Charge-Reversal Amphiphiles for Gene Delivery

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• 作者：Carla A. H. Prata ; Yuxing Zhao ; Philippe Barthelemy ; Yougen Li ; Dan Luo ; Thomas J. McIntosh ; Stephen J. Lee ; and Mark W. Grinstaff
• 刊名：Journal of the American Chemical Society
• 出版年：2004
• 出版时间：October 6, 2004
• 年：2004
• 卷：126
• 期：39
• 页码：12196 - 12197
• 全文大小：95K
• 年卷期：v.126,no.39(October 6, 2004)
• ISSN：1520-5126

文摘

Delivering a missing gene or a functional substitute of a defective gene has the potential to revolutionize current medical care. Of the two gene delivery approaches, viral and synthetic vectors, synthetic cationic vectors possess several practical advantages but suffer from poor transfection efficiency. A new approach to gene delivery using charge-reversal amphiphiles is described. This synthetic vector transforms from a cationic to an anionic amphiphile intracellularly. This amphiphile performs two roles: first, it binds and then releases DNA, and second, as an anionic multicharged amphiphile, it destabilizes lipid bilayers. A charge-reversal amphiphile was synthesized and fully characterized, including the supramolecular complex it forms with DNA. Enhanced gene transfection was observed using these vectors compared to current cationic amphiphiles.