The synergistic effect of hierarchical assemblies of siRNA and chemotherapeutic drugs co-delivered into hepatic cancer cells.

摘要: Diblock copolymers (PEI-PCL) of poly(e-caprolactone) (PCL) and linear poly(ethylene imine) (PEI) were synthesized assembled to biodegradable nano-carriers for co-delivery BCL-2 siRNA doxorubicin (DOX). Folic acid as a tumor-targeting ligand was conjugated the polyanion, glycol)-block-poly(glutamic acid) (FA-PEG-PGA). Driven by electrostatic interaction, FA-PEG-PGA coated onto surface cationic PEI-PCL nanoparticles pre-loaded with DOX, potentiating ligand-directed delivery human hepatic cancer cells Bel-7402. At certain N/P C/N ratios (N/P: nitrogen phosphate; C/N: carboxyl amine), exhibited not only high transfection efficiency but also ideally controlled release drug. Compared non-specific delivery, folate-targeted resulted in more significant gene suppression at both mRNA protein expression levels, inducing cell apoptosis improving therapeutic efficacy co-administered DOX. Herein we demonstrated that co-loading small molecular drug multifunctional hierarchical nano-assembly enabled simultaneously delivering into same cells, yielding synergistic effect RNA interference chemotherapy cancer.