Abstract：
The Helicobacter pylori infection in the stomach is the key reason for gastric mucosal bleeding. Eliminating gastric Helicobacter pylori by oral treatment remains difficult due to the presence of the gastric mucosal layer, which acts as a physical barrier to drugs via oral administration. In this study, a magnetic-navigable microneedle drug delivery platform (MNsD) for oral administration, featuring differential dual-mode drug release rate, was designed to fulfil rapid gastric hemostasis and overcome the gastric barriers for long-lasting Helicobacter pylori inhibition in stomach. MNs-D was created by rationally loading the carrier substrate, which was composed of silk fibroin with variable solubility, with antibiotics and hemostats. In vitro experiments showed MNs-D may sustainably eradicate Helicobacter pylori in stimulated gastric juices with long-lasting drug release (79 % in 24 h) and quickly establish hemostasis with instant drug release (92 % within 60 s). Most importantly, in vivo studies demonstrated MNs-D overcame the unsettling gastric mucosal barrier in traditional therapies of oral administration by insertion into the GML under magnetic navigation, resulting in sustained antibiotic release for long-lasting Helicobacter pylori eradiation (99 %). For differential dual-mode medication release against gastric Helicobacter pylori infections, this study may have firstly examined the effects of magnetic navigated microneedles administered orally.
摘要：
胃幽门螺杆菌感染是胃黏膜出血的主要原因。由于存在胃粘膜层，通过口服治疗消除胃幽门螺杆菌仍然很困难，它作为口服药物的物理屏障。在这项研究中,用于口服给药的磁性导航微针药物递送平台（MNsD），具有差分双模药物释放速率，旨在实现快速的胃止血并克服胃屏障，以长期抑制胃中的幽门螺杆菌。MNs-D是通过合理地加载载体衬底来创建的，由具有可变溶解度的丝素蛋白组成，抗生素和止血剂.体外实验表明，MNs-D可以持久地根除刺激的胃液中的幽门螺杆菌，并具有持久的药物释放（24小时内占79％），并迅速建立止血并立即释放药物（60s内占92％）。最重要的是,体内研究表明，MNs-D通过在磁导航下插入GML，克服了传统口服给药疗法中不稳定的胃粘膜屏障，导致持续的抗生素释放，长期持续的幽门螺杆菌感染(99%)。对于针对胃幽门螺杆菌感染的差异双模式药物释放，这项研究可能首先检查了口服磁性导航微针的效果。
