Dendritic nanomaterials are unique due to their flexible architectures. So far, many structural analogues of dendritic poly(l-lysine) have been developed. Since its monomer unit is a biodegradable amino acid, poly(l-lysine) derived nanocarriers are biocompatible and safe. In this overview, structural diversity of dendritic poly(l-lysine) scaffold and patents filed on them so far are described. Furthermore, biopharmaceutical properties and therapeutic activity modulations observed from their drug delivery applications are highlighted. Poly(l-lysine) based dendriplexes, dendrosomes and dendrisomes remain novel and nearly unexplored. Since structural modifications can control the biopharmaceutical properties of aforementioned scaffold, achieving programmed drug delivery is possible. Many such structures have demonstrated not only excellent carrier characteristics but few intrinsic therapeutic activities also. A poly(l-lysine) dendrimer product VivaGel is currently under consideration in a new drug application category of various regulatory bodies. As dendritic poly(l-lysine) scaffold is biocompatible unlike many other nanocarriers, its clinical utilization would prove considerably beneficial.