State Key Laboratory of Southwestern Chinese Medicine Resources, College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
Department of Rehabilitation Sciences, Faculty of Health and Social Sciences, Hong Kong Polytechnic University, Kowloon, Hong Kong SAR, China.
Sci Rep. 2024 Oct 24;14(1):25256. doi: 10.1038/s41598-024-76341-w.
Triptolide (TP), a major active component of the herb Tripterygium wilfordii Hook F, has been shown excellent pharmacological effects on rheumatoid arthritis. However, TP is prone to causing severe organ toxicity, which limits its clinical application. In recent years, microneedle technology has provided a new option for the treatment of arthritis due to its advantages of efficient local transdermal drug delivery. In this study, we constructed a microneedle platform to deliver TP locally to the joints, thereby enhancing TP penetration and reducing systemic toxicity. Additionally, we investigated whether acupoint drug delivery can produce a synergistic effect of needles and drugs. First, TP was loaded into microneedles using polyvinylpyrrolidone and hyaluronic acid as matrix materials. Next, we established a rat adjuvant-induced arthritis (AIA) model to evaluate the therapeutic effect of TP-loaded microneedles. The experiments showed that TP-loaded microneedles alleviated the AIA rats' inflammatory response, joint swelling, and bone erosion. However, there was no significant difference in the therapeutic effect observed in the acupoint and non-acupoint administration groups. In conclusion, TP-loaded microneedles have the advantages of safety, convenience, and high efficacy over conventional administration routes, laying a foundation for the transdermal drug delivery system-based treatment of rheumatoid arthritis.
雷公藤红素（TP）是中药雷公藤的主要活性成分，具有出色的抗类风湿关节炎药理学作用。然而，TP 易引起严重的器官毒性，限制了其临床应用。近年来，微针技术因其高效的局部经皮药物传递优势，为关节炎的治疗提供了新的选择。在本研究中，我们构建了一个微针平台，将 TP 局部递送至关节，从而增强 TP 的穿透性并降低全身毒性。此外，我们还研究了穴位给药是否可以产生针药协同作用。首先，我们使用聚乙烯吡咯烷酮和透明质酸作为基质材料将 TP 载入微针中。然后，我们建立了大鼠佐剂性关节炎（AIA）模型，以评估载 TP 微针的治疗效果。实验表明，载 TP 微针减轻了 AIA 大鼠的炎症反应、关节肿胀和骨侵蚀。然而，在穴位和非穴位给药组观察到的治疗效果没有显著差异。总之，载 TP 微针具有比传统给药途径更安全、方便和高效的优势，为基于经皮给药系统治疗类风湿关节炎奠定了基础。
