All-in-One Theranostic Platform Based on Hollow Microcapsules for Intragastric-Targeting Antiulcer Drug Delivery, CT Imaging, and Synergistically Healing Gastric Ulcer

Small. 2022 Mar;18(9):e2104660. doi: 10.1002/smll.202104660. Epub 2022 Feb 8.

Abstract

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.

Keywords: bismuth; computed tomography imaging; drug delivery; gallotannin; platforms.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Anti-Bacterial Agents / therapeutic use
  • Bismuth / therapeutic use
  • Capsules
  • Drug Therapy, Combination
  • Helicobacter Infections* / drug therapy
  • Helicobacter pylori*
  • Humans
  • Precision Medicine
  • Stomach Ulcer* / drug therapy
  • Tetracycline / pharmacology
  • Tetracycline / therapeutic use
  • Tomography, X-Ray Computed

Substances

  • Anti-Bacterial Agents
  • Capsules
  • Tetracycline
  • Bismuth