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      Lipid Formulations of Polyene Antifungal Drugs and Attenuation of Associated Nephrotoxicity

      a,b , c , d , b


      S. Karger AG

      Lipid formulations, Nephrotoxicity, Amphotericin B

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          Amphotericin B is an effective broad-spectrum antifungal agent, but various side effects, especially nephrotoxicity, have restricted its use. Recently, lipid formulations of amphotericin B have been developed in order to reduce its toxic side effects. Clinical trials, although in the early stages, suggest promising results, and that some of these lipid formulations are potent and less toxic, even at higher doses. We summarize herein the existing information about newer lipid formulations of polyene antifungal drugs, which could attenuate associated nephrotoxicity.

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          Most cited references 1

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          Antifungal activity of amphotericin B cochleates against Candida albicans infection in a mouse model.

           L Zarif,  D Perlin,  R Mannino (2000)
          Cochleates are lipid-based supramolecular assemblies composed of natural products, negatively charged phospholipid, and a divalent cation. Cochleates can encapsulate amphotericin B (AmB), an important antifungal drug. AmB cochleates (CAMB) have a unique shape and the ability to target AmB to fungi. The minimal inhibitory concentration and the minimum lethal concentration against Candida albicans are similar to that for desoxycholate AmB (DAMB; Fungizone). In vitro, CAMB induced no hemolysis of human red blood cells at concentrations of as high as 500 microg of AmB/ml, and DAMB was highly hemolytic at 10 microg of AmB/ml. CAMB protect ICR mice infected with C. albicans when the agent is administered intraperitoneally at doses of as low as 0.1 mg/kg/day. In a tissue burden study, CAMB, DAMB, and AmBisome (liposomal AmB; LAMB) were effective in the kidneys, but in the spleen CAMB was more potent than DAMB at 1 mg/kg/day and was equivalent to LAMB at 10 mg/kg/day. In summary, CAMB are highly effective in treating murine candidiasis and compare well with AmBisome and AmB.

            Author and article information

            S. Karger AG
            10 October 2001
            : 89
            : 3
            : 251-254
            aDepartment of Oral Medicine and Diagnostic Sciences, Harvard School of Dental Medicine, Boston, Mass., USA; bSecond Department of Pathology, Nagasaki University School of Medicine, Nagasaki, Japan; cCenter for Medical Mycology, Department of Dermatology, Case Western Reserve University, Cleveland, Ohio, USA and dDepartment of Medicine, Penn State College of Medicine, Hershey, Pa., USA
            46081 Nephron 2001;89:251–254
            © 2001 S. Karger AG, Basel

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            Page count
            References: 21, Pages: 4
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            Short Review

            Cardiovascular Medicine, Nephrology

            Amphotericin B, Lipid formulations, Nephrotoxicity


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