Comparative in vitro Antifungal Activity of Amphotericin B Lipid Complex, Amphotericin B and Fluconazole

Chemotherapy ◽  
2000 ◽  
Vol 46 (4) ◽  
pp. 235-244 ◽  
Author(s):  
Alfonso-Javier Carrillo-Muñoz ◽  
Guillermo Quindós ◽  
Cristina Tur ◽  
Maite Ruesga ◽  
Rocío Alonso ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
Lipid Complex ◽  
Amphotericin B Lipid Complex ◽  
In Vitro Antifungal Activity

scholarly journals In Vitro and In Vivo Antifungal Activity of Amphotericin B Lipid Complex: Are Phospholipases Important?

1998 ◽  
Vol 42 (4) ◽  
pp. 767-771 ◽  
Author(s):  
Christine E. Swenson ◽  
Walter R. Perkins ◽  
Patricia Roberts ◽  
Imran Ahmad ◽  
Rachel Stevens ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
Vascular Tissue ◽  
Therapeutic Index ◽  
Test Material ◽  
Lipid Complex ◽  
In Vitro Susceptibility ◽  
Amphotericin B Lipid Complex

ABSTRACT Amphotericin B lipid complex for injection (ABLC) is a suspension of amphotericin B complexed with the lipidsl-α-dimyristoylphosphatidylcholine (DMPC) andl-α-dimyristoylphosphatidylglycerol. ABLC is less toxic than amphotericin B deoxycholate (AmB-d), while it maintains the antifungal activity of AmB-d. Active amphotericin B can be released from ABLC by exogenously added (snake venom, bacteria, orCandida-derived) phospholipases or by phospholipases derived from activated mammalian vascular tissue (rat arteries). Such extracellular phospholipases are capable of hydrolyzing the major lipid in ABLC. Mutants of C. albicans that were resistant to ABLC but not AmB-d in vitro were deficient in extracellular phospholipase activity, as measured on egg yolk agar or as measured by their ability to hydrolyze DMPC in ABLC. ABLC was nevertheless effective in the treatment of experimental murine infections produced by these mutants. Isolates of Aspergillus species, apparently resistant to ABLC in vitro (but susceptible to AmB-d), were also susceptible to ABLC in vivo. We suggest that routine in vitro susceptibility tests with ABLC itself as the test material may not accurately predict the in vivo activity of ABLC and that the enhanced therapeutic index of ABLC relative to that of AmB-d in vivo may be due, in part, to the selective release of active amphotericin B from the complex at sites of fungal infection through the action of fungal or host cell-derived phospholipases.

scholarly journals Antifungal Activity of Flocculosin, a Novel Glycolipid Isolated from Pseudozyma flocculosa

2005 ◽  
Vol 49 (4) ◽  
pp. 1597-1599 ◽  
Author(s):  
Benjamin Mimee ◽  
Caroline Labbé ◽  
René Pelletier ◽  
Richard R. Bélanger
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
Cell Lines ◽  
Human Cell ◽  
Synergistic Activity ◽  
Human Cell Lines ◽  
Antifungal Properties ◽  
Pseudozyma Flocculosa ◽  
In Vitro Antifungal Activity

ABSTRACT Flocculosin, a glycolipid isolated from the yeast-like fungus Pseudozyma flocculosa, was investigated for in vitro antifungal activity. The compound displayed antifungal properties against several pathogenic yeasts. Synergistic activity was observed between flocculosin and amphotericin B, and no significant cytotoxicity was demonstrated when tested against human cell lines.

Amphotericin B in Lipid Emulsion: Stability, Compatibility, and In Vitro Antifungal Activity

1998 ◽  
Vol 42 (4) ◽  
pp. 762-766 ◽  
Author(s):  
Scott Walker ◽  
Sandra A. N. Tailor ◽  
Mark Lee ◽  
Lisa Louie ◽  
Marie Louie ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
Clinical Laboratory ◽  
National Committee ◽  
Compatibility Study ◽  
The Stability ◽  
Few Data ◽  
Reference Strains ◽  
In Vitro Antifungal Activity

ABSTRACT Newer formulations of amphotericin B (AmB) complexed with liposomes or lipid suspensions have been developed. Preliminary studies have suggested that AmB in Intralipid (IL) may be as effective as, but less toxic than, conventional formulations of AmB, but few data are available regarding its stability, compatibility, or in vitro antifungal activity. A compatibility study was done to evaluate the effects of AmB concentrations in IL containing either 10 or 20% soybean oil. The effects of temperature, shaking, and AmB and IL concentrations on the stability of AmB-IL suspensions were analyzed by visual inspection and liquid chromatography. The in vitro antifungal activity of AmB-IL, compared to that of AmB alone against reference strains of Candida species was determined by using a broth macrodilution method in accordance with National Committee for Clinical Laboratory Standards guidelines (M27-T). Samples of AmB-IL which were lightly shaken retained more than 90% of the AmB concentration over 21 days when stored at either 4 or 23°C. Varying the AmB concentration did not appear to affect the stability of AmB-IL. However, a precipitate was formed when mixtures with more than 30% lipid as a proportion of the total volume were centrifuged. AmB-IL and AmB alone had similar in vitro antifungal activities against reference strains of yeasts. Further pharmacologic and clinical studies with AmB-IL are warranted, although AmB should not be combined with IL in concentrations capable of producing a precipitate.

scholarly journals Pharmacokinetics and Pharmacodynamics of Amphotericin B Deoxycholate, Liposomal Amphotericin B, and Amphotericin B Lipid Complex in an In Vitro Model of Invasive Pulmonary Aspergillosis

2010 ◽  
Vol 54 (8) ◽  
pp. 3432-3441 ◽  
Author(s):  
Jodi M. Lestner ◽  
Susan J. Howard ◽  
Joanne Goodwin ◽  
Lea Gregson ◽  
Jayesh Majithiya ◽  
...  
Keyword(s):  
Confocal Microscopy ◽  
Amphotericin B ◽  
Liposomal Amphotericin ◽  
Invasive Pulmonary Aspergillosis ◽  
Host Cells ◽  
Pulmonary Aspergillosis ◽  
Lipid Complex ◽  
Amphotericin B Deoxycholate ◽  
Amphotericin B Lipid Complex

ABSTRACT The pharmacodynamic and pharmacokinetic (PK-PD) properties of amphotericin B (AmB) formulations against invasive pulmonary aspergillosis (IPA) are not well understood. We used an in vitro model of IPA to further elucidate the PK-PD of amphotericin B deoxycholate (DAmB), liposomal amphotericin B (LAmB) and amphotericin B lipid complex (ABLC). The pharmacokinetics of these formulations for endovascular fluid, endothelial cells, and alveolar cells were estimated. Pharmacodynamic relationships were defined by measuring concentrations of galactomannan in endovascular and alveolar compartments. Confocal microscopy was used to visualize fungal biomass. A mathematical model was used to calculate the area under the concentration-time curve (AUC) in each compartment and estimate the extent of drug penetration. The interaction of LAmB with host cells and hyphae was visualized using sulforhodamine B-labeled liposomes. The MICs for the pure compound and the three formulations were comparable (0.125 to 0.25 mg/liter). For all formulations, concentrations of AmB progressively declined in the endovascular fluid as the drug distributed into the cellular bilayer. Depending on the formulation, the AUCs for AmB were 10 to 300 times higher within the cells than within endovascular fluid. The concentrations producing a 50% maximal effect (EC50) in the endovascular compartment were 0.12, 1.03, and 4.41 mg/liter for DAmB, LAmB, and ABLC, respectively, whereas, the EC50 in the alveolar compartment were 0.17, 7.76, and 39.34 mg/liter, respectively. Confocal microscopy suggested that liposomes interacted directly with hyphae and host cells. The PK-PD relationships of the three most widely used formulations of AmB differ markedly within an in vitro lung model of IPA.

Comparison of the in vitro antifungal activity of free and liposome-encapsulated amphotericin B

1991 ◽  
Vol 10 (8) ◽  
pp. 665-668 ◽  
Author(s):  
E. Anaissie ◽  
V. Paetznick ◽  
R. Proffitt ◽  
J. Adler-Moore ◽  
G. P. Bodey
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
In Vitro Antifungal Activity

In vitro antifungal activity of amphotericin B and 11 comparators against Aspergillus terreus species complex

Mycoses ◽  
2017 ◽  
Vol 61 (2) ◽  
pp. 134-142 ◽  
Author(s):  
Afsane Vaezi ◽  
Hamed Fakhim ◽  
Amir Arastehfar ◽  
Tahereh Shokohi ◽  
Mohammad T. Hedayati ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
Species Complex ◽  
Aspergillus Terreus ◽  
In Vitro Antifungal Activity

scholarly journals Antifungal Activity of Amphotericin B, Fluconazole, and Voriconazole in an In Vitro Model of Candida Catheter-Related Bloodstream Infection

2002 ◽  
Vol 46 (11) ◽  
pp. 3499-3505 ◽  
Author(s):  
Russell E. Lewis ◽  
Dimitrios P. Kontoyiannis ◽  
Rabih O. Darouiche ◽  
Issam I. Raad ◽  
Randall A. Prince
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
Venous Catheter ◽  
Central Venous Catheters ◽  
Pharmacodynamic Model ◽  
Central Venous ◽  
Single Lumen ◽  
Vitro Model ◽  
In Vitro Antifungal Activity

ABSTRACT The activity of five simulated antifungal regimens for eradication of catheter-related bloodstream Candida infection was evaluated with an in vitro pharmacodynamic model. Single-lumen central venous catheters were colonized with Candida species by sequentially incubating central venous catheters in plasma and then in growth medium (RPMI plus morpholinepropanesulfonic acid) containing a standardized suspension (105 CFU/ml) of Candida albicans, Candida glabrata, or slime-producing Candida parapsilosis. Colonized central venous catheters were then placed in a one-compartment pharmacodynamic model where five antifungal regimens (plus control) were simulated: amphotericin B, 1.0 mg/kg every 24 h; amphotericin B, 0.5 mg/kg every 24 h; fluconazole, 400 mg every 24 h; fluconazole, 800 mg every 24 h; and voriconazole, 4 mg/kg every 12 h. During exposure to the simulated clinical regimens, samples were serially removed from the model over 48 h for quantitation of viable organisms. All antifungal regimens suppressed fungal counts by both peripheral and catheter sampling versus control (P = 0.001). Overall, antifungal activity ranked amphotericin B (1 mg/kg) > amphotericin B (0.5 mg/kg) ≥ voriconazole > fluconazole (800 mg) ≥ fluconazole (400 mg). No regimen, however, completely eradicated (by culture and electron microscopy) central venous catheter colonization. Regrowth was noted in the model during therapy against C. glabrata and C. parapsilosis but was not associated with an increase in the MICs for the isolates. Lack of in vitro antifungal activity against biofilm-encased organisms appeared to be the primary reason for mycological failure of antifungal regimens in the model.

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