Preparation of Amphotericin B dry powder for nebulization from lipids. Synthesis and Development, Formulation of dry powder, Nebulizer, Toxicity study

      Аннотация: Amphotericin B (AmB) is the drug of choice for most systemic fungal infections. It is considered to be the gold standard therapy and most commonly used to treat life-threatening conditions such as cryptococcosis, histoplasmosis, and invasive pulmonary aspergillosis. AmB in lipid drug carriers were used to prepare reconstituted dry power formulations by lyophilization process (freeze drying). Five lipid derivatives such as sodium deoxycholate (SDC), sodium deoxycholate sulfate (SDCS), potassium deoxycholate (KDC), potassium cholate (KC) and sodium cholate (SC) were chosen as lipid drug carriers effect in different salts (Na+ and K+) in reconstituted dry powder formulations for nebulization. SDCS was successfully synthesized in a laboratory and characterized by FTIR, 1H NMR, mass spectra, its Rf and melting point. KDC and KC were prepared from their corresponding acid such deoxycholic and cholic acid with potassium hydroxide in equal mole ratios. Thus, these compounds provide a desirable feature as a lipid drug carrier for reconstituted dry powder formulation, which was suitable for nebulization. AmB-lipid formulations (AmB-KC, AmB-KDC, AmB-SC, AmB-SDC and AmB-SDCS) formed solid cake

Ключевые слова: permeation, Phagocytosis, Lipid derivatives, Amphotericin B-lipid formulation, Nebulization, Lipid drug carriers, Reconstituted powder, Lyophilization, Alveolar macrophage, Ussing chambers.