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Development of nanovehicles for co-delivery of colistin and ArnT inhibitors

Valentina Pastore1, Jessica Frison2, Cristiano Pesce2

  • 1Department of Biology and Biotechnology "Charles Darwin", Sapienza University of Rome, Italy.

International Journal of Pharmaceutics
|March 27, 2025
PubMed

Insights

This study developed liposomes to co-deliver colistin and an ArnT inhibitor, isostevic acid, effectively restoring colistin

Area of Science:

  • Nanotechnology in Drug Delivery
  • Antimicrobial Resistance Research
  • Pharmaceutical Sciences

Background:

  • Antimicrobial resistance (AMR) is a major global health threat, particularly with pathogens like Pseudomonas aeruginosa.
  • Colistin, a last-resort antibiotic, exhibits reduced efficacy against resistant strains due to lipid A modifications.
  • In P. aeruginosa, the arn operon, specifically the ArnT enzyme, is crucial for colistin resistance.

Purpose of the Study:

  • To investigate a liposomal nanocarrier system for co-delivery of colistin and an ArnT inhibitor, isostevic acid (ISA).
  • To restore the efficacy of colistin against colistin-resistant P. aeruginosa strains.
  • To evaluate the synergistic effect of ISA as an adjuvant to colistin.

Main Methods:

  • Liposomes were designed to encapsulate colistin in the aqueous core and ISA within the lipid bilayer.
  • Formulations were optimized by varying cholesterol/egg phosphatidylcholine ratios for stable, high-efficiency encapsulation.
  • Antimicrobial activity was assessed by measuring the minimum inhibitory concentration (MIC) against resistant P. aeruginosa.

Main Results:

  • Co-loaded liposomes significantly enhanced antimicrobial activity, lowering colistin's MIC against resistant P. aeruginosa.
  • Dual-drug liposomes demonstrated bactericidal effects at lower colistin concentrations compared to the free drug.
  • Isostevic acid acted synergistically as an adjuvant, enhancing colistin's efficacy by targeting resistance mechanisms.

Conclusions:

  • Liposome-mediated co-delivery of colistin and ISA presents a promising strategy to combat colistin-resistant infections.
  • This approach can improve the clinical management of multidrug-resistant P. aeruginosa.
  • Liposomal systems offer potential for modulating drug release and overcoming bacterial resistance mechanisms.
Keywords:
Arn operonCo-deliveryColistinIsostevic acidLiposome

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