Schiff-linked prodrugs of pH-responsive nanoparticles to facilitate drug delivery

Abstract

Endosomal pH-responsive micelle nanoparticles were prepared by self-assembly of amphiphilic polyethylene glycol Schiff-doxorubicin (PEG-Schiff-DOX) precursor drugs. The free DOX could be encapsulated in the hydrophobic core of the nanoparticles. These nanoparticles exhibited decompose rapidly in weakly acidic environments, but can keep excellent storage stability under normal conditions. Due to the differences in drug release mechanisms and rates between encapsulated DOX and linked DOX, programmed drug release behavior was observed, which may result in higher intracellular drug concentrations and longer duration of action.CCK-8 analysis showed that the nanoparticles showed better antitumor activity than free DOX. These nanomedicines based on precursor drugs have great potential for the development of transformational DOX agents for cancer therapy.