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In recent years, there has been a significant advancement in the manufacturing of biomaterial-based nanoagents with distinctive characteristics such as biodegradability, biocompatibility, high efficacy, safety, and physicochemical properties. In particular, research on the performance and drug delivery mechanisms based on polymeric nanostructures is gaining interest in the field of health nanotechnologies. This chapter discusses all aspects of biomaterials-based nanoagent preparation methods, characterizations, and drug delivery mechanisms. Furthermore, there has been great attention to the preparation and performance of thermo-sensitive nanogels, biopolymeric nanofibers, green nanoparticles, and nanocomposites for health care systems. The unique advantages, present constraints, and potential future of green nanocarriers and target delivery of chemotherapeutic nanodrugs were highlighted, along with some novel approaches for nanoplatforms.