Functionalized polymer nanoparticles prepared from biocompatible polysaccharides have been considered promising for detection and treatment of various diseases including cancer. Particularly, stimuli-sensitive polymer nanoparticles have shown great potential in cancer diagnosis and therapy. In this presentation, we designed and prepared novel polysaccharide micelles that can respond to changes in the glucose concentration, which could be utilized as a glycolysis inhibitor by capturing glucose in cancer microenvironments. Glucose-sensitive polysaccharides were synthesized by chemical conjugation of phenylboronic acid to the backbone of either glycol chitosan or hyaluronate. Phenylboronic acid is known to specifically bind to hydroxyl groups of glucose in aqueous conditions. Various physiochemical characteristics of nanoparticles were investigated in vitro. These nanoparticles were stable at the blood glucose level. However, they disintegrated as the glucose concentration increased. The cellular uptake of glucose-sensitive nanoparticles significantly induced glucose deprivation, resulting in reduced tumor size in a tumor-bearing mouse model. This approach may provide a useful means to design functional polymer nanoparticles for efficient diagnosis and therapy of many diseases, including cancer.
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