title: Novel galactosylated biodegradable nanoparticles for hepatocyte-delivery of oridonin.
abstract: Nanoparticles based on the newly synthesized copolymers of linear PLGA blocked with two TPGS ends and galactosylated TPGS were successfully constructed as carriers of oridonin for liver-targeting. The novel copolymers were characterized by (1)H-NMR and TGA. The drug-loaded nanoparticles were prepared by a nanoprecipitation technique and characterized in terms of physicochemical properties, such as particle size, zeta potential, morphology, encapsulation efficiency, in vitro drug release behavior and physical state of the entrapped drug. The ORI-Gal-PT NPs were found to have the highest antitumor efficacy in comparison with the oridonin solution and non-galactosylated nanoparticles and induced a higher apoptotic rate of tumor cells. The targeting nanoparticles could enhance the therapeutic effect of oridonin by increasing uptake of the nanoparticles through asialoglycoprotein receptor-mediated endocytosis. The ORI-Gal-PT NPs system could be a highly promising drug delivery system to be used in liver cancer therapy.
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, Jinan 250012, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, Jinan 250012, China.
authors.forename: Xinquan
authors.initials: X
authors.lastname: Liu
authors.affiliation: Shandong Provisional Qilu Hospital, 44 West Wenhua Road, Jinan 250012, China.
authors.forename: Guangpu
authors.initials: G
authors.lastname: Liu
authors.affiliation: Jinghua Municipal Central Hospital, 35 Mingyue Street, Jinhua 321000, China.
authors.forename: Hejian
authors.initials: H
authors.lastname: Guo
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, Jinan 250012, China.
authors.forename: Caiyun
authors.initials: C
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, Jinan 250012, China.
authors.forename: Yongchun
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, Jinan 250012, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, 44 West Wenhua Road, Jinan 250012, China. Electronic address: zxzhao@sdu.edu.cn.
authors.forename: Zhongxi
authors.initials: Z
authors.lastname: Zhao
authors.affiliation: Medical Research Center, Shandong Provisional Qianfoshan Hospital, 16766 Jingshi Road, Jinan 250014, China.
authors.forename: Huiling
authors.initials: H
authors.lastname: Cheng
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry; D017209:Apoptosis / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D045786:Diterpenes, Kaurane / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry; D065546:Drug Liberation; D005690:Galactose / Q000737:chemistry; D056945:Hep G2 Cells; D022781:Hepatocytes / Q000378:metabolism*; D006801:Humans; D019344:Lactic Acid / Q000008:administration & dosage / Q000737:chemistry; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D011100:Polyglycolic Acid / Q000008:administration & dosage / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D014810:Vitamin E / Q000008:administration & dosage / Q000737:chemistry
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D045786:Diterpenes, Kaurane; D004337:Drug Carriers; C011959:oridonin; D014810:Vitamin E; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C014225:tocophersolan; D005690:Galactose
keywords: Biodegradable polymer; Drug delivery; Liver targeting; Nanoparticles; Oridonin