Particle formation using supercritical fluids: pharmaceutical applications

Tan, Hock Seng; Borsadia, S.

doi:10.1517/13543776.11.5.861

Cited by 34 publications

(23 citation statements)

References 13 publications

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“…Several review articles [23,38,39,[54][55][56][57][58][59][60][61][62][63][64][65][66] already described supercritical fluid based technologies. Different authors have used different techniques to overcome various challenges faced in controlling the particle size and morphology.…”

Section: Scf Technologies That Are Used For Particle Productionmentioning

confidence: 99%

Nanoparticles in the Pharmaceutical Industry and the Use of Supercritical Fluid Technologies for Nanoparticle Production

Sheth

Sandhu²,

Singhal³

et al. 2012

CDD

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Poor aqueous solubility of drug candidates is a major challenge for the pharmaceutical scientists involved in drug development. Particle size reduction appears as an effective and versatile option for solubility improvement. Nanonization is an attractive solution to improve the bioavailability of the poorly soluble drugs, improved therapies, in vivo imaging, in vitro diagnostics and for the production of biomaterials and active implants. In drug delivery, application of nanotechnology is commonly referred to as Nano Drug Delivery Systems (NDDS). In this article, commercially available nanosized drugs, their dosage forms and proprietors, as well as the methods used for preparation like milling, high pressure homogenization, vacuum deposition, and high temperature evaporation were listed. Unlike the traditional methods used for the particle size reduction, supercritical fluid-processing techniques offer advantages ranging from superior particle size control to clean processing. The primary focus of this review article is the use of supercritical CO2 based technologies for small particle generation. Particles that have the smooth surfaces, small particle size and distribution and free flowing can be obtained with particular SCF techniques. In almost all techniques, the dominating process variables may be thermodynamic and aerodynamic in nature, and the design of the particle collection environment. Rapid Expansion of Supercritical Solutions (RESS), Supercritical Anti Solvent (SAS) and Particles from Gas Saturated Solutions (PGSS) are three groups of processes which lead to the production of fine and monodisperse powders. Few of them may also control crystal polymorphism. Among the aforementioned processes, RESS involves dissolving a drug in a supercritical fluid (SCF) and passing it through an appropriate nozzle. Rapid depressurization of this solution causes an extremely rapid nucleation of the product. This process has been known for a long time but its application is limited. Carbon dioxide, which is the only supercritical fluid that is preferentially used in pharmaceutical processes, is not a good solvent for many Active Pharmaceutical Ingredients (API). Various researchers have modified the RESS process to overcome its solubilizing limitations, by introducing RESOLV, RESAS, and RESS-SC. Overall, all RESS based processes are difficult to scale up. The SAS processes are based on decreasing the solvent power of a polar organic solvent in which the substrate (API & polymer of interest) is dissolved, by saturating it with carbon dioxide (CO2) at supercritical conditions. CO2 causes precipitation and recrystalization of the drug. SAS is scalable and can be applied to a wide variety of APIs and polymers. Minor modifications of basic SAS process include GAS, ASES, SAS-DEM and SAS-EM. Processes where SCF is used as an anti solvent and dispersing agent include SEDS, SAA, and A-SAIS. The mechanisms and applications of these processes were briefly discussed. In PGSS, CO2 is dissolved in organic solutions or melted compound...

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Section: Scf Technologies That Are Used For Particle Productionmentioning

confidence: 99%

Nanoparticles in the Pharmaceutical Industry and the Use of Supercritical Fluid Technologies for Nanoparticle Production

Sheth

Sandhu²,

Singhal³

et al. 2012

CDD

View full text Add to dashboard Cite

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“…Inhaled corticosteroids (ICS), such as beclomethasone dipropionate (BDP), are well-established anti-inflammatory therapies for the treatment of asthma (1), recommended in national treatment guidelines as first-line therapy for this chronic disease (2). The micronization of pharmaceuticals such as BDP with well-defined physical properties and performance characteristics suitable for application in portable inhalers, including next generation dry powder inhalers (DPIs), continues to be a significant challenge for the pharmaceutical industry (3,4). The performance of the DPI strongly depends on both the design of the delivery device and the particulate formulation (5).…”

Section: Introductionmentioning

confidence: 99%

Study of the RESS Process for Producing Beclomethasone-17,21-Dipropionate Particles Suitable for Pulmonary Delivery

2008

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The purpose of this research was to micronize beclomethasone-17,21-dipropionate (BDP), an anti-inflammatory inhaled corticosteroid commonly used to treat asthma, using the rapid expansion of supercritical solution (RESS) technique. The RESS technique was chosen for its ability to produce both micron particles of high purity for inhalation, and submicron/nano particles as a powder handling aid for use in next generation dry powder inhalers (DPIs). Particle formation experiments were carried out with a capillary RESS system to determine the effect of experimental conditions on the particle size distribution (PSD). The results indicated that the RESS process conditions strongly influenced the particle size and morphology; with the BDP mean particle size decreasing to sub-micron and nanometer dimensions. An increase in the following parameters, i.e. nozzle diameter, BDP mol fraction, system pressure, and system temperature; led to larger particle sizes. Aerodynamic diameters were estimated from the SEM data using three separate relations, which showed that the RESS technique is promising to produce particles suitable for pulmonary delivery.

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“…Previous investigations have shown that ceramic membranes may provide a robust separation platform for condensed carbon dioxide [8][9][10][14][15][16][17][18], reducing energy consumption associated with compression/expansion cycles. Mesoporous membranes could be particularly effective in the development of benign carbon dioxide processes for microelectronics fabrication [19][20][21], particle synthesis [22][23][24][25], and polymerization [19,26].…”

Section: Introductionmentioning

confidence: 99%

Sorption and hydration effects on liquid carbon dioxide transport through mesoporous γ-alumina and titania membranes

Bothun

Ilias

Nelson

2006

Journal of Membrane Science

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Particle formation using supercritical fluids: pharmaceutical applications

Cited by 34 publications

References 13 publications

Nanoparticles in the Pharmaceutical Industry and the Use of Supercritical Fluid Technologies for Nanoparticle Production

Nanoparticles in the Pharmaceutical Industry and the Use of Supercritical Fluid Technologies for Nanoparticle Production

Study of the RESS Process for Producing Beclomethasone-17,21-Dipropionate Particles Suitable for Pulmonary Delivery

Sorption and hydration effects on liquid carbon dioxide transport through mesoporous γ-alumina and titania membranes

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