Nguyen Hiep X, Nguyen Chien N
Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA.
National Institute of Pharmaceutical Technology, Hanoi University of Pharmacy, Hanoi 100000, Vietnam.
Pharmaceutics. 2023 Jan 13;15(1):277. doi: 10.3390/pharmaceutics15010277.
Transdermal delivery provides numerous benefits over conventional routes of administration. However, this strategy is generally limited to a few molecules with specific physicochemical properties (low molecular weight, high potency, and moderate lipophilicity) due to the barrier function of the stratum corneum layer. Researchers have developed several physical enhancement techniques to expand the applications of the transdermal field; among these, microneedle technology has recently emerged as a promising platform to deliver therapeutic agents of any size into and across the skin. Typically, hydrophilic biomolecules cannot penetrate the skin by passive diffusion. Microneedle insertion disrupts skin integrity and compromises its protective function, thus creating pathways (microchannels) for enhanced permeation of macromolecules. Microneedles not only improve stability but also enhance skin delivery of various biomolecules. Academic institutions and industrial companies have invested substantial resources in the development of microneedle systems for biopharmaceutical delivery. This review article summarizes the most recent research to provide a comprehensive discussion about microneedle-mediated delivery of macromolecules, covering various topics from the introduction of the skin, transdermal delivery, microneedles, and biopharmaceuticals (current status, conventional administration, and stability issues), to different microneedle types, clinical trials, safety and acceptability of microneedles, manufacturing and regulatory issues, and the future of microneedle technology.
与传统给药途径相比，经皮给药具有诸多优势。然而，由于角质层的屏障功能，这种给药策略通常仅限于少数具有特定物理化学性质（低分子量、高效能和适度亲脂性）的分子。研究人员已开发出多种物理增强技术来拓展经皮给药领域的应用；其中，微针技术最近已成为一种有前景的平台，可将任何大小的治疗药物输送到皮肤内并透过皮肤。通常，亲水性生物分子无法通过被动扩散穿透皮肤。微针插入会破坏皮肤完整性并损害其保护功能，从而为大分子增强渗透创造途径（微通道）。微针不仅能提高稳定性，还能增强各种生物分子的皮肤递送效果。学术机构和工业公司已投入大量资源用于开发用于生物制药递送的微针系统。这篇综述文章总结了最新研究，以全面讨论微针介导的大分子递送，涵盖从皮肤介绍、经皮给药、微针和生物制药（现状、传统给药方式和稳定性问题）到不同微针类型、临床试验、微针的安全性和可接受性、制造和监管问题以及微针技术的未来等各种主题。
