Table 1.
AmB oral formulation summary.
| AmB oral formulation | Efficacy | Stability |
|---|---|---|
| Solid lipid nanoparticle [47] | Lower kidney tissue concentration, | 2–8 °C for 3 months, |
| 105% Fo of Fungizone® | 15 days ≥ 25 °C | |
| PLGA–PEG nanoparticle [43,48] | Increase antifungal activity 4-fold in vitro | N/A |
| Inhibit parasite load by 93.2% compared with free AmB group (74.6%) | ||
| 130% Fo of Fungizone® | ||
| Chitosan-coated nanostructured lipid carriers [42] | N/A | 63.9% AmB retained encapsulated after 30 min incubation in SIF |
| Lecithin-based mixed polymeric micelles [49] | Less toxic in HT29 cells | Increase solubility |
| 150% Fo of Fungizone® | ||
| O/W microemulsion [50] | Slightly less toxic than free DMSO | Increase the solubility by 1000 folds |
| Pickering emulsion [51] | N/A | Stable one month under refrigeration |
| Tragacanth/acrylic acid copolymer [52] | No mortality observed in mice comparing with free AmB | N/A |
| Improve oral bioavailability comparing with free AmB | ||
| Chitosan and porphyrin polymeric nanocarrier [53] | 23-fold antifungal activity than Ambisome® | Less degradation in SIF and a superior release profile for up to 12 h |
| Slightly less toxic than Fungizone® | ||
| Chitosan–EDTA microparticles [54] | N/A | 12-fold improvement in in vitro dissolution relative to pure AmB |
| Carbon Nanotubes [55,56] | Inhibit the parasite load in a dose-dependent manner | N/A |
| No evidence of toxicity in mice and hamster models | ||
| Cubosomes (cubic liquid crystal nanoparticles) [57] | low dose of AmB-loaded cubosomes shows low kidney concentration than Fungizone® | 74% detectable AmB after 3h in SIF |
| 285% bioavailability of Fungizone® | ||
| GCPQ nanoparticles [58] | Absolute Fo is 24.7% | Stable for a year on storage |
| Higher concentration in liver, lung and spleen | ||
| Cochleate–CAMB/MAT2203 [59,60] | 100% survival comparing with Fungizone® and AmBisome® | Stable for 4 months at 4 °C |
| No serious adverse event in Phase I study | ||
| SEDDS (iCo-010/019) [66] | <99% reduction in parasitic infection in a murine model | >75% over 60 days in 30 °C; >95% after 4 h in SIF |
| 95% inhibition when compared to control |
Abbreviations: SIF, simulated intestinal fluid; Fo, oral bioavailability.