(686d) Supramolecular Nanotubes By Prodrug Assembly

Nanotubes (e.g. carbon nanotubes, peptide nanotubes, DNA nanotubes, and protein nanotubes) have attracted extensive interest in cancer diagnosis and therapy over the past few years due to their unique physiochemical properties. For example, carbon nanotubes are intensively explored as drug transporters, thermal therapy agents, and imaging agents. However, they are non-biodegradable and are not metabolized by the liver, which impeded its further clinical translation. Here, we report a new platform of μm-long supramolecular nanotubes that are formed by self-assembly of rationally designed biodegradable prodrugs. In this platform, a great diversity of prodrug molecules of different surface chemistries and functionalities (e.g. cationic, anionic, non-ionic, and tumor-targeting ligands) are capable of assembling in aqueous solutions into various tubes of corresponding physiochemical properties. In addition, other functional guests such as imaging agents and small molecule drugs can be easily incorporated into these nanotubes through passive diffusion without altering their morphology, affording a facile yet effective mean to dope in a variety of different functionalities. The resulting theranostic nanotubes can track the fate of tubular therapeutics in vivo and showed a preferential tumor accumulation. Furthermore, our nanotube showed a largely enhanced antitumor efficacy on U87 MG xenografts mice model compared with commercialized prodrug. We believe that this versatile soft nanotube platform offers a facile strategy to engineer functionalities of nanotubes through both chemical and physical modification, and has a remarkable potential in cancer treatment and diagnosis.