Nanosomal Amphotericin B is an efficacious alternative to Ambisome® for fungal therapy

Sheikh, Saifuddin; Ali, Shoukath M.; Ahmad, M. S.; Ahmad, Ateeq; Mushtaq, Mohammad; Paithankar, Mahesh; Mandal, Jayanta Kumar; Saptarishi, Dipak; Sehgal, Ashish; Maheshwari, Kirti; Ahmad, Imran

doi:10.1016/j.ijpharm.2010.07.003

Cited by 30 publications

(13 citation statements)

References 16 publications

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“…Fungizone Õ is well-known for causing hemolysis mainly due to active hemolysis by pore formation and changing electrolyte balance in erythrocytes (Yu et al, 1998;Fukui et Kumar, 2010;Shao et al, 2010;Sheikh et al, 2010;Asghari, 2011). AMB at concentrations 40.5 to 1-fold the MIC has a fungicidal activity, while AMB at concentrations50.5 to 1-fold the MIC has a fungistatic activity, a finding that has been described previously (Tasset et al, 1992;Pfaller & Barry, 1994;Risovic et al, 2003;Belkherroubi-Sari et al, 2011).…”

Section: Discussionmentioning

confidence: 99%

Oral administration of amphotericin B nanoparticles: antifungal activity, bioavailability and toxicity in rats

et al. 2017

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Amphotericin B (AMB) is used most commonly in severe systemic life-threatening fungal infections. There is currently an unmet need for an efficacious (AMB) formulation amenable to oral administration with better bioavailability and lower nephrotoxicity. Novel PEGylated polylactic-polyglycolic acid copolymer (PLGA-PEG) nanoparticles (NPs) formulations of AMB were therefore studied for their ability to kill Candida albicans (C. albicans). The antifungal activity of AMB formulations was assessed in C. albicans. Its bioavalability was investigated in nine groups of rats (n ¼ 6). Toxicity was examined by an in vitro blood hemolysis assay, and in vivo nephrotoxicity after single and multiple dosing for a week by blood urea nitrogen (BUN) and plasma creatinine (PCr) measurements. The MIC of AMB loaded to PLGA-PEG NPs against C. albicans was reduced two to threefold compared with free AMB. Novel oral AMB delivery loaded to PLGA-PEG NPs was markedly systemically available compared to Fungizone Õ in rats. The addition of 2% of GA to the AMB formulation significantly (p50.05) improved the bioavailability from 1.5 to 10.5% and the relative bioavailability was4790% that of Fungizone Õ . The novel AMB formulations showed minimal toxicity and better efficacy compared to Fungizone Õ . No nephrotoxicity in rats was detected after a week of multiple dosing of AMB NPs based on BUN and PCr, which remained at normal levels. An oral delivery system of AMB-loaded to PLGA-PEG NPs with better efficacy and minimal toxicity was formulated. The addition of glycyrrhizic acid (GA) to AMB NPs formulation resulted in a significant oral absorption and improved bioavailability in rats.

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Section: Discussionmentioning

confidence: 99%

Oral administration of amphotericin B nanoparticles: antifungal activity, bioavailability and toxicity in rats

et al. 2017

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“…The potential of liposomes and micro-emulsions as drug delivery carriers for the treatment of various topical and systemic fungal infections with several antifungal drugs such as amphotericin B, fluconazole, miconazole and griseofulvin has been proved in the literature (Peira et al, 2008;Pestana et al, 2008;Bachhav & Patravale, 2009;Monforte et al, 2010;Sheikh et al, 2010;Aggarwal & Goindi, 2012;Fauvel et al, 2012;Aggarwal et al, 2013). Topical liposomes and micro-emulsions offered several advantages as drug delivery vehicles such as enhanced skin permeation, enhanced therapeutic efficacy/bioavailability, avoidance of hepatic first pass metabolism and systemic adverse effects (Bachhav & Patravale, 2009;Sheikh et al, 2010;Aggarwal & Goindi, 2012;Aggarwal et al, 2013). Moreover, the topical delivery of antifungal drug croconazole through liposomal-based gel formulation (LBGF) or microemulsion-based gel formulation (MBGF) has not been reported yet in the literature.…”

Section: Introductionmentioning

confidence: 99%

Comparative topical delivery of antifungal drug croconazole using liposome and micro-emulsion-based gel formulations

2013

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“…However, hemolysis decreases if the solution is heated due to a change in the drug's aggregation state (Darole et al, 2008). The concentration of the liposomal formulation needs to be fifteen times higher than the conventional formulation to cause the same inflow of potassium in human blood cells, which leads to cellular damage (Sheikh et al, 2010). An in vitro study comparing the microemulsion AmB to deoxycholate AmB formulations in human blood cells demonstrated that the encapsulation significantly reduces hemolysis.…”

Section: Hematotoxicitymentioning

confidence: 99%

Difficulties in antifungal therapy with amphotericin B and the continuous search for new formulations: A literature review

Voncik¹,

Fermino²,

Cardoso³

et al. 2016

Afr. J. Pharm. Pharmacol.

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Despite advances in the research on new antifungal agents, Amphotericin B (AmB) is still considered as the antifungal of choice for treating most systemic mycoses due to its potency and broad-spectrum action. However, this drug has limited use because of its toxic effects on kidneys, liver and blood. The search for new and safe formulations of AmB is essential because of the emergence of antifungal resistance to other drugs and the increased number of immunosuppressed patients. Nanoparticles are a promising alternative towards achieving lower toxicity and improved pharmacokinetic properties. This study is a literature review of the use of AmB and the toxicity of formulations. Some of the current new formulations show some advantageous characteristics as compared to AmB. However, there is still need for a continued search for an effectively improved formulation.

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Nanosomal Amphotericin B is an efficacious alternative to Ambisome® for fungal therapy

Cited by 30 publications

References 16 publications

Oral administration of amphotericin B nanoparticles: antifungal activity, bioavailability and toxicity in rats

Oral administration of amphotericin B nanoparticles: antifungal activity, bioavailability and toxicity in rats

Comparative topical delivery of antifungal drug croconazole using liposome and micro-emulsion-based gel formulations

Difficulties in antifungal therapy with amphotericin B and the continuous search for new formulations: A literature review

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