ABSTRACT

This chapter provides an overview of the beneficial features of drug nanocrystals, discusses the most important production techniques, and explores some reasons why drug nanocrystals can be seen as a universal formulation approach for poorly soluble drugs. The automation of the drug discovery process by technologies such as high-throughput screening, combinatorial chemistry, and computer-aided drug design is leading to a vast number of drug candidates possessing a very good efficacy. Drug nanocrystals have to be distinguished from polymeric nanoparticles, which consist of a polymeric matrix and an incorporated drug. The formulation of drug nanocrystals can impressively improve the bioavailability of perorally administered poorly soluble drugs. The use of drug nanocrystals leads to an increased concentration gradient between the formulation and the skin. The increased saturation solubility leads to “supersaturated” formulations, enhancing the drug absorption through the skin. Drug nanocrystals can also be produced by high-pressure homogenization using piston gap homogenizers.