Key Laboratory of Xinjiang Endemic Phytomedicine Resources Ministry of Education, Shihezi University College of Pharmacy, Shihezi, 832003, P. R. China.
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, P. R. China.
Small. 2022 Mar;18(9):e2104660. doi: 10.1002/smll.202104660. Epub 2022 Feb 8.
Bismuth-containing therapies are suggested as first-line and rescue alternatives for gastric ulcer (GU) treatment and Helicobacter pylori eradication. The current treatment strategy is called quadruple therapy and includes proton pump inhibitors, bismuth, and two broad-band antibiotics. This fact may affect medication compliance, leading to a resistance rate of more than 25% to clarithromycin or metronidazole. To counter this, from the perspective of natural products, an intragastric-targeting all-in-one theranostic platform is established: a drug carrier microcapsule composed of multiple synergistic antiulcer drugs, including bismuth, gallotannin, and antibiotics is obtained (BiG@MCs), and the therapeutic effects of BiG@MCs in rodent models are further evaluated. The results show that the BiG@MCs are spherical with homogeneous particle size (3 ± 0.5 µm) and can be response-released to the acidic environment of the stomach (pH 2.0-3.0), preventing the premature release of the BiG@MCs in physiological conditions. It is worth noting that the bismuth component can be easily identified by computed tomography and other detection instruments, which provide the possibility for drug tracing. In summary, these results indicate that BiG@MCs provide a versatile intragastric-targeting drug delivery platform for GU therapeutics.
含铋疗法被推荐为治疗胃溃疡 (GU) 和根除幽门螺杆菌的一线和救援替代方案。目前的治疗策略称为四联疗法,包括质子泵抑制剂、铋和两种广谱抗生素。这一事实可能会影响药物的依从性,导致克拉霉素或甲硝唑的耐药率超过 25%。有鉴于此,从天然产物的角度出发,建立了一种胃内靶向一体化治疗诊断平台:获得了一种由多种协同抗溃疡药物(包括铋、没食子单宁和抗生素)组成的药物载体微胶囊(BiG@MCs),并进一步评估了 BiG@MCs 在啮齿动物模型中的治疗效果。结果表明,BiG@MCs 呈球形,粒径均一(3±0.5μm),可响应释放到胃部的酸性环境(pH 2.0-3.0),防止 BiG@MCs 在生理条件下过早释放。值得注意的是,铋成分可以很容易地被计算机断层扫描和其他检测仪器识别,这为药物追踪提供了可能性。总之,这些结果表明 BiG@MCs 为 GU 治疗提供了一种通用的胃内靶向药物递送平台。
Micromachines (Basel). 2023-2-15