Solving the Matter - Crystal Engineering and Particle Design of Poorly Soluble Drugs via Rapid Expansion of Supercritical Solutions

Abstract

A growing number of new drug candidates are highly lipophilic. Statistically, 40 % of new drug molecules are thus excluded from further development at the early stages of pharmaceutical research. From a technological standpoint, particle design and crystal engineering are valuable tools to increase intrinsic solubility and low dissolution rates of lipophilic compounds.

However, traditional pharmaceutical processing techniques make ample use of organic solvents and rough process conditions. This causes stability issues of the drug products and contradicts today's growing demand for sustainable technologies. In contrast, the Rapid Expansion of Supercritical Solutions (RESS) can provide both mild process conditions and a solvent-free processing technology.

With the development of three RESS applications for micronization, nanotechnology and crystal engineering, the dissolution rate of poorly soluble compounds could be improved distinctly in this thesis. RESS thus offers a valuable technology platform with an up-to-date unexploited potential to enhance the future sector of pharmaceutical formulation science.