amphotericin-b and tripalmitin

The antifungal and antileishmanial agent amphotericin B (AmB) was formulated in tripalmitin based nanosize lipid partices (emulsomes) for macrophage targeting for the treatment of visceral leishmaniasis (VL). Emulsomes were modified by coating them with macrophage-specific ligand (O-palmitoyl mannan, OPM). The antileishmanial activity of AmB (0.5 and 1 mg/kg) was investigated in-vivo against VL by the inhibition of parasitic load in the spleen of L. donovani infected hamsters after intraperitoneal injections of AmB-Doc (Mycol), plain emulsomes (TPEs) and OPM coated emulsomes (TPEs-OPM). The formulations were found to be less effective at the dose of 0.5 mg/kg. At the dose of 1 mg/kg, formulation TPEs-OPM eliminated intracellular amastigotes of L. donovani within splenic macrophages more efficiently (62.76 ± 3.54 % parasite inhibition) than the formulation TPEs (42.68 ± 2.36 % parasite inhibition) (P < 0.01) or AmB-Doc (25.87 ± 3.87 % parasite inhibition) (P < 0.001). Our results suggest that these formulations (plain and ligand grafted emulsomes) are a promising substitute to the conventional AmB-Doc formulation for the treatment of VL.

Topics: Amphotericin B; Animals; Antiprotozoal Agents; Cricetinae; Dose-Response Relationship, Drug; Leishmaniasis, Visceral; Macrophages; Male; Parasitic Sensitivity Tests; Particle Size; Structure-Activity Relationship; Triglycerides