Supercritical assisted atomization: A novel technology for microparticles preparation of an asthma-controlling drug

Porta, Giovanna Della; Vittori, Carlo De; Reverchon, Ernesto

doi:10.1208/pt060352

Cited by 32 publications

(16 citation statements)

References 16 publications

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“…It has until now been used with success to produce micronic particles of some pharmaceutical compounds, [14][15][16] also on the pilot scale. 16 Unlike other SCF-based techniques, SAA can also be used to process water-soluble compounds (eg, CS) 14,17 ; however, SAA has only occasionally been used to test anti-inflammatory compounds. 14,17 Previous supercritical studies on the micronization of CS showed that it is not soluble in SC-CO 2 ; supercritical antisolvent micronization, an SCF technique different from SAA, 8,9 was attempted using a mixture of methanol and water as liquid solvent.…”

Section: Introductionmentioning

confidence: 99%

“…16 Unlike other SCF-based techniques, SAA can also be used to process water-soluble compounds (eg, CS) 14,17 ; however, SAA has only occasionally been used to test anti-inflammatory compounds. 14,17 Previous supercritical studies on the micronization of CS showed that it is not soluble in SC-CO 2 ; supercritical antisolvent micronization, an SCF technique different from SAA, 8,9 was attempted using a mixture of methanol and water as liquid solvent. Particles ranging from 0.1 to 20 μm in diameter were obtained, in both amorphous and crystalline form.…”

Section: Introductionmentioning

confidence: 99%

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Production of cromolyn sodium microparticles for aerosol delivery by supercritical assisted atomization

2007

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The purpose of this study was to produce cromolyn sodium (CS) micrometric particles with controlled particle size (PS) and PS distribution (PSD) suitable for aerosol delivery, using a supercritical fluids-based process. CS was micronized using the supercritical assisted atomization (SAA) technique at different solute concentrations in water and different precipitation temperatures. Two techniques were used to measure PS and PSD of produced particles: scanning electron microscopy image analysis and laser scattering analysis. The 2 techniques were compared to provide a complete description of the powder obtained. High-performance liquid chromatography analysis was used to verify the absence of degradation of CS after micronization; differential scanning calorimetry, thermogravimetric analysis (TGA), and X-ray analysis were performed to study the effect of operative conditions on the crystalline structure and on the water content of SAA micronized particles. The CS particles obtained were spherical, with a volumetric percentage of particles with a diameter ranging between 1 and 5 μm of 50% to 66%. The precipitation temperature had no significant effect on PSD, but high drying temperatures led to product degradation. Increasing the concentration of CS in water solution produced an increase in PS of the micronized particles. TGA showed that the micronized CS had a different hydration state than the untreated CS did. The micronized product was stable after 12 months of storage, and no modifications in structure, morphology, or crystallinity were detected. In conclusion, SAA is an efficient technique for micronization of CS, and stable spherical amorphous particles suitable for aerosol delivery can be produced.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Production of cromolyn sodium microparticles for aerosol delivery by supercritical assisted atomization

2007

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“…After (S) ‐IBP loading, the nanocarriers were encapsulated into CHT microparticles by SASD. In this process, the solubilization of scCO 2 in a liquid solution containing CHT and IBP‐loaded PURE‐POx takes place and the microparticles are achieved as a consequence of the enhanced atomization of the multicomponent mixture upon spraying out through the nozzle …”

Section: Resultsmentioning

confidence: 99%

Nano-in-Micro POxylated Polyurea Dendrimers and Chitosan Dry Powder Formulations for Pulmonary Delivery

Restani

Silva

Pires

et al. 2016

Part. Part. Syst. Charact.

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Pulmonary administration offers excellent advantages over conventional drug delivery routes, including increasing therapeutics bioavailability, and avoiding long‐term safety issues. Formulations of nano‐in‐micro dry powders for lung delivery are engineered using (S)‐ibuprofen as a model drug. These biodegradable formulations comprise nanoparticles of drug‐loaded POxylated polyurea dendrimers coated with chitosan using supercritical‐fluid‐assisted spray drying. The formulations are characterized in terms of morphology, particle‐size distribution, in vitro aerodynamic particle pulmonary distribution, and glutathione‐S‐transferase assay. It is demonstrated that ibuprofen‐loaded nanoparticles can be successfully incorporated into microspheres with adequate aerodynamic properties, mass median aerodynamic diameter (1.86–3.83 μm), and fine particle fraction (28%–45%), for deposition into the deep lung. The (S)‐ibuprofen dry powder formulations show enhanced solubility, high swelling behavior and a sustained drug release at physiologic pH. Also, POxylated polyureas decrease the (S)‐ibuprofen toxic effect on cancer cellular growth. The 3‐(4,5‐dimethylthiazol‐2‐yl)‐5‐(3‐carboxymethoxyphenyl)‐2‐(4‐sulfophenyl)‐2H‐tetrazolium (MTS) assays show no significant cytotoxicity on the metabolic activity of human lung adenocarcinoma ephithelial (A549) cell line for the lowest concentration (1 × 10−3 m), even for longer periods of contact with the cells (up to 120 h), and in the normal human dermal fibroblasts cell line the toxic effect is also reduced.

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“…Due to these favorable properties, supercritical fluids (mainly supercritical carbon dioxide, SC-CO 2 ) are currently proposed in a wide range of extraction applications (Reverchon and De Marco, 2006), microparticle formation (Della Porta and Reverchon, 2007a;Della Porta et al, 2005, 2006bReverchon and Adami, 2006;Reverchon and Antonacci, 2007) and membrane drying technologies . Recently, SC-CO 2 has been also proposed to extract the organic phase of oil-in-water (O/W) or water-in-oil (W/O) emulsions.…”

Section: Introductionmentioning

confidence: 99%

Nanostructured microspheres produced by supercritical fluid extraction of emulsions

Porta

Reverchon

2008

Biotech & Bioengineering

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The system poly(lactic-co-glycolic) acid/ piroxicam (PLGA/PX) was selected, as a model system, to evaluate the effectiveness of supercritical carbon dioxide (SC-CO(2)) extraction of the oily phase (ethyl acetate) from oil-in-water emulsions used in the production of polymer/drug microspheres for sustained drug release applications. The influence of process parameters like operating pressure and temperature, flow rate and contacting time between the emulsion and SC-CO(2) was studied with respect to the microsphere size, distribution and solvent residue. Different polymer concentrations in the oily phase were also tested in emulsions formulation to monitor their effects on droplets and microspheres size distribution at fixed mixing conditions. Spherical PLGA microspheres loaded with PX (10% w/w) with mean sizes ranging between 1 and 3 microm and very narrow size distributions were obtained due to the short supercritical processing time (30 min) that prevents the aggregation phenomena typically occurring during conventional solvent evaporation process. A solvent residue smaller than 40 ppm was also obtained at optimized operating conditions. DSC and SEM-EDX analyses confirmed that the produced microparticles are formed by a solid solution of PLGA and PX and that the drug is entrapped in an amorphous state into the polymeric matrix with an encapsulation efficiency in the range of 90-95%. Drug release rate studies showed very uniform drug concentration profiles, without any burst effect, confirming a good dispersion of the drug into the polymer particles.

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Supercritical assisted atomization: A novel technology for microparticles preparation of an asthma-controlling drug

Cited by 32 publications

References 16 publications

Production of cromolyn sodium microparticles for aerosol delivery by supercritical assisted atomization

Production of cromolyn sodium microparticles for aerosol delivery by supercritical assisted atomization

Nano-in-Micro POxylated Polyurea Dendrimers and Chitosan Dry Powder Formulations for Pulmonary Delivery

Nanostructured microspheres produced by supercritical fluid extraction of emulsions

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