Overcoming the barrier of skin to drug permeation for localized dermatological therapies

Bozena Michniak-Kohn, Joachim Kohn
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Abstract

Background. The skin’s uppermost layer, the stratum corneum is a very effective barrier against the penetration of compounds including pharmaceuticals and cosmetic actives. To deliver higher amounts of drugs into the skin layers or to deliver drugs deeper into the skin (e.g., into the dermis), several enhancement techniques have been established. These techniques include chemical penetration enhancers as well as physical techniques such as iontophoresis and microneedles. In addition, one of the newer approaches includes the use of nano-based carriers such as metallic nanoparticles and polymeric self-assembling nanospheres. Methods. This mini-review explores this new approach of using nano-based drug carriers for skin penetration enhancement. In particular we will explore the use of gold nanoparticles as well as biocompatible tyrosine-derived polymeric nanoparticles known as Tyrospheres. Results. The most investigated carriers in the class of metallic carriers are gold nanoparticles that can be used for both medical as well as diagnostic uses. Many investigators have reported that gold nanoparticles are able to enhance the skin transport and delivery of macromolecular and hydrophilic drugs. Meanwhile, for challenging highly lipophilic and/or unstable compounds such as adapalene and Vitamin D3 packaging them into polymeric nanocarriers such as Tyrospheres enables drug delivery to hair follicles, significantly increased aqueous solubility and resulted in elevated amounts of drug in targeted skin layers. Conclusions. The relatively new approach of using nanotechnological approaches as a way of enhancement of drug delivery to skin shows significant promise over some other established techniques such as the addition of chemical penetration enhancers to formulations used for topical/transdermal uses.
克服皮肤对局部皮肤药物渗透的障碍
背景。皮肤的最上层,角质层是一个非常有效的屏障,可以防止药物和化妆品活性物质等化合物的渗透。为了将更大量的药物输送到皮肤层或将药物输送到皮肤深处(例如,进入真皮层),已经建立了几种增强技术。这些技术包括化学渗透增强剂以及物理技术,如离子电泳和微针。此外,一种较新的方法包括使用纳米载体,如金属纳米颗粒和聚合物自组装纳米球。方法。这篇综述探讨了利用纳米药物载体增强皮肤渗透的新方法。特别地,我们将探索金纳米粒子的使用,以及生物相容性酪氨酸衍生的聚合物纳米粒子,称为酪氨酸球。结果。在金属载体类别中,研究最多的载体是金纳米颗粒,它既可用于医疗,也可用于诊断。许多研究者已经报道了金纳米颗粒能够增强大分子和亲水药物的皮肤运输和递送。同时,对于高亲脂性和/或不稳定的化合物,如阿达帕烯和维生素D3,将它们包装成聚合物纳米载体,如Tyrospheres,可以使药物递送到毛囊,显着增加水溶解度,并导致靶向皮肤层中药物量的增加。结论。相对较新的方法是使用纳米技术方法作为一种增强药物到皮肤的方式,这比其他一些已建立的技术(如在用于局部/透皮用途的配方中添加化学渗透增强剂)显示出重大的前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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