Table 3.
Physical and potassium release properties of liposomal AmB formulations prepared from DSHemsPC using DSSH buffer pH 5.5
AmB Formulation | Molar ratio | Zeta average size (nm) ± SD | Distribution | Polydispersity ± SD | Zeta potential (mv) ± SD | IC50 for potassium release (μg/ml, Lower and Upper 95% limit) |
---|---|---|---|---|---|---|
F27-DSHemsPC/DSPC/DSPG/AmB | 1.25/5.0/2.0/1.0 | 84.7±0.8 | Monomodal | 0.198±0.03 | −23.3± 6.07 | 130 (16.7–990) |
F28-DSHemsPC/DPPC/DPPG/AmB | 1.25/5.0/2.0/1.0 | 202.4±20 | Monomodal | 0.5±0.03 | −14.8±4.16 | 14710(599–361070) |
F29-DSHemsPC/DMPC/DMPG/AmB | 1.25/5.0/1.5/1.0 | 111.6±1.0 | Monomodal | 0.21±0.02 | −25.3±9.05 | 1342000(307000–58729000) |
F30-DSHemsPC/DMPC/DMPG/AmB | 1.25/5.0/2.0/1.0 | 112.8±3.2 | Monomodal | 0.207±0.01 | −25.3±13 | 114510(29560–443580) |
F31-DSHemsPC/HSPC/DSPG/AmB | 1.25/5.0/2.0/1.0 | 99.53±2.8 | Monomodal | 0.237±0.03 | −21.3±7.97 | 50 (6.6–380) |
F32-DSHemsPC/HSPC/DSPG/AmB | 1.75/5.0/1.5/1.0 | 130.1±2.0 | Monomodal | 0.384±0.01 | −24±5.13 | 217 (56–840) |
F33-DSHemsPC/DMPC/DMPG | 1.25/5.0/1.5 | 76.98±0.39 | Monomodal | 0.21±0.056 | −42.7±0.5 | Inactive |
AmBisome™ | 120.3±1.5 | Monomodal | 0.2±0.2 | −54.5±1.1 | 529.97(326.6–1101.7) | |
Fungizone™ | 0.76 (0.41–1.4) |
The IC50 of F27– F30, F32 and AmBisome™ was significantly (P < 0.01) higher than Fungizone™. The IC50 among F31 and Fungizone™ was not significantly different (P > 0.05). The IC50 of AmBisome™ was significantly (P < 0.001) greater than F27, and F32. The IC50 of F29 was significantly (P < 0.001) greater than AmBisome™.