for lithium ion storage applications. Amorphous carbon microspheres with uniformly dispersed Sn metal nanopowder are prepared in the first step of the post-treatment process under a reducing atmosphere. The post-treatment of the Sn-C composite powder at 500 °C under an air atmosphere produces carbon- and aggregation-free SnO2 hollow nanospheres through nanoscale Kirkendall diffusion. The hollow and filled SnO2 nanopowders exhibit different cycling performances, with their discharge capacities after 300 cycles being 643 and 280 mA h g−1, respectively, at a current density of 2 A g−1. The SnO2 hollow nanospheres with high structural stability exhibit superior cycling and rate performances for lithium ion storage compared to the filled ones. PMID:27033088

  9. Spray-drying process preserves the protective capacity of a breast milk-derived Bifidobacterium lactis strain on acute and chronic colitis in mice

    PubMed Central

    Burns, Patricia; Alard, Jeanne; Hrdỳ, Jiri; Boutillier, Denise; Páez, Roxana; Reinheimer, Jorge; Pot, Bruno; Vinderola, Gabriel; Grangette, Corinne

    2017-01-01

    Gut microbiota dysbiosis plays a central role in the development and perpetuation of chronic inflammation in inflammatory bowel disease (IBD) and therefore is key target for interventions with high quality and functional probiotics. The local production of stable probiotic formulations at limited cost is considered an advantage as it reduces transportation cost and time, thereby increasing the effective period at the consumer side. In the present study, we compared the anti-inflammatory capacities of the Bifidobacterium animalis subsp. lactis (B. lactis) INL1, a probiotic strain isolated in Argentina from human breast milk, with the commercial strain B. animalis subsp. lactis BB12. The impact of spray-drying, a low-cost alternative of bacterial dehydration, on the functionality of both bifidobacteria was also investigated. We showed for both bacteria that the spray-drying process did not impact on bacterial survival nor on their protective capacities against acute and chronic colitis in mice, opening future perspectives for the use of strain INL1 in populations with IBD. PMID:28233848

  10. The Anti-Inflammatory Effect of Spray-Dried Plasma Is Mediated by a Reduction in Mucosal Lymphocyte Activation and Infiltration in a Mouse Model of Intestinal Inflammation

    PubMed Central

    Pérez-Bosque, Anna; Miró, Lluïsa; Amat, Concepció; Polo, Javier; Moretó, Miquel

    2016-01-01

    Spray-dried preparations from porcine and bovine plasma can alleviate mucosal inflammation in experimental models and improve symptoms in patients with enteropathy. In rodents, dietary supplementation with porcine spray-dried plasma (SDP) attenuates intestinal inflammation and improves the epithelial barrier function during intestinal inflammation induced by Staphylococcus aureus enterotoxin B (SEB). The aim of this study was to discern the molecular mechanisms involved in the anti-inflammatory effects of SDP. Male C57BL/6 mice were fed with 8% SDP or control diet (based on milk proteins) for two weeks, from weaning until day 33. On day 32, the mice were given a SEB dose (i.p., 25 µg/mouse) or vehicle. SEB administration increased cell recruitment to mesenteric lymph nodes and the percentage of activated Th lymphocytes and SDP prevented these effects). SDP supplementation increased the expression of interleukin 10 (IL-10) or transforming growth factor- β (TGF-β) compared to the SEB group. The SEB challenge increased six-fold the expression of mucosal addressin cell adhesion molecule 1 (MAdCAM-1) and intercellular adhesion molecule 1 (ICAM-1); and these effects were attenuated by SDP supplementation. SEB also augmented NF-κB phosphorylation, an effect that was prevented by dietary SDP. Our results indicate that the anti-inflammatory effects of SDP involve the regulation of transcription factors and adhesion molecules that reduce intestinal cell infiltration and the degree of the inflammatory response. PMID:27782068

  11. Acid-base interactions in amorphous solid dispersions of lumefantrine prepared by spray-drying and hot-melt extrusion using X-ray photoelectron spectroscopy.

    PubMed

    Song, Yang; Zemlyanov, Dmitry; Chen, Xin; Su, Ziyang; Nie, Haichen; Lubach, Joseph W; Smith, Daniel; Byrn, Stephen; Pinal, Rodolfo

    2016-12-05

    This study investigates drug-excipient interactions in amorphous solid dispersions (ASDs) of the model basic compound lumefantrine (LMN), with five acidic polymers. X-ray photoelectron spectroscopy (XPS) was used to measure the extent of the protonation of the tertiary amine in LMN by the five acidic polymers. The extent/efficiency of protonation of the ASDs was assessed a function of polymer type, manufacturing process (hot-melt extrusion vs. spray drying), and drug loading (DL). The most strongly acidic polymer, polystyrene sulfonic acid (PSSA) was found to be the most efficient polymer in protonating LMN, independently of manufacturing method and DL. The rank order for the protonation extent of LMN by each polymer is roughtly the same for both manufacturing processes. However, protonation efficiency of polymers of similar acidic strength ranged from ∼0% to 75% (HPMCAS and Eudragit L100-55, respectively), suggesting an important role of molecular/mixing effects. For some polymers, including Eudragit L100 55 and HPMCP, spray-drying resulted in higher protonation efficiency compared to hot-melt extrusion. This result is attributable to a more favorable encounter between acid and base groups, when exposed to each other in solution phase. Increasing DL led to decreased protonation efficiency in most cases, particularly for polyacrylic acid, despite having the highest content of acidic groups per unit mass. These results indicate that the combined effects of acid strength and mixing phenomena regulate the efficiency of acid-base interactions in the ASDs.

  12. Advances in metered dose inhaler technology with the development of a chlorofluorocarbon-free drug delivery system.

    PubMed

    Ross, D L; Gabrio, B J

    1999-01-01

    The impending phaseout of chlorofluorocarbon (CFC)-containing metered dose inhalers (MDIs) has challenged the pharmaceutical industry to rethink and redesign many components of the technology involved in delivering asthma medication to the lungs. Along with the emergence of the first formulation using the nonozone-depleting propellant, hydrofluoroalkane (HFA) 134a to replace CFC propellants, advances in drug delivery technology have improved the performance characteristics of the MDI itself. Although MDIs have remained the mainstay of asthma therapy for 40 years, MDI technology still presents challenges. Some of the shortcomings of existing CFC MDIs affect the reliability of dosing. These challenges have been addressed in the development of the first CFC-free beta-agonist for the treatment of asthma. Airomir CFC-free (salbutamol sulfate; 3M Pharmaceuticals, St. Paul, MN), which is currently available in over 30 countries and was recently approved in the United States (Proventil HFA; Schering-Plough, Madison, NJ), incorporates numerous design and technological improvements which together with the introduction of CFC-free propellants mark the beginning of the next generation of asthma therapy. Although the new generation of CFC-free MDIs incorporates several improvements in dose reproducibility, these changes should be virtually transparent to the patient switching from a CFC MDI to a CFC-free MDI. What may be noticeable is a "softer puff," which is the result of valve and actuator redesign. The taste of the new CFC-free product may also be a little different yet totally acceptable to users.

  13. Inhalation Injuries

    MedlinePlus

    ... you can inhale that can cause acute internal injuries. Particles in the air from fires and toxic ... and lung diseases worse. Symptoms of acute inhalation injuries may include Coughing and phlegm A scratchy throat ...

  14. Asthma Inhalers

    MedlinePlus

    ... an inhaler into the lungs. But CFCs are ozone-depleting substances (ODSs) that hurt the environment. Manufacturers ... inhalers, that do not rob the atmosphere of ozone. “The FDA [Food and Drug Administration] and various ...

  15. Inhalant Abuse

    MedlinePlus

    ... Who may be abusing inhalants?The most common abusers of inhalants are teenagers, especially those who are ... to your child about the dangers of trying drugs can help him or her make the right ...

  16. Spray-dried plasma promotes growth, modulates the activity of antioxidant defenses, and enhances the immune status of gilthead sea bream (Sparus aurata) fingerlings.

    PubMed

    Gisbert, E; Skalli, A; Campbell, J; Solovyev, M M; Rodríguez, C; Dias, J; Polo, J

    2015-01-01

    Terrestrial animal byproduct meals, including nonruminant blood meal and blood products, represent the largest and largely untapped safe source of animal protein available within the international market for the aquafeed industry. Spray-dried blood and spray-dried plasma (SDP) proteins have long been recognized as high-quality feed ingredients for farmed animals. In this study, we evaluated the inclusion of SDP from porcine blood (SDPP) in growing diets for gilthead sea bream. Three isonitrogenous (CP = 51.2%) and isolipidic (fat = 12.4%) diets manufactured by cold extrusion (0.8 to 1.5 mm pellet size) were prepared by substituting high-quality fish meal with 0, 3, and 6% SDPP. The diets were tested for a period of 60 d at 22°C with 4 replicates each (400-L cylindroconical tanks, 150 fish per tank, and initial density = 0.5 kg/m(3)). The SDPP inclusion in diets for gilthead sea bream fingerlings were evaluated in terms of growth performance, feed utilization, histological organization of the intestinal mucosa, activity of oxidative stress enzymes (catalase, glutathione S-transferase, glutathione peroxidase, and glutathione reductase) in the intestine, and nonspecific serum immune parameters (lysozyme and bactericidal activity). Results from this study indicated that dietary SDPP promoted fish growth in terms of BW and length; fish fed 3% SDPP were 10.5% heavier (P < 0.05) than those fed the control diet. Spray-dried plasma from porcine blood modulated the activity of the antioxidative defenses in the intestine (P < 0.05) and increased the density of goblet cells in the intestine (P < 0.05) and benefited the host by providing an effective immune barrier against gut pathogenic microbiota. The nonspecific serum immune response in fish fed diets with SDPP was greater (P < 0.05) than in fish fed the control diet. These results indicated that the inclusion of SDPP in gilthead sea bream feed could be beneficial for the fish by enhancing intestinal and serum innate immune

  17. Facile Sol-Gel/Spray-Drying Synthesis of Interweaved Si@TiO2&CNTs Hybrid Microsphere as Superior Anode Materials for Li-Ion Batteries

    NASA Astrophysics Data System (ADS)

    Wang, Jiyun; Hou, Xianhua; Li, Yana; Ru, Qiang; Qin, Haiqing; Hu, Shejun

    2016-11-01

    A unique intertwined structure of silicon-based composite (Si@TiO2&CNTs) has been synthesized by sol-gel and spray drying methods. The Si@TiO2&CNTs is mainly composed of three kinds of materials:the prepared nanosilicon particles, TiO2, and carbon nanotubes (CNTs). A layer of TiO2 particles is found effective for enhancing the electrical conductivity and structure stability of the silicon particles. Additionally, the twisted CNTs are beneficial to build a better conductive network, consequently improving the anode working conditions when the cell is charged or discharged. As a lithium ion battery anode, a specific capacity of approximately 1521 mAh g-1 after 100 cycles is obtained.

  18. Development and beyond: Strategy for long-term maintenance of an online laser diffraction particle size method in a spray drying manufacturing process.

    PubMed

    Medendorp, Joseph; Bric, John; Connelly, Greg; Tolton, Kelly; Warman, Martin

    2015-08-10

    The purpose of this manuscript is to present the intended use and long-term maintenance strategy of an online laser diffraction particle size method used for process control in a spray drying process. A Malvern Insitec was used for online particle size measurements and a Malvern Mastersizer was used for offline particle size measurements. The two methods were developed in parallel with the Mastersizer serving as the reference method. Despite extensive method development across a range of particle sizes, the two instruments demonstrated different sensitivities to material and process changes over the product lifecycle. This paper will describe the procedure used to ensure consistent alignment of the two methods, thus allowing for continued use of online real-time laser diffraction as a surrogate for the offline system over the product lifecycle.

  19. Sodium-ion storage properties of nickel sulfide hollow nanospheres/reduced graphene oxide composite powders prepared by a spray drying process and the nanoscale Kirkendall effect

    NASA Astrophysics Data System (ADS)

    Park, G. D.; Cho, J. S.; Kang, Y. C.

    2015-10-01

    Spray-drying and the nanoscale Kirkendall diffusion process are used to prepare nickel sulfide hollow nanospheres/reduced graphene oxide (rGO) composite powders with excellent Na-ion storage properties. Metallic Ni nanopowder-decorated rGO powders, formed as intermediate products, are transformed into composite powders of nickel sulfide hollow nanospheres/rGO with mixed crystal structures of Ni3S2 and Ni9S8 phases by the sulfidation process under H2S gas. Nickel sulfide/rGO composite powders with the main crystal structure of Ni3S2 are also prepared as comparison samples by the direct sulfidation of nickel acetate-graphene oxide (GO) composite powders obtained by spray-drying. In electrochemical properties, the discharge capacities at the 150th cycle of the nickel sulfide/rGO composite powders prepared by sulfidation of the Ni/rGO composite and nickel acetate/GO composite powders at a current density of 0.3 A g-1 are 449 and 363 mA h g-1, respectively; their capacity retentions, calculated from the tenth cycle, are 100 and 87%. The nickel sulfide hollow nanospheres/rGO composite powders possess structural stability over repeated Na-ion insertion and extraction processes, and also show excellent rate performance for Na-ion storage.Spray-drying and the nanoscale Kirkendall diffusion process are used to prepare nickel sulfide hollow nanospheres/reduced graphene oxide (rGO) composite powders with excellent Na-ion storage properties. Metallic Ni nanopowder-decorated rGO powders, formed as intermediate products, are transformed into composite powders of nickel sulfide hollow nanospheres/rGO with mixed crystal structures of Ni3S2 and Ni9S8 phases by the sulfidation process under H2S gas. Nickel sulfide/rGO composite powders with the main crystal structure of Ni3S2 are also prepared as comparison samples by the direct sulfidation of nickel acetate-graphene oxide (GO) composite powders obtained by spray-drying. In electrochemical properties, the discharge capacities at the

  20. Microencapsulation of betalains obtained from cactus fruit (Opuntia ficus-indica) by spray drying using cactus cladode mucilage and maltodextrin as encapsulating agents.

    PubMed

    Otálora, María Carolina; Carriazo, José Gregorio; Iturriaga, Laura; Nazareno, Mónica Azucena; Osorio, Coralia

    2015-11-15

    The microencapsulation of betalains from cactus fruit by spray drying was evaluated as a stabilization strategy for these pigments. The betalains used as active agent were extracted from purple fruits of Opuntia ficus-indica (BE) and encapsulated with maltodextrin and cladode mucilage MD-CM and only with MD. The microcapsulates were characterized by scanning electron microscopy (SEM), thermal analysis (TGA-DSC), tristimulus colorimetry, as well as, their humidity, water activity and dietary fiber content were also determined. The active agent content was measured by UV-Vis spectrophotometry and its composition confirmed by HPLC-ESIMS. A pigment storage stability test was performed at 18 °C and different relative humidities. The addition of CM in the formulation increased the encapsulation efficiency, diminished the moisture content, and allowed to obtain more uniform size and spherical particles, with high dietary fiber content. These microencapsulates are promising functional additive to be used as natural colorant in the food industry.

  1. Effect of the pH in the formation of β-galactosidase microparticles produced by a spray-drying process.

    PubMed

    Estevinho, Berta N; Ramos, Irena; Rocha, Fernando

    2015-07-01

    The objective of this work was to investigate the influence of pH in the microencapsulation process, using a modified chitosan to microencapsulate the enzyme β-galactosidase, by a spray-drying technique. Structural analysis of the surface of the particles was performed by scanning electron microscopy (SEM), showing that the obtained microparticles have an average diameter smaller than 3.5 μm and in general a regular shape. The activity of the enzyme was studied by spectrophotometric methods using the substrate O-nitrophenyl-β,D-galactopyranoside (ONPG). The parameters of Michaelis-Menten were calculated. The value of Km decreases with the decrease of the pH, which can be associated to an increase of the affinity between the enzyme and substrate to smaller pH's. The highest value of the parameter Vmax, representing the maximum reaction rate at a given enzyme concentration, was obtained at pH 6.

  2. Dietary specific antibodies in spray-dried immune plasma prevent enterotoxigenic Escherichia coli F4 (ETEC) post weaning diarrhoea in piglets.

    PubMed

    Niewold, T A; van Dijk, A J; Geenen, P L; Roodink, H; Margry, R; van der Meulen, J

    2007-10-06

    In order to establish the mechanism of spray dried plasma powder (SDPP) in improving pig health and performance, a diet containing either 8% SDPP, spray dried immune plasma powder (SDIPP), or control protein (soybean and whey) ration was fed to piglets in an experimental model of enterotoxigenic Escherichia coli F4 (ETEC) post-weaning diarrhoea (PWD). SDIPP was obtained from pigs immunized with a vaccine containing ETEC fimbrial subunit F4 and heat-labile toxin (LT), and SDPP from non-immunized controls. Average daily growth (ADG) was determined, and daily samples of rectal faeces were assessed for diarrhoea (as percentage of dry matter), and ETEC excretion (in CFU/g). SDPP and SDIPP significantly (p<0.05) reduced diarrhoea, and SDIPP significantly reduced ETEC excretion. ADG was not significantly (p>0.05) affected. After the experiment, 30% of piglets tested F4 receptor positive (F4R+). A significant correlation between F4R status and morbidity was found. In F4R+ animals, SDIPP significantly improved diarrhoea and ADG, and decreased ETEC excretion, and SDPP significantly improved diarrhoea and ADG. Surprisingly, SDPP reduced diarrhoea in F4R+ animals without significant reduction of ETEC excretion, which is most likely related to the presence of anti-LT antibodies in SDPP. The results show that oral protection against ETEC by SDPP is attributable to spontaneous antibodies, in this case anti-LT antibodies. Furthermore, the results indicate that the combination of anti-LT and anti-F4 antibodies as in SDIPP is most effective in ETEC prevention. Finally, the F4R distribution in the herd should be taken into account to correctly assess efficacy.

  3. The effect of chitosan molecular weight on the characteristics of spray-dried methotrexate-loaded chitosan microspheres for nasal administration.

    PubMed

    Sun, Yu; Cui, Fude; Shi, Kai; Wang, Jiamiao; Niu, Mengmeng; Ma, Ruijing

    2009-03-01

    In this article, the effect of the chitosan molecular weight (MW) on the characteristics of methotrexate (MTX)-encapsulated non-cross-linked chitosan microspheres was studied. Microspheres composed of low-molecular-weight (LMW, 40,000 Da), medium-molecular-weight (MMW, 480,000 Da) and high-molecular-weight (HMW, 850,000 Da) chitosan with the same degree of deacetylation (96%) were obtained by a simple spray-drying method. The MW of chitosan had a noticeable influence on the size distribution, encapsulation efficiency, micromeritic properties (angle of repose and bulk density), controlled release behavior, and mucoadhesive properties. The entrapment efficiencies were in the range of 90-99%. Spray-dried microspheres had a D(50) value of 3.3-4.9 microm, which was suitable for nasal insufflations. The microspheres with LMW chitosan have the best flowability and highest bulk density but were found to be poor in terms of adhesion and in controlling the release behavior of MTX. The MMW chitosan microspheres exhibited the strongest adhesion to the mucosal surface, and the angle of repose values were between 34 and 47 degrees. They could control the release rate by modifying the drug/polymer ratios. Microspheres with HMW chitosan exhibited a lower adhesion than MMW chitosan and a lower release rate of MTX. The physical state of MTX in the chitosan matrix was studied by differential scanning calorimetry, which indicated the presence of a solid dispersion of the amorphous drug in the chitosan matrix. Nasal ciliotoxity showed only minor cilia irritation due to the microspheres, and consequently, they are suitable for nasal drug delivery.

  4. Ultraviolet Light (UV) Inactivation of Porcine Parvovirus in Liquid Plasma and Effect of UV Irradiated Spray Dried Porcine Plasma on Performance of Weaned Pigs

    PubMed Central

    Polo, Javier; Rodríguez, Carmen; Ródenas, Jesús; Russell, Louis E.; Campbell, Joy M.; Crenshaw, Joe D.; Torrallardona, David; Pujols, Joan

    2015-01-01

    A novel ultraviolet light irradiation (UV-C, 254 nm) process was designed as an additional safety feature for manufacturing of spray dried porcine plasma (SDPP). In Exp. 1, three 10-L batches of bovine plasma were inoculated with 105.2±0.12 tissue culture infectious dose 50 (TCID50) of porcine parvovirus (PPV) per mL of plasma and subjected to UV-C ranging from 0 to 9180 J/L. No viable PPV was detected in bovine plasma by micro-titer assay in SK6 cell culture after UV-C at 2295 J/L. In Exp. 2, porcine plasma was subjected to UV-C (3672 J/L), then spray dried and mixed in complete mash diets. Diets were a control without SDPP (Control), UV-C SDPP either at 3% (UVSDPP3) or 6% (UVSDPP6) and non-UV-C SDPP at 3% (SDPP3) or 6% (SDPP6). Diets were fed ad libitum to 320 weaned pigs (26 d of age; 16 pens/diet; 4 pigs/pen) for 14 d after weaning and a common diet was fed d 15 to 28. During d 0 to 14, pigs fed UVSDPP3, UVSDPP6, or SDPP6 had higher (P < 0.05) weight gain and feed intake than control. During d 0 to 28, pigs fed UVSDPP3 and UVSDPP6 had higher (P < 0.05) weight gain and feed intake than control and SDPP3, and SDPP6 had higher (P < 0.05) feed intake than control. Also, pigs fed UVSDPP had higher (P < 0.05) weight gain than pigs fed SDPP. In conclusion, UV-C inactivated PPV in liquid plasma and UVSDPP used in pig feed had no detrimental effects on pig performance. PMID:26171968

  5. Ultraviolet Light (UV) Inactivation of Porcine Parvovirus in Liquid Plasma and Effect of UV Irradiated Spray Dried Porcine Plasma on Performance of Weaned Pigs.

    PubMed

    Polo, Javier; Rodríguez, Carmen; Ródenas, Jesús; Russell, Louis E; Campbell, Joy M; Crenshaw, Joe D; Torrallardona, David; Pujols, Joan

    2015-01-01

    A novel ultraviolet light irradiation (UV-C, 254 nm) process was designed as an additional safety feature for manufacturing of spray dried porcine plasma (SDPP). In Exp. 1, three 10-L batches of bovine plasma were inoculated with 10(5.2 ± 0.12) tissue culture infectious dose 50 (TCID50) of porcine parvovirus (PPV) per mL of plasma and subjected to UV-C ranging from 0 to 9180 J/L. No viable PPV was detected in bovine plasma by micro-titer assay in SK6 cell culture after UV-C at 2295 J/L. In Exp. 2, porcine plasma was subjected to UV-C (3672 J/L), then spray dried and mixed in complete mash diets. Diets were a control without SDPP (Control), UV-C SDPP either at 3% (UVSDPP3) or 6% (UVSDPP6) and non-UV-C SDPP at 3% (SDPP3) or 6% (SDPP6). Diets were fed ad libitum to 320 weaned pigs (26 d of age; 16 pens/diet; 4 pigs/pen) for 14 d after weaning and a common diet was fed d 15 to 28. During d 0 to 14, pigs fed UVSDPP3, UVSDPP6, or SDPP6 had higher (P < 0.05) weight gain and feed intake than control. During d 0 to 28, pigs fed UVSDPP3 and UVSDPP6 had higher (P < 0.05) weight gain and feed intake than control and SDPP3, and SDPP6 had higher (P < 0.05) feed intake than control. Also, pigs fed UVSDPP had higher (P < 0.05) weight gain than pigs fed SDPP. In conclusion, UV-C inactivated PPV in liquid plasma and UVSDPP used in pig feed had no detrimental effects on pig performance.

  6. Preparation, characterization and pulmonary pharmacokinetics of a new inhalable zanamivir dry powder.

    PubMed

    Cai, Xingshi; Yang, Yang; Xie, Xiangyang; Yu, Fanglin; Yang, Yanfang; Yang, Zhenbo; Zhang, Tao; Mei, Xingguo

    2016-07-01

    This work describes a new dry powder for inhalation containing zanamivir, which is less hygroscopic than Relenza®. The powders were prepared via a spray-drying technique using mannitol as the carrier. A 5(3) central composite design was used to optimize the formulations. The final optimized powders, characterized with an angle of repose 37.48°, an aerodynamic diameter of 2.346 μm and in vitro deposition of 58.54%, were obtained by using the predicted variable values. Relenza® absorbed a significant amount of water at 66%, 75% and 85% relative humidity (RH; weight changes of approximately 1.38%, 2.18% and 3.72%, respectively). In contrast, the weight change for the zanamivir dry powder inhalation (DPI) was negligible when the RH was increased to 66%. The in vivo potential for the optimized powders was studied further in rats via the endotracheal administration of an 8.4 mg/kg dose. The bioavailability was 116% relative to Relenza®. Fluorescence imaging monitored the zanamivir dry powder inhalers in rats. The results indicated that the zanamivir DPIs were effectively delivered to the lung. These results indicate that the spray-dried zanamivir DPIs were promising for pulmonary delivery.

  7. Substance use - inhalants

    MedlinePlus

    Substance abuse - inhalants; Drug abuse - inhalants; Drug use - inhalants; Glue - inhalants ... symptoms and may include: Strong cravings for the drug Having mood swings from feeling depressed to agitated ...

  8. Inhalable Ipratropium Bromide Particle Engineering with Multicriteria Optimization.

    PubMed

    Vinjamuri, Bhavani Prasad; Haware, Rahul V; Stagner, William C

    2016-11-21

    Spray-dried ipratropium bromide (IPB) microspheres for oral inhalation were engineered using Quality by Design. The interrogation of material properties, process parameters, and critical product quality attributes interplay enabled rational product design. A 2(7-3) screening design exhibited the Maillard reaction between L-leucine (LL) and lactose at studied outlet temperatures (OT) >130°C. A response surface custom design was used in conjunction with multicriteria optimization to determine the operating design space to achieve inhalable microparticles. Statistically significant predictive models were developed for volume median diameter (p = 0.0001, adjusted R (2)  = 0.9938), span (p = 0.0278, adjusted R (2)  = 0.7912), yield (p = 0.0020, adjusted R (2)  = 0.9320), and OT (p = 0.0082, adjusted R (2)  = 0.8768). An independent verification batch confirmed the model's predictive capability. The prediction and actual values were in good agreement. Particle size and span were 3.32 ± 0.09 μm and 1.71 ± 0.18, which were 4.7 and 5.3% higher than the predicted values. The process yield was 50.3%, compared to the predicted value of 65.3%. The OT was 100°C versus the predicted value of 105°C. The label strength of IPB microparticles was 99.0 to 105.9% w/w suggesting that enrichment occurred during the spray-drying process. The present study can be utilized to initiate the design of the first commercial IPB dry powder inhaler.

  9. Effect of enzymatic hydrolysis of starch on pasting, rheological and viscoelastic properties of milk-barnyard millet (Echinochloa frumentacea) blends meant for spray drying.

    PubMed

    Kumar, P Arun; Pushpadass, Heartwin A; Franklin, Magdaline Eljeeva Emerald; Simha, H V Vikram; Nath, B Surendra

    2016-10-01

    The influence of enzymatic hydrolysis of starch on the pasting properties of barnyard millet was studied using a rheometer. The effects of blending hydrolyzed barnyard millet wort with milk at different ratios (0:1, 1:1, 1:1.5 and 1:2) on flow and viscoelastic behavior were investigated. From the pasting curves, it was evident that enzymatically-hydrolyzed starch did not exhibit typical pasting characteristics expected of normal starch. The Herschel-Bulkley model fitted well to the flow behaviour data, with coefficient of determination (R(2)) ranging from 0.942 to 0.988. All milk-wort blends demonstrated varying degree of shear thinning with flow behavior index (n) ranging from 0.252 to 0.647. Stress-strain data revealed that 1:1 blend of milk to wort had the highest storage modulus (7.09-20.06Pa) and an elastically-dominant behavior (phase angle <45°) over the tested frequency range. The crossover point of G' and G" shifted to higher frequencies with increasing wort content. From the flow and viscoelastic behavior, it was concluded that the 1:1 blend of milk to wort would have least phase separation and better flowability during spray drying.

  10. Preparation of Spray-Dried Soy Isoflavone-Loaded Gelatin Microspheres for Enhancement of Dissolution: Formulation, Characterization and in Vitro Evaluation

    PubMed Central

    Panizzon, Gean Pier; Bueno, Fernanda Giacomini; Ueda-Nakamura, Tânia; Nakamura, Celso Vataru; Dias Filho, Benedito Prado

    2014-01-01

    The most bioactive soy isoflavones (SI), daidzein (DAI) and genistein (GEN) have poor water solubility, which reduces their bioavailability and health benefits and limits their use in industry. The goal of this study was to develop and characterize a new gelatin matrix to microencapsulate DAI and GEN from soy extract (SE) by spray drying, in order to obtain solid dispersions to overcome solubility problems and to allow controlled release. The influences of 1:2 (MP2) and 1:3 (MP3) SE/polymer ratios on the solid state, yield, morphology, encapsulation efficiency, particle size distribution, release kinetics and cumulative release were evaluated. Analyses showed integral microparticles and high drug content. MP3 and MP2 yield were 43.6% and 55.9%, respectively, with similar mean size (p > 0.05), respectively. X-ray diffraction revealed the amorphous solid state of SE. In vitro release tests showed that dissolution was drastically increased. The results indicated that SE microencapsulation might offer a good system to control SI release, as an alternative to improve bioavailability and industrial applications. PMID:25494200

  11. Li EXCESS Li4+xTi5-xO12-δ/C COMPOSITE USING SPRAY-DRYING METHOD AND ITS ELECTRODE PROPERTIES

    NASA Astrophysics Data System (ADS)

    Yoshikawa, Daisuke; Suzuki, Norio; Kadoma, Yoshihiro; Ui, Koichi; Kumagai, Naoaki

    2012-03-01

    We have prepared a lithium excess carbon composite material, Li4+xTi5-xO12-δ/C (LTO/C), using various amounts of sucrose as a carbon source by the spray-drying method. The prepared materials were characterized by X-ray diffraction (XRD), transmission electron microscopy (TEM), and elemental analysis. The prepared material had the Li4Ti5O12 phase including 3.9-18.4 wt.% carbon. Transmission electron microscopy images and the selected area diffraction (SAD) pattern showed that the prepared materials consisted of a carbon nanonetwork in the LTO/C composite. The charge-discharge cycling tests were carried out using the R2032 coin-type cell under the following conditions; 1.2-3.0 V, 0.1 C-10 C (1 C = 175 mA g-1), 25°C. Based on the electrochemical results, the electrode performance of the prepared material was improved with increasing amounts of residual carbon, in particular, LTO/C including 6.2 wt.% residual carbon exhibited the best electrode performance of 156 mAh g-1 at 1 C during 50 cyclings when compared to the other materials.

  12. Facile spray-drying/pyrolysis synthesis of core-shell structure graphite/silicon-porous carbon composite as a superior anode for Li-ion batteries

    NASA Astrophysics Data System (ADS)

    Li, Min; Hou, Xianhua; Sha, Yujing; Wang, Jie; Hu, Shejun; Liu, Xiang; Shao, Zongping

    2014-02-01

    A silicon/graphite/amorphous carbon (Si/C) composite with a low silicon content in a core-shell structure has been easily synthesized using a simple method based on spray drying in combination with a subsequent pyrolysis process; natural graphite serves as the core, and silicon nanoparticles, which filled in the porous carbon matrix formed from the pyrolysis of citric acid and pitch precursors, serve as the shell. The combination of the core-shell structure for the composite and porous carbon-coating layer accommodates the large volume change of the silicon during the lithium intercalation/extraction process, thus stabilizing the electrode structure during discharge/charge cycles. As an anode material, the as-obtained Si/C composite demonstrates high capacity and excellent cycle stability. An initial specific discharge capacity of approximately 723.8 mAh g-1 and a reversible specific capacity of approximately 600 mAh g-1 after 100 cycles at a constant density of 100 mA g-1 are reached, about two times the values for graphite. Due to the simple synthesis process and the excellent performance of the resulted electrode, great commercial potential is envisioned.

  13. Improving the stability and antioxidant properties of sesame oil: water-soluble spray-dried emulsions from new transesterified phenolic derivatives.

    PubMed

    Alencar, Juliana; Gosset, Gaëlle; Robin, Maxime; Pique, Valérie; Culcasi, Marcel; Clément, Jean-Louis; Mercier, Anne; Pietri, Sylvia

    2009-08-26

    Hydrosoluble sesame oil fatty acid transesters having enhanced antioxidant activities were synthesized in a two-step process. The key step involved the biocatalyzed (lipase from Candida antarctica) acylation of sesame oil methanolic ester with either vanillyl (VNA) or piperonyl benzylic alcohols, or 5-hydroxymethyl resorcinol (5-HMR). These substrates were selected to introduce phenolic or sesamol structurally related frameworks. The VNA and 5-HMR-derived transesters were obtained with 20-40% yields and retained the starting proportions of sesame oil linoleic, oleic, and saturated acids, these fatty acids also being the only constituents of the nonesterified fraction. The VNA-derived transester showed the best antioxidant capacity in standard assays and was processed as the unique lipid phase of spray-dried emulsions containing a high level of linoleic acid phenolic ester. These emulsions provided a high degree of protection to UV-irradiated fibroblasts, through the potential synergy between VNA antioxidant action and replenishment of damaged membranes by unsaturated fatty acids.

  14. Preparation of Spray-Dried Soy Isoflavone-Loaded Gelatin Microspheres for Enhancement of Dissolution: Formulation, Characterization and in Vitro Evaluation.

    PubMed

    Panizzon, Gean Pier; Bueno, Fernanda Giacomini; Ueda-Nakamura, Tânia; Nakamura, Celso Vataru; Dias Filho, Benedito Prado

    2014-12-08

    The most bioactive soy isoflavones (SI), daidzein (DAI) and genistein (GEN) have poor water solubility, which reduces their bioavailability and health benefits and limits their use in industry. The goal of this study was to develop and characterize a new gelatin matrix to microencapsulate DAI and GEN from soy extract (SE) by spray drying, in order to obtain solid dispersions to overcome solubility problems and to allow controlled release. The influences of 1:2 (MP2) and 1:3 (MP3) SE/polymer ratios on the solid state, yield, morphology, encapsulation efficiency, particle size distribution, release kinetics and cumulative release were evaluated. Analyses showed integral microparticles and high drug content. MP3 and MP2 yield were 43.6% and 55.9%, respectively, with similar mean size (p > 0.05), respectively. X-ray diffraction revealed the amorphous solid state of SE. In vitro release tests showed that dissolution was drastically increased. The results indicated that SE microencapsulation might offer a good system to control SI release, as an alternative to improve bioavailability and industrial applications.

  15. Original research paper. Characterization and taste masking evaluation of microparticles with cetirizine dihydrochloride and methacrylate-based copolymer obtained by spray drying.

    PubMed

    Amelian, Aleksandra; Szekalska, Marta; Ciosek, Patrycja; Basa, Anna; Winnicka, Katarzyna

    2017-03-01

    Taste of a pharmaceutical formulation is an important parameter for the effectiveness of pharmacotherapy. Cetirizine dihydrochloride (CET) is a second-generation antihistamine that is commonly administered in allergy treatment. CET is characterized by extremely bitter taste and it is a great challenge to successfully mask its taste; therefore the goal of this work was to formulate and characterize the microparticles obtained by the spray drying method with CET and poly(butyl methacrylate-co-(2-dimethylaminoethyl) methacrylate-co-methyl methacrylate 1:2:1 copolymer (Eudragit E PO) as a barrier coating. Assessment of taste masking by the electronic tongue has revealed that designed formulations created an effective taste masking barrier. Taste masking effect was also confirmed by the in vivo model and the in vitro release profile of CET. Obtained data have shown that microparticles with a drug/polymer ratio (0.5:1) are promising CET carriers with efficient taste masking potential and might be further used in designing orodispersible dosage forms with CET.

  16. Enhanced photocatalytic performances of hierarchical ZnO/ZnAl2O4 microsphere derived from layered double hydroxide precursor spray-dried microsphere.

    PubMed

    Huo, Ruijie; Kuang, Ye; Zhao, Zhiping; Zhang, Fazhi; Xu, Sailong

    2013-10-01

    Layered double hydroxides (LDHs), also called hydrotalcites, have been widely investigated for degradation of dye molecules, in the forms of direct photocatalysts, supports or precursors to ZnO-containing photocatalysts. LDH precursor-derived ZnO/ZnAl2O4 photocatalytic nanostructures have hitherto been created, involving ZnO/ZnAl2O4 powder and templated hierarchical frameworks with laboratory-scale preparations. We herein report a scalable preparation of ZnO/ZnAl2O4 microsphere derived from ZnAl-LDH precursor spray-dried microsphere. Survey of textural properties shows that ZnO/ZnAl2O4 microspheres maintain the hierarchically spherical feature and the relatively large surface area. Photocatalytic evaluation under UV irradiation shows that the ZnO/ZnAl2O4 microspheres exhibit highly enhanced photodegradation performance to methylene blue (MB) in comparison with the commercial ZnO powder. A preferential photodegradation to methyl orange (MO) of the MO/MB mixture was also observed, which was illustrated experimentally in terms of the favorable interaction and distribution between basic MO molecules and the acidic-site ZnO/ZnAl2O4 photocatalyst. Our results may initiate large-scale production of microspheres with promising photocatalytic performances.

  17. Influence of heat treatment on spray-dried mixtures of Amioca starch and Carbopol 974P used as carriers for nasal drug delivery.

    PubMed

    Coucke, D; Pringels, E; Foreman, P; Adriaensens, P; Carleer, R; Remon, J P; Vervaet, C

    2009-08-13

    A mucoadhesive spray-dried starch/poly(acrylic acid) powder underwent different heat treatments in order to induce cross-linking between the functional groups of starch (Amioca) and poly(acrylic acid) (Carbopol 974P). After heat treatment the water-absorbing capacity, viscosity and elasticity of the mucoadhesive powder increased. NMR analysis in combination with FT-IR indicated that heat treatment induced a low degree of cross-linking between the polymers. Nasal administration of Amioca/Carbopol 974P powders without heat treatment resulted in an absolute bioavailability in rabbits of 8.2+/-3.0% for insulin. Due to the difference in water-absorbing capacity (which opened the tight junctions of the nasal mucosa), elasticity and plasticity (which reduced mucociliairy clearance and prolonged residence time) heat treatment at 120 degrees C improved the bioavailability: 26.4+/-21.9, 36.5+/-11.0 and 19.3+/-17.3% after heat treatment during 30 min, 1 h and 4 h, respectively. Heat treatment at 60 degrees C was less efficient. This study demonstrated that the nasal insulin absorption improved via heat treatment of the Amioca/Carbopol 974P powder (prior to the addition of insulin). The bioavailability-enhancing effect of a 1 h heat treatment at 120 degrees C was confirmed using the same polymer matrix in combination with different drugs (salmon calcitonin, human growth hormone and metoprolol tartrate).

  18. Effect of bovine colostrum, cheese whey, and spray-dried porcine plasma on the in vitro growth of probiotic bacteria and Escherichia coli.

    PubMed

    Champagne, Claude P; Raymond, Yves; Pouliot, Yves; Gauthier, Sylvie F; Lessard, Martin

    2014-05-01

    The aim of this study is to evaluate the effects of defatted colostrum (Col), defatted decaseinated colostrum whey, cheese whey, and spray-dried porcine plasma (SDPP) as supplements of a growth medium (de Man - Rogosa - Sharpe (MRS) broth) on the multiplication of lactic acid bacteria, probiotic bacteria, and potentially pathogenic Escherichia coli. Using automated spectrophotometry (in vitro system), we evaluated the effect of the 4 supplements on maximum growth rate (μ(max)), lag time (LagT), and biomass (OD(max)) of 12 lactic acid bacteria and probiotic bacteria and of an E. coli culture. Enrichment of MRS broth with a Col concentration of 10 g/L increased the μ(max) of 5 of the 12 strains by up to 55%. Negative effects of Col or SDPP on growth rates were also observed with 3 probiotic strains; in one instance μ(max) was reduced by 40%. The most effective inhibitor of E. coli growth was SDPP, and this effect was not linked to its lysozyme content. The positive effect of enrichment with the dairy-based ingredient might be linked to enrichment in sugars and increased buffering power of the medium. These in vitro data suggest that both Col and SDPP could be considered as supplements to animal feeds to improve intestinal health because of their potential to promote growth of probiotic bacteria and to inhibit growth of pathogenic bacteria such as E. coli.

  19. Characterization of a New High-Dose Dry Powder Inhaler (DPI) Based on a Fluidized Bed Design

    PubMed Central

    Farkas, Dale R.; Hindle, Michael; Longest, P. Worth

    2015-01-01

    The objective of this study was to develop a new high-efficiency dry powder inhaler (DPI) that can effectively aerosolize large masses (25–100 mg) of spray dried powder formulations. The DPI was designed to implement a concept similar to a fluidized bed for aerosolization using small mixing balls made of polytetrafluoroethylene (PTFE) along with a larger, hollow dosing sphere filled with the powder. The performance of the fluidized bed DPI was compared, based on emitted dose (ED) and aerosolization efficiency, to other recently developed capsule-based DPIs that were designed to accommodate smaller powder masses (~2–20 mg). The inhalers were tested with spray dried excipient enhanced growth formulations that contained an antibiotic (ciprofloxacin) and hygroscopic excipient (mannitol). The new fluidized bed design produced an ED of 71% along with a mass median aerodynamic diameter (MMAD) of 1.53 µm and fine particle fractions (FPFs) less than 5 µm and 1 µm of 93% and 36%, respectively, when used to deliver a 100 mg loaded mass of EEG powder with the advantage of not requiring multiple capsules. Surprisingly, performance of the device was further improved by removing the mixing balls from the inhaler and only retaining the dose containment sphere. PMID:25986955

  20. Characterization of a New High-Dose Dry Powder Inhaler (DPI) Based on a Fluidized Bed Design.

    PubMed

    Farkas, Dale R; Hindle, Michael; Longest, P Worth

    2015-11-01

    The objective of this study was to develop a new high-efficiency dry powder inhaler (DPI) that can effectively aerosolize large masses (25-100 mg) of spray dried powder formulations. The DPI was designed to implement a concept similar to a fluidized bed for aerosolization using small mixing balls made of polytetrafluoroethylene along with a larger, hollow dosing sphere filled with the powder. The performance of the fluidized bed DPI was compared, based on emitted dose (ED) and aerosolization efficiency, to other recently developed capsule-based DPIs that were designed to accommodate smaller powder masses (~2-20 mg). The inhalers were tested with spray dried excipient enhanced growth (EEG) formulations that contained an antibiotic (ciprofloxacin) and hygroscopic excipient (mannitol). The new fluidized bed design produced an ED of 71% along with a mass median aerodynamic diameter of 1.53 μm and fine particle fractions <5 and 1 μm of 93 and 36%, respectively, when used to deliver a 100 mg loaded mass of EEG powder with the advantage of not requiring multiple capsules. Surprisingly, performance of the device was further improved by removing the mixing balls from the inhaler and only retaining the dose containment sphere.

  1. Effects of spray-drying and choice of solid carriers on concentrations of Labrasol® and Transcutol® in solid self-microemulsifying drug delivery systems (SMEDDS).

    PubMed

    Li, Liang; Yi, Tao; Lam, Christopher Wai-Kei

    2013-01-02

    Solid self-microemulsifying drug delivery systems (SMEDDS) have been used increasingly for improving the bioavailability of hydrophobic drugs. Labrasol® and Transcutol® are used widely as surfactant and solubilizer in the formulation of solid SMEDDS. We investigated the effects of spray-drying and the use of different solid carriers on concentrations of Labrasol® and Transcutol® in solid SMEDDS with scutellarin as the formulated drug. Liquid and gas chromatography tandem mass spectrometry (LC-MS and GC-MS) methods were developed for measuring low concentrations of Labrasol® and Transcutol®. In the preparation of solid SMEDDS, lactose, hydroxypropylmethyl cellulose (HPMC) and microcrystalline cellulose (MCC) were used as solid carriers. Judging from the retention ratios of Labrasol® and Transcutol®, the droplet size of solid SMEDDS increased after spray-drying of liquid SMEDDS, and concentrations of these excipients decreased after the solidifying procedure. In such reduction, Lactose and HPMC were found to preserve Labrasol® and Transcutol® better than MCC during spray-drying, and the resultant droplet sizes were smaller than that of MCC. Labrasol® and Transcutol® showed good thermal stability at 60 °C degree for 10 days. It can be concluded that spray-drying could increase the droplet size of solid SMEDDS and decreased the concentration of Labrasol® and Transcutol® therein, while water-soluble solid carriers could preserve Labrasol® and Transcutol® better than insoluble carriers in the solid SMEDDS.

  2. Ciclesonide Oral Inhalation

    MedlinePlus

    ... ciclesonide inhaler while you are near an open flame or a heat source. The inhaler may explode ... inhaler near a heat source or an open flame. Protect the inhaler from freezing and direct sunlight. ...

  3. Fluticasone Oral Inhalation

    MedlinePlus

    ... aerosol inhaler while you are near an open flame or a heat source. The inhaler may explode ... inhaler near a heat source or an open flame. Protect the inhaler from freezing and direct sunlight. ...

  4. Flunisolide Oral Inhalation

    MedlinePlus

    ... flunisolide inhaler while you are near an open flame or a heat source. The inhaler may explode ... inhaler near a heat source or an open flame. Protect the inhaler from freezing and direct sunlight. ...

  5. Solid dispersions of itraconazole for inhalation with enhanced dissolution, solubility and dispersion properties.

    PubMed

    Duret, Christophe; Wauthoz, Nathalie; Sebti, Thami; Vanderbist, Francis; Amighi, Karim

    2012-05-30

    The purpose of this study was to produce a dry powder for inhalation (DPI) of a poorly soluble active ingredient (itraconazole: ITZ) that would present an improved dissolution rate and enhanced solubility with good aerosolization properties. Solid dispersions of amorphous ITZ, mannitol and, when applicable, D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) were produced by spray-drying hydro-alcoholic solutions in which all agents were dissolved. These dry formulations were characterized in terms of their aerosol performances and their dissolution, solubility and physical properties. Modulate differential scanning calorimetry and X-ray powder diffraction analyses showed that ITZ recovered from the different spray-dried solutions was in an amorphous state and that mannitol was crystalline. The inlet drying temperature and, indirectly, the outlet temperature selected during the spray-drying were critical parameters. The outlet temperature should be below the ITZ glass transition temperature to avoid severe particle agglomeration. The formation of a solid dispersion between amorphous ITZ and mannitol allowed the dry powder to be produced with an improved dissolution rate, greater saturation solubility than bulk ITZ and good aerosol properties. The use of a polymeric surfactant (such as TPGS) was beneficial in terms of dissolution rate acceleration and solubility enhancement, but it also reduced aerosol performance. For example, significant dissolution rate acceleration (f(2)<50) and greater saturation solubility were obtained when introducing 1% (w/w) TPGS (mean dissolution time dropped from 50.4 min to 36.9 min and saturation solubility increased from 20 ± 3 ng/ml to 46 ± 2 ng/ml). However, the fine particle fraction dropped from 47 ± 2% to 37.2 ± 0.4%. This study showed that mannitol solid dispersions may provide an effective formulation type for producing DPIs of poorly soluble active ingredients, as exemplified by ITZ.

  6. Spherical agglomerates of pure drug nanoparticles for improved pulmonary delivery in dry powder inhalers

    NASA Astrophysics Data System (ADS)

    Hu, Jun; Dong, Yuancai; Pastorin, Giorgia; Ng, Wai Kiong; Tan, Reginald B. H.

    2013-04-01

    The aim of this study was to produce micron-sized spherical agglomerates of pure drug nanoparticles to achieve improved aerosol performance in dry powder inhalers (DPIs). Sodium cromoglicate was chosen as the model drug. Pure drug nanoparticles were prepared through a bottom-up particle formation process, liquid antisolvent precipitation, and then rapidly agglomerated into porous spherical microparticles by immediate (on-line) spray drying. Nonporous spherical drug microparticles with similar geometric size distribution were prepared by conventional spray drying of the aqueous drug solution, which together with the mechanically micronized drug particles were used as the control samples. The three samples were characterized by field emission scanning electron microscopy, laser diffraction, Brunauer-Emmett-Teller analysis, density measurement, powder X-ray diffraction, and in vitro aerosol deposition measurement with a multistage liquid impinger. It was found that drug nanoparticles with a diameter of 100 nm were precipitated and agglomerated into highly porous spherical microparticles with a volume median diameter ( D 50 %) of 2.25 ± 0.08 μm and a specific surface area of 158.63 ± 3.27 m2/g. In vitro aerosol deposition studies showed the fine particle fraction of such spherical agglomerates of drug nanoparticles was increased by more than 50 % in comparison with the control samples, demonstrating significant improvements in aerosol performance. The results of this study indicated the potential of the combined particle engineering process of liquid antisolvent precipitation followed by immediate (on-line) spray drying in the development of novel DPI drug products with improved aerosol performance.

  7. Inhalation Injury.

    DTIC Science & Technology

    1994-01-01

    alpha,-antitrypsin resulting cur most often as the result of tracheal in prolonged action of proteases such as or laryngeal damage from the endotra... curs is determined by physicochemical Turbulent airflow, such as at bifurca- properties of the inhaled substance, its tions of the airway, separates

  8. Evaluation of spray-dried lignin-based formulations and adjuvants as solar protectants for the granulovirus of the codling moth, Cydia pomonella (L).

    PubMed

    Arthurs, S P; Lacey, L A; Behle, R W

    2006-10-01

    Commercial formulations of the codling moth, Cydia pomonella L., granulovirus (CpGV) are limited by their short residual activity under orchard conditions in the Pacific Northwest. We evaluated spray-dried lignin-encapsulated formulations of CpGV for improved solar stability based on laboratory bioassays with a solar simulator and in field tests in an infested apple orchard. In laboratory tests, aqueous lignin formulations containing a high dosage of 3 x 10(10) occlusion bodies (OB)/L, with and without the additives titanium dioxide (TiO(2)) and sugar, provided significant solar protection of virus, i.e., mortality of codling moth exposed to lignin formulations that had been irradiated with 9.36 x 10(6) joules/m(2) was 92-94%, compared with 66-67% from a glycerin-stabilized product (Cyd-X) or suspension of pure unformulated virus at the same rates. By comparison, a lower dosage of the lignin formulation (3 x 10(8)OB/L) did not provide significant solar protection. Equivalent dosage-dependent patterns in solar protection were observed in further tests with the lignin formulation, when an intermediate (3 x 10(9)OB/L) as well as the low dosage provided no solar protection. Equivalent rates of a blank lignin formulation (containing no virus) did not affect larval mortality, suggesting a protective effect of the lignin on the virus at the high rate. The use of several spray adjuvants, 'NuFilm-17' and 'Organic Biolink' (sticker-spreaders at 0.06% v/v), 'Raynox' (sunburn protectant at 5% v/v), and 'Trilogy'(neem oil at 1% v/v) did not provide solar protection of a commercial CpGV preparation in laboratory tests. In season long orchard tests (Golden Delicious), the lignin formulation of CpGV applied at 6.57 x 10(12)OB/ha did not significantly improve control of codling moth or protection of fruit compared with Cyd-X at equivalent rates. Our studies show that lignin-based CpGV formulations provided solar protection at relatively high virus dosages. The testing of lignin

  9. Subsequent growth performance and digestive physiology of broilers fed on starter diets containing spray-dried porcine plasma as a substitute for meat meal.

    PubMed

    Beski, S S M; Swick, R A; Iji, P A

    2015-01-01

    A 4 × 2 factorial experiment was conducted to investigate the effect of inclusion of spray-dried porcine plasma (SDPP), in lieu of meat meal, in the starter diet on performance and digestive physiology of broiler chickens between hatch and 35 d of age. Four levels of SDPP (0, 5, 10 or 20 g/kg) were included in the starter diets in lieu of meat meal on either wheat- or maize-based diets. Over the first 10 d, and throughout the 35-d experimental period, birds gained more body weight with increasing concentrations of SDPP regardless to the type of grain used. Inclusion of SDPP in the starter diet markedly improved feed per gain in the starter phase and across the 35-d study. There was no significant effect of the type of grain and its interaction with SDPP on the body weight gain and feed per gain for the two assessed periods. At d 10, the relative weight of the gizzard+proventriculus, spleen and liver increased with increasing concentrations of SDPP. At 24 d of age, the grain and SDPP inclusion significantly interacted, depressing the weight of bursa and spleen in birds that received the highest concentration of SDPP in the maize-based diet. Birds fed on the maize-based diets had higher relative weight of pancreas than those on the wheat-based diets. Increasing concentrations of SDPP in the starter diet improved the activities of maltase, sucrase and alkaline phosphatase at 24 d of age. The interaction of grain and SDPP concentration was significant for sucrase activity in birds on the wheat-based diets. Chickens on maize-based diets had higher alkaline phosphatase and maltase activities than those on wheat-based diets. Chicks that were offered SDPP-containing starter diets had longer villi, deeper crypts and lower villi/crypt than the control at 24 d of age regardless of the grain type used. Furthermore, longer villi and larger villi/crypt were found in chicken groups fed on wheat-based diets than those on maize-based diets. Chickens on maize-based diets had higher

  10. Tetracycline-HCl-loaded poly(DL-lactide-co-glycolide) microspheres prepared by a spray drying technique: influence of gamma-irradiation on radical formation and polymer degradation.

    PubMed

    Bittner, B; Mäder, K; Kroll, C; Borchert, H H; Kissel, T

    1999-05-01

    Tetracycline-HCl (TCH)-loaded microspheres were prepared from poly(lactide-co-glycolide) (PLGA) by spray drying. The drug was incorporated in the polymer matrix either in solid state or as w/o emulsion. The spin probe 4-hydroxy-2,2,6, 6-tetramethyl-piperidine-1-oxyl (TEMPOL) and the spin trap tert-butyl-phenyl-nitrone (PBN) were co-encapsulated into the TCH-loaded and placebo particles. We investigated the effects of gamma-irradiation on the formation of free radicals in polymer and drug and the mechanism of chain scission after sterilization. Gamma-Irradiation was performed at 26.9 and 54.9 kGy using a 60Co source. The microspheres were characterized especially with respect to the formation of radicals and in vitro polymer degradation. Electron paramagnetic resonance (EPR) spectroscopy, gel permeation chromatography (GPC), differential scanning calorimetry (DSC), high-performance liquid chromatography (HPLC), gas chromatography-mass spectroscopy (GC-MS), and scanning electron microscopy (SEM) were used for characterization of the microspheres. Using EPR spectroscopy, we successfully detected gamma-irradiation induced free radicals within the TCH-loaded microspheres, while unloaded PLGA did not contain radicals under the same conditions. The relatively low glass transition temperature of the poly(dl-lactide-co-glycolide) (37-39 degrees C) seems to favor subsequent reactions of free radicals due to the high mobility of the polymeric chains. Because of the high melting point of TCH (214 degrees C), the radicals can only be stabilized in drug loaded microspheres. In order to determine the mechanism of polymer degradation after exposure to gamma-rays, the spin trap PBN and the spin probe TEMPOL were encapsulated in the microspheres. gamma-Irradiation of microspheres containing PBN resulted in the formation of a lipophilic spin adduct, indicating that a polymeric radical was generated by random chain scission. Polymer degradation by an unzipping mechanism would have

  11. Dry Powder Formulation of Plasmid DNA and siRNA for Inhalation.

    PubMed

    Chow, Michael Y T; Lam, Jenny K W

    2015-01-01

    Nucleic acid therapeutics has huge potential for the treatment of a wide range of diseases including respiratory diseases. Plasmid DNA (pDNA) and small interfering RNA (siRNA) are the two most widely investigated nucleic acids for therapeutic development. However, efficient and safe delivery of nucleic acids is still a major hurdle in translating nucleic acid therapy into clinical practice. For the treatment of respiratory diseases, administration via inhalation is the most direct and effective way to deliver therapeutic nucleic acids to the lungs. Although liquid aerosol formulation is investigated in most of the studies, it is not desirable in terms of maintaining the stability of nucleic acid especially during long-term storage. This problem could be circumvented by formulating the therapeutic nucleic acids into dry powder for inhalation, and should be considered as the future direction of developing inhalable nucleic acids. In this review, the three major particle engineering methods investigated for the preparation of inhalable pDNA and siRNA formulations, including spray drying (SD), spray freeze drying (SFD) and supercritical fluid (SFC) drying, are discussed and compared. Moreover, common assessment methods and the challenges of evaluating the biological activities of inhalable nucleic acid powders are also reviewed.

  12. Spray-dried milk supplemented with alpha-linolenic acid or eicosapentaenoic acid and docosahexaenoic acid decreases HMG Co A reductase activity and increases biliary secretion of lipids in rats.

    PubMed

    Ramaprasad, Talahalli R; Srinivasan, Krishnapura; Baskaran, Vallikannan; Sambaiah, Kari; Lokesh, Belur R

    2006-05-01

    In our earlier study, we have shown that rats fed spray-dried milk containing alpha-linolenic acid (LNA 18:3 n-3) or eicosapentaenoic acid (EPA 20:5 n-3) and docosahexaenoic acid (DHA 22:6 n-3) had significantly lower amounts of serum and liver cholesterol. To evaluate the mechanism for hypocholesterolemic effect of n-3 fatty acids containing milk formulation, we fed male Wistar rats with spray-dried milk containing linseed oil (LSO) (source of LNA) or fish oil (FO) (source of EPA+DHA) for 8 weeks. Feeding n-3 fatty acid containing milk formulation lowered the hepatic 3-hydroxy-methylglutaryl coenzyme A (HMG Co A) activity by 17-22% compared to rats given control diet devoid of n-3 fatty acids. The cholesterol level in liver microsomes was found to be decreased by 16% and 20%, respectively, in LSO and FO containing formulation fed rats. The bile flow was enhanced to an extent of 19-23% in experimental groups compared to control animals. The biliary cholesterol and phospholipid secretion was increased to an extent of 49-55% and 140-146%, respectively, in rats fed n-3 fatty acid containing formulation. The increase in the total bile acids secretion in bile was mainly reflected on an increase in the levels of taurine conjugated bile acids. These results indicated that n-3 fatty acid containing spray-dried milk formulation would bring about the hypocholesterolemic effect by lowering HMG Co A reductase activity in liver and by increasing the secretion of bile constituents.

  13. Induction of protective immunity against H1N1 influenza A(H1N1)pdm09 with spray-dried and electron-beam sterilised vaccines in non-human primates.

    PubMed

    Scherließ, Regina; Ajmera, Ankur; Dennis, Mike; Carroll, Miles W; Altrichter, Jens; Silman, Nigel J; Scholz, Martin; Kemter, Kristina; Marriott, Anthony C

    2014-04-17

    Currently, the need for cooled storage and the impossibility of terminal sterilisation are major drawbacks in vaccine manufacturing and distribution. To overcome current restrictions a preclinical safety and efficacy study was conducted to evaluate new influenza A vaccine formulations regarding thermal resistance, resistance against irradiation-mediated damage and storage stability. We evaluated the efficacy of novel antigen stabilizing and protecting solutions (SPS) to protect influenza A(H1N1)pdm09 split virus antigen under experimental conditions in vitro and in vivo. Original or SPS re-buffered vaccine (Pandemrix) was spray-dried and terminally sterilised by irradiation with 25 kGy (e-beam). Antigen integrity was monitored by SDS-PAGE, dynamic light scattering, size exclusion chromatography and functional haemagglutination assays. In vitro screening experiments revealed a number of highly stable compositions containing glycyrrhizinic acid (GA) and/or chitosan. The most stable composition was selected for storage tests and in vivo assessment of seroconversion in non-human primates (Macaca fascicularis) using a prime-boost strategy. Redispersed formulations with original adjuvant were administered intramuscularly. Storage data revealed high stability of protected vaccines at 4°C and 25°C, 60% relative humidity, for at least three months. Animals receiving original Pandemrix exhibited expected levels of seroconversion after 21 days (prime) and 48 days (boost) as assessed by haemagglutination inhibition and microneutralisation assays. Animals vaccinated with spray-dried and irradiated Pandemrix failed to exhibit seroconversion after 21 days whereas spray-dried and irradiated, SPS-protected vaccines elicited similar seroconversion levels to those vaccinated with original Pandemrix. Boost immunisation with SPS-protected vaccine resulted in a strong increase in seroconversion but had only minor effects in animals treated with non SPS-protected vaccine. In conclusion

  14. Influence of formulation and preparation process on ambroxol hydrochloride dry powder inhalation characteristics and aerosolization properties.

    PubMed

    Ren, Yachao; Yu, Chaoqun; Meng, Kangkang; Tang, Xing

    2008-09-01

    The objective of this study is to evaluate the influence of formulation and preparation process on ambroxol hydrochloride (AH) dry powder inhalation (DPI) characteristics and aerosolization properties. Spray-dried samples of AH, AH/leucine, and AH/leucine/mannitol were prepared from their corresponding water solutions under the same conditions to study the influence of the composition, and the AH/leucine/mannitol (2.5/0.5/1 by weight) formulation was used for investigation of the effect of the preparation process. Following spray-drying, the resulting powders were characterized using scanning electron microscopy, laser diffraction, tapped density, and angle of repose measurements, and the aerosolization performance was determined using a twin-stage liquid impinger. AH/leucine/mannitol (2.5/0.5/1 by weight) obtained by cospray-drying improved the AH aerosolization properties. The AH/leucine/mannitol (2.5/0.5/1 by weight) preparation exhibited the following properties: 62.34% yield, 0.34 g/cm(3) tap density, 2.71 microm d(ae), 33.45 degrees angle of repose, and 30.93% respirable fraction. The influence of the preparation process on DPI characteristics and aerosolization properties was relatively small, but the influence of the composition was relatively large. Optimization of DPI can be achieved by selecting the most appropriate formulation and preparation process.

  15. Levalbuterol Oral Inhalation

    MedlinePlus

    Levalbuterol comes as a solution (liquid) to inhale by mouth using a nebulizer (machine that turns medication into a mist that can be inhaled), a concentrated solution to be mixed with normal saline and inhaled ...

  16. Effect of fishmeal replacement with spray-dried animal plasma and colistin on intestinal structure, intestinal microbiology, and performance of weanling pigs challenged with Escherichia coli K99.

    PubMed

    Torrallardona, D; Conde, M R; Badiola, I; Polo, J; Brufau, J

    2003-05-01

    We evaluated spray-dried animal plasma (SDAP) as an alternative to antimicrobial medication with colistin sulfate in weanling pigs challenged with Escherichia coli K99. Forty-eight piglets weaned at 24 d of age were distributed into 12 pens, and each pen was assigned to one of four dietary treatments. All the piglets were given an oral dose of 5 x 10(7) cfu of E. coli K99 at weaning. The dietary treatments followed a factorial arrangement with two levels of SDAP (0 and 7%) and two levels of colistin (0 and 300 mg/kg of diet). The ADG and ADFI were measured on d 7 and 14 of trial. Three piglets from each treatment were killed on d 7 and 14 to remove the small intestine, and to obtain ileal and cecal digestive contents. The inclusion of SDAP improved ADG by 68 g (P < 0.05) and ADFI by 41 g (P < 0.10) in wk 1 of trial. During wk 2, SDAP improved ADG by 41 g (P < 0.10) and gain:feed ratio (G:F) by 25% (P < 0.01). On the other hand, whereas colistin had no effect on performance in wk 1, it improved ADG by 102 g (P < 0.01), ADFI by 62 g (P < 0.01), and G:F by 26% (P < 0.01) in wk 2. Over the 14 d of the trial, ADG was improved by 54 (P < 0.05) and 75 g (P < 0.05), and G:F was improved by 35 (P < 0.05) and 32% (P < 0.05) due to SDAP and colistin, respectively. There was interaction between colistin and SDAP for ADFI in wk 2 and between d 0 to 14 (P < 0.05), which indicates that their effects were not additive. The use of colistin was advantageous in the maintenance of the integrity of the intestinal mucosa of the pigs, as suggested by a small intestine that was 93 g heavier (P < 0.10) and with the tallest villi 106 microm longer (P < 0.10) than in pigs without colistin. The inclusion of SDAP in the diet favored the growth of lactobacilli in the ileum (P < 0.10) and the cecum (P < 0.05), whereas colistin reduced the number of enterococci in the cecum (P < 0.05) and of Escherichia coli both in the ileum and the cecum (P < 0.001). These results suggest that SDAP may be an

  17. Effects of spray-dried porcine plasma on growth performance, immune response, total antioxidant capacity, and gut morphology of nursery pigs.

    PubMed

    Tran, H; Bundy, J W; Li, Y S; Carney-Hinkle, E E; Miller, P S; Burkey, T E

    2014-10-01

    Two experiments were conducted to evaluate the effects of spray-dried porcine plasma (SDPP) on growth performance, immunity, antioxidant capacity, and gut morphology of nursery pigs. In Exp. 1, 96 weaned pigs (Nebraska female × Danbred sire; 20 ± 1 d of age; initial BW = 6.06 ± 0.02 kg) were assigned to 16 pens and randomly allotted to the control (CTL; no SDPP) or the CTL + SDPP treatment in 2 phases (phase 1: d 0 to 14, 5% SDPP; phase 2: d 14 to 28, 2.5% SDPP). Blood samples were collected on d 0 and weekly thereafter to quantify IgG, IgA, and total antioxidant capacity. On d 14, pigs (n = 16; 8 pigs/treatment) were selected and euthanized for small intestine tissue and alveolar macrophage collection. On d 7, pigs fed SDPP had greater ADG, ADFI (P = 0.001), and G:F (P = 0.019) compared with CTL pigs. On d 28, pigs fed SDPP had greater BW (P = 0.024) and tended to have greater ADG (P = 0.074) and ADFI (P = 0.062) compared with CTL pigs. There were no differences between treatments for serum IgG, IgA, and total antioxidant capacity. On d 14, greater villus height (P = 0.011) and villus:crypt (P = 0.008) were observed in duodenal tissue sections obtained from SDPP-fed pigs compared with CTL pigs. To evaluate effects of SDPP on immune biomarkers, alveolar macrophages collected from 3 pigs/treatment on d 14 were cultured in vitro and challenged with lipopolysaccharide (LPS; 10 ng/mL). Therefore, 4 treatments included 1) CTL diet with no LPS, 2) CTL diet with LPS (CTL+), 3) SDPP diet with no LPS, and 4) SDPP diet with LPS. There were no diet effects on tumor necrosis factor-α gene expression or secretion by alveolar macrophages. For IL-10 gene expression, a diet × LPS interaction (P = 0.009) was observed where CTL+ had greater (P < 0.05) IL-10 mRNA abundance compared with other treatments. A second experiment was conducted to evaluate the in vitro effects of porcine plasma using model porcine jejunal epithelial cells (IPEC-J2). The treatments applied to the IPEC

  18. Efficacy of dietary spray dried plasma protein to mitigate the negative effects on performance of pigs fed diets with corn naturally contaminated with multiple mycotoxins.

    PubMed

    Weaver, A C; Campbell, J M; Crenshaw, J D; Polo, J; Kim, S W

    2014-09-01

    The ability of spray dried plasma protein (SDPP) to reduce the negative effects of multiple mycotoxins from naturally contaminated corn on weaned pig performance and health was investigated (n = 180; 6.84 ± 0.11 kg). For 12 d after weaning, pigs were fed phase 1 nursery diets with either 0% SDPP (PP0) or 6% SDPP (PP6). After 12 d, pigs were fed phase 2 diets for 3 wk. Pigs fed PP0 in phase 1 continued to be fed a phase 2 diet with no SDPP (PP0/PP0) or were fed a diet including corn naturally contaminated with multiple mycotoxins (M), labeled PP0/PP0M. Pigs fed SDPP in phase 1 were fed either a diet with no SDPP (PP6/PP0), a diet with M and no SDPP (PP6/PP0M), a diet with M and 3% SDPP (PP6/PP3M), or a diet with M and 6% SDPP (PP6/PP6M). During phase 1, pigs fed PP6 had increased (P < 0.05) ADG, ADFI, and G:F, whereas immunological parameters were not altered. During phase 2, pigs consuming PP0/PP0M had reduced ADG (P < 0.01) and ADFI (P < 0.05) in contrast to pigs fed PP0/PP0, whereas the performance of pigs fed PP6/PP0M was intermediate to pigs fed PP0/PP0M and PP6/PP0. The ADG and ADFI did not differ for pigs fed PP0/PP0M and PP6/PP0M during phase 2. Performance of pigs fed PP6/PP3M in contrast to pigs fed PP6/PP0M during phase 2 did not differ; however, these pigs had lower (P < 0.05) tumor necrosis factor α and tended (P = 0.094) to have lower DNA damage. During phase 2, ADG and ADFI of pigs fed PP6/PP6M did not differ from pigs fed PP6/PP0M, but G:F tended (P = 0.067) to be increased in pigs fed PP6/PP6M. Over the entire study period, pigs fed PP0/PP0M had reduced (P < 0.05) ADG and tended (P = 0.067) to have reduced ADFI. During this time, pigs fed PP6/PP0M tended to have greater ADG and ADFI (P = 0.093 and P = 0.067, respectively) compared with pigs fed PP0/PP0M. Overall, feeding a diet with SDPP improved growth performance and feed intake of young pigs directly after weaning. Feeding multiple M had a negative impact on growth performance of pigs during

  19. The influence of feedstock and process variables on the encapsulation of drug suspensions by spray-drying in fast drying regime: the case of novel antitubercular drug–palladium complex containing polymeric microparticles.

    PubMed

    Giovagnoli, Stefano; Palazzo, Francesco; Di Michele, Alessandro; Schoubben, Aurelie; Blasi, Paolo; Ricci, Maurizio

    2014-04-01

    The purpose of this study was to address the effect of feedstock properties and process variables on the characteristics of antitubercular drug–palladium (Pd) containing poly(lactic) acid (PLA) microparticles (MP) obtained by spray-drying of noncolloidal particle dispersions in fast drying regime. Two different systems were compared: capreomycin–Pd (C–Pd) and ofloxacin–Pd (Ofx–Pd) dispersions in acetonitrile PLA solution. Particle size, dynamic light scattering, differential scanning calorimetry, SEM–energy dispersive X-ray, and spectrophotometric methods were used for MP characterization. C–Pd-loaded MP were optimized preliminarily by experimental design and compared with Ofx–Pd-loaded MP investigated in our previous work. Morphology of feedstock particles had a dominant role in determining MP morphology. The Charlesworth and Marshall theory was used to explain such behavior. The smaller and homogeneous C–Pd microparticulates favored MP inflation and buckling by forming a thick and nonporous shell. A percolation effect was proposed for the larger and irregular Ofx–Pd particles that produced smaller MP with a more porous shell. Increasing feedstock concentration led to higher particle loss. A tentative descriptive scheme of MP formation according to feedstock particle arrangement was proposed. This work suggested that spray-drying of drug dispersions should carefully consider the morphology of feedstock particles as a major parameter influencing final MP properties.

  20. Electrochemical properties of yolk-shell structured ZnFe2O4 powders prepared by a simple spray drying process as anode material for lithium-ion battery

    PubMed Central

    Won, Jong Min; Choi, Seung Ho; Hong, Young Jun; Ko, You Na; Kang, Yun Chan

    2014-01-01

    ZnFe2O4 yolk–shell powders were prepared by applying a simple spray-drying process. Dextrin was used as a drying additive and carbon source material, and thus played a key role in the preparation of the powders. The combustion of precursor powders consisting of zinc and iron salts and dextrin obtained by a spray-drying process produced the yolk–shell-structured ZnFe2O4 powders even at a low post-treatment temperature of 350°C. The ZnFe2O4 powders prepared from the spray solution without dextrin had a filled and pockmarked structure. The initial discharge capacities of the ZnFe2O4 yolk–shell and filled powders post-treated at 450°C at a current density of 500 mA g−1 were 1226 and 993 mA h g−1, respectively, and the corresponding initial Coulombic efficiencies were 74 and 58%. The discharge capacities of the ZnFe2O4 powders with yolk–shell and filled structures post-treated at 450°C after 200 cycles were 862 and 332 mA h g−1, respectively. The ZnFe2O4 yolk–shell powders with high structural stability during cycling had superior electrochemical properties to those of the powders with filled structure. PMID:25168407

  1. Effects of feeding a spray-dried multivalent polyclonal antibody preparation on feedlot performance, feeding behavior, carcass characteristics, rumenitis, and blood gas profile of Brangus and Nellore yearling bulls.

    PubMed

    Millen, D D; Pacheco, R D L; DiLorenzo, N; Martins, C L; Marino, C T; Bastos, J P S T; Mariani, T M; Barducci, R S; Sarti, L M N; DiCostanzo, A; Rodrigues, P H M; Arrigoni, M D B

    2015-09-01

    The objective of this study was to evaluate the effects of replacing monensin (MON) with a spray-dried multivalent polyclonal antibody preparation (PAP) against several ruminal microorganisms on feedlot performance, carcass characteristics, feeding behavior, blood gas profile, and the rumenitis incidence of Brangus and Nellore yearling bulls. The study was designed as a completely randomized design with a 2 × 2 factorial arrangement, replicated 6 times (4 bulls per pen and a total of 24 pens), in which bulls ( = 48) of each biotype were fed diets containing either MON fed at 300 mg/d or PAP fed at 3 g/d. No significant feed additive main effects were observed for ADG ( = 0.27), G:F ( = 0.28), HCW ( = 0.99), or dressing percentage ( = 0.80). However, bulls receiving PAP had greater DMI ( = 0.02) and larger ( = 0.02) final LM area as well as greater ( < 0.01) blood concentrations of bicarbonate and base excess in the extracellular fluid than bulls receiving MON. Brangus bulls had greater ( < 0.01) ADG and DMI expressed in kilograms, final BW, heavier HCW, and larger initial and final LM area than Nellore bulls. However, Nellore bulls had greater daily DMI fluctuation ( < 0.01), expressed as a percentage, and greater incidence of rumenitis ( = 0.05) than Brangus bulls. In addition, Brangus bulls had greater ( < 0.01) DMI per meal and also presented lower ( < 0.01) DM and NDF rumination rates when compared with Nellore bulls. Significant interactions ( < 0.05) between biotype and feed additive were observed for SFA, unsaturated fatty acids (UFA), MUFA, and PUFA concentrations in adipose tissues. When Nellore bulls were fed PAP, fat had greater ( < 0.05) SFA and PUFA contents but less ( < 0.01) UFA and MUFA than Nellore bulls receiving MON. For Brangus bulls, MON led to greater ( < 0.05) SFA and PUFA and less ( < 0.05) UFA and MUFA than Brangus bulls fed PAP. Feeding a spray-dried PAP led to similar feedlot performance compared with that when feeding MON. Spray-dried

  2. A novel inhaled multi-pronged attack against respiratory bacteria.

    PubMed

    Lee, Sie Huey; Teo, Jeanette; Heng, Desmond; Zhao, Yanli; Ng, Wai Kiong; Chan, Hak-Kim; Tan, Li Teng; Tan, Reginald B H

    2015-04-05

    Airway mucus hypersecretion is a common clinical feature of many severe respiratory diseases, and when complicated by a recalcitrant bacterial infection, the whole treatment regimen thereby becomes more challenging and protracted. The accumulation of thickened mucus secretions in the lower airways provides a nutrient-rich breeding ground for bacteria that promotes their growth and limits the ease of effective eradication. Unfortunately, no direct-inhaled dry powder formulation to treat these respiratory mucoid infections more effectively is available commercially. This work therefore seeks to develop a highly-efficacious ternary dry powder inhaler (DPI) formulation (ciprofloxacin hydrochloride (CIP), gatifloxacin hydrochloride (GAT) and ambroxol hydrochloride (AMB)) capable of delivering a novel multi-pronged attack (synergy, quorum quenching and mucociliary clearance) on Pseudomonas aeruginosa, a common respiratory bacteria found in mucoid infections. The powders were prepared via spray drying, evaluated on their aerosol performance via a multi-stage liquid impinger (MSLI) and tested for their efficacies in bacteria-spiked artificial sputum medium (ASM). The optimized particles were of respirable-size (d50 of ∼1.61±0.03μm) and slightly corrugated. When dispersed via an Aerolizer® inhaler at 60L/min, the powder showed concomitant in vitro deposition, minimal capsule, device and throat retention, and highly promising and uniform fine particle fractions (of the loaded dose) of ∼64-69%, which was a vast improvement over the singly-delivered actives. Favourably, when tested on bacteria-spiked ASM, the optimized ternary formulation (with AMB) was more effective at killing bacteria (i.e. faster rate of killing) than just the synergistic antibiotics alone (binary formulation; without AMB). In conclusion, a ternary antibiotic-(non-antibiotic) DPI formulation involving a unique multi-pronged attack mechanism was successfully pioneered and optimized for mucoid

  3. Development of a microparticle-based dry powder inhalation formulation of ciprofloxacin hydrochloride applying the quality by design approach.

    PubMed

    Karimi, Keyhaneh; Pallagi, Edina; Szabó-Révész, Piroska; Csóka, Ildikó; Ambrus, Rita

    2016-01-01

    Pulmonary drug delivery of ciprofloxacin hydrochloride offers effective local antibacterial activity and convenience of easy application. Spray drying is a trustworthy technique for the production of ciprofloxacin hydrochloride microparticles. Quality by design (QbD), an up-to-date regulatory-based quality management method, was used to predict the final quality of the product. According to the QbD-based theoretical preliminary parameter ranking and priority classification, dry powder inhalation formulation tests were successfully performed in practice. When focusing on the critical parameters, the practical development was more effective and was in correlation with our previous findings. Spray drying produced spherical microparticles. The dry powder formulations prepared were examined by particle size analysis, scanning electron microscopy, Fourier-transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro drug release and aerodynamic particle size analyses were also performed. These formulations showed an appropriate particle size ranging between 2 and 4 μm and displayed an enhanced aerosol performance with fine particle fraction up to 80%.

  4. Development of a microparticle-based dry powder inhalation formulation of ciprofloxacin hydrochloride applying the quality by design approach

    PubMed Central

    Karimi, Keyhaneh; Pallagi, Edina; Szabó-Révész, Piroska; Csóka, Ildikó; Ambrus, Rita

    2016-01-01

    Pulmonary drug delivery of ciprofloxacin hydrochloride offers effective local antibacterial activity and convenience of easy application. Spray drying is a trustworthy technique for the production of ciprofloxacin hydrochloride microparticles. Quality by design (QbD), an up-to-date regulatory-based quality management method, was used to predict the final quality of the product. According to the QbD-based theoretical preliminary parameter ranking and priority classification, dry powder inhalation formulation tests were successfully performed in practice. When focusing on the critical parameters, the practical development was more effective and was in correlation with our previous findings. Spray drying produced spherical microparticles. The dry powder formulations prepared were examined by particle size analysis, scanning electron microscopy, Fourier-transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro drug release and aerodynamic particle size analyses were also performed. These formulations showed an appropriate particle size ranging between 2 and 4 μm and displayed an enhanced aerosol performance with fine particle fraction up to 80%. PMID:27784991

  5. Inhalation Therapy in Horses.

    PubMed

    Cha, Mandy L; Costa, Lais R R

    2017-04-01

    This article discusses the benefits and limitations of inhalation therapy in horses. Inhalation drug therapy delivers the drug directly to the airways, thereby achieving maximal drug concentrations at the target site. Inhalation therapy has the additional advantage of decreasing systemic side effects. Inhalation therapy in horses is delivered by the use of nebulizers or pressured metered dose inhalers. It also requires the use of a muzzle or nasal mask in horses. Drugs most commonly delivered through inhalation drug therapy in horses include bronchodilators, antiinflammatories, and antimicrobials.

  6. Heat-Stable Dry Powder Oxytocin Formulations for Delivery by Oral Inhalation.

    PubMed

    Fabio, Karine; Curley, Kieran; Guarneri, Joseph; Adamo, Benoit; Laurenzi, Brendan; Grant, Marshall; Offord, Robin; Kraft, Kelly; Leone-Bay, Andrea

    2015-12-01

    In this work, heat stable dry powders of oxytocin (OT) suitable for delivery by oral inhalation were prepared. The OT dry powders were prepared by spray drying using excipients chosen to promote OT stability including trehalose, isoleucine, polyvinylpyrrolidone, citrate (sodium citrate and citric acid), and zinc salts (zinc chloride and zinc citrate). Characterization by laser diffraction indicated that the OT dry powders had a median particle size of 2 μm, making them suitable for delivery by inhalation. Aerodynamic performance upon discharge from proprietary dry powder inhalers was evaluated by Andersen cascade impaction (ACI) and in an anatomically correct airway (ACA) model, and confirmed that the powders had excellent aerodynamic performance, with respirable fractions up to 77% (ACI, 30 L/min). Physicochemical characterization demonstrated that the powders were amorphous (X-ray diffraction) with high glass transition temperature (modulated differential scanning calorimetry, MDSC), suggesting the potential for stabilization of the OT in a glassy amorphous matrix. OT assay and impurity profile were conducted by reverse phase HPLC and liquid chromatography-mass spectrometry (LC-MS) after storage up to 32 weeks at 40°C/75%RH. Analysis demonstrated that OT dry powders containing a mixture of citrate and zinc salts retained more than 90% of initial assay after 32 weeks storage and showed significant reduction in dimers and trisulfide formation (up to threefold reduction compared to control).

  7. Synergistic combination dry powders for inhaled antimicrobial therapy

    NASA Astrophysics Data System (ADS)

    Heng, Desmond; Lee, Sie Huey; Teo, Jeanette; Ng, Wai Kiong; Chan, Hak-Kim; Tan, Reginald B. H.

    2013-06-01

    Combination products play an important role in medicine as they offer improved clinical effectiveness, enhanced patient adherence, and reduced administrative costs. In combination antimicrobial therapy, the desired outcome is to extend the antimicrobial spectrum and to achieve a possible synergistic effect. However, adverse antagonistic species may sometimes emerge from such combinations, leading to treatment failure. Therefore, it is crucial to screen the drug candidates for compatibility and possible antagonistic interactions. This work aims to develop a novel synergistic dry powder inhaler (DPI) formulation for antimicrobial combination therapy via the pulmonary route. Binary and ternary combinations were prepared via spray drying on a BUCHI® Nano Spray Dryer B-90. All powders were within the respirable size range, and were consisted of spherical particles that were slightly corrugated. The powers yielded fine particle fractions (of the loaded dose) of over 40% when dispersed using an Aerolizer® DPI at 60 L/min. Time-kill studies carried out against common respiratory tract pathogenic bacteria Pseudomonas aeruginosa, Staphylococcus aureus, Klebsiella pneumonia and Acinetobacter baumannii at 1x the minimum inhibitory concentration (MIC) over 24 hours revealed no antagonistic behavior for both combinations. While the interactions were generally found to be indifferent, a favorable synergistic effect was detected in the binary combination when it was tested against Pseudomonas aeruginosa bacteria.

  8. Formoterol Oral Inhalation

    MedlinePlus

    ... until you are ready to inhale your dose. Pull off the inhaler cover and twist the mouthpiece open in the direction shown by the arrow on the mouthpiece. Push the buttons on each side to be sure ...

  9. Albuterol Oral Inhalation

    MedlinePlus

    Albuterol is used to prevent and treat difficulty breathing, wheezing, shortness of breath, coughing, and chest tightness ... for oral inhalation is also used to prevent breathing difficulties during exercise. Albuterol inhalation aerosol (Proair HFA, ...

  10. Smoke inhalation injury

    NASA Astrophysics Data System (ADS)

    Birky, M.

    The cause of death by fires was studied. The present results and information are, however, not enough to reduce loss of life or inhalation injury. The magnitude and type of inhalation injury for civilians and firefighters represents the most inadequately defined human element of accidental fires. Little information is available on compounds other than carbon monoxide, which are responsible for respiration injury or toxicological syndrome. Effective treatment methods for inhalation victims and studies on fatalities, inhalation injury and animals are suggested.

  11. Focus on Inhalants.

    ERIC Educational Resources Information Center

    Challenge: Safe, Disciplines, and Drug-Free Schools, 1994

    1994-01-01

    The use of inhalants is a major health concern among the school-age population. Information presented in this publication dispels the myths about inhalant use and presents common warning signs that alert teachers to a student's use. The short- and long-term effects of inhalant use are described to shed light on the health risks involved. Lesson…

  12. Inhalable DNase I microparticles engineered with biologically active excipients.

    PubMed

    Osman, Rihab; Al Jamal, Khuloud T; Kan, Pei-Lee; Awad, Gehanne; Mortada, Nahed; El-Shamy, Abd-Elhameed; Alpar, Oya

    2013-12-01

    Highly viscous mucus poses a big challenge for the delivery of particulates carrying therapeutics to patients with cystic fibrosis. In this study, surface modifying DNase I loaded particles using different excipients to achieve better lung deposition, higher enzyme stability or better biological activity had been exploited. For the purpose, controlled release microparticles (MP) were prepared by co-spray drying DNase I with the polymer poly-lactic-co-glycolic acid (PLGA) and the biocompatible lipid surfactant 1,2-dipalmitoyl-Sn-phosphatidyl choline (DPPC) using various hydrophilic excipients. The effect of the included modifiers on the particle morphology, size, zeta potential as well as enzyme encapsulation efficiency, biological activity and release had been evaluated. Powder aerosolisation performance and particle phagocytosis by murine macrophages were also investigated. The results showed that more than 80% of enzyme activity was recovered after MP preparation and that selected surface modifiers greatly increased the enzyme encapsulation efficiency. The particle morphology was greatly modified altering in turn the powders inhalation indices where dextran, ovalbumin and chitosan hydrochloride increased considerably the respirable fraction compared to the normal hydrophilic carriers lactose and PVP. Despite of the improved aerosolisation caused by chitosan hydrochloride, yet retardation of chitosan coated particles in artificial mucus samples discouraged its application. On the other hand, dextran and polyanions enhanced DNase I effect in reducing cystic fibrosis mucus viscosity. DPPC proved good ability to reduce particles phagocytic uptake even in the presence of the selected adjuvants. The prepared MP systems were biocompatible with lung epithelial cells. To conclude, controlled release DNase I loaded PLGA-MP with high inhalation indices and enhanced mucolytic activity on CF sputum could be obtained by surface modifying the particles with PGA or dextran.

  13. Dynamics of airflow in a short inhalation

    PubMed Central

    Bates, A. J.; Doorly, D. J.; Cetto, R.; Calmet, H.; Gambaruto, A. M.; Tolley, N. S.; Houzeaux, G.; Schroter, R. C.

    2015-01-01

    During a rapid inhalation, such as a sniff, the flow in the airways accelerates and decays quickly. The consequences for flow development and convective transport of an inhaled gas were investigated in a subject geometry extending from the nose to the bronchi. The progress of flow transition and the advance of an inhaled non-absorbed gas were determined using highly resolved simulations of a sniff 0.5 s long, 1 l s−1 peak flow, 364 ml inhaled volume. In the nose, the distribution of airflow evolved through three phases: (i) an initial transient of about 50 ms, roughly the filling time for a nasal volume, (ii) quasi-equilibrium over the majority of the inhalation, and (iii) a terminating phase. Flow transition commenced in the supraglottic region within 20 ms, resulting in large-amplitude fluctuations persisting throughout the inhalation; in the nose, fluctuations that arose nearer peak flow were of much reduced intensity and diminished in the flow decay phase. Measures of gas concentration showed non-uniform build-up and wash-out of the inhaled gas in the nose. At the carina, the form of the temporal concentration profile reflected both shear dispersion and airway filling defects owing to recirculation regions. PMID:25551147

  14. Aggregated Nanotransfersomal Dry Powder Inhalation of Itraconazole for Pulmonary Drug Delivery

    PubMed Central

    Hassanpour Aghdam, Mehdi; Ghanbarzadeh, Saeed; Javadzadeh, Yousef; Hamishehkar, Hamed

    2016-01-01

    Purpose: Local therapy is a valuable and strategic approach in the treatment of lung associated diseases and dry powder inhalation (DPI) formulations play the key role in this plan. Transfersome has been introduced as a novel biocompatible vesicular system with potential for administration in pulmonary drug delivery. The present study was designed to prepare Itraconazole-loaded nanotrantransfersomal DPI formulation. Methods: Itraconazole-loaded nanotransfersomes with three different types of surfactant in varying concentrations were prepared and characterized in the point of particle size distribution and morphology by laser light scattering and scanning electron microscopy (SEM) methods. The optimized transferosomal formulations were co-spray dried with mannitol and the aerosolization efficiency and aerodynamic properties of dry powders were determined by next generation impactor using a validated HPLC technique. Results: The volume mean diameter of optimized nanotransfersomal formulation with lecithin:Span® 60 in the ratio of 90:10 was 171 nm with narrow size distribution pattern which increased up to 518 nm after drug loading. Different types of surfactant did not influence the particle size significantly. SEM images confirmed the formation of aggregated nanoparticles in the suitable range (1-5 µm) for the pulmonary drug delivery. Aerosolization evaluation of co-spray dried formulations with different amounts of mannitol indicated that 2:1 ratio of mannitol:transfersome (w:w) showed the best aerosolization efficiency (fine particle fraction (FPF)=37%). Increasing of mannitol significantly decreased the FPF of the optimized formulations. Conclusion: The results of this study was introduced the potential application of nanotransfersomes in the formulation of DPIs for lung delivery of various drugs. PMID:27123418

  15. Rifapentine-Proliposomes for Inhalation: In Vitro and In Vivo Toxicity

    PubMed Central

    Patil-Gadhe, Arpana A.; Kyadarkunte, Abhay Y.; Pereira, Michael; Jejurikar, Gauri; Patole, Milind S.; Risbud, Arun; Pokharkar, Varsha B.

    2014-01-01

    Background: Oral therapy for pulmonary tuberculosis (TB) treatment suffers from the limitation of hepatic metabolism leading insufficient concentration of antitubercular (anti-TB) drugs in alveolar macrophage which harbors Mycobacterium tuberculosis (MTB). Targeted aerosol delivery of antituberculous drug to lung is efficient for treating local lung TB infection. Objective: The present study was aimed to evaluate rifapentine (RPT) loaded proliposomal dry powder for inhalation (RLDPI) for anti-TBactivity and cytotoxicity in vitro. In vivo toxicity study was also undertaken in Wistar rats to determine safe concentration of RLDPI for administration. Materials and Methods: Anti-TB activity of developed RLDPI was assessed using drug susceptibility testing (DST) on Mycobacteria growth indicator tube (MGIT) method. In vitro cytotoxicity was performed in A549 cell lines and IC50 values were used to compare the cytotoxicity of formulation with pure RPT. In vivo repeated dose toxicity study was undertaken using Wistar rats at three different doses for 28-days by intratracheal insufflations method. Results: The results of DST study revealed sensitivity of tubercle bacteria to RLDPI at concentration equivalent to 10 μg/mL of RPT. This study confirmed anti-TB potential of RPT in spray-dried RLDPI, though the spray drying method is reported to reduce activity of drugs. Cytotoxicity study in A549 cells demonstrated that RPT when encapsulated in liposomes as RLDPI was safe to cells as compared to pure RPT. In vivo toxicity study revealed that RPT in the form of RLDPI was safe at 1 and 5 mg/kg dose. However, mortality was seen at higher dose (10 mg/kg), possibly because of liver and kidney damage. Conclusion: Thus, these studies demonstrated safety of RLDPI for the treatment of pulmonary TB. PMID:25948966

  16. The ADMIT series - Issues in inhalation therapy. 4) How to choose inhaler devices for the treatment of COPD.

    PubMed

    Vincken, Walter; Dekhuijzen, Pn Richard; Barnes, Peter

    2010-03-01

    For patients with COPD, inhalation is the preferred route of administration of respiratory drugs for both maintenance and acute treatment. Numerous inhaler types and devices have been developed, each with their own particularities, advantages and disadvantages. Nevertheless, published COPD management guidelines pay little attention to the optimal choice of inhaler devices for COPD patients. Although efficacy and safety are the primary factors determining the choice of an inhaler device, randomised controlled trials (RCTs) directly comparing the efficacy and safety of different inhalers in COPD patients are scarce. Systematic reviews on this subject failed to find significant differences between devices for any of the clinical outcomes studied. When selecting a device for the delivery of inhaled drugs in 'real life' patients with COPD, other factors should be considered. These include availability and affordability of the inhaled drugs and inhaler devices, the uniformity of inhaler devices when several drugs are to be inhaled, the ability of patients to handle correctly the selected device - in particular taking into account the advanced age of the average COPD patient, and finally the patient's preference. The prescribing clinician's task is to provide comprehensive instructions for correct handling of the device and to review regularly the patient's inhalation technique.

  17. Synthesis of Reduced Graphene Oxide-Modified LiMn0.75Fe0.25PO4 Microspheres by Salt-Assisted Spray Drying for High-Performance Lithium-Ion Batteries

    PubMed Central

    Kim, Myeong-Seong; Kim, Hyun-Kyung; Lee, Suk-Woo; Kim, Dong-Hyun; Ruan, Dianbo; Chung, Kyung Yoon; Lee, Sang Hyun; Roh, Kwang Chul; Kim, Kwang-Bum

    2016-01-01

    Microsized, spherical, three-dimensional (3D) graphene-based composites as electrode materials exhibit improved tap density and electrochemical properties. In this study, we report 3D LiMn0.75Fe0.25PO4/reduced graphene oxide microspheres synthesized by one-step salt-assisted spray drying using a mixed solution containing a precursor salt and graphene oxide and a subsequent heat treatment. During this process, it was found that the type of metal salt used has significant effects on the morphology, phase purity, and electrochemical properties of the synthesized samples. Furthermore, the amount of the chelating agent used also affects the phase purity and electrochemical properties of the samples. The composite exhibited a high tap density (1.1 g cm−3) as well as a gravimetric capacity of 161 mA h g−1 and volumetric capacity of 281 mA h cm−3 at 0.05 C-rate. It also exhibited excellent rate capability, delivering a discharge capacity of 90 mA h g−1 at 60 C-rate. Furthermore, the microspheres exhibited high energy efficiency and good cyclability, showing a capacity retention rate of 93% after 1000 cycles at 10 C-rate. PMID:27220812

  18. Porous micro-spherical aggregates of LiFePO 4/C nanocomposites: A novel and simple template-free concept and synthesis via sol-gel-spray drying method

    NASA Astrophysics Data System (ADS)

    Yu, Feng; Zhang, Jingjie; Yang, Yanfeng; Song, Guangzhi

    Porous micro-spherical aggregates of LiFePO 4/C nanocomposites were prepared with a process of spray drying at 200 °C and subsequent heat treatment at 700 °C for 12 h by a novel and simple template-free sol-gel-SD method independent of surfactants or templates. The results indicate that the as-obtained LiFePO 4 porous microspheres have the mean diameter of 19.8 μm, average pore size of 45 nm, and large specific surface area (20.2 m 2 g -1) with evenly distributed carbon (4.5 wt.%). The particles can be easily brought into contact with electrolyte, facilitating electric and lithium ion diffusion. They present large reversible discharge capacity of 137.5 mAh g -1 at the current density of 0.1 C, good rate capacity of 53.8 mAh g -1 at 10 C, and excellent capacity retention rate closed to 100% after various current densities in the region of 2.0-4.3 V.

  19. Synthesis of Reduced Graphene Oxide-Modified LiMn0.75Fe0.25PO4 Microspheres by Salt-Assisted Spray Drying for High-Performance Lithium-Ion Batteries

    NASA Astrophysics Data System (ADS)

    Kim, Myeong-Seong; Kim, Hyun-Kyung; Lee, Suk-Woo; Kim, Dong-Hyun; Ruan, Dianbo; Chung, Kyung Yoon; Lee, Sang Hyun; Roh, Kwang Chul; Kim, Kwang-Bum

    2016-05-01

    Microsized, spherical, three-dimensional (3D) graphene-based composites as electrode materials exhibit improved tap density and electrochemical properties. In this study, we report 3D LiMn0.75Fe0.25PO4/reduced graphene oxide microspheres synthesized by one-step salt-assisted spray drying using a mixed solution containing a precursor salt and graphene oxide and a subsequent heat treatment. During this process, it was found that the type of metal salt used has significant effects on the morphology, phase purity, and electrochemical properties of the synthesized samples. Furthermore, the amount of the chelating agent used also affects the phase purity and electrochemical properties of the samples. The composite exhibited a high tap density (1.1 g cm‑3) as well as a gravimetric capacity of 161 mA h g‑1 and volumetric capacity of 281 mA h cm‑3 at 0.05 C-rate. It also exhibited excellent rate capability, delivering a discharge capacity of 90 mA h g‑1 at 60 C-rate. Furthermore, the microspheres exhibited high energy efficiency and good cyclability, showing a capacity retention rate of 93% after 1000 cycles at 10 C-rate.

  20. Synthesis of Reduced Graphene Oxide-Modified LiMn0.75Fe0.25PO4 Microspheres by Salt-Assisted Spray Drying for High-Performance Lithium-Ion Batteries.

    PubMed

    Kim, Myeong-Seong; Kim, Hyun-Kyung; Lee, Suk-Woo; Kim, Dong-Hyun; Ruan, Dianbo; Chung, Kyung Yoon; Lee, Sang Hyun; Roh, Kwang Chul; Kim, Kwang-Bum

    2016-05-25

    Microsized, spherical, three-dimensional (3D) graphene-based composites as electrode materials exhibit improved tap density and electrochemical properties. In this study, we report 3D LiMn0.75Fe0.25PO4/reduced graphene oxide microspheres synthesized by one-step salt-assisted spray drying using a mixed solution containing a precursor salt and graphene oxide and a subsequent heat treatment. During this process, it was found that the type of metal salt used has significant effects on the morphology, phase purity, and electrochemical properties of the synthesized samples. Furthermore, the amount of the chelating agent used also affects the phase purity and electrochemical properties of the samples. The composite exhibited a high tap density (1.1 g cm(-3)) as well as a gravimetric capacity of 161 mA h g(-1) and volumetric capacity of 281 mA h cm(-3) at 0.05 C-rate. It also exhibited excellent rate capability, delivering a discharge capacity of 90 mA h g(-1) at 60 C-rate. Furthermore, the microspheres exhibited high energy efficiency and good cyclability, showing a capacity retention rate of 93% after 1000 cycles at 10 C-rate.

  1. Rapid formation of the Bi{sub 2{minus}x}Pb{sub x}Sr{sub 2}Ca{sub 2}Cu{sub 3}O{sub y} high {Tc}-phase, using spray-dried nitrate precursor powders

    SciTech Connect

    Van Driessche, I.; Mouton, R.; Hoste, S.

    1996-08-01

    This study describes the use of spray-dried nitrate precursor powders in the synthesis of Bi-2223 high {Tc}-superconductors. The decomposition of the precursor powder is studied using TGA/DTA, XRD, IR, and nitrogen analyses. The particle size is determined using SEM. The low decomposition temperature of the nitrates ({approximately}600 C) and the small particle size of the spray dried powder ({approximately}3{center_dot}10{sup {minus}6} m), resulting in a lowering of the calcination temperature and a shortening of the sinter time, enabled the authors to synthesize a > 96% pure Bi-2223 phase (from XRD peak intensities) after a thermal process of 5h at 650 C and 60 h at 855 C.

  2. Inhalant allergies in children.

    PubMed

    Mims, James W; Veling, Maria C

    2011-06-01

    Children with chronic or recurrent upper respiratory inflammatory disease (rhinitis) should be considered for inhalant allergies. Risk factors for inhalant allergies in children include a first-degree relative with allergies, food allergy in infancy, and atopic dermatitis. Although inhalant allergies are rare in infancy, inhalant allergies are common in older children and impair quality of life and productivity. Differentiating between viral and allergic rhinitis can be challenging in children, but the child's age, history, and risk factors can provide helpful information. Allergic rhinitis is a risk factor for asthma, and if one is present, medical consideration of the other is warranted.

  3. Inhalant Abuse and Dextromethorphan.

    PubMed

    Storck, Michael; Black, Laura; Liddell, Morgan

    2016-07-01

    Inhalant abuse is the intentional inhalation of a volatile substance for the purpose of achieving an altered mental state. As an important, yet underrecognized form of substance abuse, inhalant abuse crosses all demographic, ethnic, and socioeconomic boundaries, causing significant morbidity and mortality in school-aged and older children. This review presents current perspectives on epidemiology, detection, and clinical challenges of inhalant abuse and offers advice regarding the medical and mental health providers' roles in the prevention and management of this substance abuse problem. Also discussed is the misuse of a specific "over-the-counter" dissociative, dextromethorphan.

  4. Development of controlled-release cisplatin dry powders for inhalation against lung cancers.

    PubMed

    Levet, Vincent; Rosière, Rémi; Merlos, Romain; Fusaro, Luca; Berger, Gilles; Amighi, Karim; Wauthoz, Nathalie

    2016-12-30

    The present study focuses on the development of dry powders for inhalation as adjuvant chemotherapy in lung cancer treatment. Cisplatin was chosen as a potential candidate for a local treatment as it remains the main platinum component used in conventional chemotherapies, despite its high and cumulative systemic toxicities. Bulk cisplatin was reduced to submicron sizes using high-pressure homogenization, mixed with a solubilized lipid and/or PEGylated component and then spray-dried to produce controlled-release dry powder formulations. The obtained formulations were characterized for their physicochemical properties (particle size and morphology), aerodynamic performance and release profiles. Cisplatin content and integrity were assessed by electrothermal atomic absorption spectrometry and (195)Pt nuclear magnetic resonance spectroscopy. DPI formulations with cisplatin contents ranging from 48.5 to 101.0% w/w exhibited high fine particle fractions ranging from 37.3% to 51.5% of the nominal dose. Formulations containing cisplatin microcrystals dispersed in solid lipid microparticles based on acceptable triglycerides for inhalation and PEGylated excipients showed a controlled-release for more than 24h and a limited burst effect. These new formulations could provide an interesting approach to increasing and prolonging drug exposure in the lung while minimizing systemic toxicities.

  5. Modeling Deposition of Inhaled Particles

    EPA Science Inventory

    The mathematical modeling of the deposition and distribution of inhaled aerosols within human lungs is an invaluable tool in predicting both the health risks associated with inhaled environmental aerosols and the therapeutic dose delivered by inhaled pharmacological drugs. Howeve...

  6. Formulation of pH responsive peptides as inhalable dry powders for pulmonary delivery of nucleic acids

    PubMed Central

    Liang, Wanling; Kwok, Philip C.L.; Chow, Michael Y.T.; Tang, Patricia; Mason, A. James; Chan, Hak-Kim; Lam, Jenny. K.W.

    2013-01-01

    Nucleic acids have the potential to be used as therapies or vaccines for many different types of disease but delivery remains the most significant challenge to their clinical adoption. pH responsive peptides containing either histidine or derivatives of 2,3-diaminopropionic acid (Dap) can mediate effective DNA transfection in lung epithelial cells with the latter remaining effective even in the presence of lung surfactant containing bronchoalveolar fluid (BALF), making this class of peptides attractive candidates for delivering nucleic acids to lung tissues. To further assess the suitability of pH responsive peptides for pulmonary delivery by inhalation, dry powder formulations of pH responsive peptides and plasmid DNA, with mannitol as carrier, were produced by either spray drying (SD) or spray freeze drying (SFD). The properties of the two types of powders were characterised and compared using scanning electron microscopy (SEM), next generation impaction (NGI), gel retardation and in vitro transfection via a twin-stage impinger (TSI) following aerosolisation by a dry powder inhaler (Osmohaler™). Although the aerodynamic performance and transfection efficacy of both powders were good, the overall performance revealed SD powders to have a number of advantages over SFD powders and are the more effective formulation with potential for efficient nucleic acid delivery through inhalation. PMID:23702276

  7. Pharmacokinetics, Metabolism and Partial Biodistribution of 'Pincer Therapeutic' Nitazoxanide in Mice Following Pulmonary Delivery of Inhalable Particl.

    PubMed

    Gupta, Anuradha; Tulsankar, Sachin L; Bhatta, Rabi S; Misra, Amit

    2017-03-06

    Nitazoxanide (NTZ) induces autophagy in mammalian cells and also has mycobactericidal activity, displaying a two-pronged therapeutic effect-- on the host as well as the pathogen. The pharmacokinetics and biodistribution of inhaled NTZ were investigated. Particles containing NTZ in a matrix of PLGA were prepared by spray drying. HPLC and LC-MS/MS methods were developed and validated. Particles were administered as inhalations to mice. Drug concentrations in plasma and tissues were estimated at different time points. Drug loading (~36%), entrapment efficiency (>90%) and the conversion of NTZ into metabolites in plasma and lung homogenates were assessed satisfactorily by HPLC. NTZ pharmacokinetics and biodistribution following intravenous administration or inhalation were established by LC-MS. NTZ converted in to TZX (99% in 30 min) and other metabolites. Pulmonary delivery of NTZ entrapped in particles increased the half-life of the drug by factors of 3, 12 and 200 in the plasma, lung tissue and alveolar macrophages respectively. Targeted delivery and prolonged lung retention along with dose sparing of the liver and kidneys was observed upon pulmonary delivery as compared to intravenous administration.

  8. TARGETED DELIVERY OF INHALED PHARMACEUTICALS USING AN IN SILICO DOSIMETRY MODEL

    EPA Science Inventory

    We present an in silico dosimetry model which can be used for inhalation toxicology (risk assessment of inhaled air pollutants) and aerosol therapy ( targeted delivery of inhaled drugs). This work presents scientific and clinical advances beyond the development of the original in...

  9. Nonthermal Inhalation Injury.

    DTIC Science & Technology

    1992-01-01

    understand the effects of the various byproducts of combustion on the human body. A thorough knowledge of the physiological mechanisms , relevant...as soon as possible. Overview of Smoke Inhalation Physiology The physiologic mechanisms of injury from smoke inhalation are multiple and complex...to breathe Lower airway obstruction Dyspnea, tachypnea, wheezing, rhonchi, carbonaceous sputum Parenchymal injury Dyspnea, tachypnea, rales Table 1

  10. ASSOCIATION BETWEEN THE INTRODUCTION OF A NEW CYSTIC FIBROSIS INHALED ANTIBIOTIC CLASS AND CHANGE IN PREVALENCE OF PATIENTS RECEIVING MULTIPLE INHALED ANTIBIOTIC CLASSES

    PubMed Central

    Dasenbrook, Elliott C.; Konstan, Michael W.; VanDevanter, Donald R.

    2014-01-01

    Background In 2010, aztreonam for inhalation solution joined aminoglycosides and colistimethate as a new cystic fibrosis (CF) chronic inhaled antimicrobial therapy. We studied how introduction of this new inhaled antibiotic class changed management of US CF patients. Methods Use of inhaled aminoglycosides, colistimethate, and aztreonam among patients followed in the CF Foundation Patient Registry was analyzed by age group, lung disease stage, and microbiologic status both annually, and at individual visits between 2009 and 2012. Results The overall prevalence of inhaled antibiotic use did not change during the period, but the prevalence of annual and any visit treatment with >1 inhaled antibiotic class more than doubled. Adults, those with advanced lung disease, and those with >1 Pseudomonas aeruginosa respiratory culture were more likely to receive >1 antibiotic class. Conclusions Inhaled antibiotic management of US CF patients has dramatically changed in association with the introduction of a third inhaled antibiotic class. PMID:25496726

  11. Inhalants in Peru.

    PubMed

    Lerner, R; Ferrando, D

    1995-01-01

    In Peru, the prevalence and consequences of inhalant abuse appear to be low in the general population and high among marginalized children. Inhalant use ranks third in lifetime prevalence after alcohol and tobacco. Most of the use appears to be infrequent. Among marginalized children, that is, children working in the streets but living at home or children living in the street, the problem of inhalant abuse is a serious problem. Among children working in the streets but living at home, the lifetime prevalence rate for inhalant abuse is high, ranging from 15 to 45 percent depending on the study being cited. For children living in the streets, the use of inhalant is even more severe. As mentioned earlier in this chapter, most of these street children use inhalants on a daily basis. The lack of research on the problem of inhalant abuse is a serious impediment to development of intervention programs and strategies to address this problem in Peru. Epidemiologic and ethnographic research on the nature and extent of inhalant abuse are obvious prerequisites to targeted treatment and preventive intervention programs. The urgent need for current and valid data is underscored by the unique vulnerability of the youthful population at risk and the undisputed harm that results from chronic abuse of inhalants. Nonetheless, it is important to mention several programs that work with street children. Some, such as the Information and Education Center for the Prevention of Drug Abuse, Generation, and Centro Integracion de Menores en Abandono have shelters where street children are offered transition to a less marginal lifestyle. Teams of street educators provide the children with practical solutions and gain their confidence, as well as offer them alternative socialization experiences to help them survive the streets and avoid the often repressive and counterproductive environments typical of many institutions. Most of the children who go through these programs tend to abandon

  12. Production of nano-solid dispersions using a novel solvent-controlled precipitation process - Benchmarking their in vivo performance with an amorphous micro-sized solid dispersion produced by spray drying.

    PubMed

    Duarte, Íris; Corvo, M Luísa; Serôdio, Pedro; Vicente, João; Pinto, João F; Temtem, Márcio

    2016-10-10

    A novel solvent controlled precipitation (SCP) process based on microfluidization was assessed to produce solid dispersions of carbamazepine, a poorly water-soluble drug with dissolution-rate limited absorption. A half-factorial design (2(3-1)+2 central points) was conducted to study the effect of different formulation variables (viz. polymer type, drug load, and feed solids' concentration) on the particle size and morphology, drug's solid state and drug's molecular distribution within the carrier of the co-precipitated materials produced. Co-precipitated powders were isolated via spray drying (SD). Nano-composite aggregated particles were obtained among all the tests. The particle size of the aggregates was dependent on the feed solids' concentration, while the level of aggregation between nanoparticles was dependent on the drug-polymer ratio. Both amorphous and crystalline nano-solid dispersions were produced using the proposed SCP process. The solid dispersion produced was dependent on both the type of polymeric stabilizer chosen and the drug load. Controls of amorphous and crystalline nano-solid dispersions produced by SCP and an amorphous micro-solid dispersion produced by SD were tested for: in vitro dissolution, in vivo pharmacokinetics in mice, and long-term storage physical stability. Both nano-amorphous and nano-crystalline presented faster dissolution rates and enhanced bioavailabilities than the micro-sized amorphous powder. The reduction of particle size to the nano-scale was found to be more important than the amorphization of the drug. The long-term physical stability of the amorphous nano-solid dispersion and the amorphous micro-solid dispersion were comparable.

  13. Novel Inhaled Combination Powder Containing Amorphous Colistin and Crystalline Rifapentine with Enhanced Antimicrobial Activities against Planktonic Cells and Biofilm of Pseudomonas aeruginosa for Respiratory Infections.

    PubMed

    Zhou, Qi Tony; Sun, Si-Ping; Chan, John Gar Yan; Wang, Ping; Barraud, Nicolas; Rice, Scott A; Wang, Jiping; Li, Jian; Chan, Hak-Kim

    2015-08-03

    Colistin has been increasingly used for the treatment of respiratory infections caused by Gram-negative bacteria. Unfortunately parenteral administration of colistin can cause severe adverse effects. This study aimed to develop an inhaled combination dry powder formulation of colistin and rifapentine for the treatment of respiratory infections. The combination formulation was produced by spray-drying rifapentine particles suspended in an aqueous colistin solution. The combination dry powder had enhanced antimicrobial activities against planktonic cells and biofilm cultures of Pseudomonas aeruginosa, with both minimum inhibitory concentration (MIC) and minimum biofilm inhibitory concentration (MBIC) values (2 and 4 mg/L, respectively) being half that of pure colistin (MIC 4 mg/L and MBIC 8 mg/L) and 1/16th that of pure rifapentine (MIC 32 mg/L and MBIC 64 mg/L). High aerosol performance, as measured via an Aerolizer device, was observed with emitted doses>89% and fine particle fraction (FPF) total>76%. The proportion of submicron particles of rifapentine particles was minimized by the attachment of colistin, which increased the overall particle mass and aerodynamic size distribution. Using the spray-drying method described here, stable particles of amorphous colistin and crystalline rifapentine were distributed homogeneously in each stage of the impinger. Unlike the colistin alone formulation, no deterioration in aerosol performance was found for the combination powder when exposed to a high relative humidity of 75%. In our previous study, surface coating by rifampicin contributed to the moisture protection of colistin. Here, a novel approach with a new mechanism was proposed whereby moisture protection was attributed to the carrier effect of elongated crystalline rifapentine particles, which minimized contact between hygroscopic colistin particles. This inhaled combination antibiotic formulation with enhanced aerosol dispersion efficiency and in vitro efficacy

  14. Formulation, stability and pharmacokinetics of sugar-based salmon calcitonin-loaded nanoporous/nanoparticulate microparticles (NPMPs) for inhalation.

    PubMed

    Amaro, Maria Inês; Tewes, Frederic; Gobbo, Oliviero; Tajber, Lidia; Corrigan, Owen I; Ehrhardt, Carsten; Healy, Anne Marie

    2015-04-10

    A challenge exists to produce dry powder inhaler (DPI) formulations with appropriate formulation stability, biological activity and suitable physicochemical and aerosolisation characteristics that provide a viable alternative to parenteral formulations. The present study aimed to produce sugar-based nanoporous/nanoparticulate microparticles (NPMPs) loaded with a therapeutic peptide - salmon calcitonin (sCT). The physicochemical properties of the powders and their suitability for pulmonary delivery of sCT were determined. Production of powders composed of sCT loaded into raffinose or trehalose with or without hydroxypropyl-β-cyclodextrin was carried out using a laboratory scale spray dryer. Spray dried microparticles were spherical, porous and of small geometric size (≤2 μm). Aerodynamic assessment showed that the fine particle fraction (FPF) less than 5 μm ranged from 45 to 86%, depending on the formulation. The mass median aerodynamic diameter (MMAD) varied between 1.9 and 4.7 μm. Compared to unprocessed sCT, sCT:raffinose composite systems presented a bioactivity of approximately 100% and sCT:trehalose composite systems between 70-90% after spray drying. Storage stability studies demonstrated composite systems with raffinose to be more stable than those containing trehalose. These sugar-based salmon calcitonin-loaded NPMPs retain reasonable sCT bioactivity and have micromeritic and physicochemical properties which indicate their suitability for pulmonary delivery. Formulations presented a similar pharmacokinetic profile to sCT solution. Hence the advantage of a dry powder formulation is its non-invasive delivery route and ease of administration of the sCT.

  15. Budesonide Oral Inhalation

    MedlinePlus

    Budesonide is used to prevent difficulty breathing, chest tightness, wheezing, and coughing caused by asthma. Budesonide powder for oral inhalation (Pulmicort Flexhaler) is used in adults and children 6 ...

  16. Acetylcysteine Oral Inhalation

    MedlinePlus

    Acetylcysteine inhalation is used along with other treatments to relieve chest congestion due to thick or abnormal ... that causes problems with breathing, digestion, and reproduction). Acetylcysteine is in a class of medications called mucolytic ...

  17. Zanamivir Oral Inhalation

    MedlinePlus

    ... you use an inhaled medication to treat asthma, emphysema, or other breathing problems and you are scheduled ... the air passages that lead to the lungs); emphysema (damage to air sacs in the lungs); or ...

  18. Ipratropium Oral Inhalation

    MedlinePlus

    Ipratropium oral inhalation is used to prevent wheezing, shortness of breath, coughing, and chest tightness in people ... damage to the air sacs in the lungs). Ipratropium is in a class of medications called bronchodilators. ...

  19. Pirbuterol Acetate Oral Inhalation

    MedlinePlus

    ... mouth or throat irritation, rinse your mouth with water, chew gum, or suck sugarless hard candy after using pirbuterol.Inhalation devices require regular cleaning. Once a week, remove the mouthpiece cover, turn ...

  20. Umeclidinium Oral Inhalation

    MedlinePlus

    ... chest tightness caused by chronic obstructive pulmonary disease (COPD; a group of diseases that affect the lungs ... Do not use umeclidinium inhalation during a sudden COPD attack. Your doctor will prescribe a short-acting ( ...

  1. Olodaterol Oral Inhalation

    MedlinePlus

    ... chest tightness caused by chronic obstructive pulmonary disease (COPD; a group of diseases that affect the lungs ... Do not use olodaterol inhalation during a sudden COPD attack. Your doctor will prescribe a short-acting ( ...

  2. Effects of Inhalable Microparticles of Seonpyejeongcheon-Tang in an Asthma Mouse Model

    PubMed Central

    Yang, Won-Kyung; Lee, Chul-Hwa; Kim, Min-Hee; Kim, Seung-Hyeong; Choi, Hae-Yoon; Yeo, Yoon; Park, Yang-Chun

    2016-01-01

    Objectives: Allergic asthma generally presents with symptoms of wheezing, coughing, breathlessness, and airway inflammation. Seonpyejeongcheon-tang (SJT) consists of 12 herbs. It originated from Jeongcheon-tang (JT), also known as Ding-chuan-tang, composed of 7 herbs, in She-sheng-zhong-miao-fang. This study aimed to evaluate the effects of local delivery of SJT via inhalable microparticles in an asthma mouse model. Methods: Microparticles containing SJT were produced by spray-drying with leucine as an excipient. SJT microparticles were evaluated with respect to their aerodynamic properties, in vitro cytotoxicity, in vivo toxicity, and therapeutic effects on ovalbumin (OVA)-induced asthma in comparison with orally-administered SJT. Results: SJT microparticles provided desirable aerodynamic properties (fine particle fraction of 48.9% ± 6.4% and mass median aerodynamic diameter of 3.7 ± 0.3 μm). SJT microparticles did not show any cytotoxicity against RAW 264.7 macrophages at concentrations of 0.01 - 3 mg/mL. Inhaled SJT microparticles decreased the levels of IL-4, IL-5, IL-13, IL-17A, eotaxin and OVA-IgE in bronchoalveolar lavage fluid (BALF) in mice with OVA-induced asthma. These effects were verified by histological evaluation of the levels of infiltration of inflammatory cells and collagen, destructions of alveoli and bronchioles, and hyperplasia of goblet cells in lung tissues. The effects of SJT microparticles in the asthma model were equivalent to those of orally-administered SJT extract. Conclusion: This study suggests that SJT is a promising agent for inhalation therapy for patients with asthma. PMID:28097040

  3. Inhaled human insulin.

    PubMed

    Strack, Thomas R

    2006-04-01

    The benefit of subcutaneous insulin therapy in patients with diabetes is frequently limited due to difficulty in convincing patients of the importance of multiple daily insulin injections to cope effectively with meal-associated glycemic changes. Thus, the aim of achieving tight glycemic control, which is critical for reducing the risk of long-term diabetes-related complications, frequently remains elusive. The successful development of an inhalable insulin as a noninvasive alternative promises to change the management of diabetes. The first product to become available to patients is inhaled human insulin, a dry-powder formulation packaged into discrete blisters containing 1 or 3 mg of dry-powder human insulin and administered via a unique pulmonary inhaler device. It has recently been approved in both the United States and the European Union for the control of hyperglycemia in adult patients with type 1 or type 2 diabetes. The pharmacokinetic profile of inhaled human insulin closely mimics the natural pattern of insulin secretion, and resembles that of rapid-acting subcutaneous analogs. Similarly to rapid-acting subcutaneous analogs, inhaled human insulin has a more rapid onset of glucose-lowering activity compared to subcutaneous regular insulin, allowing it to be administered shortly before meals. It has a duration of glucose-lowering activity comparable to subcutaneous regular insulin and longer than rapid-acting insulin analogs. Inhaled human insulin effectively controls postprandial glucose concentrations in patients with type 1 or type 2 diabetes without increasing the risk of hypoglycemia, and even improves fasting glucose levels compared to subcutaneous insulin. Inhaled human insulin has an overall favorable safety profile. There are small reductions in lung function (1-1.5% of total lung forced expiratory volume in the first second [FEV1] capacity) after onset of treatment that are reversible in most patients if treatment is discontinued. Inhaled human

  4. Fabrication and electrochemical performance of 0.6Li2MnO3-0.4Li(Ni1/3Co1/3Mn1/3)O2 microspheres by two-step spray-drying process

    PubMed Central

    Son, Mun Yeong; Lee, Jung-Kul; Kang, Yun Chan

    2014-01-01

    0.6Li2MnO3–0.4Li(Ni1/3Co1/3Mn1/3)O2 composite microspheres with dense structures are prepared by a two-step spray-drying process. Precursor powders with hollow and porous structures prepared by the spray-drying process are post-treated at a low temperature of 400°C and then wet-milled to obtain a slurry with high stability. The slurry of the mixture of metal oxides is spray-dried to prepare precursor aggregate powders several microns in size. Post-treatment of these powders at high temperatures (>700°C) produces 0.6Li2MnO3–0.4Li(Ni1/3Co1/3Mn1/3)O2 composite microspheres with dense structures and high crystallinity. The mean size and geometric standard deviation of the composite microspheres post-treated at 900°C are 4 μm and 1.38, respectively. Further, the initial charge capacities of the aggregated microspheres post-treated at 700, 800, 900, and 1000°C are 336, 349, 383, and 128 mA h g−1, respectively, and the corresponding discharge capacities are 286, 280, 302, and 77 mA h g−1, respectively. The discharge capacity of the composite microspheres post-treated at an optimum temperature of 900°C after 100 cycles is 242 mA h g−1, and the corresponding capacity retention is 80%. PMID:25168912

  5. A comparative study of a range of polymeric microspheres as potential carriers for the inhalation of proteins.

    PubMed

    Sivadas, Neeraj; O'Rourke, Desmond; Tobin, Aoife; Buckley, Vivienne; Ramtoola, Zeibun; Kelly, John G; Hickey, Anthony J; Cryan, Sally-Ann

    2008-06-24

    The aim of this study was to compare protein-loaded inhalable microparticles manufactured using a range of biocompatible polymers including hydroxypropyl cellulose (HPC), chitosan, hyaluronic acid, alginate, gelatin, ovalbumin and poly(lactide-co-glycolide) (PLGA). Spray-drying was used to prepare microparticles containing bovine serum albumin labeled with fluorescein isothiocyanate (BSA-FITC). Particles of respirable size and high protein loading were obtained. No evidence of BSA degradation was seen from PAGE analysis. The microparticles were mixed with mannitol as a carrier and powder aerosolization was assessed with a multi-dose dry powder inhaler (DPI) using a multi-stage cascade impactor. The mass median aerodynamic diameter (MMAD) ranged between 2.9 and 4.7 microm. Potential polymer toxicity in the lungs was compared by impinging the particles on Calu-3 monolayers and assessing the cytotoxicity, induction of cytokine release, changes in transepithelial permeability and electrical resistance. No toxic effects were observed with most of the polymers though some evidence of compromised cell monolayer integrity was seen for PLGA and ovalbumin. PLGA and gelatin microparticles caused a significant increase in IL-8 release. Of the polymers studied, PLGA showed the greatest toxicity. Certain polymers showed particular promise for specific protein delivery needs in the lungs, such as HPC to improve flow properties, sodium hyaluronate for controlled release, and chitosan and ovalbumin for systemic delivery.

  6. Inhaled Antibiotics for Lower Airway Infections

    PubMed Central

    Quon, Bradley S.; Goss, Christopher H.

    2014-01-01

    Inhaled antibiotics have been used to treat chronic airway infections since the 1940s. The earliest experience with inhaled antibiotics involved aerosolizing antibiotics designed for parenteral administration. These formulations caused significant bronchial irritation due to added preservatives and nonphysiologic chemical composition. A major therapeutic advance took place in 1997, when tobramycin designed for inhalation was approved by the U.S. Food and Drug Administration (FDA) for use in patients with cystic fibrosis (CF) with chronic Pseudomonas aeruginosa infection. Attracted by the clinical benefits observed in CF and the availability of dry powder antibiotic formulations, there has been a growing interest in the use of inhaled antibiotics in other lower respiratory tract infections, such as non-CF bronchiectasis, ventilator-associated pneumonia, chronic obstructive pulmonary disease, mycobacterial disease, and in the post–lung transplant setting over the past decade. Antibiotics currently marketed for inhalation include nebulized and dry powder forms of tobramycin and colistin and nebulized aztreonam. Although both the U.S. Food and Drug Administration and European Medicines Agency have approved their use in CF, they have not been approved in other disease areas due to lack of supportive clinical trial evidence. Injectable formulations of gentamicin, tobramycin, amikacin, ceftazidime, and amphotericin are currently nebulized “off-label” to manage non-CF bronchiectasis, drug-resistant nontuberculous mycobacterial infections, ventilator-associated pneumonia, and post-transplant airway infections. Future inhaled antibiotic trials must focus on disease areas outside of CF with sample sizes large enough to evaluate clinically important endpoints such as exacerbations. Extrapolating from CF, the impact of eradicating organisms such as P. aeruginosa in non-CF bronchiectasis should also be evaluated. PMID:24673698

  7. Acute Inhalation Injury

    PubMed Central

    Gorguner, Metin; Akgun, Metin

    2010-01-01

    Inhaled substances may cause injury in pulmonary epithelium at various levels of respiratory tract, leading from simple symptoms to severe disease. Acute inhalation injury (AII) is not uncommon condition. There are certain high risk groups but AII may occur at various places including home or workplace. Environmental exposure is also possible. In addition to individual susceptibility, the characteristics of inhaled substances such as water solubility, size of substances and chemical properties may affect disease severity as well as its location. Although AII cases may recover in a few days but AII may cause long-term complications, even death. We aimed to discuss the effects of short-term exposures (minutes to hours) to toxic substances on the lungs. PMID:25610115

  8. Inhalation exposure methodology.

    PubMed Central

    Phalen, R F; Mannix, R C; Drew, R T

    1984-01-01

    Modern man is being confronted with an ever-increasing inventory of potentially toxic airborne substances. Exposures to these atmospheric contaminants occur in residential and commercial settings, as well as in the workplace. In order to study the toxicity of such materials, a special technology relating to inhalation exposure systems has evolved. The purpose of this paper is to provide a description of the techniques which are used in exposing laboratory subjects to airborne particles and gases. The various modes of inhalation exposure (whole body, head only, nose or mouth only, etc.) are described at length, including the advantages and disadvantages inherent to each mode. Numerous literature citations are included for further reading. Among the topics briefly discussed are the selection of appropriate animal species for toxicological testing, and the types of inhalation studies performed (acute, chronic, etc.). PMID:6383799

  9. New aspects of developing a dry powder inhalation formulation applying the quality-by-design approach.

    PubMed

    Pallagi, Edina; Karimi, Keyhaneh; Ambrus, Rita; Szabó-Révész, Piroska; Csóka, Ildikó

    2016-09-10

    The current work outlines the application of an up-to-date and regulatory-based pharmaceutical quality management method, applied as a new development concept in the process of formulating dry powder inhalation systems (DPIs). According to the Quality by Design (QbD) methodology and Risk Assessment (RA) thinking, a mannitol based co-spray dried formula was produced as a model dosage form with meloxicam as the model active agent. The concept and the elements of the QbD approach (regarding its systemic, scientific, risk-based, holistic, and proactive nature with defined steps for pharmaceutical development), as well as the experimental drug formulation (including the technological parameters assessed and the methods and processes applied) are described in the current paper. Findings of the QbD based theoretical prediction and the results of the experimental development are compared and presented. Characteristics of the developed end-product were in correlation with the predictions, and all data were confirmed by the relevant results of the in vitro investigations. These results support the importance of using the QbD approach in new drug formulation, and prove its good usability in the early development process of DPIs. This innovative formulation technology and product appear to have a great potential in pulmonary drug delivery.

  10. Comparison of particle sizing techniques in the case of inhalation dry powders.

    PubMed

    Bosquillon, C; Lombry, C; Preat, V; Vanbever, R

    2001-12-01

    The objectives of this work were (i) to validate electrical zone sensing and laser diffraction for the analysis of primary particle size in the case of inhalation dry powders and (ii) to study the influence of the aggregation state of the powder on the sizing techniques. Free-flowing dry powders were prepared by spray-drying with a combination of albumin, lactose, and dipalmitoylphosphatidylcholine. The replacement of lactose by mannitol, the removal of albumin, and the atomization at high relative humidity all increased powder cohesion. Automated measurements were compared with primary particle sizes collected by light and electron microscopy. The mass mode obtained by electrical zone sensing and the mass median diameter measured by laser diffraction following dispersion with compressed air at a pressure of 3 bar or following suspension in water and ultrasonic dispersion at a power of 60 W for 30 s each provided primary particle sizes close to microscopy measurements. However, these conditions only applied in the case of slightly to moderately aggregated powders. For strongly agglomerated powders, an exact measurement of the size was only collected by laser diffraction in the wet state combined with ultrasonic dispersion. Our study underlies how measurement of primary particle size highly depends on both powder material and proper particle dispersion.

  11. MODELING DEPOSITION OF INHALED PARTICLES

    EPA Science Inventory

    Modeling Deposition of Inhaled Particles: ABSTRACT

    The mathematical modeling of the deposition and distribution of inhaled aerosols within human lungs is an invaluable tool in predicting both the health risks associated with inhaled environmental aerosols and the therapeut...

  12. Effect of dry- versus wet-autoclaving of spray-dried egg albumen compared with casein as protein sources on apparent nitrogen and energy balance, plasma urea nitrogen and glucose concentrations, and growth performance of neonatal swine.

    PubMed

    Watkins, K L; Veum, T L

    2010-08-01

    Forty crossbred neonatal pigs with an average initial age of 4 d and BW of 2.16 kg were used in a 28-d experiment to evaluate the nutritional effects of autoclaving a commercial sugar-free, spray-dried egg albumen (EA) compared with casein. Basal diet protein sources were lactic acid casein and EA. Two more dietary treatments were made by replacing the EA with dry-autoclaved EA (DAEA) or wet-autoclaved EA (WAEA, EA and water mixed in a 1.0:1.2 ratio before autoclaving). The DAEA and WAEA were autoclaved at 121 degrees C and 1.75 kg/cm(2) pressure for 30 min, and WAEA was oven-dried after autoclaving. Analyzed trypsin inhibitor units/mg of EA, DAEA, and WAEA were 535.0, 9.0, and 6.5, respectively. Pigs were fed the diets in gruel form to appetite in individual metabolism cages every 2 h during the experiment. Blood samples were taken on d 7, 14, and 21, and total urine and fecal grab-samples were collected from d 14 to 21 of the experiment. Response criteria were N and energy balance, plasma urea N (PUN) and glucose concentrations, and growth performance. The WAEA was a higher quality protein source for neonatal pigs than DAEA. Pigs fed the diet containing WAEA absorbed and retained more (P < 0.05) grams of N/d, had higher (P < 0.05) percentages of N and energy that were absorbed and retained/intake, had lower (P < 0.05) concentrations of PUN overall, and had higher (P < 0.05) ADG and G:F than pigs fed the diet containing DAEA. Most response criteria of pigs fed the diets containing DAEA or EA were not different, although pigs fed the diet containing DAEA had lower (P < 0.05) overall PUN concentrations, and pigs fed the diet containing EA had higher (P < 0.05) percentages of energy absorbed and retained/intake, and higher ADG and G:F than pigs fed the diet containing DAEA. Growth performance was not different for pigs fed the diets containing WAEA or casein. However, pigs fed the diet containing casein excreted less (P < 0.05) fecal N, retained more (P < 0/05) grams

  13. Inhalants. Specialized Information Service.

    ERIC Educational Resources Information Center

    Do It Now Foundation, Phoenix, AZ.

    The document presents a collection of articles about inhalant abuse. Article 1 presents findings on the psychophysiological effects related to the use of amyl or butyl nitrate as a "recreational drug." Article 2 suggests a strong association between chronic sniffing of the solvent toulene and irreversible brain damage. Article 3 warns…

  14. Efficient Nose-to-Lung (N2L) Aerosol Delivery with a Dry Powder Inhaler

    PubMed Central

    Golshahi, Laleh; Behara, Srinivas R.B.; Tian, Geng; Farkas, Dale R.; Hindle, Michael

    2015-01-01

    Abstract Purpose: Delivering aerosols to the lungs through the nasal route has a number of advantages, but its use has been limited by high depositional loss in the extrathoracic airways. The objective of this study was to evaluate the nose-to-lung (N2L) delivery of excipient enhanced growth (EEG) formulation aerosols generated with a new inline dry powder inhaler (DPI). The device was also adapted to enable aerosol delivery to a patient simultaneously receiving respiratory support from high flow nasal cannula (HFNC) therapy. Methods: The inhaler delivered the antibiotic ciprofloxacin, which was formulated as submicrometer combination particles containing a hygroscopic excipient prepared by spray-drying. Nose-to-lung delivery was assessed using in vitro and computational fluid dynamics (CFD) methods in an airway model that continued through the upper tracheobronchial region. Results: The best performing device contained a 2.3 mm flow control orifice and a 3D rod array with a 3-4-3 rod pattern. Based on in vitro experiments, the emitted dose from the streamlined nasal cannula had a fine particle fraction <5 μm of 95.9% and mass median aerodynamic diameter of 1.4 μm, which was considered ideal for nose-to-lung EEG delivery. With the 2.3-343 device, condensational growth in the airways increased the aerosol size to 2.5–2.7 μm and extrathoracic deposition was <10%. CFD results closely matched the in vitro experiments and predicted that nasal deposition was <2%. Conclusions: The developed DPI produced high efficiency aerosolization with significant size increase of the aerosol within the airways that can be used to enable nose-to-lung delivery and aerosol administration during HFNC therapy. PMID:25192072

  15. Development and evaluation of a dry powder formulation of liposome-encapsulated oseltamivir phosphate for inhalation.

    PubMed

    Tang, Yue; Zhang, Heyang; Lu, Xifeng; Jiang, Liqun; Xi, Xinyuan; Liu, Jianping; Zhu, Jiabi

    2015-01-01

    This study aims to develop oseltamivir phosphate (OP) liposomes as inhalation powders by spray-drying based on the single factor investigation, which was mainly composed of lactose, L-leucine and mannitol. It was found that the ratio of OP and liposomes (1:10), inlet temperature (110 °C) and airflow rate (2.3 mL/min) showed optimized physical properties of OP liposomes. Deposition was evaluated after the aerosolization of powders at 600 L/h via the Aerolizer® into a twin-stage impinger. The concentrations of OP and oseltamivir carboxylate (OSCA) in rats plasma using LC-MS have been determined and performed via pharmacokinetic software DAS 2.0 package. The liposomal OP dry powders displayed an average particle size around 3.5 µm with fine particle fraction (FPF = 35.40%). In vitro evaluation demonstrated a sustained release pattern accounting for 20% drug release compared to that of OP solution up to 90% drug release in 2 h. And the cumulative release percentage was up to 50% in 20 h. Atrioventricular fitting results indicated that all preparations were best fitted with a two-compartment model. There was a significant difference in MRT, Cmax and Tmax (p < 0.01) between the two groups of liposomal OP dry powders and OP solution with t-test, which indicated that the drug released slowly from liposomal OP dry powders in the lung. To sum up, dry powders formulation of liposome-encapsulated OP for inhalation was suitable for pulmonary administration, which offering the opportunity to reduce dosing frequency.

  16. In Vitro Evaluation of Inhalable Verapamil-Rifapentine Particles for Tuberculosis Therapy.

    PubMed

    Parumasivam, T; Chan, J G Y; Pang, A; Quan, D H; Triccas, J A; Britton, W J; Chan, H K

    2016-03-07

    Recent studies have demonstrated that efflux pumps of Mycobacterium tuberculosis (M. tb) provide a crucial mechanism in the development of drug resistant to antimycobacterial drugs. Drugs that inhibit these efflux pumps, such as verapamil, have shown the potential in enhancing the treatment success. We therefore hypothesized that the combined inhaled administration of verapamil and a first-line rifamycin antibiotic will further improve the treatment efficacy. An inhalable dry powder consisting of amorphous verapamil and crystalline rifapentine with l-leucine as an excipient was produced by spray drying. The in vitro aerosol characteristic of the powder, its microbiological activity and stability were assessed. When the powder was dispersed by an Osmohaler, the total fine particle fraction (FPFtotal, wt % of particles in aerosol <5 μm) of verapamil and rifapentine was 77.4 ± 1.1% and 71.5 ± 2.0%, respectively. The combination drug formulation showed a minimum inhibitory concentration (MIC90) similar to that of rifapentine alone when tested against both M. tb H37Ra and M. tb H37Rv strains. Importantly, the combination resulted in increased killing of M. tb H37Ra within the infected macrophage cells compared to either verapamil or rifapentine alone. In assessing cellular toxicity, the combination exhibited an acceptable half maximal inhibitory concentration (IC50) values (62.5 μg/mL) on both human monocytic (THP-1) and lung alveolar basal epithelial (A549) cell lines. Finally, the powder was stable after 3 months storage in 0% relative humidity at 20 ± 3 °C.

  17. Food hypersensitivity by inhalation

    PubMed Central

    Ramirez, Daniel A; Bahna, Sami L

    2009-01-01

    Though not widely recognized, food hypersensitivity by inhalation can cause major morbidity in affected individuals. The exposure is usually more obvious and often substantial in occupational environments but frequently occurs in non-occupational settings, such as homes, schools, restaurants, grocery stores, and commercial flights. The exposure can be trivial, as in mere smelling or being in the vicinity of the food. The clinical manifestations can vary from a benign respiratory or cutaneous reaction to a systemic one that can be life-threatening. In addition to strict avoidance, such highly-sensitive subjects should carry self-injectable epinephrine and wear MedicAlert® identification. Asthma is a strong predisposing factor and should be well-controlled. It is of great significance that food inhalation can cause de novo sensitization. PMID:19232116

  18. Treatment of Inhalation Injury

    DTIC Science & Technology

    1983-01-21

    injuries not visible with endoscopy. . Thermal and especially chemical inhalation injuries. Direct damage to the surfactant is probably implicated. o...exists a set of indirect alveolar lesions, subordinated to the skin burn itself, which is common in patients with extensive burns. This we call the...normo or hypocapnia. Very likely, a 5th lesional level exists which is the capillary itself(Venus et al). By primary or secondary damage , it affects the

  19. How to Use Metered-Dose Inhalers

    MedlinePlus

    ... inhaler the right way so that the full dose of medication reaches your lungs. You can use ... inhaler.These directions explain how to use metered-dose inhalers. If you are using a different type ...

  20. Inhaled formulations and pulmonary drug delivery systems for respiratory infections.

    PubMed

    Zhou, Qi Tony; Leung, Sharon Shui Yee; Tang, Patricia; Parumasivam, Thaigarajan; Loh, Zhi Hui; Chan, Hak-Kim

    2015-05-01

    Respiratory infections represent a major global health problem. They are often treated by parenteral administrations of antimicrobials. Unfortunately, systemic therapies of high-dose antimicrobials can lead to severe adverse effects and this calls for a need to develop inhaled formulations that enable targeted drug delivery to the airways with minimal systemic drug exposure. Recent technological advances facilitate the development of inhaled anti-microbial therapies. The newer mesh nebulisers have achieved minimal drug residue, higher aerosolisation efficiencies and rapid administration compared to traditional jet nebulisers. Novel particle engineering and intelligent device design also make dry powder inhalers appealing for the delivery of high-dose antibiotics. In view of the fact that no new antibiotic entities against multi-drug resistant bacteria have come close to commercialisation, advanced formulation strategies are in high demand for combating respiratory 'super bugs'.

  1. Inhalation exposure of animals.

    PubMed Central

    Phalen, R F

    1976-01-01

    Relative advantages and disadvantages and important design criteria for various exposure methods are presented. Five types of exposures are discussed: whole-body chambers, head-only exposures, nose or mouth-only methods, lung-only exposures, and partial-lung exposures. Design considerations covered include: air cleaning and conditioning; construction materials; losses of exposure materials; evenness of exposure; sampling biases; animal observation and care; noise and vibration control, safe exhausts, chamber loading, reliability, pressure fluctuations; neck seals, masks, animal restraint methods; and animal comfort. Ethical considerations in use of animals in inhalation experiments are also discussed. PMID:1017420

  2. Pharmacokinetics and pharmacodynamics of controlled release insulin loaded PLGA microcapsules using dry powder inhaler in diabetic rats.

    PubMed

    Hamishehkar, Hamed; Emami, Jaber; Najafabadi, Abdolhossien Rouholamini; Gilani, Kambiz; Minaiyan, Mohsen; Hassanzadeh, Kambiz; Mahdavi, Hamid; Koohsoltani, Maryam; Nokhodchi, Ali

    2010-03-01

    The pulmonary route is an alternative route of administration for the systemic delivery of peptide and proteins with short-half lives. A long-acting formulation of insulin was prepared by encapsulation of protein into respirable, biodegradable microcapsules prepared by an oil in oil emulsification/solvent evaporation method. Insulin-loaded PLGA microcapsules prepared as a dry powder inhaler formulation were administered via the pulmonary route to diabetic rats and serum insulin and glucose concentrations were monitored. Control treatments consisted of respirable spray-dried insulin (RSDI) powder administered by intratracheal insufflation, insulin-loaded PLGA microcapsules and NPH (long-acting) insulin administered by subcutaneous (SC) administration. Pharmacokinetic analysis demonstrated that insulin administered in PLGA microcapsules illustrated a sustained release profile which resulted in a longer mean residence time, 4 and 5 fold longer than those after pulmonary administration of RSDI and SC injection of NPH insulin, respectively. Accordingly, the hypoglycemic profile followed a stable and sustained pattern which remained constant between 10 and 48 h. Results of the in vitro experiments were in good agreement with those of in vivo studies. Bronchoalveolar lavage fluid analysis indicated that microcapsules administration did not increase the activities of lactate dehydrogenase and total protein. However, histological examination of the lung tissue indicated a minor but detectable effect on the normal physiology of the rat lung. These findings suggest that the encapsulation of peptides and proteins into PLGA microcapsules technique could be a promising controlled delivery system for pulmonary administration.

  3. Inhaled insulin--does it become reality?

    PubMed

    Siekmeier, R; Scheuch, G

    2008-12-01

    After more than 80 years of history the American and European Drug Agencies (FDA and EMEA) approved the first pulmonary delivered version of insulin (Exubera) from Pfizer/Nektar early 2006. However, in October 2007, Pfizer announced it would be taking Exubera off the market, citing that the drug had failed to gain market acceptance. Since 1924 various attempts have been made to get away from injectable insulin. Three alternative delivery methods where always discussed: Delivery to the upper nasal airways or the deep lungs, and through the stomach. From these, the delivery through the deep lungs is the most promising, because the physiological barriers for the uptake are the smallest, the inspired aerosol is deposited on a large area and the absorption into the blood happens through the extremely thin alveolar membrane. However, there is concern about the long-term effects of inhaling a growth protein into the lungs. It was assumed that the large surface area over which the insulin is spread out would minimize negative effects. But recent news indicates that, at least in smokers, the bronchial tumour rate under inhaled insulin seems to be increased. These findings, despite the fact that they are not yet statistical significant and in no case found in a non-smoker, give additional arguments to stop marketing this approach. Several companies worked on providing inhalable insulin and the insulin powder inhalation system Exubera was the most advanced technology. Treatment has been approved for adults only and patients with pulmonary diseases (e.g., asthma, emphysema, COPD) and smokers (current smokers and individuals who recently quitted smoking) were excluded from this therapy. Pharmacokinetics and pharmacodynamics of Exubera are similar to those found with short-acting subcutaneous human insulin or insulin analogs. It is thus possible to use Exubera as a substitute for short-acting human insulin or insulin analogs. Typical side effects of inhaled insulin were coughing

  4. Blood Gases as an Indicator of Inhalation Injury and Prognosis in Burn Patients

    PubMed Central

    Megahed, M.A.; Ghareeb, F.; Kishk, T.; El-Barah, A.; Abou-Gereda, H.; El-Fol, H.; El-Sisy, A.; Omran, A.M.

    2008-01-01

    Summary Inhalation injury greatly increases the incidence of respiratory failure and the acute respiratory distress syndrome. It is also the cause of most early deaths in burn victims. The aim of our research was to study the incidence, early diagnosis, complications, and management of inhalation injury and to discuss the relation between inhalation injury and death in burn patients.This study included 130 burn patients with inhalation injury admitted to Menoufiya University Hospital Burn Center, Egypt, from January 2004 to April 2008 (61 males and 69 females). We found that the presence of inhalation injury, increasing burn size, and advancing age were all associated with increased mortality (p < 0.01). The incidence of inhalation injury in our study was 46.3% (130 patients were identified as having inhalation injury out of 281). The overall mortality for patients with inhalation injury was 41.5% (54 patients out of 130) compared with 7.2% (11 patients out of 151) for patients without inhalation injury. These statistical data make it clear that inhalation injury is an important factor for the prediction of mortality in burn patients. Approximately 80% of fire-related deaths are due not to the burn injury to the airway but to the inhalation of toxic products, especially carbon monoxide and hydrogen cyanide gases. Inhalation injury is generally caused by thermal burns, mostly confined to the upper airways.Major airway, pulmonary, and systemic complications may occur in cases of inhalation injury and thus increase the incidence of burn patient mortality PMID:21991136

  5. Inhalation delivery of protein therapeutics.

    PubMed

    Kane, Colleen; O'Neil, Karyn; Conk, Michelle; Picha, Kristen

    2013-04-01

    Inhaled therapeutics are used routinely to treat a variety of pulmonary diseases including asthma, COPD and cystic fibrosis. In addition, biological therapies represent the fastest growing segment of approved pharmaceuticals. However, despite the increased availability of biological therapies, nearly all inhaled therapeutics are small molecule drugs with only a single inhaled protein therapeutic approved. There remains a significant unmet need for therapeutics in pulmonary diseases, and biological therapies with potential to alter disease progression represent a significant opportunity to treat these challenging diseases. This review provides a background into efforts to develop inhaled biological therapies and highlights some of the associated challenges. In addition, we speculate on the ideal properties of a biologic therapy for inhaled delivery.

  6. New dry powders for inhalation containing temozolomide-based nanomicelles for improved lung cancer therapy.

    PubMed

    Rosière, Rémi; Gelbcke, Michel; Mathieu, Véronique; Van Antwerpen, Pierre; Amighi, Karim; Wauthoz, Nathalie

    2015-09-01

    Besides the numerous advantages of a chemotherapy administered by the inhalation route for lung cancer therapy, dry powder for inhalation (DPI) offers many advantages compared to other techniques and seems to be a technique that is well-adapted to an anticancer treatment. DPI formulations were developed using the cytotoxic drug temozolomide and a new folate-grafted self-assembling copolymer, a conjugate of three components, folate-polyethylene glycol-hydrophobically-modified dextran (F-PEG-HMD). F-PEG-HMD was synthesized using carbodiimide-mediated coupling chemistry in three main steps. F-PEG-HMD was characterized by 1H-NMR, mass spectrometry and thermal analysis. F-PEG-HMD presented a critical micellar concentration in water of 4x10-7 M. F-PEG-HMD nanomicelles were characterized by a trimodal particle size distribution with Z-average diameter of 83±1 nm in water. Temozolomide-loaded nanomicelles were prepared by solubilization of F-PEG-HMD in the presence of temozolomide. Temozolomide solubility in water was increased in the presence of F-PEG-HMD (2-fold increase in molar solubility) which could potentially lead to increased local concentrations in the tumor site. The temozolomide-loaded F-PEG-HMD nanomicelles were characterized by a Z-average diameter of ~50 to ~60 nm, depending on the F-PEG-HMD concentration used. The nanomicelles were then spray-dried to produce dry powders. Temozolomide remained stable during all the formulation steps, confirmed by similar in vitro anticancer properties for the DPI formulations and a raw temozolomide solution. Two of the developed DPI formulations were characterized by good aerodynamic properties (with a fine particle fraction of up to 50%) and were able to release the F-PEG-HMD nanomicelles quickly in aqueous media. Moreover, in vitro, the two DPI formulations showed wide pulmonary deposition in the lower respiratory tract where adenocarcinomas are more often found. The present study, therefore, shows that F

  7. Exubera. Inhale therapeutic systems.

    PubMed

    Bindra, Sanjit; Cefalu, William T

    2002-05-01

    Inhale, in colaboration with Pfizer and Aventis Pharma (formerly Hoechst Marion Roussel; HMR), is developing an insulin formulation utilizing its pulmonary delivery technology for macromolecules for the potential treatment of type I and II diabetes. By July 2001, the phase III program had been completed and the companies had begun to assemble data for MAA and NDA filings; however, it was already clear at this time that additional data might be required for filing. By December 2001, it had been decided that the NDA should include an increased level of controlled, long-term pulmonary safety data in diabetic patients and a major study was planned to be completed in 2002, with the NDA filed thereafter (during 2002). US-05997848 was issued to Inhale Therapeutic Systems in December 1999, and corresponds to WO-09524183, filed in February 1995. Equivalent applications have appeared to date in Australia, Brazil, Canada, China, Czech Republic, Europe, Finland, Hungary, Japan, Norway, New Zealand, Poland and South Africa. This family of applications is specific to pulmonary delivery of insulin. In February 1999, Lehman Brothers gave this inhaled insulin a 60% probability of reaching market, with a possible launch date of 2001. The analysts estimated peak sales at $3 billion in 2011. In May 2000, Aventis predicted that estimated peak sales would be in excess of $1 billion. In February 2000, Merrill Lynch expected product launch in 2002 and predicted that it would be a multibillion-dollar product. Analysts Merril Lynch predicted, in September and November 2000, that the product would be launched by 2002, with sales in that year of e75 million, rising to euro 500 million in 2004. In April 2001, Merrill Lynch predicted that filing for this drug would occur in 2001. Following the report of the potential delay in regulatory filing, issued in July 2001, Deutsche Banc Alex Brown predicted a filing would take place in the fourth quarter of 2002 and launch would take place in the first

  8. Inhaled matters of the heart

    PubMed Central

    Zaky, Ahmed; Ahmad, Aftab; Dell’Italia, Louis J; Jahromi, Leila; Reisenberg, Lee Ann; Matalon, Sadis; Ahmad, Shama

    2015-01-01

    Inhalations of atmospheric pollutants, especially particulate matters, are known to cause severe cardiac effects and to exacerbate preexisting heart disease. Heart failure is an important sequellae of gaseous inhalation such as that of carbon monoxide. Similarly, other gases such as sulphur dioxide are known to cause detrimental cardiovascular events. However, mechanisms of these cardiac toxicities are so far unknown. Increased susceptibility of the heart to oxidative stress may play a role. Low levels of antioxidants in the heart as compared to other organs and high levels of reactive oxygen species produced due to the high energetic demand and metabolic rate in cardiac muscle are important in rendering this susceptibility. Acute inhalation of high concentrations of halogen gases is often fatal. Severe respiratory injury and distress occurs upon inhalation of halogens gases, such as chlorine and bromine; however, studies on their cardiac effects are scant. We have demonstrated that inhalation of high concentrations of halogen gases cause significant cardiac injury, dysfunction, and failure that can be critical in causing mortalities following exposures. Our studies also demonstrated that cardiac dysfunction occurs as a result of a direct insult independent of coexisting hypoxia, since it is not fully reversed by oxygen supplementation. Therefore, studies on offsite organ effects of inhaled toxic gases can impact development of treatment strategies upon accidental or deliberate exposures to these agents. Here we summarize the knowledge of cardiovascular effects of common inhaled toxic gases with the intent to highlight the importance of consideration of cardiac symptoms while treating the victims. PMID:26665179

  9. Rifapentine-loaded PLGA microparticles for tuberculosis inhaled therapy: Preparation and in vitro aerosol characterization.

    PubMed

    Parumasivam, Thaigarajan; Leung, Sharon S Y; Quan, Diana Huynh; Triccas, Jamie A; Britton, Warwick J; Chan, Hak-Kim

    2016-06-10

    Inhaled delivery of drugs incorporated into poly (lactic-co-glycolic acid) (PLGA) microparticles allows a sustained lung concentration and encourages phagocytosis by alveolar macrophages that harboring Mycobacterium tuberculosis. However, limited data are available on the effects of physicochemical properties of PLGA, including the monomer ratio (lactide:glycide) and molecular weight (MW) on the aerosol performance, macrophage uptake, and toxicity profile. The present study aims to address this knowledge gap, using PLGAs with monomer ratios of 50:50, 75:25 and 85:15, MW ranged 24 - 240kDa and an anti-tuberculosis (TB) drug, rifapentine. The PLGA-rifapentine powders were produced through a solution spray drying technique. The particles were spherical with a smooth surface and a volume median diameter around 2μm (span ~2). When the powders were dispersed using an Osmohaler(®) at 100L/min for 2.4s, the fine particle fraction (FPFtotal, wt.% particles in aerosol <5μm relative to the total recovered drug mass) was ranged between 52 and 57%, with no significant difference between the formulations. This result suggests that the monomer ratio and MW are not crucial parameters for the aerosol performance of PLGA. The phagocytosis analysis was performed using Thp-1 monocyte-derived macrophages. The highest rate of uptake was observed in PLGA 85:15 followed by 75:25 and 50:50 with about 90%, 80% and 70%, respectively phagocytosis over 4h of exposure. Furthermore, the cytotoxicity analysis on Thp-1 and human lung adenocarcinoma epithelial cells demonstrated that PLGA concentration up to 1.5mg/mL, regardless of the monomer composition and MW, were non-toxic. In conclusion, the monomer ratio and MW are not crucial in determining the aerosol performance and cytotoxicity profile of PLGA however, the particles with high lactide composition have a superior tendency for macrophage uptake.

  10. Dry powder inhalation of macromolecules using novel PEG-co-polyester microparticle carriers.

    PubMed

    Tawfeek, Hesham M; Evans, Andrew R; Iftikhar, Abid; Mohammed, Afzal R; Shabir, Anjum; Somavarapu, Satyanarayana; Hutcheon, Gillian A; Saleem, Imran Y

    2013-01-30

    This study investigated optimizing the formulation parameters for encapsulation of a model mucinolytic enzyme, α-chymotrypsin (α-CH), within a novel polymer; poly(ethylene glycol)-co-poly(glycerol adipate-co-ω-pentadecalactone), PEG-co-(PGA-co-PDL) which were then applied to the formulation of DNase I. α-CH or DNase I loaded microparticles were prepared via spray drying from double emulsion (w(1)/o/w(2)) utilizing chloroform (CHF) as the organic solvent, L-leucine as a dispersibility enhancer and an internal aqueous phase (w(1)) containing PEG4500 or Pluronic(®) F-68 (PLF68). α-CH released from microparticles was investigated for bioactivity using the azocasein assay and the mucinolytic activity was assessed utilizing the degradation of mucin suspension assay. The chemical structure of PEG-co-(PGA-co-PDL) was characterized by (1)H NMR and FT-IR with both analyses confirming PEG incorporated into the polymer backbone, and any unreacted units removed. Optimum formulation α-CH-CHF/PLF68, 1% produced the highest bioactivity, enzyme encapsulation (20.08±3.91%), loading (22.31±4.34 μg/mg), FPF (fine particle fraction) (37.63±0.97%); FPD (fine particle dose) (179.88±9.43 μg), MMAD (mass median aerodynamic diameter) (2.95±1.61 μm), and the mucinolytic activity was equal to the native non-encapsulated enzyme up to 5h. DNase I-CHF/PLF68, 1% resulted in enzyme encapsulation (17.44±3.11%), loading (19.31±3.27 μg/mg) and activity (81.9±2.7%). The results indicate PEG-co-(PGA-co-PDL) can be considered as a potential biodegradable polymer carrier for dry powder inhalation of macromolecules for treatment of local pulmonary diseases.

  11. Microparticulate/Nanoparticulate Powders of a Novel Nrf2 Activator and an Aerosol Performance Enhancer for Pulmonary Delivery Targeting the Lung Nrf2/Keap-1 Pathway.

    PubMed

    Muralidharan, Priya; Hayes, Don; Black, Stephen M; Mansour, Heidi M

    2016-01-01

    This systematic and comprehensive study reports for the first time on the successful rational design of advanced inhalable therapeutic dry powders containing dimethyl fumarate, a first-in-class Nrf2 activator drug to treat pulmonary inflammation, using particle engineering design technology for targeted delivery to the lungs as advanced spray dried (SD) one-component DPIs. In addition, two-component co-spray dried (co-SD) DMF:D-Man DPIs with high drug loading were successfully designed for targeted lung delivery as advanced DPIs using organic solution advanced spray drying in closed mode. Regional targeted deposition using design of experiments (DoE) for in vitro predictive lung modeling based on aerodynamic properties was tailored based on composition and spray drying parameters. These findings indicate the significant potential of using D-Man in spray drying to improve particle formation and aerosol performance of small molecule with a relatively low melting point. These respirable microparticles/nanoparticles in the solid-state exhibited excellent aerosol dispersion performance with an FDA-approved human DPI device. Using in vitro predictive lung deposition modeling, the aerosol deposition patterns of these particles show the capability to reach lower airways to treat inflammation in this region in pulmonary diseases such as acute lung injury (ALI), chronic obstructive pulmonary disease (COPD), pulmonary hypertension (PH), and pulmonary endothelial disease.

  12. Umeclidinium and Vilanterol Oral Inhalation

    MedlinePlus

    ... chest tightness caused by chronic obstructive pulmonary disease (COPD; a group of diseases that affect the lungs ... use umeclidinium and vilanterol inhalation during a sudden COPD attack. Your doctor will prescribe a short-acting ( ...

  13. Fluticasone and Vilanterol Oral Inhalation

    MedlinePlus

    ... and chest tightness caused by chronic obstructive pulmonary (COPD; a group of diseases that affect the lungs ... use fluticasone and vilanterol inhalation during a sudden COPD attack. Your doctor will prescribe a short acting ( ...

  14. Fluticasone and Salmeterol Oral Inhalation

    MedlinePlus

    ... caused by asthma and chronic obstructive pulmonary disease (COPD; a group of lung diseases that includes chronic ... and salmeterol during an attack of asthma or COPD. Your doctor will prescribe a short-acting inhaler ...

  15. Potent Inhalational Anesthetics for Dentistry

    PubMed Central

    Satuito, Mary; Tom, James

    2016-01-01

    Nitrous oxide and the volatile inhalational anesthetics have defined anxiety and pain control in both dentistry and medicine for over a century. From curious experimentation to spectacular public demonstrations, the initial work of 2 dentists, Horace Wells and William T. G. Morton, persists to this day in modern surgery and anesthesia. This article reviews the history, similarities, differences, and clinical applications of the most popular inhalational agents used in contemporary dental surgical settings. PMID:26866411

  16. Physical Characterization of Tobramycin Inhalation Powder: I. Rational Design of a Stable Engineered-Particle Formulation for Delivery to the Lungs.

    PubMed

    Miller, Danforth P; Tan, Trixie; Tarara, Thomas E; Nakamura, John; Malcolmson, Richard J; Weers, Jeffry G

    2015-08-03

    A spray-dried engineered particle formulation, Tobramycin Inhalation Powder (TIP), was designed through rational selection of formulation composition and process parameters. This PulmoSphere powder comprises small, porous particles with a high drug load. As a drug/device combination, TOBI Podhaler enables delivery of high doses of drug per inhalation, a feature critical for dry powder delivery of anti-infectives for treatment of cystic fibrosis. The objective of this work was to characterize TIP on both the particle and molecular levels using multiple orthogonal physical characterization techniques. Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), electron spectroscopy for chemical analysis (ESCA), and Raman measurements show that a TIP particle consists of two phases: amorphous, glassy tobramycin sulfate with a glass transition temperature of about 100 °C and a gel-phase phospholipid (DSPC) with a gel-to-liquid-crystal transition temperature of about 80 °C. This was by design and constituted a rational formulation approach to provide Tg and Tm values that are well above the temperatures used for long-term storage of TIP. Raman and ESCA data provide support for a core/shell particle architecture of TIP. Particle surfaces are enriched with a porous, hydrophobic coating that reduces cohesive forces, improving powder fluidization and dispersibility. The excellent aerosol dispersibility of TIP enables highly efficient delivery of fine particles to the respiratory tract. Collectively, particle engineering has enabled development of TOBI Podhaler, an approved inhaled drug product that meaningfully reduces the treatment burden to cystic fibrosis patients worldwide.