Recent Advances in the Delivery Carriers and Chemical Conjugation Strategies for Nucleic Acid Drugs

SIMPLE SUMMARY: In recent years, nucleic acid drugs, such as antisense oligonucleotides (ASOs) and small interfering RNAs (siRNAs), have attracted attention as a new modality for cancer treatment. In this review, we introduce and discuss an overview of various drug delivery systems (DDSs) and ligand modification technologies that are being employed to improve the success and development of these drugs. It is our belief this review will increase the awareness of nucleic acid drugs worldwide and build momentum for the future development of new cancer-targeted versions of these drugs. ABSTRACT: With the development of new anticancer medicines, novel modalities are being explored for cancer treatment. For many years, conventional modalities, such as small chemical drugs and antibody drugs, have worked by “inhibiting the function” of target proteins. In recent years, however, nucleic acid drugs, such as ASOs and siRNAs, have attracted attention as a new modality for cancer treatment because nucleic acid drugs can directly promote the “loss of function” of target genes. Recently, nucleic acid drugs for use in cancer therapy have been extensively developed and some of them have currently been under investigation in clinical trials. To develop novel nucleic acid drugs for cancer treatment, it is imperative that cancer researchers, including ourselves, cover and understand those latest findings. In this review, we introduce and provide an overview of various DDSs and ligand modification technologies that are being employed to improve the success and development of nucleic acid drugs, then we also discuss the future of nucleic acid drug developments for cancer therapy. It is our belief this review will increase the awareness of nucleic acid drugs worldwide and build momentum for the future development of new cancer-targeted versions of these drugs.