Nguyen Hiep X, Banga Ajay K
Faculty of Pharmacy, Phenikaa University, Yen Nghia, Ha Dong, Hanoi 12116, Viet Nam.
Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA.
Int J Pharm. 2025 Feb 10;670:125118. doi: 10.1016/j.ijpharm.2024.125118. Epub 2024 Dec 20.
Transdermal drug delivery presents numerous advantages over conventional administration routes, including non-invasiveness, enhanced patient adherence, circumvention of hepatic first-pass metabolism, self-administration capabilities, controlled release, and increased bioavailability. Nevertheless, the barrier function of stratum corneum limits this strategy to molecules possessing requisite physicochemical attributes. To expand the field of transdermal delivery, researchers have pioneered physical enhancement techniques, with micron-sized needles emerging as a particularly promising platform for the transdermal and intradermal delivery of therapeutic agents across a spectrum of molecular sizes. Microneedles function by disrupting the skin's integrity, generating microchannels that facilitate efficient drug permeation. This innovative technology boasts a captivating profile characterized by non-invasive drug delivery, enhanced efficacy and onset time, improved patient acceptability, self-administration possibilities, and precise dosing capabilities. Consequently, both academic institutions and industry have invested substantial resources in the development of microneedle systems for pharmaceutical delivery. This comprehensive review elucidates the multifaceted aspects of microneedle technology, encompassing its historical evolution, diverse materials, innovative designs, fabrication methodologies, and characterization techniques. The review extends to various microneedle types, including solid, hollow, coated, dissolving, swelling, and porous microneedles, as well as cutting-edge designs such as stimulus-responsive, iontophoresis-assisted, and bionic microneedles. Furthermore, we explore microneedle applications in vaccination, targeted delivery, and the administration of biologics, long-acting therapeutic agents, and cosmetics. Critical challenges in microneedle development, including dimensional considerations, safety concerns, acceptability factors, production scalability, regulatory hurdles, and sustainability issues, are thoroughly addressed, alongside a presentation of future prospects in this rapidly evolving field.
与传统给药途径相比,经皮给药具有诸多优势,包括无创性、患者依从性增强、规避肝脏首过代谢、自我给药能力、控释以及生物利用度提高。然而,角质层的屏障功能将这一策略限制于具有必要物理化学特性的分子。为了拓展经皮给药领域,研究人员开创了物理增强技术,微米级针头作为一种特别有前景的平台崭露头角,可用于跨多种分子大小的治疗药物的经皮和皮内给药。微针通过破坏皮肤完整性发挥作用,产生微通道以促进药物有效渗透。这项创新技术具有引人入胜的特点,包括无创给药、疗效和起效时间增强、患者接受度提高、自我给药可能性以及精确给药能力。因此,学术机构和行业都在微针系统用于药物递送的研发上投入了大量资源。这篇全面的综述阐明了微针技术的多方面内容,包括其历史演变、多样的材料、创新设计、制造方法和表征技术。综述涵盖了各种微针类型,包括实心、空心、包衣、溶解、肿胀和多孔微针,以及刺激响应、离子电渗辅助和仿生微针等前沿设计。此外,我们还探讨了微针在疫苗接种、靶向递送以及生物制品、长效治疗药物和化妆品给药方面的应用。微针开发中的关键挑战,包括尺寸考量、安全问题、可接受因素、生产可扩展性、监管障碍和可持续性问题,都得到了全面解决,同时还介绍了这个快速发展领域的未来前景。
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