title: Preparation of novel butyryl galactose ester-modified coix component microemulsions and evaluation on hepatoma-targeting in vitro and in vivo.
abstract: The butyryl galactose ester-modified coix component microemulsions (But-Gal-CMEs) was developed for enhanced liver tumor-specific targeting. The study was aimed to evaluate the hepatoma-targeting potential of But-Gal-CMEs in vitro and in vivo. But-Gal-CMEs with a uniform spherical shape exhibited a small particle size (56.68 ± 0.07 nm), a narrow polydispersity (PDI, 0.144 ± 0.005) and slightly negative surface charge (-0.102 ± 0.008 mV). In the cell uptake studies, But-Gal-CMEs showed a significant enhancement on the intracellular fluorescent intensity on HepG2 cells model, which was 1.93-fold higher relative to coix component microemulsions (CMEs). The IC50of But-Gal-CMEs against HepG2 cells was 64.250 μg/mL, which was notably stronger than that of CMEs. In the cell apoptosis studies, compared with CMEs, But-Gal-CMEs (50 μg/mL) treatment resulted in a 1.34-fold rise in total apoptosis cells of HepG2. In the biodistribution studies in vivo, the intratumorous fluorescence of Cy5-loaded But-Gal-CMEs was 1.43-fold higher relative to that of Cy5-loaded CMEs, suggesting an obviously enhanced accumulation in the tumor sites. Taken as together, But-Gal could be incorporated into the coix component microemulsions as a novel ligand for realizing hepatoma-targeting drugs delivery.
authors.affiliation: a Multicomponent of Traditional Chinese Medicine and Microecology Research Center, Jiangsu Provincial Academy of Chinese Medicine , Nanjing , China and.|b Department of Pharmacy , Jiangsu University , Zhen Jiang , China.
authors.forename: Ming Jian
authors.initials: MJ
authors.lastname: Liu
authors.affiliation: a Multicomponent of Traditional Chinese Medicine and Microecology Research Center, Jiangsu Provincial Academy of Chinese Medicine , Nanjing , China and.
authors.forename: Ding
authors.initials: D
authors.lastname: Qu
authors.affiliation: a Multicomponent of Traditional Chinese Medicine and Microecology Research Center, Jiangsu Provincial Academy of Chinese Medicine , Nanjing , China and.
authors.forename: Yan
authors.initials: Y
authors.lastname: Chen
authors.affiliation: a Multicomponent of Traditional Chinese Medicine and Microecology Research Center, Jiangsu Provincial Academy of Chinese Medicine , Nanjing , China and.
authors.forename: Cong Yan
authors.initials: CY
authors.lastname: Liu
authors.affiliation: a Multicomponent of Traditional Chinese Medicine and Microecology Research Center, Jiangsu Provincial Academy of Chinese Medicine , Nanjing , China and.
authors.forename: Yu Ping
authors.initials: YP
authors.lastname: Liu
authors.affiliation: a Multicomponent of Traditional Chinese Medicine and Microecology Research Center, Jiangsu Provincial Academy of Chinese Medicine , Nanjing , China and.
authors.forename: Xue Fang
authors.initials: XF
authors.lastname: Ding
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy*; D045744:Cell Line, Tumor; D031742:Coix / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D004655:Emulsions / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D004952:Esters / Q000737:chemistry*; D005690:Galactose / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy*; D010316:Particle Size; D010936:Plant Extracts / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D014018:Tissue Distribution
chemical_list: D004337:Drug Carriers; D004655:Emulsions; D004952:Esters; D010936:Plant Extracts; D005690:Galactose
keywords: Asialoglycoprotein receptor; cellar uptake; coix component; liver tumor targeting; microemulsions; near-infrared imaging