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Carbon nanotubes, acting as nanocarriers, can be combined with drug molecules through various chemical or physical routes in which hydrophilic modifications of the nanotubes are required. Such types of hydrophilic modifications typically involve addition reactions at the nanotube sidewalls, the reactions of nanotube-bound carboxylic groups, and/or coating of the nanotubes with amphiphilic molecules. In this chapter, we introduce detailed approaches for covalently linking drug compounds to multiwalled carbon nanotubes, as well as labeling the synthesized drug-bearing carbon nanotube conjugates with fluorescent or radioactive molecules.