pH-responsive prodrug nanoparticles for anti-tumor drug delivery

Abstract

Endosomal pH-responsive micellar nanoparticles are prepared from an amphiphilic PEG-Schiff-DOX prodrug by the solution self-assembly. These nanoparticles have one outstanding advantage they can be stable in water for about 1 week if common conditions are provided. However, in a faintly acidic environment, it is unstable and easily disassembled. The concentration of DOX in the nanoparticle solutions could reach a high level of 265 μg/mL, along with an enormous drug loading capacity of 41.7%. The increase of intracellular DOX contents and the extension of circulation time are benefits of a pH-triggered drug release mechanism. CCK-8 found that these prepared nanoparticles possessed better antitumor ability than that of the free DOX against the Hela cells. These nanoparticles are expected to become a new DOX-supported dosage form for tumor research.