This review outlines research and patents relating to the use of inorganic nanomaterial, layered double hydroxide, as nanocontainers for drug delivery and gene reservoirs. Various intercalative synthetic routes including coprecipitation, ion exchange, reconstruction and exfoliation-reassembly have been explored to incorporate drug or gene molecules. Its unique two-dimensional structure allows layered double hydroxide to act as a nanospace for the stabilization, targeted delivery or controlled release of gene or drug molecules. Intercalative hybrid nanomaterials have uses such as pharmaceutically active ingredients, in oral- or cellular delivery systems, cosmetic ingredients, molecular coding units and etc. Toxicological studies have found layered double hydroxides to be biocompatible compared with widely used nanoparticles such as iron oxide, silica, and single-walled carbon nanotubes. Due to their versatile functionality and biocompatibility, layered double hydroxides have been widely studied and their applicability can be expanded to other nanoparticle based bio-medical applications.