Qiao Yanqi, Han Mengfan, Fu Hongli, Xu Yaying, Bai Yueping, Wang Shuo, Yu Jie, Men Changjun, Yin Yongmei, Zhao Xiujie, Xi Rimo, Meng Meng
State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and KLMDASR of Tianjin, Nankai University, Tianjin, 300350, China.
State Key Laboratory of Southern Medicine Utilization, College of Pharmaceutical Science, Yunnan University of Chinese Medicine, Yunnan Province, Kunming, 650500, China.
Small. 2024 May;20(20):e2306909. doi: 10.1002/smll.202306909. Epub 2023 Dec 15.
Helicobacter pylori (H. pylori) infection presents increasing challenges to antibiotic therapies in limited penetration through gastric mucus, multi-drug resistance (MDR), biofilm formation, and intestinal microflora dysbiosis. To address these problems, herein, a mucus-penetrating phototherapeutic nanomedicine (RLs@T780TG) against MDR H. pylori infection is engineered. The RLs@T780TG is assembled with a near-infrared photosensitizer T780T-Gu and an anionic component rhamnolipids (RLs) for deep mucus penetration and light-induced anti-H. pylori performances. With optimized suitable size, hydrophilicity and weak negative surface, the RLs@T780TG can effectively penetrate through the gastric mucus layer and target the inflammatory site. Subsequently, under irradiation, the structure of RLs@T780TG is disrupted and facilitates the T780T-Gu releasing to target the H. pylori surface and ablate multi-drug resistant (MDR) H. pylori. In vivo, RLs@T780TG phototherapy exhibits impressive eradication against H. pylori. The gastric lesions are significantly alleviated and intestinal bacteria balance is less affected than antibiotic treatment. Summarily, this work provides a potential nanomedicine design to facilitate in vivo phototherapy in treatment of H. pylori infection.
幽门螺杆菌（H. pylori）感染在抗生素治疗方面面临着越来越多的挑战，包括在胃黏液中的穿透性有限、多重耐药性（MDR）、生物膜形成以及肠道微生物群失调。为了解决这些问题，本文设计了一种针对多重耐药性幽门螺杆菌感染的黏液穿透性光疗纳米药物（RLs@T780TG）。RLs@T780TG由近红外光敏剂T780T-Gu和阴离子成分鼠李糖脂（RLs）组装而成，用于深层黏液穿透和光诱导抗幽门螺杆菌性能。RLs@T780TG具有优化的合适尺寸、亲水性和弱负表面，能够有效穿透胃黏液层并靶向炎症部位。随后，在光照下，RLs@T780TG的结构被破坏，促进T780T-Gu释放以靶向幽门螺杆菌表面并消融多重耐药性（MDR）幽门螺杆菌。在体内，RLs@T780TG光疗对幽门螺杆菌表现出令人印象深刻的根除效果。与抗生素治疗相比，胃部病变得到显著缓解，对肠道细菌平衡的影响较小。总之，这项工作提供了一种潜在的纳米药物设计，以促进体内光疗治疗幽门螺杆菌感染。
