The novel DOX-PMs-NPMBP nanoparticle system could markedly modulate the functional activity of P-gp, thereby reducing the drug pumping P-gp-mediated efflux of Rho123 in the resistant ALL cells in comparison to DOX, suggesting the classical MDR phenotype-dependent mechanism was involved in the action of DOX-PMs-NPMBP on DOX-resistant cells. Here, PGP is linked to acute lymphoblastic leukemia.