Cochleate formulations of Amphotericin b designed for oral administration using a naturally occurring phospholipid

The purpose of this work was to formulate the poor soluble antifungal and antiparasitic agent Amphotericin B (AmB) in cost-effective lipid-based formulations suitable for oral use developing countries, overcoming limitations water solubility, nephrotoxicity low bioavailability. formulated, at different molar proportions, cochleate nanocarriers prepared using an accessible naturally occurring phospholipid rich phosphatidylserine (Lipoid PSP70). These nanoassemblies were by condensation negatively charged membrane vesicles with divalent cations (Ca2+). Small-angle X-ray scattering studies revealed Ca2+-triggered loosely packed multilamellar into tightly bilayers strongly dehydrated organization characterized narrow Bragg peaks. Transmission electron microscopy quasi-elastic light demonstrated formation nanosized particles. AmB drug loading above 55% all formulations. Circular dichroism prevalence monomeric complexed forms over toxic aggregates. stability gastric medium improved cochleates its release gastrointestinal media retarded. Confocal in-vitro interactions Lipoid PSP70-based Caco2 intestinal cell monolayers. results suggest that low-cost AmB-loaded may increase therapeutic range drug.