The development of drug delivery platforms based on nanofillers guarantees reliable localization of the drug to the site of action. In this regard, many known organic and inorganic nanostructures are being incorporated as nanofillers into drug delivery systems to obtain nanocomposite platforms with novel and value-added properties. This synergism between the scaffold and nanofillers can enhance the nanocomposite platforms’ characteristic physiochemical and pharmacological features. Notably, the type, size, morphological structures, and amount added to the drug delivery platforms affect the platforms’ in vitro or in vivo biocompatibility, capacity for drug, encapsulation stability, and efficiency. This chapter elaborates on the recent trends in the use of diverse types of nanofillers (clays, organic, inorganic, and carbon nanostructure) in delivering various types of therapeutic agents, including protein, anticancer agents, antibiotics, and antiinflammatory drugs. Also, we will shed light on most of the nanofiller-based drug delivery platforms currently on the market or at the clinical levels.