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Preparation of Binary and Ternary Deep Eutectic Systems
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Boosting antibiotics performance by new formulations with deep eutectic solvents.

Sónia N Pedro1, Ana T P C Gomes2, Párástu Oskoei2

  • 1CICECO-Aveiro Institute of Materials, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.

International Journal of Pharmaceutics
|February 13, 2022
PubMed
Summary
This summary is machine-generated.

Deep eutectic solvents (DES) significantly boost antibiotic solubility, stability, and effectiveness against resistant bacteria. These novel DES formulations also reduce antibiotic toxicity, offering a promising approach to combat antimicrobial resistance.

Keywords:
AntibioticsCiprofloxacinDeep eutectic solventsSolubilityStabilityTherapeutic efficacy

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Area of Science:

  • Pharmaceutical Science
  • Drug Delivery
  • Antimicrobial Research

Background:

  • Antimicrobial resistance (AMR) necessitates novel therapeutic strategies.
  • Conventional antibiotic formulations face limitations in solubility, stability, and efficacy, particularly against resistant strains.

Purpose of the Study:

  • To investigate the potential of deep eutectic solvents (DES) in enhancing antibiotic properties.
  • To evaluate the impact of DES formulations on the solubility, stability, and therapeutic efficacy of ciprofloxacin.
  • To assess the effect of DES on antibiotic toxicity.

Main Methods:

  • Formulation of ciprofloxacin with aqueous deep eutectic solvents (DES).
  • Assessment of ciprofloxacin solubility and stability in DES solutions.
  • Evaluation of bacterial susceptibility and therapeutic efficacy against Gram-negative and Gram-positive bacteria.
  • In vitro toxicity testing on HaCat cells.

Main Results:

  • DES aqueous solutions increased ciprofloxacin solubility by up to 430-fold and enhanced its stability.
  • Formulations improved bacterial susceptibility (2-4 fold) to ciprofloxacin, including resistant strains.
  • Therapeutic efficacy was enhanced at sub-inhibitory concentrations without inducing tolerance.
  • DES incorporation reduced ciprofloxacin's toxicity to HaCat cells.

Conclusions:

  • Deep eutectic solvents represent a pioneering approach for developing advanced fluoroquinolone formulations.
  • DES significantly improve antibiotic solubility, stability, and efficacy while reducing toxicity.
  • This strategy offers a promising avenue for overcoming antimicrobial resistance.