Dr. Maša Knez, Assisstant Professor, Faculty of Chemistry and Chemical Engineering, University of Maribor, Slovenia

Title: Formulation of nimodipine, fenofibrate, and o-vanillin with Brij S100 and PEG 4000 using the PGSSTM process

Abstract: The e pharmaceutical industry is interested in obtaining the successful formulation of poorly soluble active compounds in order to increase their bioavailability and dissolution rate. The current delivery options for improving the dissolution properties of drugs are particle size reduction, crystal modification, pH modification, self-emulsification, amorphization and the formulation of drugs with surfactant carriers and amorphous polymers. Particle size reduction and drug formulation with polymeric carriers incorporate the most promising options in this regard. A number of conventional methods have been developed to improve the dissolution properties of drugs. Many of these methods possess drawbacks, such as thermal and chemical degradation of drugs, large quantity organic solvent use, broad particle size distribution and low drug load. To overcome these limitations, supercritical fluid technology promises to be an excellent option. The reasons for the widespread use of supercritical fluids mainly lie in the simplicity of the processes, high purity of products, no organic solvents in the process, no communication steps in drug preparation, mildness of operating conditions and the possibility of obtaining non-contaminated fine particles with narrow size distributions. Production of fine particles with improved characteristics using supercritical fluids has been obtained with rapid expansion of supercritical solutions (RESS), the gas antisolvent process (GAS), supercritical antisolvents (SAS), solution enhanced supercritical dispersion processes (SEDS), aerosol solvent extraction systems (ASES), supercritical fluid extraction of emulsions (SFEE) and particles from gas-saturated solution (PGSSTM). In particular, the PGSSTM used in our study is an organic solvent-free process in which polymeric carriers with the target pharmaceutical drug to be micronized and encapsulated are loaded into a high-pressure autoclave together with supercritical CO₂.

Keywords: encapsulation, particle generation, dissolution rate, active drugs, polymer, PGSS^TM