BiopolymersBiopolymers are among the most widely used nanomaterialsNanomaterials for oral drug delivery applications. They are biodegradable, biocompatibleBiocompatible, nontoxic and safer to administer through oral route. Oral route is most commonly used administration route for various types of medications as it eases to administer and easy to formulate compared to other route of administration. Integration of material science, nanotechnologyNanotechnology and pharmaceutical science has led to the development of biopolymer-based nano formulations to overcome the possible limitations associated with orally administered drugs. In this chapter, we explored various biopolymers which are extensively used for formulation of oral nanocarriersNanocarriers including polysaccharide-based, protein-based, poly phenol-based and polyester-based polymers and their preparation methods. In addition, we have explored the various types of nanocarriers formulated with biopolymersBiopolymers for oral drug delivery applications, the challenges associated with them, various targeting strategies that could be used to overcome them and future trends in this field.