Dendrimers are new artificial macromolecules which have the structure like a tree. They are hyperbranched and monodisperse three-dimensional molecules with defined molecular weights, large numbers of functional groups on the surface and well-established host-guest entrapment properties. Recently, dendrimers have successfully proved themselves as promising nanocarriers for drug delivery because they can render drug molecules a greater water-solubility, bioavailability, and biocompatibility. In this review, recent progress in the pharmaceutical applications of dendrimers as delivery systems for drugs, particularly, the non-steroidal anti-inflammatory, anti-microbial/anti-viral and potent anti-cancer drugs is discussed. Three possible interaction mechanisms between dendrimers and drug molecules are presented. In addition, the pharmacodynamic and pharmacokinetic properties of both dendrimer/drug complex and dendrimer-drug conjugation after their administration to animals are evaluated.

Dendrimers are a new class of artificial macromolecules with well-defined hyperbranched structures which enable bio-active molecules such as drugs to be presented in a highly multi-valent fashion. Covalent conjugation of drugs to the surface of dendrimers can be easily achieved either by direct chemical reactions between dendrimers and drug molecules including esterification and amidation or through cleavable linkers, depending on the functional groups on the surface of dendrimers. The pharmacological properties of these dendrimer-based prodrugs such as biocompatibility, biodistribution, biostability, bioadhesion and biopermeability can be modulated by further modifying dendrimers with specific functional molecules to fit a specific medicinal purpose. In this mini-review, recent advances on the use of dendrimers as prodrug nano-scaffolds were briefly demonstrated. The design and synthesis of dendrimer-based prodrugs as well as screening their intrinsic properties in biological systems were fully discussed.

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