Effect of edge activators on the formation and transfection efficiency of ultradeformable liposomes
Effect of edge activators on the formation and transfection efficiency of ultradeformable liposomes
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DOI：
10.1016/j.biomaterials.2004.02.020
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发表时间：
2005-01-01
期刊：
影响因子：
14
通讯作者：
Kim, CK
中科院分区：
文献类型：
--
作者：
Lee, EH;Kim, A;Kim, CK
高度可变形的亲水脂质囊泡已被研究用于治疗活性小分子和蛋白质的经皮递送。在这里，我们报告了边缘激活剂对超可成型脂质体（UL）形成和透皮基因传递的影响。胆酸钠、脱氧胆酸钠和Tween 80作为边缘活化剂进行了测试。在边缘激活剂中，胆酸钠和脱氧胆酸钠比Tween 80的UL尺寸更小，zeta电位更高。此外，脱氧胆酸钠基的UL显示出最高的正zeta电位，这可能导致其与带负电荷的DNA结合更牢固。局部应用于小鼠后，DNA与含有胆酸钠或脱氧胆酸钠的UL络合显示出大量的透皮吸收。相比之下，DNA与基于Tween 80的UL复合物没有显示出体内透皮吸收。这些数据表明，UL可能用作质粒DNA的透皮递送系统，并且边缘激活剂的选择可能在通过UL的质粒DNA透皮递送中起重要作用。(C) 2004 Elsevier Ltd.版权所有。
Highly deformable hydrophilic lipid vesicles have been studied for transdermal delivery of therapeutically active small molecules and proteins. Here, we report the effects of edge activators on the formation of ultradeformable liposomes (UL) and transdermal gene delivery. Sodium cholate, sodium deoxycholate, and Tween 80 were tested as edge activators. Of the edge activators, sodium cholate and sodium deoxycholate resulted in the smaller sizes of UL and more positive zeta potentials than did Tween 80. Moreover, sodium deoxycholate-based UL showed the highest positive zeta potentials, which might lead to the firmer binding with negatively charged DNA. Following topical application onto mice, DNA complexed with UL containing either sodium cholate or sodium deoxycholate showed substantial transdermal absorption. In contrast, DNA complexed with Tween 80-based UL did not show in vivo transdermal absorption. These data suggest that UL might be of use as a transdermal delivery system of plasmid DNA, and that the choice of edge activators may play an important, role in the transdermal delivery of plasmid DNA via UL. (C) 2004 Elsevier Ltd. All rights reserved.