Zwitterionic meso-silica/polypeptide hybrid nanoparticles for efficient azithromycin delivery and photodynamic therapy for synergistic treatment of drug-resistant bacterial infection

Int J Biol Macromol. 2022 Oct 31:219:597-610. doi: 10.1016/j.ijbiomac.2022.08.022. Epub 2022 Aug 8.

Abstract

The treatment of drug-resistant bacterial infections attributed to the overuse of antibiotics still remains a serious challenge globally. Herein, zwitterionic charge switchable meso-silica/polypeptide hybrid nanoparticles (MSPNs) were prepared for the synergistic chemo-photodynamic therapy in the treatment of drug-resistant bacterial infections. Subsequently, azithromycin (AZT) and methylene blue (MB) were loaded in the MSPNs to form the combined chemo-photodynamic therapeutic nanoparticles (MSPNs-AZT/MB) for the treatment of methicillin-resistant Staphylococcus aureus (MRSA). Remarkably, the as-prepared MSPNs-AZT/MB exhibited a negative surface charge of -5.2 mV at physiological pH while switching into positive surface charge of 24.7 mv in an acidic environment, leading to enhanced binding with bacterial surface. The lipase-triggered AZT release up to 77.9 % was achieved, and the loaded MB demonstrated efficient singlet oxygen (1O2) generation for photodynamic therapy. The in vitro experimental results displayed an excellent antibacterial effect against MRSA in both planktonic and biofilm phenotypes. Additionally, the as-prepared MSPNs-AZT/MB exhibited synergistic and enhanced antibacterial infection effect up to 94 % comparing to monotherapy in a mice model. Considering the above advantages, the as-prepared combined chemo-photodynamic therapeutic nanoparticles showed promising biocompatibility and clinical potential for the efficient therapy of drug-resistant bacteria.

Keywords: Antibacteria; Chemo-photodynamic combined therapy; Nanocomposites.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / pharmacology
  • Anti-Bacterial Agents / therapeutic use
  • Azithromycin / pharmacology
  • Azithromycin / therapeutic use
  • Lipase / pharmacology
  • Methicillin-Resistant Staphylococcus aureus*
  • Methylene Blue / pharmacology
  • Mice
  • Microbial Sensitivity Tests
  • Nanoparticles*
  • Peptides / pharmacology
  • Peptides / therapeutic use
  • Photochemotherapy* / methods
  • Photosensitizing Agents / pharmacology
  • Photosensitizing Agents / therapeutic use
  • Silicon Dioxide / pharmacology
  • Singlet Oxygen
  • Staphylococcal Infections* / drug therapy

Substances

  • Anti-Bacterial Agents
  • Peptides
  • Photosensitizing Agents
  • Singlet Oxygen
  • Silicon Dioxide
  • Azithromycin
  • Lipase
  • Methylene Blue