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Dendrimers are highly defined artificial macromolecules, which are characterized by a combination of a high number of functional groups and a compact molecular structure. A rapid increase of importance in the chemistry of dendrimers has been observed since the first dendrimers were prepared. Dendrimers have gained considerable interest as a delivery system due to their exceptional properties including high water solubility, monodispersity, biocompatibility, and low immunogenicity. These multiple branched monomers have well-defined 3D structures with favorable manufacturing approaches at a large scale. Thus dendrimer-based delivery systems possess unique features that are advantageous for drug delivery in clinics. Various types of drug molecules, including hydrophobic or hydrophilic small molecules and large nucleic acid molecules, can be loaded into dendrimers by either physical or chemical interactions.