Pt(IV) Prodrugs Designed to Embed in Nanotubes of a Polysaccharide for Drug Delivery.

Cisplatin exhibits a sufficient killing effect on cancer cells; however, it damages normal cells simultaneously. Herein, we developed a prodrug delivery system based on branched ß-(1→3)-d-glucan. This natural biomacromolecule-based polysaccharide nanotube was modified with cisplatin embedded in the hollow cavity (BFCP), showing high anticancer activity and low toxicity in vitro. It is a broad-prospect system, which is based on biocompatible nanomaterials loaded with Pt(IV) prodrugs for cancer cell absorption with subsequent release in tumors by utilizing the intracellular reducibility. BFCP chains adopted a nanotube conformation in water, observed by transmission electron microscopy. In comparison to cisplatin, the Pt(IV) prodrugs not only displayed better antitumor properties but also had significant tumor targeting. A potent natural complex conjugated with redox-responsive platinum prodrugs is a significantly efficient tumor drug demonstrated in vitro and in vivo.