Kalia Yogeshvar N, Naik Aarti, Garrison James, Guy Richard H
School of Pharmacy, University of Geneva, Geneva, Switzerland.
Adv Drug Deliv Rev. 2004 Mar 27;56(5):619-58. doi: 10.1016/j.addr.2003.10.026.
The composition and architecture of the stratum corneum render it a formidable barrier to the topical and transdermal administration of therapeutic agents. The physicochemical constraints severely limit the number of molecules that can be considered as realistic candidates for transdermal delivery. Iontophoresis provides a mechanism to enhance the penetration of hydrophilic and charged molecules across the skin. The principal distinguishing feature is the control afforded by iontophoresis and the ability to individualize therapies. This may become significant as the impact of interindividual variations in protein expression and the effect on drug metabolism and drug efficacy is better understood. In this review we describe the underlying mechanisms that drive iontophoresis and we discuss the impact of key experimental parameters-namely, drug concentration, applied current and pH-on iontophoretic delivery efficiency. We present a comprehensive and critical review of the different therapeutic classes and molecules that have been investigated as potential candidates for iontophoretic delivery. The iontophoretic delivery of peptides and proteins is also discussed. In the final section, we describe the development of the first pre-filled, pre-programmed iontophoretic device, which is scheduled to be commercialized during the course of 2004.
角质层的组成和结构使其成为治疗药物经皮给药的巨大障碍。物理化学限制严重限制了可被视为经皮递送实际候选分子的数量。离子电渗疗法提供了一种增强亲水性和带电分子透过皮肤的机制。其主要区别特征在于离子电渗疗法所提供的控制以及个性化治疗的能力。随着对个体间蛋白质表达差异及其对药物代谢和药物疗效影响的更好理解,这一点可能会变得很重要。在本综述中,我们描述了驱动离子电渗疗法的潜在机制,并讨论了关键实验参数(即药物浓度、施加电流和pH值)对离子电渗递送效率的影响。我们对已作为离子电渗递送潜在候选物进行研究的不同治疗类别和分子进行了全面且批判性的综述。还讨论了肽和蛋白质的离子电渗递送。在最后一部分,我们描述了首个预填充、预编程离子电渗装置的开发情况,该装置计划于2004年投入商业化生产。