FDA/CDER/DPQR, White Oak, LS Building 64, Room 1082, 10903 New Hampshire Ave, Silver Spring, MD-20993-002, USA.
Curr Drug Deliv. 2010 Apr;7(2):125-36. doi: 10.2174/156720110791011765.
The stratum corneum (SC) is a primary rate limiting barrier to permeation of drug molecules through the skin. Small molecular weight lipophilic drugs that are effective at low doses can be effectively delivered by passive transdermal delivery. The SC does not permit passage of polar/hydrophilic and macromolecules. Passive and physical penetration enhancements strategies are used to overcome this barrier property of the SC. Passive penetration enhancement techniques include use of supersaturated solutions and penetration enhancers. In general, the drug delivery potential of chemical modalities is limited. Therefore, physical permeation enhancement techniques gained a lot of focus in the recent past. Physical penetration enhancement techniques include iontophoresis, electroporation and sonophoresis. Electroporation utilizes high voltage pulses that are applied for a very short time to permeabilize the skin to facilitate transport of macromolecules and hydrophilic compounds. Several drugs have been administered via this system successfully. This review presents an overview of in-vitro and in-vivo studies demonstrating therapeutic benefits offered by electroporation assisted permeation. Factors affecting electroporation, synergism between electroporation and other penetration enhancing strategies are also discussed.
角质层（SC）是药物分子经皮渗透的主要限速屏障。小分子量亲脂性药物，低剂量有效，可以通过被动透皮给药有效地递送至体内。SC 不允许极性/亲水性和大分子通过。因此，人们采用被动和物理渗透增强策略来克服 SC 的这种屏障特性。被动渗透增强技术包括使用超饱和溶液和渗透增强剂。一般来说，化学传递方式的药物递送潜力有限。因此，物理渗透增强技术在最近受到了广泛关注。物理渗透增强技术包括离子电渗法、电穿孔和声透法。电穿孔利用短时间内施加的高压脉冲来使皮肤穿孔，以促进大分子和亲水化合物的转运。已经成功地通过该系统给药了几种药物。本文综述了体外和体内研究，这些研究证明了电穿孔辅助渗透带来的治疗益处。还讨论了影响电穿孔的因素以及电穿孔与其他渗透增强策略的协同作用。
