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Self-assembly behavior of colistin and its prodrug colistin methanesulfonate : implications for solution stability and solubilization

Wallace, Stephanie J., Li, Jian, Nation, Roger L., Prankerd, Richard J., Velkov, Tony and Boyd, Ben J. 2010, Self-assembly behavior of colistin and its prodrug colistin methanesulfonate : implications for solution stability and solubilization, Journal of physical chemistry B, vol. 114, no. 14, pp. 4836-4840, doi: 10.1021/jp100458x.

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Title Self-assembly behavior of colistin and its prodrug colistin methanesulfonate : implications for solution stability and solubilization
Author(s) Wallace, Stephanie J.
Li, Jian
Nation, Roger L.
Prankerd, Richard J.
Velkov, Tony
Boyd, Ben J.
Journal name Journal of physical chemistry B
Volume number 114
Issue number 14
Start page 4836
End page 4840
Publisher American chemical society
Place of publication Washington, D.C.
Publication date 2010
ISSN 1520-6106
1520-5207
Summary 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.
Language eng
DOI 10.1021/jp100458x
Field of Research 111599 Pharmacology and Pharmaceutical Sciences not elsewhere classified
Socio Economic Objective 970111 Expanding Knowledge in the Medical and Health Sciences
HERDC Research category C1.1 Refereed article in a scholarly journal
Copyright notice ©2010, American Chemical Society
Persistent URL http://hdl.handle.net/10536/DRO/DU:30041035

Document type: Journal Article
Collection: School of Medicine
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Created: Tue, 13 Dec 2011, 14:17:21 EST by Leanne Swaneveld

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