Progress, innovation, and development of new chemical entities fetched new defies in the drug delivery arena, and also put forward several issues including bioavailability with intestinal metabolism or efflux mechanism. However, some excipients such as surfactants have demonstrated improvement in drug bioavailability. Thus, these excipients can no longer be considered inert and require attention from a pharmaceutical regulatory perception. Biopolymers and their derivatives are gaining attention in pharmaceutical manufacturing due to their biodegradability and compatibility. However, based on the Food and Drug and Administration (FDA) guidelines, the manufacturers are required to evaluate their pharmacokinetic and toxicological properties. Several methods including Rule-of-Five and Biopharmaceutical Classification System (BCS) are used for early pharmacokinetic prediction of active and inactive pharmaceutical ingredients. Although polymers differ from therapeutic agents, similar methods can be smeared for the understanding of the absorption, distribution, metabolism, and excretion profile of bio-based pharmaceutical excipients. This chapter explores pharmacokinetic and pharmacodynamics information of biopolymers used in the design, and development of several pharmaceutical formulations.