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Galactosylated Poly(Ethyleneglycol)‐Lithocholic Acid Selectively Kills Hepatoma Cells, While Sparing Normal Liver Cells
Author(s) -
Gankhuyag Nomundelger,
Singh Bijay,
Maharjan Sushila,
Choi YunJaie,
Cho ChongSu,
Cho MyungHaing
Publication year - 2015
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201400475
Subject(s) - lithocholic acid , apoptosis , chemistry , cancer cell , asialoglycoprotein receptor , programmed cell death , biochemistry , peg ratio , in vivo , cell , in vitro , cancer , bile acid , biology , hepatocyte , microbiology and biotechnology , finance , economics , genetics
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.