Chitosan is a cationic biopolymer which exerts promising properties such as bioadhesivity, biocompatibility, biodegradability and penetration enhancement as well as bioactive properties including antimicrobial, wound healing, anti-inflammatory, immunostimulatory, and tissue regeneration. With all these properties together, it has become an attracting biomaterial in biomedical field for both therapeutic purposes and delivery of the drugs in different forms such as gels, fibers, films, sponges, micro and nanoparticulate systems, etc. In this chapter, we will focus specifically on chitosan microbeads and their applications in drug delivery. After highlighting the potential of chitosan beads for drug delivery with respect to their physico-chemical and biological properties, their recent applications in the pharmaceutical field will be reviewed. Finally, the possibilities and limitations will be discussed in regard to quality, efficacy, and safety aspects.