This review made a summary of the functions and types of activated carbon nanoparticles for sustained drug delivery system. The physical and chemical properties of activated carbon nanoparticles as the carrier of natural extractives and medicine were reviewed. The research progresses in activated carbon nanoparticles as the carrier of traditional Chinese medicine or natural extractives from plants have been summaried. The technical bottleneck in preparation and utilization of activated carbon nanoparticles as the active ingredient sustained-release were also analyzed.