期刊
JOURNAL OF LIPOSOME RESEARCH
卷 22, 期 1, 页码 62-71出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/08982104.2011.592495
关键词
Macrophage; targeting; amphotericin B; O-palmitoyl mannan
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.
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