A SWNT-based biotin-taxoid conjugate, in which biotin was introduced as the tumor-targeting moiety, was designed and synthesized for tumor-specific drug delivery. The conjugate includes a novel self-immolative disulfide-containing linker to trigger the drug release. The cellular uptake of the fluorescence-labeled conjugate and the drug release were investigated by means of confocal fluorescent microscopy using L1210FR leukemia cell line, which overexpresses biotin receptors. The successful real-time observation of the receptor-mediated endocytosis and the intracellular drug release of the fluorescence-labeled biotin-SWNT-taxoid conjugate will be presented.