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Chondroitin is mostly available as CS form, which is a sulfated glycosaminoglycan comprising D-glucuronic residue and N-Acetyl D-galactosamine residue. In supplements, CS is usually isolated from cartilages of shark, cow, and pig. Despite of its greater variability of the source of extraction, the activity profile of CS was observed. Because of the biodegradable and biocompatible nature, it is the primary choice to treat osteoarthritis and tissue engineering applications. CS has been used for pharmaceutical applications, mainly in drug delivery and drug targeting. CS has also been used for controlled release drug carrier, drug targeting (for anticancer drugs), protein delivery, etc. The chapter provides a detailed overview of pharmaceutical uses of CS obtained from the natural source.