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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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Mechanical properties of glutaraldehyde vapor crosslinked gelatin nanofibers with and without drug loading. The gelatin fiber mat was crosslinked with glutaraldehyde for 48 hours. For amphotericin B- and natamycin-loaded gelatin fiber mats 3-hour glutaraldehyde crosslinking was used.Abbreviation: AmpB, amphotericin B.
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f11-ijn-9-2439: Mechanical properties of glutaraldehyde vapor crosslinked gelatin nanofibers with and without drug loading. The gelatin fiber mat was crosslinked with glutaraldehyde for 48 hours. For amphotericin B- and natamycin-loaded gelatin fiber mats 3-hour glutaraldehyde crosslinking was used.Abbreviation: AmpB, amphotericin B.

Mentions: The mechanical properties of polyene-loaded fiber mats were evaluated (Figure 11) and compared with uncrosslinked and crosslinked gelatin mats (Table 2). Mechanical strength measurements showed a slight increase in Young’s modulus of antifungal-loaded gelatin compared to uncrosslinked gelatin. For natamycin-loaded fiber mats, the ultimate tensile stress and the ultimate tensile strain decreased compared to uncrosslinked gelatin fiber mats. However, amphotericin B-loaded fiber mats had improved tensile strain, although a slight decrease in the ultimate tensile stress was observed compared to the uncrosslinked gelatin fiber mats. When compared to crosslinked gelatin fibers, the antifungal-loaded fibers had improved elasticity, an important requirement for wound dressing.33


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)

Mechanical properties of glutaraldehyde vapor crosslinked gelatin nanofibers with and without drug loading. The gelatin fiber mat was crosslinked with glutaraldehyde for 48 hours. For amphotericin B- and natamycin-loaded gelatin fiber mats 3-hour glutaraldehyde crosslinking was used.Abbreviation: AmpB, amphotericin B.
© Copyright Policy
Related In: Results  -  Collection

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

f11-ijn-9-2439: Mechanical properties of glutaraldehyde vapor crosslinked gelatin nanofibers with and without drug loading. The gelatin fiber mat was crosslinked with glutaraldehyde for 48 hours. For amphotericin B- and natamycin-loaded gelatin fiber mats 3-hour glutaraldehyde crosslinking was used.Abbreviation: AmpB, amphotericin B.
Mentions: The mechanical properties of polyene-loaded fiber mats were evaluated (Figure 11) and compared with uncrosslinked and crosslinked gelatin mats (Table 2). Mechanical strength measurements showed a slight increase in Young’s modulus of antifungal-loaded gelatin compared to uncrosslinked gelatin. For natamycin-loaded fiber mats, the ultimate tensile stress and the ultimate tensile strain decreased compared to uncrosslinked gelatin fiber mats. However, amphotericin B-loaded fiber mats had improved tensile strain, although a slight decrease in the ultimate tensile stress was observed compared to the uncrosslinked gelatin fiber mats. When compared to crosslinked gelatin fibers, the antifungal-loaded fibers had improved elasticity, an important requirement for wound dressing.33

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