Multi-walled carbon nanotubes have been covalentlyfunctionalised via 1,3-dipolar cycloaddition of azomethine ylides with orthogonally protected amino functions that can be selectively deprotected and subsequently modified with drugs and fluorescent probes. Functionalisation of carbon nanotubes (CNT) is a key step for the integration of this new material into different systems for technological and biomedical applications. One of the most powerful approaches for rendering carbon nanotubes soluble in a wide range of solvents is the covalent functionalisation of their side-walls and tips. As a consequence, functionalised carbon nanotubes (f-CNT) are emerging as novel components in nanovector formulations for the delivery of therapeutic molecules. f-CNT loaded with different peptides, proteins and nucleic acids are able to deliver their cargos into cells.