Challenges and benefits for oral colon-targeted nanoparticulate drug delivery system: A brief review

Abstract

Oral colon-targeted drug delivery systems (OCTDDS) are increasingly recognized for their therapeutic potential in both local conditions, such as inflammatory bowel disease, colorectal cancer, and intestinal infections, and systemic disorders in which colonic absorption is advantageous. Nanoparticulate carriers have gained particular attention because they offer several advantages over conventional systems, including improved stability, protection from enzymatic degradation, controlled drug release, and enhanced bioavailability. Despite these benefits, the gastrointestinal environment presents significant challenges to selective colon delivery. Variability in pH, digestive enzymes, mucus layering, and the influence of gut microbiota often hinder predictable performance. To overcome these barriers, diverse nanoscale platforms—such as polymeric nanoparticles, lipid-based systems, dendrimers, and hybrid nano-in-micro carriers—have been developed, each offering unique mechanisms to optimize targeting and therapeutic outcomes. This review brings together recent advances in nanoparticle-mediated colon targeting, highlighting design principles, advantages, and translational prospects. Regulatory considerations and early clinical findings are also discussed, emphasizing the importance of bridging laboratory innovation with clinical application to realize the full potential of these emerging systems.