scholarly journals Physicochemical and Aerosolization Assessment of Inhalable Spray Dried Fluconazole Powder

2018 ◽  
Vol 24 (3) ◽  
pp. 219-226 ◽  
Author(s):  
Hamed Hamishehkar ◽  
Maryam Pourtahmaseb ◽  
Afshin Babazadeh ◽  
Shohreh Alipour

Background: Respiratory fungal diseases therapy is still facing challenges as a result of increasing autoimmune disorders, cancers, and immunosuppressive medication usage. Fluconazole is a wide spectrum antifungal agent and is still used successfully in the treatment of opportunistic infections in combination with other antifungal agents. Since, the treatment of respiratory fungal diseases requires prolonged hospitalization; it may increase the chances of other opportunistic infections. Considering the reported drug resistance and adverse effects of systemic administration, it appears that localized pulmonary antifungal therapy may be a suitable alternative route. According to the reported suitable inhalation properties of spray dried powders; spray drying technique was used to prepare fluconazole powders. Methods: Different spray drying parameters such as inlet temperature, pump rate, aspiration%, solvent type, as well as fluconazole concentration were evaluated for powder production. The optimized formulations were characterized using scanning electron microscopy (SEM), x-ray diffraction (XRD), differential scanning calorimetry (DSC) and aerodynamic parameters. Results: All selected formulations showed a smooth surface with similar mass median aerodynamic diameter (MMAD) in a respiratory acceptable range. While optimized powder showed a lower geometric standard deviation (GSD) of 1.5 with higher fine particle fraction (FPF) of 26% and almost complete deposition recovery of 97%. Conclusion: Based on in vitro characterization results, it appears that spray drying is an appropriate and cost-effective technique for the production of inhalable fluconazole powder. It is characterized by a narrower size distribution and delivers a higher dose which may be more cost effective for mass production.

2018 ◽  
Vol 38 (8) ◽  
pp. 775-783 ◽  
Author(s):  
Israr Ahmed ◽  
Muhammad Bilal Khan Niazi ◽  
Zaib Jahan ◽  
Salman Raza Naqvi

Abstract This study focuses on the thermal, morphological and physical properties of spray-dried chicory root inulin using a thermogravimetric analyzer, environmental scanning electron microscopy, X-ray diffractogram and modulated differential scanning calorimetry. Different spray-drying conditions were investigated by varying inlet temperature, outlet temperature and aspirator speed. The starting material was semicrystalline. A feed temperature of 95°C was employed, which produced a completely transparent solution for spray drying. At that particular temperature, the powder samples obtained were entirely amorphous and morphology resembled each other except for higher solid content. The low glass transition temperature (Tg) (106.83°C) was evident by treating low-molecular-weight samples, whereas high-molecular-weight samples exhibited high Tg (125.81°C). The semicrystalline samples due to the high concentration and milky dispersion exhibited high decomposition temperature. The feed temperature, molecular weight and concentration of the samples tend to have a significant effect on the properties of spray-dried inulin.


Author(s):  
Kusuma P. ◽  
Syukri Y ◽  
Sholehuddin F. ◽  
Fazzri N. ◽  
Romdhonah . ◽  
...  

The most efficient tablet processing method is direct compression. For this method, the filler-binder can be made by coprocessing via spray drying method. The purpose of this study was to investigate the effect of spray dried co-processing on microcrystalline cellulose (MCC) PH 101, lactose and Kollidon® K 30 as well as to define the optimum proportions. Spray dried MCC PH 101, lactose, and Kollidon® K 30 were varied in 13 different mixture design proportions to obtain compact, free-flowing filler-binder co-processed excipients (CPE). Compactibility and flow properties became the key parameters to determine the optimum proportions of CPE that would be compared to their physical mixtures. The result showed that the optimum proportion of CPE had better compactibility and flow properties than the physical mixtures. The optimum CPE, consisting of only MCC PH 101 and Kollidon® K 30 without lactose, that were characterized using infrared spectrophotometer, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscope (SEM) indicated no chemical change therein. Therefore, this study showed that spray dried MCC PH 101, lactose and Kollidon® K 30 could be one of the filler-binder alternatives for direct compression process.


Author(s):  
Aliasgar J Kundawala ◽  
Khushbu S Chauhan ◽  
Harsha V Patel ◽  
Swati K Kurtkoti

Budesonide is an anti-asthmatic agent which is used to control the symptoms of asthma like bronchospasm, oedema. Drug delivered to lung through inhalation will provide systemic and local drug delivery at lower dose in chronic and acute diseases. Dry powder inhalers are the best choice for targeting the anti-asthmatic drugs through pulmonary route. The objective of the present study is to prepare inhalable lipid coated budesonide microparticles by spray drying method so effective delivery of budesonide to the lungs can be achieved. The microparticles in the form of dry powder were obtained by either spray drying liposomal drug suspension or lipid drug suspension. The liposomes were initially prepared by solvent evaporation method using Hydrogenated Soyabean Phosphatidylcholine and Cholesterol (1:1, 1:2, 2:1) as lipid carrier and then spray dried later with mannitol as bulking agent at different lipid to diluent ratio (1:1.25, 1:2.5 & 1:5). The liposomes and liposomal dry powder were evaluated for vesicle size, % entrapment efficiency, in vitro drug release studies, powder characteristics, aerosol performance and stability studies. The liposomes prepared showed vesicle size (2-8 µm), Entrapment efficiency (92.22%) at lipid: drug ratio of (2.5:1) and observed 80.41 % drug release in 24 hrs. Pro-liposomes prepared by spray drying of liposomal drug suspension (LSD1) showed emitted dose, mean mass aerodynamic diameter, geometric standard deviation and fine particle fraction of 99.01%, 3.12 µm, 1.78 and 43.5% along with good powder properties. The spray dried powder was found to be stable at 4 ± 2 °C & 65% ± 5 % RH. The inhalable microparticles containing Budesonide containing lipid dry powder was successfully prepared by spray drying method that showed good aerodynamic properties and stability with mannitol as diluent. The microparticles produced with this novel approach could deliver drug on target via inhalation route and also ease manufacture process at large scale in fewer production steps.


Author(s):  
Aleksandra A. Jovanović ◽  
Steva M. Lević ◽  
Vladimir B. Pavlovic ◽  
Smilja B. Markovic ◽  
Rada V. Pjanovic ◽  
...  

Freeze drying was compared with spray drying regarding feasibility to process wild thyme drug in order to obtain dry formulations at laboratory scale starting from liquid extracts produced by different extraction methods: maceration, heat-, ultrasound-, and microwave-assisted extractions. Higher powder yield (based on the dry weight prior to extraction) was achieved by freeze than spray drying and lower loss of total polyphenol content (TPC) and total flavonoid content (TFC) due to the drying process. Gelatin as a coating agent (5% w/w) provided better TPC recovery by 70% in case of lyophilization and higher powder yield in case of spray drying by diminishing material deposition on the wall of the drying chamber. The resulting gelatin-free and gelatin-containing powders carried polyphenols in amount ~190 and 53-75 mg gallic acid equivalents GAE/g of powder, respectively. Microwave-assisted extract formulation distinguished from others by higher content of polyphenols, proteins and sugars, higher bulk density and lower solubility. The type of the drying process affected mainly position of the gelatin-derived -OH and amide bands in FTIR spectra. Spray dried formulations compared to freeze dried expressed higher thermal stability as confirmed by differential scanning calorimetry analysis and higher diffusion coefficient; the last feature can be associated with the lower specific surface area of irregularly shaped freeze-dried particles (151-223 µm) compared to small microspheres (~8 µm) in spray-dried powder.


2019 ◽  
Vol 3 (Supplement_1) ◽  
Author(s):  
Jiseon Park ◽  
Soon Bae Kwon ◽  
Hye Jeong Kwon

Abstract Objectives The purpose of this study was to investigate optimization of spray drying conditions for water-soluble powder using response surface methodology that is a statistical procedure used for optimization studies. Methods First, conditions of the extract used for spray drying were set. We compared heat water extraction (60–100 °C) with ethanol extraction (10–50%). After final selection of the method of extract used for spray drying, spray drying conditions were set. Independent variables included the additive contents of maltodextrin (X1), inlet temperature (X2), and air flow rate (X3). The dependent variables were yield, water absorption index (WAI) and total phenolic compounds. Results The yield was highest in 100 °C heat water extraction. The content of rutin was 29.77 mg/100 g in 90 °C heat water extraction, 28.07 mg/100 g in 100 °C heat water extraction and 24.24 mg/100 g in 10% ethanol extraction. The heat water extraction method at 100 °C was selected as an extract of the spray dryer. Statistical analysis revealed that independent variables significantly affected all the responses. A maximum yield was obtained at 15.55% of X1, 167.87 °C of X2 and 50.00 mL/min of X3. The water absorption index of asparagus increased with increasing MD ratio (X1), higher inlet temperature (X2) and higher air flow rate (X3). The total polyphenol contents of asparagus were higher when the MD addition ratio (X1) was 16.56%, the inlet temperature (X2) was higher and the air flow rate (X3) was higher. Conclusions In this study, extracts of asparagus using different extraction methods were compared for yield and spray-dried asparagus powders were investigated for their physicochemical characteristics. We were vary the range of the temperature, air flow rate, dextrin rate and set the best method for the functionality content of asparagus. Asparagus was spray - dried using 100 °C water extraction with high yield and high rutin content. The maximum spray drying yield was obtained at 15.55% of MD ratio, 167.87 °C of inlet temperature and 50.00 mL/min of air flow rate. There will be additional processed goods development made with what we have found. Funding Sources This study was supported by 2018 Regional Specialized Technology Development Project, Rural Development Administration, Republic of Korea. Supporting Tables, Images and/or Graphs


Author(s):  
Munawiroh S. Z. ◽  
Lipipun V. ◽  
Ritthidej G. C.

The present work describes the optimization of spray dried powder of solid lipid-based nanosystems to improve drug stability, surface modification and to obtain nanosystems after redispersion. Chitosan coated solid lipid nanoparticles containing bromocriptine mesylate (cBMSLN) were prepared by high pressure homogenization technique following by chitosan addition. For spray drying, response surface methodology with central composite rotatable design was to optimize 3 parameters: inlet temperature, pump rate and feed concentration. From regression analysis, powder yield, moisture content and size of redispersed nanoaggregates as responses were fitted well with linear, quadratic and quadratic equation models, respectively. Spherical powders with size of 4-5 µm and 70% yield were obtained at optimum parameters which were also used to prepare powder of chitosan coated nanostructured lipid carriers containing BM (cBMNLC). Amorphous characteristics were confirmed from powder XRD patterns and DSC chromatograms in all prepared powders. Redispersion of powders yielded nanosystems of some original nanosize and a greater portion of larger size. Smoother surface of NLC systems was observed, so was with chitosan coating. Drug entrapment was >85% but significantly decreased in chitosan coated formulations while drug retention after spray drying showed opposite results. After storage, spray dried powder could retain higher drug content than the original nanosystems. Obviously, NLC systems had better drug stability results than SLN systems. It could be concluded that redispersible spray dried powders of chitosan coated lipid-based nanosystems especially NLC systems were successfully obtained with surface modification, nanoaggregate size range and improved drug stability.Keywords: Solid lipid nanoparticles, nanostructure lipid carriers, chitosan, spray drying, optimization, redispersion, bromocriptine mesylate


Author(s):  
Danielle Grace D. Evangelista ◽  
Ryan Rhay P. Vicerra ◽  
Argel A. Bandala ◽  
Edwin Sybingco ◽  
Elmer P. Dadios ◽  
...  

Spray drying is a rapid, continuous, cost-effective, reproducible, and scalable process for reducing the moisture content of a fluid material into a solid powder. To improve this process in juice powder production, automation can be applied to increase efficiency and productivity. Hence, fuzzy logic is used in this study as a control system in the spray-drying process of concentrated liquid bignay juice into juice powder, where the inlet temperature and carrier agent concentrations affecting the properties of the juice powder, such as moisture content and product yield, are considered. The proposed fuzzy system can provide feedback to the control variables, inlet temperature, and carrier agent concentration based on the moisture content and product yield of the juice powder.


Author(s):  
HARITA R. DESAI ◽  
ARCHANA B. RAJADHYAX ◽  
PURNIMA D. AMIN

Objective: The objective of the current study was to explore top down methods of size reduction like high speed homogenisation and media milling in synergism with spray drying in amorphization and solubility enhancement of BCS Class II antilipidemic drug Simvastatin USP. Methods: Spray-dried micronized simvastatin USP was formulated by homogenisation and media milling of drug suspension in optimized stabilizer solution. Stabilizer combination, duration of homogenisation and ball milling and drug: stabilizer ratio was optimized. The obtained dispersion was transformed into solid powder using spray drying. The obtained Spray-dried micronized Simvastatin USP was evaluated for visual morphology, Infrared spectroscopy, Differential scanning calorimetry, in vitro drug release studies, X-Ray diffractometry, Scanning electron microscopy, contact angle measurement, solubility studies, dispersibility studies and intrinsic dissolution rate testing. Results: Spray-dried micronized simvastatin USP was found to show amorphization of crystalline Simvastatin USP as confirmed by the absence of drug peak in Differential scanning calorimetry and lowered signal intensity in X-Ray diffraction studies. Spray-dried micronized Simvastatin USP was found to show enhanced drug hydrophilicity and solubility as confirmed by lowering in contact angle and increase in solubility and ease of dispersibility observations. In vitro dissolution testing and intrinsic dissolution rate testing were found to show an increase in drug release from 11% to 79% and 4 mg min-1 cm-2 to 17 mg min-1 cm-2 for drug and Spray-dried micronized Simvastatin USP respectively. Conclusion: Media milling in synergism with spray-drying was found to be a prospective solubility enhancement technique for poorly-soluble Simvastatin USP.


Author(s):  
Yu Von Germaine Chng ◽  
Lee Sin Chang ◽  
Liew Phing Pui

Kuini (Mangifera odorata) is known for its intense flavour, attractive colour, rich fibre content and antioxidant properties. However, its short shelf life (bruise within a week) limits the availability of this fruit. Hence, spray drying was proposed to transform this fruit into powder to increase its application. The maltodextrin concentration of 5–20% (w/w) and inlet temperatures of 140–180°C were applied to produce kuini powders. The effect of maltodextrin concentrations at constant inlet temperature (160°C) showed that a higher amount of maltodextrin (20% w/w) produced powder with a low water activity (0.16 ± 0.01 Aw), moisture content (2.16 ± 0.60%) and hygroscopicity (20.45 ± 0.60 g/100g) but the orange colour of the powder turned pale. The kuini powder was further spray dried at different inlet temperatures at constant optimal maltodextrin concentration (20% w/w). The kuini powder that was spray dried at 160°C had the optimal properties: low water activity (0.17 ± 0.01 Aw) and hygroscopicity (22.12 ± 0.09 g/100g) with high water solubility index, WSI (79.90 ± 1.85%) and wettability (279 ± 8 s), indicating the powder can be applied as a food ingredient with high solubility. The optimal spray-drying condition for the production of kuini powder was 20% (w/w) maltodextrin concentration at 160°C inlet temperature to have the highest yield of 43.08 ± 2.77%. Eventhough the reconstituted kuini powder had lower viscosity, colour and β-carotene content than kuini juice, this study showed the feasibility of production of kuini powder using spray drying operation which may broaden its application in the food industry.


PeerJ ◽  
2021 ◽  
Vol 9 ◽  
pp. e11134
Author(s):  
Benjawan Thumthanaruk ◽  
Natta Laohakunjit ◽  
Grady W. Chism

Background Fresh Gac (Momordica cochinchinensis) fruit is rich in carotenoids, mainly β-carotene and lycopene, but these compounds are sensitive to degradation. Spray drying is used to encapsulate the sensitive β-carotene and lycopene with different materials. Only a few reports of using highly branched cyclodextrin (HBCD) have been published. Additionally, studies of β-carotene and lycopene losses in Gac powders during storage are limited. Therefore, the encapsulation of β-carotene and lycopene of Gac aril with HBCD by spray drying at different inlet temperatures were compared. The shelf life of β-carotene and lycopene during storage was also calculated. Methods The fresh Gac aril was separated and kept frozen before the experiment. Gac aril and water (1:5 w/v) were centrifuged at 8,000 g at 20 °C for 15 min using a high-speed centrifuge (Sorval; Dupont, Wilmington, DE, USA). The supernatant was filtered twice and concentrated until 15° Brix using a rotary evaporator (R-200; Buchi, Flawil, Switzerland). The mixture of concentrated aril extract and highly branched cyclodextrin at 5% (w/v) was dried at three inlet temperatures by a spray dryer (B-290; Buchi, Flawil, Switzerland) with drying air flow rate, compressor air pressure, and feed rate set at 473 L/h, 40 m3/h, and 3 mL/min, respectively . The physicochemical qualities, particle image morphology, and estimated storage time of β-carotene and lycopene were determined. Results Increased inlet temperatures of spray drying decreased the bulk density, β-carotene, and lycopene content of spray-dried powders significantly. The color values of dried powders had significant differences in yellowness (b*) and chroma, but not lightness (L*), redness (a*), and hue when the inlet temperature increased from 160 °C to 180 °C. The maximum reduction of β-carotene and lycopene observed during storage at 55 °C was 90.88% and 91.11% for 33 and 18 days. For β-carotene, the estimated shelf-life (retention of 50% of β-carotene) was 9.9, 48.4, and 91.6 days at 25 °C, 10 °C, and 4 °C. The shelf-life of lycopene was 26, 176, and 357 days at 25 °C, 10 °C, and 4 °C, respectively. HBCD could be potentially used as an encapsulating agent in spray-dried Gac aril, but the shelf-life of β-carotene and lycopene needs to be improved to be useful as a food ingredient.


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