title: Novel methods for the encapsulation of meglumine antimoniate into liposomes.
abstract: 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.
authors.affiliation: Fisiologia e Biofísica, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brasil. frezard@mono.icb.ufmg.br
authors.forename: F
authors.initials: F
authors.lastname: Frézard
authors.forename: M S
authors.initials: MS
authors.lastname: Michalick
authors.forename: C F
authors.initials: CF
authors.lastname: Soares
authors.forename: C
authors.initials: C
authors.lastname: Demicheli
mesh_terms: D000704:Analysis of Variance; D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000627:therapeutic use; D006224:Cricetinae; D003681:Dehydration; D004339:Drug Compounding / Q000379:methods; D007893:Leishmania donovani / Q000187:drug effects; D007898:Leishmaniasis, Visceral / Q000188:drug therapy*; D008081:Liposomes / Q000737:chemistry*; D008536:Meglumine / Q000737:chemistry* / Q000627:therapeutic use; D000077485:Meglumine Antimoniate; D008647:Mesocricetus; D009942:Organometallic Compounds / Q000737:chemistry* / Q000627:therapeutic use
chemical_list: D000981:Antiprotozoal Agents; D008081:Liposomes; D009942:Organometallic Compounds; D008536:Meglumine; D000077485:Meglumine Antimoniate