1. Preparation of novel butyryl galactose ester-modified coix component microemulsions and evaluation on hepatoma-targeting in vitro and in vivo
- Author
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Ding Qu, Xue Fang Ding, Yan Chen, Cong Yan Liu, Yu Ping Liu, and Ming Jian Liu
- Subjects
Biodistribution ,Carcinoma, Hepatocellular ,Pharmaceutical Science ,Apoptosis ,02 engineering and technology ,030226 pharmacology & pharmacy ,03 medical and health sciences ,chemistry.chemical_compound ,Drug Delivery Systems ,0302 clinical medicine ,In vivo ,Cell Line, Tumor ,Humans ,Tissue Distribution ,Microemulsion ,Particle Size ,Coix ,Drug Carriers ,biology ,Plant Extracts ,Liver Neoplasms ,Galactose ,Esters ,Hep G2 Cells ,General Medicine ,021001 nanoscience & nanotechnology ,biology.organism_classification ,In vitro ,chemistry ,Biochemistry ,Emulsions ,Asialoglycoprotein receptor ,0210 nano-technology ,Intracellular - 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 IC50 of 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-CME...
- Published
- 2016
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