This review focuses on nano-structured delivery devices prepared from biodegradable and biocompatible natural and synthetic polymers, organic raw materials, metals, metal oxides, and their other compounds that culminated in the preparation of various nano-entities depending on the preparative techniques, and starting raw materials’ utilizations. Many nanoparticles (NPs) made of polymeric, metallic, magnetic, and non-magnetic origins, liposomes, hydrogels, dendrimers, and other carbon-based nano-entities have been produced. Developments in nanomaterial substrate and end products’ design, structural specifications, preparative strategies, chemo-biological interfacing to involve the biosystems interactions, surface functionalization, and on-site biomolecular and physiology-mediated target-specific delivery concepts, examples, and applications are outlined. The inherent toxicity, and safety of the design concepts in nanomaterial preparation, and their applications in biomedical fields, especially to the organs, cellular and sub-cellular deliveries are deliberated. Bioapplications, the therapeutic delivery modules’ pharmacokinetics and medicinal values, nanopharmaceutical designs, and their contributions as nano-entities in the healthcare biotechnology of drug delivery domains have also been discussed. The importance of site-specific triggers in nano-scale deliveries, the inherent and induced structural specifications of numerous nanomaterial entities belonging to NPs, nano-scale composites, nano-conjugates, and other nano-devices of organic and inorganic origins, near biological systems are detailed. Modifications that provide nano-deliveries of their intrinsic therapeutic actions, through structural and physicochemical characteristics modifications, and the proven success of various nano-delivery devices and currently available commercial nanomedicinal and nanopharmaceutical products are also provided.