Nature has provided us a gamut of indigenous materials, which abodes rich, sustainable, and renewable resources. Biopolymers are one such elite asset, which are emphasized globally and, in many ways, have become an indispensable part of our life. On the stark contrast are the synthetic, nondegradable, and chemically driven polymers that are indisputably playing a dominant and destructive role in our society, urging for its minimalism. This has invoked many industrialists to embrace the nature-driven advanced and sophisticated materials that are biocompatible and biodegradable. The most appealing attribute of biopolymeric material is that it pleasantly sings in harmony with the environment, which is the utmost demand for the raising issues. The framework of this chapter is emphasized on elaborating the multifarious applications of natural bio-based polymers on the two most extensively researched arena of cancer nanotherapeutics and tissue engineering and regenerative medicine. This cohesively enumerates the various potential biopolymers and their "smart" derivatives, which prevails the modernized nanomedicine. © 2022 John Wiley & Sons, Inc.