Background: Amphotericin B (AmB) is important for the treatment of systemic fungal infections.
Nowadays, only intravenous administration (IV) of AmB has been available due to its low
aqueous solubility. Two forms of AmB are available. The first is Fungizone®, a mixture of AmB and
sodium deoxcycholate that produces severe nephrotoxicity. The second are lipid-based formulations
that reduce nephrotoxicity, but they are costly and require higher dose than Fungizone®. Thus, a
cheaper delivery system with reduced AmB toxicity is required.
Objective: To develop and characterize AmB loaded-nanostructured lipid carriers (AmB-loaded NLCs)
for IV administration to reduce AmB toxicity.
Methods: AmB-loaded NLCs with different solid lipids were prepared by the high-pressure homogenization
technique. Their physicochemical properties and the drug release profile were examined. The
molecular structure of AmB, antifungal and hemolysis activities of developed AmB-loaded NLCs were
Results: AmB-loaded NLCs ~110 to ~140 nm in diameter were successfully produced with a zeta potential
of ~-19 mV and entrapment efficiency of ~75%. In vitro release showed fast release characteristics.
AmB-loaded NLCs could reduce the AmB molecular aggregation as evident from the absorbance
ratio of the first to the fourth peak showing a partial aggregation of AmB. This result suggested that
AmB-loaded NLCs could offer less nephrotoxicity compared to Fungizone®. In vitro antifungal activity
of AmB-loaded NLCs showed a minimum inhibitory concentration of 0.25 µgmL-1.
Conclusion: AmB-loaded NLCs present high potential carriers for effective IV treatment with prolonged
circulation time and reduced toxicity.