title: Glycyrrhetinic acid-poly(ethylene glycol)-glycyrrhetinic acid tri-block conjugates based self-assembled micelles for hepatic targeted delivery of poorly water soluble drug.
abstract: The triblock 18β-glycyrrhetinic acid-poly(ethylene glycol)18β-glycyrrhetinic acid conjugates (GA-PEG-GA) based self-assembled micelles were synthesized and characterized by FTIR, NMR, transmission electron microscopy, and particle size analysis. The GA-PEG-GA conjugates having the critical micelle concentration of 6 × 10(-5) M were used to form nanosized micelles, with mean diameters of 159.21 ± 2.2 nm, and then paclitaxel (PTX) was incorporated into GA-PEG-GA micelles by self-assembly method. The physicochemical properties of the PTX loaded GA-PEG-GA micelles were evaluated including in vitro cellular uptake, cytotoxicity, drug release profile, and in vivo tissue distribution. The results demonstrate that the GA-PEG-GA micelles had low cytotoxicity and good ability of selectively delivering drug to hepatic cells in vitro and in vivo by the targeting moiety glycyrrhetinic acid. In conclusion, the GA-PEG-GA conjugates have potential medical applications for targeted delivery of poor soluble drug delivery.
authors.affiliation: Department of Pharmacy and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, No. 37 Guoxue Alley, Chengdu, Sichuan 610041, China.
authors.forename: Fengbo
authors.initials: F
authors.lastname: Wu
authors.affiliation: Department of Pharmacy and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, No. 37 Guoxue Alley, Chengdu, Sichuan 610041, China.
authors.forename: Ting
authors.initials: T
authors.lastname: Xu
authors.affiliation: Department of Pharmacy and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, No. 37 Guoxue Alley, Chengdu, Sichuan 610041, China.
authors.forename: Chi
authors.initials: C
authors.lastname: Liu
authors.affiliation: The First Affiliated Hospital of Chengdu Medical College, Chengdu, Sichuan 610500, China.
authors.forename: Can
authors.initials: C
authors.lastname: Chen
authors.affiliation: Department of Pharmacy and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, No. 37 Guoxue Alley, Chengdu, Sichuan 610041, China.
authors.forename: Xiangrong
authors.initials: X
authors.lastname: Song
authors.affiliation: Department of Pharmacy and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, No. 37 Guoxue Alley, Chengdu, Sichuan 610041, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Zheng
authors.affiliation: Department of Pharmacy and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, No. 37 Guoxue Alley, Chengdu, Sichuan 610041, China.
authors.forename: Gu
authors.initials: G
authors.lastname: He
mesh_terms: D016503:Drug Delivery Systems; D006034:Glycyrrhetinic Acid / Q000737:chemistry*; D008099:Liver / Q000378:metabolism*; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D017239:Paclitaxel / Q000008:administration & dosage* / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014867:Water / Q000737:chemistry
chemical_list: D008823:Micelles; D014867:Water; D011092:Polyethylene Glycols; D006034:Glycyrrhetinic Acid; D017239:Paclitaxel