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Formulation Optimization and Stability of Polymyxin B Based on Sodium Deoxycholate Sulfate Micelles

Sunisa Kaewpaiboon1, Teerapol Srichana1

  • 1Drug Delivery System Excellence Center, Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90110, Thailand.

Journal of Pharmaceutical Sciences
|March 1, 2022
PubMed

Insights

Optimizing the ratio of Polymyxin B (PMB) and sodium deoxycholate sulfate (SDCS) created stable micelles. Lower SDCS ratios stabilized PMB, maintaining antimicrobial activity against Pseudomonas aeruginosa.

Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Biochemistry

Background:

  • Polymyxin B (PMB) is a critical antibiotic, but its stability and delivery require optimization.
  • Sodium deoxycholate sulfate (SDCS) is a bile salt with surfactant properties, potentially useful for drug formulation.

Purpose of the Study:

  • To optimize the mole ratios of PMB and SDCS for stable micelle formation.
  • To characterize the self-assembly, stability, and antimicrobial activity of PMB-SDCS formulations.

Main Methods:

  • Dynamic light scattering (DLS) for micelle size and self-assembly.
  • Fourier-transform infrared spectroscopy (FTIR) and 1H-NMR for chemical characterization.
  • Tandem mass spectrometry for chemical stability assessment.
  • Antimicrobial testing against Pseudomonas aeruginosa.

Main Results:

  • Optimized PMB-SDCS mole ratios yielded micelles with hydrodynamic diameters ranging from 193 to 318 nm.
  • FTIR confirmed hydrogen bonding between PMB and SDCS; NMR showed no significant chemical shift changes.
  • Lower SDCS:PMB ratios (e.g., 5:1) stabilized PMB, enabling release within 30 minutes and maintaining antimicrobial activity (MBC = 2 μg/ml).

Conclusions:

  • The optimized PMB-SDCS micellar system provides physical and chemical stability for Polymyxin B.
  • Specific mole ratios, particularly lower SDCS content, are crucial for effective PMB stabilization and controlled release.
  • This formulation holds promise for enhancing the therapeutic utility of Polymyxin B.
Keywords:
Antimicrobial activityMicellesPolymyxinsSodium deoxycholate sulfateStability

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