Co-delivery of hesperidin and clarithromycin in a nanostructured lipid carrier for the eradication of Helicobacter pylori in vitro

Bioorg Chem. 2021 Jul:112:104896. doi: 10.1016/j.bioorg.2021.104896. Epub 2021 Apr 7.

Abstract

Effective and precise eradication of Helicobacter pylori (H. pylori) is the most promising approach to avoid H. pylori-related gastrointestinal disorders. The present study was conducted to demonstrate the efficacy of the co-delivery of hesperidin (Hesp) and clarithromycin (CLR) in nanostructured lipid carriers (NLCs) against H. pylori. We have produced a new delivery system by combining bioflavonoid Hesp and CLR NLCs to address the failure in single antibiotic therapies. Briefly, a blend of solid lipid, liquid lipid, and surfactant was used. Homogeneous NLCs with all the formulations showed a nano size and surface-negative charge and presented high in vitro stability and slow release of the drug even after 24 h. Bioimaging studies by scanning electron microscopy, transmission electron microscopy, and imaging flow cytometry indicated that NLCs interacted with the membrane by adhering to the outer cell membrane and disrupted the membrane that resulted in the leakage of cytoplasmic contents. The prepared NLCs provide sustained and controlled drug release that can be used to increase the rate of H. pylori eradication.

Keywords: Anti-microbial resistance; Drug delivery; Hesperidin; Membrane interaction; Nanostructure lipid carrier; Targeting.

Publication types

  • Letter
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Bacterial Outer Membrane Proteins / analysis
  • Clarithromycin / chemistry
  • Clarithromycin / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Carriers / chemistry
  • Drug Delivery Systems*
  • Helicobacter pylori / drug effects*
  • Hesperidin / chemistry
  • Hesperidin / pharmacology*
  • Lipids / chemistry*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Nanoparticles / chemistry*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Bacterial Outer Membrane Proteins
  • Drug Carriers
  • Lipids
  • Hesperidin
  • Clarithromycin