Novel methods for the encapsulation of meglumine antimoniate into liposomes

The antimonial drug, meglumine antimoniate, was successfully encapsulated in dehydration-rehydration vesicles and in freeze-dried empty liposomes (FDELs). High encapsulation efficiencies (from 28 to 58%) and low weight ratios of lipids to encapsulated antimony (from 1:0.15 to 1:0.3) were achieved. T...

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Bibliographic Details
Published in:Brazilian journal of medical and biological research 2000-07, Vol.33 (7), p.841-846
Main Authors: Frézard, F, Michalick, M S, Soares, C F, Demicheli, C
Format: Article
Language:English
Subjects:
Analysis of Variance
Animals
Antiprotozoal Agents - chemistry
Antiprotozoal Agents - therapeutic use
BIOLOGY
Cricetinae
Dehydration
Drug Compounding - methods
encapsulation
glucantime
Leishmania donovani - drug effects
leishmaniasis
Leishmaniasis, Visceral - drug therapy
liposomes
Liposomes - chemistry
MEDICINE, RESEARCH & EXPERIMENTAL
Meglumine - chemistry
Meglumine - therapeutic use
Meglumine Antimoniate
Mesocricetus
Organometallic Compounds - chemistry
Organometallic Compounds - therapeutic use
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Summary:The antimonial drug, meglumine antimoniate, was successfully encapsulated in dehydration-rehydration vesicles and in freeze-dried empty liposomes (FDELs). High encapsulation efficiencies (from 28 to 58%) and low weight ratios of lipids to encapsulated antimony (from 1:0.15 to 1:0.3) were achieved. These formulations, contrary to those obtained by conventional methods, can be stored as intermediate lyophilized forms and reconstituted just before use. The efficacy of FDEL-encapsulated meglumine antimoniate was evaluated in hamsters experimentally infected with Leishmania chagasi. A significant reduction of liver parasite burdens was observed in animals treated with this preparation, when compared to control animals treated with empty liposomes. In contrast, free meglumine antimoniate was found to be inefficient when administered at a comparable dose of antimony. This novel liposome-based meglumine antimoniate formulation appears to be promising as a pharmaceutical product for the treatment of visceral leishmaniasis.
ISSN:0100-879X
1414-431X
0100-879X
1414-431X
DOI:10.1590/S0100-879X2000000700016