Inflammatory bowel diseases (IBD) are the incurable chronic recurrent gastrointestinal disorders and currently lack in safe and effective drugs. In this study, patchouli alcohol, a main active compound of traditional Chinese herb patchouli, was developed into biomimetic liposomes for macrophage-targeting delivery for IBD treatment. The developed lactoferrin-modified liposomes (LF-lipo) can specifically bind to LRP-1 expressed on the activated colonic macrophages and achieve cell-targeting anti-inflammatory therapy. LF-lipo reduced the levels of inflammatory cytokines and ROS and suppressed the MAPK/NF-κB pathway. LF-lipo also suppressed the formation of NLRP3 inflammasome and the consequent IL-1β activation. LF-lipo showed improved therapeutic efficacy in a DSS-induced colitis murine model, evidenced by the reduced disease activity index, the improved colon functions, and the downregulated inflammatory cytokines in the colon. LF-lipo provided an effective and safe macrophage-targeting delivery and therapeutic strategy for addressing the unmet medical need in IBD management.

炎症性肠病（IBD）是无法治愈的慢性胃肠道疾病，目前缺乏安全有效的药物。在这项研究中，广patch香醇是中药广patch香的主要活性化合物，被开发为仿生脂质体，用于靶向巨噬细胞的IBD治疗。研发的乳铁蛋白修饰脂质体（LF-lipo）可以与活化结肠巨噬细胞上表达的LRP-1特异性结合，并实现针对细胞的抗炎治疗。LF-脂减少炎性细胞因子和ROS的水平和抑制MAPK / NF- κ乙通路。LF-脂质也抑制了NLRP3炎性小体的形成以及随之而来的IL- 1β激活。LF-脂质在DSS诱导的结肠炎小鼠模型中显示出改善的治疗功效，这由降低的疾病活动指数，改善的结肠功能和结肠中炎性细胞因子下调所证明。LF-脂质为解决IBD管理中未满足的医疗需求提供了有效且安全的巨噬细胞靶向递送和治疗策略。