Application of supercritical fluid technology for solid dispersion to enhance solubility and bioavailability of poorly water-soluble drugs

Abstract

Many new chemical entities (NCEs) have been discovered with the development of the pharmaceutical industry. However, the main disadvantage of these drugs is their low aqueous solubility, which results in poor bioavailability, posing a challenge for pharmaceutical scientists in the field of drug development. Solid dispersion (SD) technology is one of the most successful techniques used to resolve these problems. SD has been widely used to improve the solubility and bioavailability of poorly water-soluble drugs using several methods such as melting, supercritical fluid (SCF), solvent evaporation, spray drying, hot-melt extrusion, and freeze-drying. Among them, SCF with carbon dioxide (CO₂) has recently attracted great attention owing to its enhanced dissolution and bioavailability with non-toxic, economical, non-polluting, and high-efficiency properties. Compared with the conventional methods using organic solvents in the preparation of the formulation (solvent evaporation method), SCF used CO₂ to replace the organic solvent with high pressure to avoid the limitation of solvent residues. The solubility of a substance in CO₂ plays an important role in the success of the formulation. In the present review, the various processes involved in SCF technology, application of SCF to prepare SD, and future perspectives of SCF are described.

Keywords: Bioavailability; Solid dispersion; Solubility; Supercritical fluid technology.