Abstract
Oligonucleotide therapeutics have attracted great attention in recent years as a new modality of molecular–targeted drugs. To stabilize fragile oligonucleotides in the bloodstream and deliver them to target tissue, numerous oligonucleotide nanomedicines have been proposed. Although some of them are clinically approved, the current oligonucleotide nanomedicines can target only the liver. Here, we constructed a series of nano–assemblies (polyion complexes (PICs)) from anionic oligonucleotides and cationic polymers. Fine–tuning of the polymer/oligonucleotide structures provides well–organized PICs having controlled structures, physicochemical properties, and biological properties. These PIC systems successfully delivered the oligonucleotides to various tissues, including tumors. Our approach could provide a promising platform for oligonucleotides delivery.
