Supramolecular Self-assembly of Tanshinone IIA to Construct an Antitumor Drug Delivery Platform

<i>Salvia miltiorrhiza</i> has been reported to exhibit significant antitumor effects, primarily due to its active ingredient, Tanshinone IIA (TSA). However, its low solubility and bioavailability pose challenges for its application. This study employed the antisolvent precipitation method to explore the self-assembly potential of TSA molecules for developing possible soluble nanomedicine. It was found that the morphology of self-assembled TSA aggregates was nanorods, and finally, numerous TSA nanorods (TSA NRs) were synthesized. Our findings indicate that TSA can self-assemble into nanorods through hydrophobic interactions and π-π stacking. Additionally, a polydopamine (PDA) coating, along with polyethylene glycol (PEG) and folic acid (FA) modifications, was applied to the TSA NRs to achieve high drug loading capacity, high stability, and a targeted delivery system. The resulting nanomedicine, PEG-PDA@TSA NRs, exhibits excellent dispersion and stability, remaining stable under physiological conditions. The antitumor efficacy of this system was evaluated using an H22 tumor mouse model, and the results demonstrated that FA-modified PEG-PDA@TSA NRs can significantly inhibit tumor growth <i>in vivo</i>. This study successfully developed a FA-PEG-PDA@TSA NR nanodrug delivery system, effectively enhancing the pharmacological activity of TSA and providing a novel formulation strategy for cancer treatment.