title: Galactose-decorated pH-responsive nanogels for hepatoma-targeted delivery of oridonin.
abstract: Nanogels based on the polymers of galactosylated chitosan-graft-poly (N-isopropylacrylamide) (Gal-CS-g-PNIPAm) were used as carriers of oridonin (ORI) for tumor targeting. Three ORI-loaded nanogels with various degrees of galactose substitution were prepared, and their characteristics were evaluated. The release behavior of ORI from these nanogels was pH-dependent, and the release could be accelerated under mildly acidic conditions. The cytotoxicity of ORI-loaded nanogels was pH-sensitive. ORI-loaded nanogels exhibited a higher antitumor activity than drug-loaded nanogels without galactosylation, and the anticancer activity increased in relation to increases in the number of galactose moieties of the nanogels in HepG2 cells. In contrast, the cytotoxicity of ORI-loaded nanogels against MCF-7 cells decreased compared with that of drug-loaded nanogels without galactosylation. Results demonstrated that these nanogels could enhance the uptake of ORI into HepG2 cells via asialoglycoprotein receptor-mediated endocytosis. These galactose-decorated pH-responsive nanogels were well-suited for targeted drug delivery to liver cancer cells.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Shandong University, Jinan, P R China.
authors.forename: Cunxian
authors.initials: C
authors.lastname: Duan
authors.forename: Jian
authors.initials: J
authors.lastname: Gao
authors.forename: Dianrui
authors.initials: D
authors.lastname: Zhang
authors.forename: Lejiao
authors.initials: L
authors.lastname: Jia
authors.forename: Yue
authors.initials: Y
authors.lastname: Liu
authors.forename: Dandan
authors.initials: D
authors.lastname: Zheng
authors.forename: Guangpu
authors.initials: G
authors.lastname: Liu
authors.forename: Xiaona
authors.initials: X
authors.lastname: Tian
authors.forename: Fengshan
authors.initials: F
authors.lastname: Wang
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
mesh_terms: D000178:Acrylamides / Q000737:chemistry; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy*; D048271:Chitosan / Q000737:chemistry; D045786:Diterpenes, Kaurane / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D004337:Drug Carriers / Q000378:metabolism / Q000627:therapeutic use*; D005690:Galactose / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy; D000080385:Nanogels; D011092:Polyethylene Glycols / Q000627:therapeutic use*; D011094:Polyethyleneimine / Q000627:therapeutic use*
chemical_list: D000178:Acrylamides; D045786:Diterpenes, Kaurane; D004337:Drug Carriers; D000080385:Nanogels; C413692:polyethylene glycol polyethyleneimine nanogel; C011959:oridonin; D011092:Polyethylene Glycols; D011094:Polyethyleneimine; D048271:Chitosan; C067295:N-isopropylacrylamide; D005690:Galactose