Rationale: Anti-tumor necrosis factor (TNF) therapy is a very effective way to treat inflammatory bowel disease. However, systemic exposure to anti-TNF-α antibodies through current clinical systemic administration can cause serious adverse effects in many patients. Here, we report a facile prepared self-assembled supramolecular nanoparticle based on natural polyphenol tannic acid and poly(ethylene glycol) containing polymer for oral antibody delivery./nMethod: This supramolecular nanoparticle was fabricated within minutes in aqueous solution and easily scaled up to gram level due to their pH-dependent reversible assembly. DSS-induced colitis model was prepared to evaluate the ability of inflammatory colon targeting ability and therapeutic efficacy of this antibody-loaded nanoparticles./nResults: This polyphenol-based nanoparticle can be aqueous assembly without organic solvent and thus scaled up easily. The oral administration of antibody loaded nanoparticle achieved high accumulation in the inflamed colon and low systemic exposure. The novel formulation of anti-TNF-α antibodies administrated orally achieved high efficacy in the treatment of colitis mice compared with free antibodies administered orally. The average weight, colon length, and inflammatory factors in colon and serum of colitis mice after the treatment of novel formulation of anti-TNF-α antibodies even reached the similar level to healthy controls./nConclusion: This polyphenol-based supramolecular nanoparticle is a promising platform for oral delivery of antibodies for the treatment of inflammatory bowel diseases, which may have promising clinical translation prospects.

中文翻译：

---

经天然多酚介导的超分子组装屏蔽的抗TNF抗体的口服给药，用于炎症性肠病治疗。

理由：抗肿瘤坏死因子（TNF）治疗是一种治疗炎症性肠病的非常有效的方法。但是，通过当前的临床全身性给药全身性暴露于抗TNF-α抗体会在许多患者中引起严重的不良反应。这里，我们报告一个浅显制备的自组装的超分子的纳米粒子基于天然多酚单宁酸和包含用于delivery./n口服抗体聚合物聚（乙二醇）的方法：该超分子的纳米颗粒在水溶液分钟内制造且容易地按比例放大到由于它们依赖于pH值的可逆装配，因此其克数为1克。制备了DSS诱导的结肠炎模型，以评估炎性结肠靶向能力和该抗体负载纳米颗粒的治疗功效。结果：这种基于多酚的纳米颗粒可以在没有有机溶剂的情况下进行水性组装，因此易于放大。口服抗体负载的纳米颗粒在发炎的结肠中获得了很高的积累，并且全身暴露率较低。与口服施用的游离抗体相比，口服施用的抗TNF-α抗体的新型制剂在结肠炎小鼠的治疗中实现了高功效。新的抗TNF-α抗体制剂治疗后，结肠炎小鼠的平均体重，结肠长度和结肠和血清中的炎症因子甚至达到了与健康对照组相似的水平。/n结论： 这种基于多酚的超分子纳米颗粒是用于治疗炎症性肠病的抗体口服给药的有前途的平台，其可能具有有前途的临床翻译前景。