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Updated: Jun 14, 2026

Synthesis and Characterization of Supramolecular Colloids
Published on: April 22, 2016
Self-assembly behavior of colistin and its prodrug colistin methanesulfonate: implications for solution stability and
Stephanie J Wallace1, Jian Li, Roger L Nation
1Facility for Anti-Infective Drug Development and Innovation, Monash Institute of Pharmaceutical Sciences, Parkville, Melbourne, Victoria 3052, Australia.
Abstract:
Colistin is an amphiphilic antibiotic that has re-emerged into clinical use due to the increasing prevalence of difficult-to-treat Gram-negative infections. The existence of self-assembling colloids in solutions of colistin and its derivative prodrug, colistin methanesulfonate (CMS), was investigated. Colistin and CMS reduced the air-water interfacial tension, and dynamic light scattering (DLS) studies showed the existence of 2.07 +/- 0.3 nm aggregates above 1.5 mM for colistin and of 1.98 +/- 0.36 nm aggregates for CMS above 3.5 mM (mean +/- SD). Above the respective critical micelle concentrations (CMC) the solubility of azithromycin, a hydrophobic antibiotic, increased approximately linearly with increasing surfactant concentration (5:1 mol ratio colistin:azithromycin), suggestive of hydrophobic domains within the micellar cores. Rapid conversion of CMS to colistin occurred below the CMC (60% over 48 h), while conversion above the CMC was less than 1%. The formation of colistin and CMS micelles demonstrated in this study is the proposed mechanism for solubilization of azithromycin and the concentration-dependent stability of CMS.
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A solution is a homogeneous mixture composed of a solvent, the major component, and a solute, the minor component. The physical state of a solution—solid, liquid, or gas—is typically the same as that of the solvent. Solute concentrations are often described with qualitative terms such as dilute (of relatively low concentration) and concentrated (of relatively high concentration).
In a solution, the solute particles (molecules, atoms, and/or ions)...
