Joint Department of Biomedical Engineering, University of North Carolina at Chapel Hill and North Carolina State University, Raleigh, NC 27695, USA; Division of Pharmacoengineering and Molecular Pharmaceutics, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Department of Medicine, University of North Carolina School of Medicine, Chapel Hill, NC 27599, USA.
Adv Drug Deliv Rev. 2018 Mar 1;127:106-118. doi: 10.1016/j.addr.2018.01.015. Epub 2018 Jan 31.
The intrinsic properties of therapeutic proteins generally present a major impediment for transdermal delivery, including their relatively large molecule size and susceptibility to degradation. One solution is to utilize microneedles (MNs), which are capable of painlessly traversing the stratum corneum and directly translocating protein drugs into the systematic circulation. MNs can be designed to incorporate appropriate structural materials as well as therapeutics or formulations with tailored physicochemical properties. This platform technique has been applied to deliver drugs both locally and systemically in applications ranging from vaccination to diabetes and cancer therapy. This review surveys the current design and use of polymeric MNs for transdermal protein delivery. The clinical potential and future translation of MNs are also discussed.
治疗性蛋白质的固有特性通常对透皮给药构成重大障碍,包括其相对较大的分子尺寸和易降解性。一种解决方案是利用微针 (MNs),它能够无痛地穿过角质层并将蛋白质药物直接转移到系统循环中。MNs 可以设计为包含适当的结构材料以及具有定制物理化学性质的治疗药物或制剂。该平台技术已应用于从疫苗接种到糖尿病和癌症治疗等各种应用中局部和系统地递药。本文综述了用于透皮蛋白传递的聚合物 MNs 的当前设计和应用。还讨论了 MNs 的临床潜力和未来转化。