Incorporation of Amphotericin B Into Self-Assembled Hydrophobized Kollicoat IR Nanoparticles

Kollicoat IR (KOL) is a new poly(ethylene glycol)-poly(vinyl alcohol) graft copolymer that is a promising material for medical applications because of its biocompatibility and hydrophilic nature. Amphotericin B (AmB) is a broad-spectrum fungicidal antibiotic used primarily in the treatment of life-t...

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Bibliographic Details
Published in:Journal of drug delivery science and technology 2013-01, Vol.23 (6), p.591-596
Main Authors: Yamamoto, S., Kaneo, Y., Ishizu, T., Yamaguchi, Y., Haraguchi, H.
Format: Article
Language:English
Subjects:
Amphotericin B
Antimicrobial activities
Biodisposition
Hemolysis
Kollicoat IR
Nanoparticle
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Summary:Kollicoat IR (KOL) is a new poly(ethylene glycol)-poly(vinyl alcohol) graft copolymer that is a promising material for medical applications because of its biocompatibility and hydrophilic nature. Amphotericin B (AmB) is a broad-spectrum fungicidal antibiotic used primarily in the treatment of life-threatening systemic fungal infections. However, AmB is limited in clinical use because of its poor water solubility. In this study, we synthesized AmB-loaded hydrophobized KOL nanoparticles for the first time. These self-assembled, stable nanoparticles exhibited a high AmB content. Among the hydrophobized KOL nanoparticles, a cholesterol-grafted KOL nanoparticle reduced AmB toxicity with respect to hemolysis and effectively increased the overall water solubility of AmB. Furthermore, a relatively high retention of AmB in the plasma was demonstrated in vivo in an animal experiment at early time after injection, suggesting that the cholesterol-grafted KOL nanoparticles could enable new pharmaceutical applications for AmB.
ISSN:1773-2247
DOI:10.1016/S1773-2247(13)50090-6