L. Zarif et al., Antifungal activity of amphotericin B cochleates against Candida albicans infection in a mouse model, ANTIM AG CH, 44(6), 2000, pp. 1463-1469
Cochleates are lipid-based supramolecular assemblies composed of natural pr
oducts, negatively charged phospholipid, and a divalent cation, Cochleates
can encapsulate amphotericin B (AmB), an important antifungal drug. AmB coc
hleates (CAMB) have a unique shape and the ability to target AmB to fungi.
The minimal inhibitory concentration and the minimum lethal concentration a
gainst Candida albicans are similar to that for desoxycholate AmB (DAMB; Fu
ngizone), In vitro, CARIB induced no hemolysis of human red blood cells at
concentrations of as high as 500 mu g of AmB/ml, and DAMB was highly hemoly
tic at 10 mu g of AmB/ml. CAMB protect ICR mice infected with C, albicans w
hen the agent is administered intraperitoneally at doses of as low as 0.1 m
g/kg/day, In a tissue burden study, CAMB, DAME, and AmBisome (liposomal AmB
; LAMB) were effective in the kidneys, but in the spleen CARIB was more pot
ent 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 comp
are well with AmBisome and AmB.