title: In vitro and in vivo evaluation of pectin-based nanoparticles for hepatocellular carcinoma drug chemotherapy.
abstract: 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.
authors.affiliation: Institute of Pharmacy & Pharmacology, Department of Pharmacy, University of South China , Hengyang 421001, China.
authors.forename: Cui-Yun
authors.initials: CY
authors.lastname: Yu
authors.forename: Yan-Mei
authors.initials: YM
authors.lastname: Wang
authors.forename: Na-Mei
authors.initials: NM
authors.lastname: Li
authors.forename: Ge-Sha
authors.initials: GS
authors.lastname: Liu
authors.forename: Sa
authors.initials: S
authors.lastname: Yang
authors.forename: Guo-Tao
authors.initials: GT
authors.lastname: Tang
authors.forename: Dong-Xiu
authors.initials: DX
authors.lastname: He
authors.forename: Xiang-Wen
authors.initials: XW
authors.lastname: Tan
authors.forename: Hua
authors.initials: H
authors.lastname: Wei
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D001681:Biological Assay; D002214:Capsules / Q000737:chemistry; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D016503:Drug Delivery Systems; D006801:Humans; D020128:Inhibitory Concentration 50; D008113:Liver Neoplasms / Q000188:drug therapy*; D051379:Mice; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry / Q000627:therapeutic use*; D010316:Particle Size; D010368:Pectins / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D051381:Rats
chemical_list: D000970:Antineoplastic Agents; D002214:Capsules; D010368:Pectins