Self-Assembled Folic Acid-Targeted Pectin-Multi-Arm Polyethylene Glycol Nanoparticles for Tumor Intracellular Chemotherapy

Yanxue Liu; Tianjiao Kong; Zixuan Yang; Yawen Zhang; Jiandu Lei; Peng Zhao

doi:10.1021/acsomega.0c04350

Self-Assembled Folic Acid-Targeted Pectin-Multi-Arm Polyethylene Glycol Nanoparticles for Tumor Intracellular Chemotherapy

ACS Omega. 2021 Jan 7;6(2):1223-1234. doi: 10.1021/acsomega.0c04350. eCollection 2021 Jan 19.

Authors

Yanxue Liu^{1

2}, Tianjiao Kong², Zixuan Yang², Yawen Zhang¹, Jiandu Lei², Peng Zhao¹

Affiliations

¹ College of Veterinary Medicine, Shandong Provincial Key Laboratory of Animal Biotechnology and Disease Control and Prevention, Shandong Provincial Engineering Technology Research Center of Animal Disease Control and Prevention, Shandong Agricultural University, Tai'an 271018, Shandong, P. R. China.
² Beijing Key Laboratory of Lignocellulosic Chemistry, College of Material Science and Technology, Beijing Forestry University, Beijing 100083, PR China.

Abstract

Ursolic acid is widely used as an effective anticancer drug for the treatment of various cancers. However, its poor water solubility, short circulation time in vivo, and lack of targeting have made it a burden for clinical applications. We report a self-assembled folate-modified pectin nanoparticle for loading ursolic acid (HCPT@F-Pt-PU NPs) and embed the anticancer drug hydroxycamptothecin to achieve synergistic treatment with ursolic acid. In addition, the galactose residue of the pectin molecule can be recognized by the asialoglycoprotein receptor on the surface of the liver cancer cell, promoting the rapid penetration and release of HCPT@F-Pt-PU NPs intracellularly. In particular, the introduction of multiarm polyethylene glycol can improve the uniformity (106 nm) and concealment of the nanoparticles and avoid the early release of the drug or the toxicity to normal cells. HCPT@F-Pt-PU NPs have a high drug loading (7.27 wt %) and embedding efficiency (19.84 wt %) and continuous circulation up to 80 h, leading to more apoptosis (91.61%). HCPT@F-Pt-PU NP intracellular drug delivery will be a promising strategy.