This review article highlights recent activities in the field of biomimetic systems and their application in controlled drug delivery. A definition and overview of biomimetic processes is given, with a focus on synthesis and assembly for the creation of novel biomaterials. In particular, systems are classified on the basis of three subsets, which include biological, biohybrid and synthetic structures. Examples focus on the current and proposed clinical significance for systems that mimic processes where the underlying molecular principles are well understood. Biomimetic materials and systems are presented as exceptional candidates for various controlled drug delivery applications and have enormous potential in medicine for the treatment of disease.