Bioactivity and toxicity studies of amphotericin B incorporated in liquid crystals.

The main objective of the present work was to evaluate the bioactivity and safety of amphotericin B-liquid crystal mixtures (AmB-LC). The effects of liquid crystal (LC) materials and AmB-LC ratios on bioactivity and toxicity to respiratory cell lines were investigated. The formation of AmB-LC mixtures did not change the physical properties of LC when the AmB loading was not more than a 1:3 mole ratio (25%).

Physicochemical properties and antifungal activity of amphotericin B incorporated in cholesteryl carbonate esters.

The antifungal activity of amphotericin B (AmB) incorporated in three cholesteryl carbonate esters (CCEs), sodium cholesteryl carbonate, cholesteryl palmityl carbonate, and dicholesteryl carbonate, was examined to assess their potential for use in a dry powder aerosol. Formulations containing dissolved AmB were stable for 6 months. The particle size varied inversely with liquid crystalline content with observed mass median aerodynamic diameters ranging from 4 to 8 μ m.

Interaction of Amphotericin B with cholesteryl palmityl carbonate ester.

A cholesteryl carbonate ester was prepared and evaluated as a possible thermotropic liquid crystal excipient for dry powder inhalers. Cholesteryl palmityl carbonate (CPC) was synthesized, and the phase behavior was characterized by differential scanning calorimetry, transmission electron microscopy, polarized light microscope, small angle X-ray diffraction, and solid-state nuclear magnetic resonance spectroscopy. Amphotericin B (AmB) was incorporated into CPC at various mole% (7.