Abstract |
Amphotericin B (AmB) was formulated in trilaurin-based emulsomes (nanosize lipid particles) stabilized by soya phosphatidylcholine (PC), as a new delivery system 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- deoxycholate (AmB-Doc) and emulsome entrapped AmB was tested in vitro in Leishmania donovani infected macrophage-amastigote system (J774A.1 cells), which showed higher efficacy of OPM grafted AmB emulsomes (TLEs-OPM) over plain AmB emulsomes (TLEs) and AmB-Doc. The in vivo antileishmanial activity of the AmB (0.5 mg/kg) was tested in AmB-Doc, TLEs and TLEs-OPM forms against VL in L. donovani infected hamsters. Formulation TLEs-OPM eliminated intracellular amastigotes of L. donovani within splenic macrophages more efficiently (73.7 +/- 6.7% parasite inhibition) than the formulation TLEs (51.7 +/- 5.4% parasite inhibition) (P < 0.01) or AmB-Doc (30.4 +/- 4.8% parasite inhibition) (P < 0.001). Our results suggest that these newer formulations (plain and ligand appended emulsomes) are a promising alternative to the conventional AmB-Doc formulation for the treatment of VL.
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Authors | Swati Gupta, Anuradha Dube, Suresh P Vyas |
Journal | Journal of drug targeting
(J Drug Target)
Vol. 15
Issue 6
Pg. 437-44
(Jul 2007)
ISSN: 1061-186X [Print] England |
PMID | 17613662
(Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Drug Carriers
- Drug Combinations
- Trypanocidal Agents
- Deoxycholic Acid
- Amphotericin B
- amphotericin B, deoxycholate drug combination
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Topics |
- Amphotericin B
(administration & dosage, therapeutic use)
- Animals
- Cricetinae
- Deoxycholic Acid
(administration & dosage, therapeutic use)
- Disease Models, Animal
- Drug Carriers
- Drug Combinations
- Leishmania donovani
(drug effects)
- Leishmaniasis, Visceral
(drug therapy, parasitology)
- Macrophages
(drug effects, parasitology)
- Male
- Mesocricetus
- Mice
- Nanoparticles
- Trypanocidal Agents
(administration & dosage, therapeutic use)
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