Self-assembly of a Biocompatible Prodrug with High Drug Loading Content for the Antitumor Therapy

Endosomal pH-responsive micellar nanoparticles were prepared by self-assembly of amphiphilic polyethylene glycol-Schiff base bond-doxorubicin (PEG-Schiff-DOX) prodrug prodrugs, and free DOX can be encapsulated within the hydrophobic cores of the nanoparticles. These nanoparticles exhibited excellent storage stability under normal conditions for more than a week but were rapidly disassembled in a slightly acidic environment. The DOX loading within the nanoparticle can be up to 61%. The CCK-8 assay showed that the nanoparticles exhibited better antitumor activity against HeLa cells than free DOX. Consequently, we are optimistic about the potential of these prodrug-based nanomedicines in developing translational DOX formulations for cancer treatment.