Antifungal Activity of Amphotericin B Cochleates against
            <i>Candida albicans</i>
            Infection in a Mouse Model

Zarif, Leila; Graybill, John R.; Perlin, David S.; Najvar, Laura K.; Bocanegra, Rosie; Mannino, Raphael J.

doi:10.1128/aac.44.6.1463-1469.2000

Cited by 111 publications

(80 citation statements)

References 16 publications

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“…Our prepared liposomal LipoB and LipoI have equivalent antifungal activity in vivo of AmBisome. Present data are in line with report of Zarif et al (2000) which the author have shown AmBisome is highly effective in treating murine candidiasis in kidney.…”

Section: Effect On Target Organs Of Liposomal Amphotericin Bsupporting

confidence: 80%

Development and Evaluation of Antifungal in vivo of Liposomal Amphotericin B

Minh¹,

Thanh²,

Tuan³

et al. 2015

International J. of Biological Chemistry

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Amphotericin B is a polyene antifungal drug used intravenously for systemic fungal infections. It has severe and potentially lethal side effects, therefore, it has been limited use in clinical. Liposomes are widely used as vehicles to target organ in pharmaceutical technology due to their ability to improve the delivery of drugs, increasing therapeutic efficacy and decreasing toxicity. The aim of this study is to prepare a liposomal amphotericin B by hydration of a thin lipid film and ethanol-injection methods and evaluate its antifungal activity in vivo. Prepared liposomal amphotericin B by both methods has particle size smaller than 150 nm, quite homogeneous and the entrapment drug was greater than 90%. The antifungal activity of liposomal amphotericin B was studied on three strains Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus fungal infection in mice models. Our results have shown that liposomal amphotericin B prepared by both methods have strong effect to prolong the survival in the infected mice and significantly reduced the Colony Forming Units (CFU) in target organ with similar effect of AmBisome.

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Section: Effect On Target Organs Of Liposomal Amphotericin Bsupporting

confidence: 80%

Development and Evaluation of Antifungal in vivo of Liposomal Amphotericin B

Minh¹,

Thanh²,

Tuan³

et al. 2015

International J. of Biological Chemistry

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show abstract

“…A number of strategies such as polymeric and peptide hydrogels, nanoparticles, microemulsion, liposomes, niosomes, or ethosomes that can function as drug depots for delivering the antifungals at the site of infections have been reported. [15][16][17][18][19][20] However, these formulations need to be applied frequently to maintain sustained release of the drugs. 21 Nonwoven fiber mats produced by electrospinning have the potential for a wide range of applications such as filters, composites, drug carriers, wound dressing, and tissue regeneration.…”

Section: Introductionmentioning

confidence: 99%

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

Lakshminarayanan

Sridhar

Loh

et al. 2014

IJN

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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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“…In particular, complete clearance of the organism from the lungs was observed at 2.5 mg/kg/day of oral AmB cochleates (Santangelo et al, 2000). The high efficacy and low toxicity of AmB cochleates can be explained by direct fusion between the outer lipid layer of cochleates and the fungal cell membrane, but it is not known whether cochleates are absorbed and enter the circulation as intact particles (Zarif et al, 2000). In February 2009, AmB-loaded cochleates developed by the University of British Columbia (licensed to BioDelivery Sciences International, Raleigh, NC) gave a favorable outcome after oral administration in a Phase I trial, with a positive therapeutic effect equivalent to IV therapy (Thornton & Wasan, 2009).…”

Section: Cochleatesmentioning

confidence: 99%

Design of amphotericin B oral formulation for antifungal therapy

2017

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Amphotericin B (AmB) remains the ''gold standard'' for systemic antifungal therapy, even though new drugs are emerging as the attractive antifungal agents. Since AmB has negligible oral absorption as a consequence of its unfavorable physicochemical characterizations, its use is restricted to parenteral administration which is accompanied by severe side effects. As greater understanding of the gastrointestinal tract has developed, the advanced drug delivery systems are emerging with the potential to overcome the barriers of AmB oral delivery. Much research has demonstrated that oral AmB formulations such as lipid formulations may have beneficial therapeutic efficacy with reduced adverse effects and suitable for clinical application. Here we reviewed the different formulation strategies to enhance oral drug efficacy, and discussed the current trends and future perspectives for AmB oral administration in the treatment of antifungal infections.

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Antifungal Activity of Amphotericin B Cochleates against Candida albicans Infection in a Mouse Model

Cited by 111 publications

References 16 publications

Development and Evaluation of Antifungal in vivo of Liposomal Amphotericin B

Development and Evaluation of Antifungal in vivo of Liposomal Amphotericin B

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

Design of amphotericin B oral formulation for antifungal therapy

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