The fabrication and evaluation of a natural
pectin-based drug delivery system are reported in this study. The drug delivery system displays specific active targeting ability to
hepatocellular carcinoma due to the presence of excess
galactose residues in the
polymer structure as the natural targeting
ligands. The system was prepared under very mild conditions in an aqueous medium containing Ca(2+) and CO3(2-)
ions, generating uniform
pectin-based nanoparticles with an average diameter of 300 nm, and the
drug-loading content of anticancer
drug 5-fluorouracil (5-FU) is around 24.8%. Cytotoxicity study of the 5-FU-loaded nanoparticles (5-FU-NPs) in HepG2 and A549 cell lines demonstrated their greater potency in killing
cancer cells with overexpressed
asialoglycoprotein receptor (ASGPR) on the cell surface, compared to that of the free
drug. Pharmacokinetics study using Sprague-Dawley (SD) rats further confirmed that the
drug-loaded nanoparticles showed a much longer half-life in the circulation fluids than the free
drug. Tissue distribution was investigated on Kunming mice, and the results also demonstrated that the 5-FU-NPs has a long circulation effect. Taken together, the
pectin-based drug delivery systems exhibit size-induced prolonged circulation as well as ASGP receptor-mediated targeting ability to
cancer cell lines; therefore, it is a promising platform for the treatment of
hepatocellular carcinoma.