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Molecules 2018, 23(3), 596; https://doi.org/10.3390/molecules23030596

Antibacterial and Antifungal Activities of Poloxamer Micelles Containing Ceragenin CSA-131 on Ciliated Tissues

1
Department of Chemistry and Biochemistry, Brigham Young University, C100 BNSN, Provo, UT 84602, USA
2
N8 Medical, Dublin, OH 43017, USA
*
Author to whom correspondence should be addressed.
Received: 5 February 2018 / Revised: 25 February 2018 / Accepted: 2 March 2018 / Published: 7 March 2018
(This article belongs to the Special Issue Antimicrobial Peptides and Peptidomimetics)
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Abstract

Ceragenins were designed as non-peptide mimics of endogenous antimicrobial peptides, and they display broad-spectrum antibacterial and antifungal activities, including the ability to eradicate established biofilms. These features of ceragenins make them attractive potential therapeutics for persistent infections in the lung, including those associated with cystic fibrosis. A characteristic of an optimal therapeutic for use in the lungs and trachea is the exertion of potent antimicrobial activities without damaging the cilia that play a critical role in these tissues. In previous work, potent antimicrobial activities of ceragenin CSA-131 have been reported; however, we found in ex vivo studies that this ceragenin, at concentrations necessary to eradicate established biofilms, also causes loss of cilia function. By formulating CSA-131 in poloxamer micelles, cilia damage was eliminated and antimicrobial activity was unaffected. The ability of CSA-131, formulated with a poloxamer, to reduce the populations of fungal pathogens in tracheal and lung tissue was also observed in ex vivo studies. These findings suggest that CSA-131, formulated in micelles, may act as a potential therapeutic for polymicrobial and biofilm-related infections in the lung and trachea. View Full-Text
Keywords: ceragenin; cilia; poloxamer; micelles; biofilm; antibacterial activity; antifungal activity ceragenin; cilia; poloxamer; micelles; biofilm; antibacterial activity; antifungal activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Hashemi, M.M.; Holden, B.S.; Taylor, M.F.; Wilson, J.; Coburn, J.; Hilton, B.; Nance, T.; Gubler, S.; Genberg, C.; Deng, S.; Savage, P.B. Antibacterial and Antifungal Activities of Poloxamer Micelles Containing Ceragenin CSA-131 on Ciliated Tissues. Molecules 2018, 23, 596.

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