Biodegradable and biocompatible polymeric nanomaterials, serving as biomedical devices have garnered significant attention as a promising solution to therapeutic management of many chronic diseases. Despite their potentials, majority of the synthetic nanomaterials used in biomedical applications lack crucial properties, for example, ligand binding sites, responsiveness, and switchability to efficiently deliver intended drugs to the target site. Advancements in manipulating nanoscale geometry have incurred the incorporation of triggered release mechanism within the nanomaterials design. This expanded their potential applications beyond nanocarriers to theranostics exhibiting both tandem drug delivery and diagnostic capabilities. Additionally, it highlights possibilities to design nanomaterials that could translate chemical response(s) to photometric display, thus making affordable biosensors and actuators readily available for biomedical exploitation. It is anticipated that, in the near future, these implementations could be made to access some of the most difficult therapy locations, for example, blood brain barrier to provide efficient management of Alzheimer, Huntington, and other neurodegenerative diseases. This review aims to serve as a reference platform by providing the readers with the overview of the recent advancements and cutting-edge techniques employed in the production and instrumentation of such nanomaterials.