Leukocyte-Mimetic Nanoparticles for Tumor-Targeted Drug Delivery

摘要

To achieve high tumor accumulation of nanoparticles (NP), biodegradable polymer was modified with a derivative of quinic acid, a synthetic mimic of sialyl-Lewis x (sLe~x). It is expected that the quinic acid-modified NPs will have increased interaction with E-selectin, a glycoprotein expressed on the peritumoral endothelium, to have a higher chance to extravasate at the tumor than NPs dependent on the enhanced permeability and retention (EPR) effect alone. A new synthesis protocol to create quinic acid-modified poly(lactic-co-glycolic acid) (PLGA) was established. Quinic acid-PLGA conjugate was identified and characterized by NMR and mass spectroscopy. NPs based on the quinic acid-PLGA were prepared by the single emulsion method.