Since 2001, intercalated or biohybridised ceramics based on layered double (M 2z ,M 3z ) hydroxide nanoparticles (LDHN) have been evaluated as a passive vector for drug and non-viral gene delivery. This paper identifies the attributes of LDHN as a passive delivery platform, judiciously selects and discusses issues in synthesis of physiologically relevant compositions, and demonstrates surface activation of (Mg 2z ,Al 3z ) LDHN; the latter a critical first step in the surface functionalisation process for active targeting. After a description of the layered double hydroxide (LDH) structure and unique attributes of LDHN as a passive platform, the advantages and issues of a robust LDHN surface functionalisation process for active targeting are identified. Next, the judicious selection of physiological relevant (Mg 2z ,Fe 3z ) and (Zn 2z ,Fe 3z ) LDH compositions is made, and their synthesis by precipitation and potential difficulties are discussed. Finally, the surface activation of (Mg 2z ,Al 3z ) LDHN is demonstrated by a bimolecular, nucleophilic substitution type reaction using acryloyl chloride.