Despite advances in treatment modalities, colon cancer (CC) is the third most common cause of cancer-related death worldwide. Subsequent unfavorable effects owing to toxicity of conventional drugs are a challenging problem associated with chemotherapy. There is noticeable concern toward site-specific/targeted delivery of chemotherapeutic drugs specifically to the affected site of the colon in a predictable and reproducible manner. However, the biggest challenge in successful drug targeting for the colon is avoidance of drug absorption and/or degradation in the upper gastrointestinal tract before the drug reaches the colon. Nanoparticles endowed with targeting abilities offer a novel approach for site-specific delivery of chemotherapeutic agents. The present review focuses on recent approaches for colon-specific drug delivery (CDDS) and aims to unveil the emerging possibilities and advances in the treatment of CC with CDDS. © 2017 Elsevier Ltd