Self-assembled nanoparticles based on α-tocopherol succinate-modified heparin for targeted delivery of paclitaxel

Abstract

of PS has been hampered due to its poor water-solubility and relatively short half-life. To overcome the hurdle, the self-assembled nanoparticles based on eightarm-polyethylene glycol–pterostilbene (8arm-PEG-PS) conjugates were first presented. The 8arm-PEG-PS conjugates were synthesized by anesterification reaction between the carboxyl group of 8arm-polyethylene glycol and the hydroxyl group of PS. Then, they self-assembled into nanoparticles (Figure 1) to improve their pharmacological profiles. The nanoparticles have a small size (~100 nm) and exhibited significantly high water solubility and excellent in vitro anticancer activity compared with free PS. In vivo study demonstrated the superior therapeutic effect of nanoparticles on inhibition of tumor growth with lower systemic toxicity. On the basis of these results, we believe that the8arm-PEG-PS nanoparticles have great promise toward cancer therapy.