Efficient Delivery of Antisense Oligodeoxyribonucleotide G3139 by Human Serum Albumin-Coated Liposomes

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• 作者：Wanlop Weecharangsan ; Bo Yu ; Yu Zheng ; Shujun Liu ; Jiu Xia Pang ; L. James Lee ; Guido Marcucci ; Robert J. Lee
• 刊名：Molecular Pharmaceutics
• 出版年：2009
• 出版时间：December 7, 2009
• 年：2009
• 卷：6
• 期：6
• 页码：1848-1855
• 全文大小：225K
• 年卷期：v.6,no.6(December 7, 2009)
• ISSN：1543-8392

文摘

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.