期刊
MACROMOLECULAR BIOSCIENCE
卷 15, 期 6, 页码 777-787出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/mabi.201400475
关键词
anti-cancer drugs; apoptosis; hepatocyte-specific; lithocholic acid; nanoparticles
资金
- National Research Foundation - Ministry of Science, ICT & Future Planning [2012M3A9B6055304]
- Brain Korea 21 program for the Veterinary Science of Seoul National University
- Research Institute for Veterinary Science, Seoul National University
Delivering drugs selectively to cancer cells but not to nearby normal cells is a major obstacle in drug therapy. In this study, lithocholic acid (LCA), a potent anti-cancer drug, is converted to two forms of poly(ethyleneglycol) (PEG) conjugates, viz., PEG-LCA (PL) and lactobionic acid (LBA) conjugated PEG-LCA (LPL). The latter form contains a galactose ligand in LBA to target the hepatocytes. Both forms are self-assembled to form nanoparticle formulation, and they have high potency than LCA to kill HepG2 cancer cells, sparing normal LO2 cells. Besides, LPL has high specificity to mouse liver cells in vivo. Western blot results confirm that the cell death is occurred through apoptosis induced by LPL nanoparticles. In conclusion, the induction of apoptosis and cell death is much more efficient with LPL nanoparticles than LCA molecules.
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