Supercritical Fluid Particle Design for Poorly Water-soluble Drugs (Review)

Abstract

Supercritical fluid particle design (SCF PD) offers a number of routes to improve solubility and dissolution rate for enhancing the bioavailability of poorly water-soluble drugs, which can be adopted through an in-depth knowledge of SCF PD processes and the molecular properties of active pharmaceutical ingredients (API) and drug delivery system (DDS). Combining with research experiences in our laboratory, this review focuses on the most recent development of different routes (nano-micron particles, polymorphic particles, composite particles and bio-drug particles) to improve solubility and dissolution rate of poorly water-soluble drugs, covering the fundamental concept of SCF and the principle of SCF PD processes which are typically used to control particle size, shape, morphology and particle form and hence enable notable improvement in the dissolution rate of the poorly water-soluble drugs. The progress of the industrialization of SCF PD processes in pharmaceutical manufacturing environment with scaled-up plant under current good manufacturing process (GMP) specification is also considered in this review.

Drug loading of polymer implants by supercritical CO 2 assisted impregnation: A review

“…It has enabled to improve the solubility and the dissolution rate of poorly water soluble drugs such as crystalline drugs [102,103]. The StaniTab® process patented by Stanipharm is a bottom-up process based on scCO 2 for the manufacturing of poorly-soluble drug nanoparticles and an auxiliary substance commonly found in tablets.…”

Properties of PLA/PCL particles as vehicles for oral delivery of the androgen hormone 17α-methyltestosterone

“…Among the several methods currently available for the production of polymeric particles to be used in controlled drug release, supercritical fluid-based technologies emerge as attractive alternatives, especially those employing CO 2 as supercritical fluid [12,[19][20][21], which have particular interest in the case of drugs poorly soluble in water. A specific modality, in which the supercritical fluid is used as an anti-solvent (SAS method), has been increasingly used in the production of particles [12] and even of fibers with potential use in the pharmaceutical industry field [22].…”

Supercritical fluid assisted production of micrometric powders of the labile trypsin and chitosan/trypsin composite microparticles

“…Hence, development of micronization techniques favorable for a delivery system that protects the protein/peptide and aids in enhancing its absorption with good maintenance of biological activity is of great importance. As for particle design, supercritical fluid (SCF)-based techniques are emerging as viable alternatives to conventional processes (Shoyele and Cawthorne, 2006;Sun, 2014). Concerning protein and polymer/protein composite, since the solubility of proteins in supercritical fluid, usually supercritical CO 2 (SC-CO 2 ), is very limited and SC-CO 2 hardly has any antisolvent effect on aqueous solutions, conventional SCF-based micronization methods have some limitations for protein (Du et al, 2011).…”