J Biomed Nanotechnol. 2021 Mar 1;17(3):357-368. doi: 10.1166/jbn.2021.3022.
Ferulic acid (FA), an active component extracted from Chinese medicine, shows excellent anti-inflammatory properties and favorable safety in various animal models. However, the application of FA as an anti-inflammatory drug is hindered by its instability and short half-life in vivo . In this paper, we synthesize PEGylated diphenylalanine nanoparticles by using glutaraldehyde (GTA) as a cross-linker of diphenylalanine NH₂ -Phe-Phe-COOH and poly(ethylene glycol) methyl ether amine (PEG -NH₂). The PEGylated Phe-Phe nanoparticles are used to deliver FA for the treatment of Rheumatoid arthritis (RA). We find that the FA-loaded PEGylated Phe-Phe nanoparticles are biocompatible and inhibit the production of reactive oxygen species (ROS) from cells effectively. After being intravenously administrated in vivo , the FA-loaded PEGylated Phe-Phe nanoparticles show prolonged circulation time and accumulate in arthritic joints. More importantly, we show that the pre-arthritis treatment with the FA-loaded PEGylated Phe-Phe nanoparticles can significantly block the progression of RA.
阿魏酸（FA）是一种从中药中提取的有效成分，在各种动物模型中表现出优异的抗炎特性和良好的安全性。然而，FA 作为一种抗炎药物的应用受到其在体内的不稳定性和半衰期短的限制。在本文中，我们使用戊二醛（GTA）作为二苯丙氨酸 NH₂-Phe-Phe-COOH 和聚乙二醇甲醚胺（PEG-NH₂）的交联剂，合成了聚乙二醇化的二苯丙氨酸纳米粒子。用聚乙二醇化的 Phe-Phe 纳米粒来输送 FA 治疗类风湿关节炎（RA）。我们发现负载 FA 的聚乙二醇化 Phe-Phe 纳米粒具有生物相容性，并能有效抑制细胞内活性氧（ROS）的产生。在体内静脉给药后，负载 FA 的聚乙二醇化 Phe-Phe 纳米粒表现出延长的循环时间并在关节炎关节中积累。更重要的是，我们表明，负载 FA 的聚乙二醇化 Phe-Phe 纳米粒的关节炎前期治疗可以显著阻断 RA 的进展。
