Development and characterization of amphotericin B nanosuspensions for oral administration through a simple top-down method.

Abstract

Amphotericin B (AmB) is regarded as a life-saving drug in treating severe systemic fungal infections. However, the poor solubility and permeability limits its oral administration. The main purpose of this study is to evaluate AmB nanosuspensions in enhancing its solubility for the oral application. Magnetic stirring method with very low energy input, as a top-down technology, was firstly used to prepare the drug nanosuspensions. Sodium deoxycholate and carbomer were screened as the stabilizers through a single-factor experiment. Under the optimum conditions, AmB nanosuspensions were spherically shaped with the average particle size of 348.9±21.2 nm. X-ray diffraction analysis and differential scanning calorimetry confirmed that the initial crystalline state was preserved after particle size reduction. Saturated solubility and dissolution rate of AmB nanosuspensions exhibited the better dissolution properties compared with raw drug. Stability study demonstrated that AmB nanosuspensions maintained a good stability at 4oC for 30 days. In conclusion, AmB nanosuspensions potentially improved the oral absorption and magnetic stirring method could be acted as an effective method to produce AmB nanosuspensions.