Targeted drug delivery to the colon is more desirable for local treatment of a variety of bowel diseases and systemic delivery of protein and peptide drugs. Targeting depends on exploiting a unique feature of specific site and protecting the drug until it reaches to the site. To achieve the delivery of intact drugs to the colon, different primary as well as potential novel approaches are used. To achieve the maximum site specific delivery of drugs to colon, combination of two or more approaches are preferred over individual approaches. Because of limited success of primary approaches newly developed approaches are preferred.