title: Development and evaluation of tripalmitin emulsomes for the treatment of experimental visceral leishmaniasis.
abstract: 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.
authors: Nanomedicine Research Center, Department Of Pharmaceutics, I.S.F. College Of Pharmacy , Moga 142 001 (PB) , INDIA.
authors: Ajay
authors: A
authors: Pal
authors: Swati
authors: S
authors: Gupta
authors: Anil
authors: A
authors: Jaiswal
authors: Anuradha
authors: A
authors: Dube
authors: Suresh P
authors: SP
authors: Vyas
mesh_terms: D000666:Amphotericin B / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D007898:Leishmaniasis, Visceral / Q000188:drug therapy*; D008264:Macrophages / Q000187:drug effects; D008297:Male; D021261:Parasitic Sensitivity Tests; D010316:Particle Size; D013329:Structure-Activity Relationship; D014280:Triglycerides / Q000737:chemistry*
chemical_list: D000981:Antiprotozoal Agents; D014280:Triglycerides; D000666:Amphotericin B; C005859:tripalmitin