关节炎发病率、致残致畸率高，是一种难治性疾病；尽管类型各异，但均存在关节腔的炎性反应，引发各种临床症状。中药治疗关节炎具有独特优势，但受到皮肤屏障及关节囊屏障的限制，常规给药途径难以满足关节腔内有效的药物浓度，影响了治疗效果。提高药物的关节囊渗透性，实现关节靶向，是增效减毒、提高关节炎治疗效果的核心。基于此，本课题以白芍总苷为模型，基于皮肤-关节囊屏障特点设计叶酸修饰醇质体经皮给药系统：①以微针阵列在皮肤表层形成非损伤性渗透微孔，为完整醇质体透皮吸收提供高效通道；②发挥完整醇质体的柔性变形特点，突破关节囊屏障，实现关节腔内转运；③通过醇质体表面修饰叶酸与滑膜活化巨噬细胞的特异性结合，实现炎性细胞主动靶向。通过体外透皮、活体成像、在体微透析等技术，对微针介导叶酸修饰白芍总苷醇质体透皮及关节靶向性能进行评价，探讨经皮-关节靶向给药系统的可行性及关键问题，为中药关节靶向制剂的研究提供参考。

Arthritis is one of the refractory diseases for high rate of incidence, disability and teratogenesis. It is divided into different types, but all of which have the same symptom——inflammatory in articular cavity, which causes many other clinical symptoms. TCM has a unique advantage in the treatment of arthritis. However, for the barriers of skin and articular capsule, the concentration in the articular cavity is very low, which leads to poor effective on arthritis. How to improve the permeability of articular capsule and to achieve articular targeting are the two important factors to reduce toxicity and enhance efficacy for arthritic treatment. So, an articular targeting system of FA-TGP-E is prepared based on the characteristic of skin and articular capsule barrier: ① micro needle array is employed on the surface of the skin to form non-invasive penetration pores, which promote transdermal absorption and ensure the structural integrity of FA-TGP-E; ② FA-TGP-E break through the articular capsule to the articular cavity taking the advantage of flexible deformation; ③ FA on the surface of FA-TGP-E bind to β-FA receptors on those activated macrophages of synovial membrane, then a system targeted to inflammatory cells is prepared. The permeability and articular targeting of this system（micro needles mediated FA-TGP-E）are evaluated by transdermal experiment, vivo imaging, micro-dialysis, and et al. The feasibility and key questions of this dermal drug delivery and articular targeting system are also investigated and discussed, that will provide credible references to some other TCM articular targeting preparations.