The pharmacological implications of chirality in drugs and the strict legislation in this regard have led to the development of efficient enantioselective technologies to obtain enantiomerically pure compounds and to analyze their quality. However, although the most popular technique for enantioselective analysis is HPLC, the advent of nanotechnologies opens up great possibilities regarding the development of high throughput methods and processes. This tutorial review describes the state of the art in the application of nanoparticles or nanostructured materials to enantioseparation. The possibilities for this kind of materials, previously modified to include conventional chiral selectors, or the use as chiral selectors of those intrinsically chiral are considered.