Dendrimers, commonly referred to as arborols, offer tremendous opportunities for drug delivery, diagnostics, and treatment applications. This may be attributed to the characteristic features of their three architectural components: core, branches, and terminal groups. These components provide vast flexibility to designers. They act as highly moldable platforms that can be modified to suit the needs of application designers. Effectively, the type, length, and molecular weight of the core, branches and terminal groups may be customized to achieve desired characteristics and satisfy the demands of numerous applications. These perfectly designed multifunctional structures are reviewed in the current paper, focusing on their complex archetypical design for interphase applications; novel drug delivery applications, especially oral, ocular, pulmonary, transdermal; targeted, and controlled-release; and diagnosis and treatment of diseases like cancer, diabetes, and autoimmune disorders.