The incorporation of biopolymers (BIPs) in the development of therapeutic delivery systems is gaining popularity due to its multiple advantages over traditional polymers. BIPs offer numerous advantages, including biodegradability, biological compatibility, sustainability, cost-effectiveness, and availability, making them ideal for producing materials for biomedical applications. Additionally, BIPs are appropriate as they enrich functioning and boost human life. In pharmaceutical treatments for acute and critical disorders, parenteral medication delivery is essential. As lyophilization aids, medicinal components, and drug carriers, polymers are essential formulation ingredients. In addition to offering therapeutic benefits and shelf-stability, they also alter the pharmacokinetic and pharmacodynamics behavior of drugs in vivo, increasing therapeutic activity, decreasing toxicity, and focusing on specific organs or cells. BIPs are generally utilized as a carriers in various drug delivery system like nanoparticles, hydrogels or micellar formulation which may enhance the bioavailability of the drug. They can be also used for targeted drug delivery system. This chapter emphasizes the types of BIP used for parenteral formulation and their mechanism of action with their application regulatory consideration.