Guangdong Provincial Key laboratory of research and development of Natural drugs, School of Pharmacology, Guangdong Medical University, Dongguan, 523808, China.
Research Center of Nano Technology and Application Engineering, Dongguan Innovation Institute, Guangdong Medical University, Dongguan, 523808, China.
J Transl Med. 2024 Sep 30;22(1):878. doi: 10.1186/s12967-024-05662-1.
An oral colon-targeted drug delivery system holds great potential in preventing systemic toxicity and preserving the therapeutic benefits of ulcerative colitis (UC) treatment. In this study, we developed a negatively charged PLGA-PEG nanoparticle system for encapsulating naringin (Nar). Additionally, chitosan and mannose were coated on the surface of these nanoparticles to enhance their mucosal adsorption and macrophage targeting abilities. The resulting nanoparticles, termed MC@Nar-NPs, exhibited excellent resistance against decomposition in the strong acidic gastrointestinal environment and specifically accumulated at inflammatory sites. Upon payload release, MC@Nar-NPs demonstrated remarkable efficacy in alleviating colon inflammation as evidenced by reduced levels of pro-inflammatory cytokines in both blood and colon tissues, as well as the scavenging of reactive oxygen species (ROS) in the colon. This oral nanoparticle delivery system represents a novel approach to treating UC by utilizing Chinese herbal ingredient-based oral delivery and provides a theoretical foundation for local and precise intervention in specific UC treatment.
一种口服结肠靶向药物传递系统在预防系统性毒性和保持溃疡性结肠炎(UC)治疗的治疗效果方面具有巨大潜力。在这项研究中,我们开发了一种带负电荷的 PLGA-PEG 纳米颗粒系统来包裹柚皮苷(Nar)。此外,壳聚糖和甘露糖被涂覆在这些纳米颗粒的表面,以增强它们的黏膜吸附和巨噬细胞靶向能力。所得的纳米颗粒,称为 MC@Nar-NPs,在强酸性胃肠道环境中表现出出色的抗分解能力,并特异性地聚集在炎症部位。在负载物释放后,MC@Nar-NPs 表现出显著的缓解结肠炎症的功效,这表现在血液和结肠组织中的促炎细胞因子水平降低,以及结肠中活性氧(ROS)的清除。这种口服纳米颗粒传递系统通过利用基于中草药的口服传递为治疗 UC 提供了一种新方法,并为在特定 UC 治疗中进行局部和精确干预提供了理论基础。