An attempt is made to describe an emerging convergence science: "nanomedicine". In particular, inorganic compounds such as anionic clays, layered double hydroxides (LDHs), at nanoscale, are underlined, with regard to how they could interact with bioactive and/or drug molecules to form novel intercalative hybrid drug systems with biocompatibility, imaging and targeting functions eventually for gene and/or drug delivery. In this regard, LDHs are focused as an important inorganic biomaterial for drug and gene delivery carriers with very high additive value in the near future, especially in biomedical industries including pharmaceutical, cosmeceutical, and nutraceutical ones, compared to any other industrial applications. In this review, the drug delivery systems based on clay nanoparticles are described in terms of nanotoxicity, intercellular uptake mechanism, and intracellular trafficking pathways in vitro, and finally passive and active targeting functions in vivo. In addition, several studies highlighting recent advances in chemotherapy and gene therapy with nano LDHs are also discussed, from the viewpoint of state-of-the-art convergence technology based on nanomedicine.