Abstract：
A transdermal delivery system offers high bioavailability and favorable patient adherence, constituting an optimal approach for localized administration in rheumatoid arthritis (RA) treatment. However, the stratum corneum (SC) impedes the delivery efficiency of conventional transdermal drug delivery systems. Microneedles (MNs) can temporarily create micropores within the SC, enabling drug distribution via bypassing this barrier and enhancing transdermal delivery effectiveness. Notably, MNs provide a painless method of drug delivery through the skin and may directly modulate inflammation in immune cells by delivering drugs via the lymphatic system during transdermal administration. However, the MN delivery system is not suitable for drugs with low water solubility and stability. Additionally, major concerns exist regarding the safety of using MN delivery for highly cytotoxic drugs, given that it could result in high local drug concentration at the delivery site. While MNs exhibit some degree of targeted delivery to the immune and inflammatory environment, their targeting efficiency remains suboptimal. Nanoformulations have the potential to significantly address the limitations of MNs in RA treatment by improving drug targeting, solubility, stability, and biocompatibility. Therefore, this review provides a concise overview of the advantages, disadvantages, and mechanisms of different types of MNs for RA treatment. It specifically focuses on the application and advantages of combining nanoformulation with MNs for RA treatment and summarizes the current trends in the development of nanoformulations combined with MNs in the field of RA treatment, offering theoretical support for future advancements and clinical applications.
摘要：
透皮给药系统提供高生物利用度和良好的患者依从性，构成类风湿关节炎（RA）治疗局部给药的最佳方法。然而,角质层(SC)阻碍常规经皮药物递送系统的递送效率。微针（MNs）可以在SC内暂时产生微孔，通过绕过该屏障并增强透皮递送有效性来实现药物分布。值得注意的是,MN提供了通过皮肤递送药物的无痛方法,并且可以通过在经皮施用期间经由淋巴系统递送药物来直接调节免疫细胞中的炎症。然而,MN给药系统不适用于水溶性和稳定性较低的药物。此外,存在关于使用MN递送高细胞毒性药物的安全性的主要问题，考虑到这可能会导致分娩部位的局部药物浓度很高。虽然MN表现出一定程度的靶向递送至免疫和炎症环境,他们的瞄准效率仍然不理想。纳米制剂有可能通过改善药物靶向来显著解决RA治疗中MNs的局限性，溶解度，稳定性,和生物相容性。因此,这篇综述简要概述了这些优点，缺点,以及不同类型MNs治疗RA的机制。它特别着重于将纳米制剂与MNs结合用于RA治疗的应用和优势，并总结了纳米制剂与MNs结合在RA治疗领域中的当前发展趋势。为未来的进步和临床应用提供理论支持。
