An analysis is given of the physicochemical behavior of GNPs including drug loading, release, particle size, zeta-potential, cytotoxicity, cellular uptake and stability. This review also attempts to provide an overview of the major applications of GNPs in drug delivery and gene therapy and their in vivo pharmacological performances, as well as site-specific drug targeting using various ligands modifying the surface of GNPs. Finally, nanocomplexes of gelatin with polymers, lipids or inorganic materials are also discussed.