There are various routes of drug administration. Oral administration is considered the most preferred route in drug administration for systemic effects, but the oral administration is not suitable for people with ulcerative colitis, crohn's disease, bowel cancer, diarrhea, treatment of diseases that sensitive to circadian rhythms such as asthma and angina, as well as for steroids administration. The delivery of targeted drugs has the goal of achieving the desired therapeutic profile by delivering the drug to the target site. This study conducted by reviewing related articles based on specify keywords on Science Direct database that has been published for the last 10 y. In recent decades, research has been conducted to develop methods that can target drugs to specific organs. The focusing on targeted drug delivery system to the colon, the various ways that were carried out for its approach, as well as the evaluation. By this study, some challenges in the colon drug delivery system could be overcome along with new approaches.