Can colorectal delivery technology provide a platform for enteral oligonucleotide-based therapeutics?

Nucleic acid-based therapeutics including antisense and siRNA oligonucleotides has been expected as an innovative treatment for intractable diseases. Oral drug delivery is the most patient-friendly route of administration but developing an effective delivery system for oligonucleotides remains a major challenge. In this commentary, we discuss the potential benefits of the colorectal route as another platform for the development of oral oligonucleotide therapeutics. The importance of the targeting or the availability of oligonucleotides in targeted tissue is highlighted in contrast to systemic availability, while the liver-targeted enteral siRNA delivery technology that we recently developed is introduced.