Dhote Vinod, Bhatnagar Punit, Mishra Pradyumna K, Mahajan Suresh C, Mishra Dinesh K
Mahakal Institute of Pharmaceutical Studies, Ujjain, M. P., India.
Sci Pharm. 2012 Jan-Mar;80(1):1-28. doi: 10.3797/scipharm.1108-20. Epub 2011 Dec 13.
The delivery of drugs into systemic circulation via skin has generated much attention during the last decade. Transdermal therapeutic systems propound controlled release of active ingredients through the skin and into the systemic circulation in a predictive manner. Drugs administered through these systems escape first-pass metabolism and maintain a steady state scenario similar to a continuous intravenous infusion for up to several days. However, the excellent impervious nature of the skin offers the greatest challenge for successful delivery of drug molecules by utilizing the concepts of iontophoresis. The present review deals with the principles and the recent innovations in the field of iontophoretic drug delivery system together with factors affecting the system. This delivery system utilizes electric current as a driving force for permeation of ionic and non-ionic medications. The rationale behind using this technique is to reversibly alter the barrier properties of skin, which could possibly improve the penetration of drugs such as proteins, peptides and other macromolecules to increase the systemic delivery of high molecular weight compounds with controlled input kinetics and minimum inter-subject variability. Although iontophoresis seems to be an ideal candidate to overcome the limitations associated with the delivery of ionic drugs, further extrapolation of this technique is imperative for translational utility and mass human application.
在过去十年中,通过皮肤将药物输送到体循环引起了广泛关注。透皮治疗系统主张以可预测的方式使活性成分通过皮肤并进入体循环。通过这些系统给药的药物可避免首过代谢,并在长达数天的时间内维持类似于持续静脉输注的稳态情况。然而,皮肤出色的不透性对利用离子电渗疗法的概念成功递送药物分子提出了最大挑战。本综述探讨了离子电渗药物递送系统领域的原理、最新创新以及影响该系统的因素。这种递送系统利用电流作为离子和非离子药物渗透的驱动力。使用该技术的基本原理是可逆地改变皮肤的屏障特性,这可能会改善蛋白质、肽和其他大分子等药物的渗透,以增加高分子量化合物的全身递送,同时具有可控的输入动力学和最小的个体间变异性。尽管离子电渗疗法似乎是克服与离子药物递送相关局限性的理想选择,但为了实现转化应用和大规模人体应用,对该技术进行进一步拓展势在必行。