Detailed physicochemical characterization of charged and neutral LeciPlex®: loading efficiency and in vitro activity of Voriconazole and Amphotericin B.

In the present study, Voriconazole (VCNZ) and Amphotericin B (AmpB), drugs from BCS class II and IV, respectively, were selected for loading in phospholipid vesicular system, LeciPlex® fabricated by the nanoprecipitation method. The influence of biocompatible solvent and lipid type on VCNZ and AmpB loading in cationic, anionic, and nonionic LeciPlex® was studied for particle size, size distribution, and encapsulation efficiency. Transmission electron microscopy revealed the formation of vesicular systems in the blank, VCNZ, and AmpB-loaded LeciPlex®. VCNZ and AmpB were encapsulated and probably solubilized within the lipid bilayer of the LeciPlex® system.In vitro haemolysis studies proved the LeciPlex® formulations to be haemocompatible compared to the drug solutions. The three LeciPlex® systems showed comparable in vitro antifungal activity against Candida albicans and Aspergillus fumigatus to the respective drug solutions. Compared to the AmpB drug solution, the AmpB loaded anionic LeciPlex® exhibited potent anti-parasitic activity against Leishmania infantum (intra-macrophage) and Trypanosoma cruzi (intra-fibroblast). AmpB LeciPlex® showed higher IC50 value against MRC-5 human lung fibroblast while lower IC50 value against primary peritoneal mouse macrophages (PMM) infected with L. infantum indicating enhanced efficacy and selectivity of LeciPlex® when compared with AmpB solution.