Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
Department of Pharmacy, the Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou 310058, China.
Int J Pharm. 2021 Jun 1;602:120598. doi: 10.1016/j.ijpharm.2021.120598. Epub 2021 Apr 20.
The transdermal delivery of macromolecular drugs has become one of the focused topics in pharmaceutical research since it enables highly specific and effective delivery, while avoiding the pain and needle phobia associated with injection, or incidences like drug degradation and low bioavailability of oral administration. However, the passive absorption of macromolecular drugs via skin is highly restricted by the stratum corneum owing to high molecular weight. Therefore, various strategies have been extensively developed and conducted to facilitate the transdermal delivery of macromolecular drugs, among which, mechanical force-assisted techniques occupy dominant positions. Such techniques include ultrasound, needle-free jet injection, temporary pressure and microneedles. In this review, we focus on recent transdermal enhancing strategies utilizing mechanical force, and summarize their mechanisms, advantages, limitations and clinical applications respectively.
大分子药物的经皮给药已成为药物研究的重点课题之一，因为它能够实现高度特异性和有效性的药物递送，同时避免了与注射相关的疼痛和针恐惧症，或口服给药时药物降解和生物利用度低等问题。然而，由于分子量高，大分子药物通过皮肤的被动吸收受到角质层的高度限制。因此，人们已经广泛开发和应用了各种策略来促进大分子药物的经皮递送，其中，机械力辅助技术占据主导地位。这些技术包括超声、无针喷射注射、临时压力和微针。在本综述中，我们重点关注最近利用机械力的经皮增强策略，并分别总结了它们的机制、优点、局限性和临床应用。
