Water-soluble amphotericin B–polyvinylpyrrolidone complexes with maintained antifungal activity against Candida spp. and Aspergillus spp. and reduced haemolytic and cytotoxic effects

Charvalos, Ekatherina; Tzatzarakis, Manolis; Bambeke, Françoise Van; Tulkens, Paul M.; Tsatsakis, Aristidis; Tzanakakis, George N.; Mingeot‐Leclercq, Marie‐Paule

doi:10.1093/jac/dki455

Cited by 53 publications

(37 citation statements)

References 47 publications

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“…52,53 On the other hand, polyvinylpyrrolidone has been shown to complex AmB, but suffers from very low (0.249% w/w) AmB loading. 54 Polymeric micelle systems have also been developed; however, encapsulation in the polymeric micelles decreased the in vitro antifungal activity of the drug. 40 Moreover, these micelles have been shown to be unstable in the presence of serum due to disruption of their integrity, 55 resulting in rapid and near-complete release of core-loaded molecules from circulating micelles in an uncontrolled fashion.…”

Section: Resultsmentioning

confidence: 99%

Self-assembled amphotericin B-loaded polyglutamic acid nanoparticles: preparation, characterization and in vitro potential against Candida albicans

Zia¹,

Khan²,

Zubair³

et al. 2015

IJN

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In the present study, we developed a self-assembled biodegradable polyglutamic acid (PGA)-based formulation of amphotericin B (AmB) and evaluated its in vitro antifungal potential against Candida albicans . The AmB-loaded PGA nanoparticles were prepared in-house and had a mean size dimension of around 98±2 nm with a zeta potential of −35.2±7.3 mV. Spectroscopic studies revealed that the drug predominantly acquires an aggregated form inside the formulation with an aggregation ratio above 2. The PGA-based AmB formulation was shown to be highly stable in phosphate-buffered saline as well as in serum (only 10%–20% of the drug was released after 10 days). The AmB–PGA nanoparticles were less toxic to red blood cells (<15% lysis at an AmB concentration of 100 μg/mL after 24 hours) when compared with Fungizone ® , a commercial antifungal product. An MTT assay showed that the viability of mammalian cells (KB and RAW 264.7) was negligibly affected at AmB concentrations as high as 200 μg/mL. Histopathological examination of mouse kidney revealed no signs of tissue necrosis. The AmB–PGA formulation showed potent antimicrobial activity similar to that of Fungizone against C. albicans . Interestingly, AmB-bearing PGA nanoparticles were found to inhibit biofilm formation to a considerable extent. In summary, AmB–PGA nanoparticles showed highly attenuated toxicity when compared with Fungizone, while retaining equivalent active antifungal properties. This study indicates that the AmB–PGA preparation could be a promising treatment for various fungal infections.

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Section: Resultsmentioning

confidence: 99%

Self-assembled amphotericin B-loaded polyglutamic acid nanoparticles: preparation, characterization and in vitro potential against Candida albicans

Zia¹,

Khan²,

Zubair³

et al. 2015

IJN

View full text Add to dashboard Cite

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“…and reduced the haemolytic and cytotoxic effects of AmB. 81 The most important inconvenience of this formulation is the high amount of polyvinylpirrolidone required to obtain the complexes, about 2 g per 5 mg of AmB. Another inconvenience is the use of methanol to prepare the complexes, about 100 mL per 5 mg of AmB.…”

Section: Non-commercialized Amb Formulationsmentioning

confidence: 99%

Amphotericin B Formulations and Drug Targeting

Torrado

Espada

Ballesteros

et al. 2008

Journal of Pharmaceutical Sciences

254

236

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“…These conjugates were found to be more effective than both liposomal and deoxycholate formulations in eradicating yeast cells from target organs and were also effective and safe against leishmanial parasite infections. AmB has been covalently conjugated to ergosterol (16), and poly(vinyl pyrrolidone) (17) and the resulting conjugates were found to be biologically active.…”

Section: Introductionmentioning

confidence: 99%

Amphotericin B-Gum Arabic Conjugates: Synthesis, Toxicity, Bioavailability, and Activities Against Leishmania and Fungi

et al. 2007

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The drug conjugates were stable, non-hemolytic and non-toxic to the internal organs of the animal and showed good anti-fungal and anti-leishmanial activity in vitro. In spite of the large molecular weight of the polysaccharide, AmB from the conjugates showed bioavailability after i.v injection. Since the highest concentration of AmB was found in the spleen after a single injection, these conjugates may have potential in anti-leishmanial therapy.

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Water-soluble amphotericin B–polyvinylpyrrolidone complexes with maintained antifungal activity against Candida spp. and Aspergillus spp. and reduced haemolytic and cytotoxic effects

Abstract: AmB-PVP complexes compared favourably with AmB for antifungal activity, were less haemolytic and cytotoxic than AmB, and show a similar cytotoxicity profile to AmBisome.

Cited by 53 publications

References 47 publications

Self-assembled amphotericin B-loaded polyglutamic acid nanoparticles: preparation, characterization and in vitro potential against Candida albicans

Self-assembled amphotericin B-loaded polyglutamic acid nanoparticles: preparation, characterization and in vitro potential against Candida albicans

Amphotericin B Formulations and Drug Targeting

Amphotericin B-Gum Arabic Conjugates: Synthesis, Toxicity, Bioavailability, and Activities Against Leishmania and Fungi

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