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Interaction of gelatin with polyenes modulates antifungal activity and biocompatibility of electrospun fiber mats.

Lakshminarayanan R, Sridhar R, Loh XJ, Nandhakumar M, Barathi VA, Kalaipriya M, Kwan JL, Liu SP, Beuerman RW, Ramakrishna S - Int J Nanomedicine (2014)

Bottom Line: Terbinafine-loaded mats were effective against three filamentous fungal species.Among the two azole antifungals compared, the itraconazole-loaded mat was potent against Aspergillus strains.As a result, the polyenes stabilized the triple helical conformation of gelatin and the presence of gelatin decreased the hemolytic activity of polyenes.

View Article: PubMed Central - PubMed

Affiliation: Singapore Eye Research Institute, Singapore ; Signature Research Program in Neuroscience and Behavioral Disorders, Duke-NUS Graduate Medical School, Singapore.

ABSTRACT
Topical application of antifungals does not have predictable or well-controlled release characteristics and requires reapplication to achieve therapeutic local concentration in a reasonable time period. In this article, the efficacy of five different US Food and Drug Administration-approved antifungal-loaded (amphotericin B, natamycin, terbinafine, fluconazole, and itraconazole) electrospun gelatin fiber mats were compared. Morphological studies show that incorporation of polyenes resulted in a two-fold increase in fiber diameter and the mats inhibit the growth of yeasts and filamentous fungal pathogens. Terbinafine-loaded mats were effective against three filamentous fungal species. Among the two azole antifungals compared, the itraconazole-loaded mat was potent against Aspergillus strains. However, activity loss was observed for fluconazole-loaded mats against all of the test organisms. The polyene-loaded mats displayed rapid candidacidal activities as well. Biophysical and rheological measurements indicate strong interactions between polyene antifungals and gelatin matrix. As a result, the polyenes stabilized the triple helical conformation of gelatin and the presence of gelatin decreased the hemolytic activity of polyenes. The polyene-loaded fiber mats were noncytotoxic to primary human corneal and sclera fibroblasts. The reduction of toxicity with complete retention of activity of the polyene antifungal-loaded gelatin fiber mats can provide new opportunities in the management of superficial skin infections.

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Morphology of Candida albicans grown on polyene-loaded fiber mats. Scanning electron micrographs of C. albicans treated with (A) gelatin fiber mats without antifungals; (B) amphotericin B-loaded fiber mats; and (C) natamycin-loaded fiber mats.Note: Inset scale bar =10 μm.
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f7-ijn-9-2439: Morphology of Candida albicans grown on polyene-loaded fiber mats. Scanning electron micrographs of C. albicans treated with (A) gelatin fiber mats without antifungals; (B) amphotericin B-loaded fiber mats; and (C) natamycin-loaded fiber mats.Note: Inset scale bar =10 μm.

Mentions: The changes in morphology of C. albicans incubated with polyene-loaded fiber mats were investigated by SEM. C. albicans incubated with gelatin alone had smooth and intact surfaces (Figure 7A). However, cells treated with the polyene antifungals had extensive surface deformation and leakage of some intracellular components (Figure 7B and C). The damage caused by antifungals was more noticeable in the amphotericin B-loaded fiber mats than in natamycin-loaded fiber mats. These results confirm that the polyene-loaded fiber mats retained the antifungal activity even in the presence of gelatin.


Interaction of gelatin with polyenes modulates antifungal activity and biocompatibility of electrospun fiber mats.

Lakshminarayanan R, Sridhar R, Loh XJ, Nandhakumar M, Barathi VA, Kalaipriya M, Kwan JL, Liu SP, Beuerman RW, Ramakrishna S - Int J Nanomedicine (2014)

Morphology of Candida albicans grown on polyene-loaded fiber mats. Scanning electron micrographs of C. albicans treated with (A) gelatin fiber mats without antifungals; (B) amphotericin B-loaded fiber mats; and (C) natamycin-loaded fiber mats.Note: Inset scale bar =10 μm.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4043707&req=5

f7-ijn-9-2439: Morphology of Candida albicans grown on polyene-loaded fiber mats. Scanning electron micrographs of C. albicans treated with (A) gelatin fiber mats without antifungals; (B) amphotericin B-loaded fiber mats; and (C) natamycin-loaded fiber mats.Note: Inset scale bar =10 μm.
Mentions: The changes in morphology of C. albicans incubated with polyene-loaded fiber mats were investigated by SEM. C. albicans incubated with gelatin alone had smooth and intact surfaces (Figure 7A). However, cells treated with the polyene antifungals had extensive surface deformation and leakage of some intracellular components (Figure 7B and C). The damage caused by antifungals was more noticeable in the amphotericin B-loaded fiber mats than in natamycin-loaded fiber mats. These results confirm that the polyene-loaded fiber mats retained the antifungal activity even in the presence of gelatin.

Bottom Line: Terbinafine-loaded mats were effective against three filamentous fungal species.Among the two azole antifungals compared, the itraconazole-loaded mat was potent against Aspergillus strains.As a result, the polyenes stabilized the triple helical conformation of gelatin and the presence of gelatin decreased the hemolytic activity of polyenes.

View Article: PubMed Central - PubMed

Affiliation: Singapore Eye Research Institute, Singapore ; Signature Research Program in Neuroscience and Behavioral Disorders, Duke-NUS Graduate Medical School, Singapore.

ABSTRACT
Topical application of antifungals does not have predictable or well-controlled release characteristics and requires reapplication to achieve therapeutic local concentration in a reasonable time period. In this article, the efficacy of five different US Food and Drug Administration-approved antifungal-loaded (amphotericin B, natamycin, terbinafine, fluconazole, and itraconazole) electrospun gelatin fiber mats were compared. Morphological studies show that incorporation of polyenes resulted in a two-fold increase in fiber diameter and the mats inhibit the growth of yeasts and filamentous fungal pathogens. Terbinafine-loaded mats were effective against three filamentous fungal species. Among the two azole antifungals compared, the itraconazole-loaded mat was potent against Aspergillus strains. However, activity loss was observed for fluconazole-loaded mats against all of the test organisms. The polyene-loaded mats displayed rapid candidacidal activities as well. Biophysical and rheological measurements indicate strong interactions between polyene antifungals and gelatin matrix. As a result, the polyenes stabilized the triple helical conformation of gelatin and the presence of gelatin decreased the hemolytic activity of polyenes. The polyene-loaded fiber mats were noncytotoxic to primary human corneal and sclera fibroblasts. The reduction of toxicity with complete retention of activity of the polyene antifungal-loaded gelatin fiber mats can provide new opportunities in the management of superficial skin infections.

Show MeSH
Related in: MedlinePlus