Efficient delivery of antisense oligodeoxyribonucleotide G3139 by human serum albumin-coated liposomes

Wanlop Weecharangsan, Bo Yu, Yu Zheng, Shujun Liu, JiuXia Pang, L. James Lee, Guido Marcucci, Robert J. Lee

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26 Scopus citations


Human serum albumin (HSA)-coated liposomal formulations were synthesized and evaluated for the delivery of antisense oligodeoxyribonucleotide (ODN) G3139 in KB human oral carcinoma cells. Liposomes composed of dimethyldioctadecyl ammonium bromide/egg phosphatidylcholine/α-tocopheryl polyethylene glycol 1000 succinate (58:40:2 molar ratio) complexed with G3139 and coated with HSA were investigated for Bcl-2 downregulating activity. Cellular uptake of HSA-coated liposome-ODN complexes was more efficient than the uncoated liposome-ODN complexes. Treatment of the cells with HSA-coated liposome-ODN complexes resulted in efficient Bcl-2 mRNA downregulation that was approximately 3-fold greater than with uncoated liposomes (p < 0.05) and 6-fold greater than with free ODN. The transfection efficiency of liposome-ODN complexes coated with HSA was dependent on the concentration of HSA used and on the contents of α-helix and β-strand in HSA. HSA-coated liposomes are effective delivery vehicles for antisense ODN.

Original languageEnglish (US)
Pages (from-to)1848-1855
Number of pages8
JournalMolecular pharmaceutics
Issue number6
StatePublished - Dec 7 2009
Externally publishedYes


  • Antisense oligonucleotide
  • Bcl-2
  • Cancer
  • Drug delivery
  • G3139
  • Human serum albumin
  • Lipoplex
  • Liposomes


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