During the last few years, there has been a tremendous amount of optimism and expectation about nanotechnology and its impact on various fields including medicine and pharmaceutical development. One of the most promising materials being developed during the nanotechnological renaissance we are currently experiencing is the carbon nanotube. Before any biology-related application can even be envisaged, the aqueous solubility of carbon nanotubes has to be resolved. Recently, a variety of methodologies have been proposed which lead to biologically compatible carbon nanotubes. Covalent functionalization of their surface is one methodology, allowing the first attempts towards applications in the field of nanomedicine. The possibility of incorporating functionalized carbon nanotubes into cells and the biological milieu offers numerous advantages for potential applications in biology and pharmacology. One of the most promising is their utilization as a new carrier system for the delivery of therapeutic molecules. In the present article, the first attempts to transform carbon nanotubes from biologically incompatible nanomaterials to biologically relevant components of advanced therapeutics and the ensuing novel structures obtained in our laboratories are presented.