Various advancements were made in the field of tissue engineering to address the critical need for functional tissue regeneration in different clinical settings. Biomolecule delivery systems are crucial for orchestrating the tissue repair process by modulating the spatiotemporal release of bioactive molecules. The successful delivery of bioactive agents can result in various cellular interactions to promote the repair of defective tissues. Chitosan derived from chitin is a promising multifunctional biopolymer utilized in regeneration applications due to its exceptional properties, such as biocompatibility, biodegradability and antimicrobial activities. It has a unique backbone structure containing free amine groups, which allows for versatile chemical modifications, enhancing its functionality in various biomaterial applications in tissue engineering. It can be processed alone or blended with other polymers to formulate hydrogels, nanoparticles, microparticles, films or scaffolds, depending on the required release kinetics for the delivery of biomolecules. This chapter covers the latent applications of chitosan as a flexible platform for the delivery of biomolecules in tissue engineering and discusses future approaches for its growth in regenerative medicine.