Denet Anne-Rose, Vanbever Rita, Préat Véronique
Unité de Pharmacie Galénique, Université Catholique de Louvain, Avenue E. Mounier, 73 UCL 7320, 1200 Brussels, Belgium.
Adv Drug Deliv Rev. 2004 Mar 27;56(5):659-74. doi: 10.1016/j.addr.2003.10.027.
Electroporation is the transitory structural perturbation of lipid bilayer membranes due to the application of high voltage pulses. Its application to the skin has been shown to increase transdermal drug delivery by several orders of magnitude. Moreover, electroporation, used alone or in combination with other enhancement methods, expands the range of drugs (small to macromolecules, lipophilic or hydrophilic, charged or neutral molecules) which can be delivered transdermally. Molecular transport through transiently permeabilized skin by electroporation results mainly from enhanced diffusion and electrophoresis. The efficacy of transport depends on the electrical parameters and the physicochemical properties of drugs. The in vivo application of high voltage pulses is well tolerated but muscle contractions are usually induced. The electrode and patch design is an important issue to reduce the discomfort of the electrical treatment in humans.
电穿孔是由于施加高压脉冲而导致脂质双分子层膜的短暂结构扰动。已证明将其应用于皮肤可使经皮给药增加几个数量级。此外，单独使用电穿孔或与其他增强方法联合使用，可扩大能够经皮递送的药物范围（从小分子到大分子，亲脂性或亲水性，带电或中性分子）。通过电穿孔使皮肤短暂通透后的分子转运主要源于扩散增强和电泳。转运效率取决于电参数和药物的物理化学性质。体内施加高压脉冲耐受性良好，但通常会引起肌肉收缩。电极和贴片设计是减少人体电治疗不适感的一个重要问题。
