Abstract: Drug delivery systems (DDS) hold high potential to improve the safety and efficacy of pharmaceutical agents. The pharmacokinetics and biodistribution of a drug depend on the drug delivery system and the drug itself. Inorganic ceramic nanoparticles having the structure of layered double hydroxides (LDH) have been studied since the mid-19th century for a variety of applications including catalysis, anion exchange, adsorbents for many industrial applications, and antacid, but more recently as a potential drug and gene delivery system. The current study presents the partial development of a targeted DDS, based on colloidal LDH nanoparticles. The first objective of this study was to assimilate information from documented literature on LDH and to assess the material from a perspective of drug delivery. The second objective was to develop a LDH synthesis method, followed by functionalization of LDH for its suitability as a targeted DDS. In summary, this preliminary work has been successful in identifying the important aspects related to the use of LDH as a targeted DDS. For example, the selections of magnesium, zinc, and iron as components for the LDH structure were based on the highest degree of biocompatibility and safety. Additionally, the coprecipitation process that leads to formation of crystalline magnesium-iron LDH has been demonstrated, along with the identification of synthesis conditions that will lead to formation of zinc-iron LDH. Furthermore, the effects of synthesis conditions for the formation of LDH nanoparticles with a well defined morphology and an average diameter of less than 150 nm were studied using a variety of characterization methods including X-ray diffraction, field emission scanning electron microscopy and high-resolution transmission electron microscopy. Finally, surface activation of LDH has been successfully accomplished through covalent attachment of acryloyl chloride molecules onto LDH surface. This surface activation step enables further functionalization of LDH for targeted DDS. (Abstract shortened by UMI.)