Massachusetts Institute of Technology, Department of Chemical Engineering, 77 Massachusetts Avenue, Cambridge, MA 02139, USA.
Expert Opin Drug Deliv. 2010 Dec;7(12):1415-32. doi: 10.1517/17425247.2010.538679.
Transdermal delivery of macromolecules provides an attractive alternative route of drug administration when compared to oral delivery and hypodermic injection because of its ability to bypass the harsh gastrointestinal tract and deliver therapeutics non-invasively. However, the barrier properties of the skin only allow small, hydrophobic permeants to traverse the skin passively, greatly limiting the number of molecules that can be delivered via this route. The use of low-frequency ultrasound for the transdermal delivery of drugs, referred to as low-frequency sonophoresis (LFS), has been shown to increase skin permeability to a wide range of therapeutic compounds, including both hydrophilic molecules and macromolecules. Recent research has demonstrated the feasibility of delivering proteins, hormones, vaccines, liposomes and other nanoparticles through LFS-treated skin. In vivo studies have also established that LFS can act as a physical immunization adjuvant. LFS technology is already clinically available for use with topical anesthetics, with other technologies currently under investigation.
This review provides an overview of mechanisms associated with LFS-mediated transdermal delivery, followed by an in-depth discussion of the current applications of LFS technology for the delivery of hydrophilic drugs and macromolecules, including its use in clinical applications.
The reader will gain an insight into the field of LFS-mediated transdermal drug delivery, including how the use of this technology can improve on more traditional drug delivery methods.
Ultrasound technology has the potential to impact many more transdermal delivery platforms in the future due to its unique ability to enhance skin permeability in a controlled manner.
与口服给药和皮下注射相比,大分子经皮给药提供了一种有吸引力的药物给药途径,因为它能够绕过恶劣的胃肠道并无创地输送治疗剂。然而,皮肤的屏障特性仅允许小的、疏水性的渗透物被动地穿过皮肤,极大地限制了可以通过该途径输送的分子数量。低频超声用于药物经皮传递,称为低频声透法(LFS),已被证明可以增加对广泛治疗化合物的皮肤通透性,包括亲水分子和大分子。最近的研究已经证明了通过 LFS 处理的皮肤输送蛋白质、激素、疫苗、脂质体和其他纳米颗粒的可行性。体内研究还表明,LFS 可以作为物理免疫佐剂。LFS 技术已经在临床中可用于局部麻醉剂,其他技术目前正在研究中。
本综述提供了与 LFS 介导的经皮输送相关的机制概述,然后深入讨论了 LFS 技术在亲水性药物和大分子输送中的当前应用,包括其在临床应用中的应用。
读者将深入了解 LFS 介导的经皮药物输送领域,包括了解这项技术如何改善更传统的药物输送方法。
由于超声技术具有以可控方式增强皮肤通透性的独特能力,因此它有可能在未来影响更多的经皮输送平台。