The diosgenin prodrug nanoparticles with pH-responsive as a drug delivery system uniquely prevents thrombosis without increased bleeding risk

The nanoparticle, a novel prodrug based on conjugating diosgenin to PEG with Schiff-base bond, could self-assemble into micelles in aqueous solutions. The prodrug micelles exhibited stability at different temperatures, and targeted release of drugs by pH-response in the position of thrombus in vivo. The prodrug micelles had a long circulation time in blood and better antithrombotic activity than commercial antithrombotic agents as aspirin. Furthermore, the prodrug micelles were not observed to cause histological damages on tissues, and bleeding risk. Importantly, we found that the targeted delivery prodrug micelles inhibited platelet activation by suppressing apoptosis of platelet in final state. These results confirmed that the prodrug micelles are a promising new class of agent for targeted therapy of multiple thrombus diseases.194