We have developed a self-assembling polymeric nanocarrier to deliver the potent immunosuppressive drug Cyclosporine A (CsA) to inflammatory lesions in ulcerative colitis (UC) patients. Our nanocarrier has a high drug loading capacity and efficiently targets its CsA payload to the diseased tissue after local administration. Tissue drug levels were several orders of magnitude higher in animals suffering from a trinitrobenzene-sulfonic acid (TNBS) – induced colitis, compared to healthy control animals; no drug was detectable in the plasma, underlining the localized delivery strategy. An efficient reduction in inflammation score was obtained with a CsA dose of 1 mg/mL. Therapeutic efficacy was comparable to 5-aminosalicylic acid (5-ASA), the positive control treatment in the TNBS-induced colitis model. Repetitive treatment of healthy animals with CsA nanocarriers for seven days was well tolerated with no alterations in colon histology.

我们已经开发了一种自组装聚合物纳米载体，可以将有效的免疫抑制药环孢菌素A（CsA）递送至溃疡性结肠炎（UC）患者的炎性病变。我们的纳米载体具有很高的载药量，可在局部给药后有效地将其CsA有效载荷靶向患病的组织。与健康对照组动物相比，患有三硝基苯磺酸（TNBS）引起的结肠炎的动物的组织药物水平高出几个数量级。在血浆中没有检测到药物，这强调了局部递送策略。使用1 mg / mL的CsA剂量可有效降低炎症评分。在TNBS诱导的结肠炎模型中，阳性疗效与5-氨基水杨酸（5-ASA）相当。