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Emulgel based on amphotericin B and bacuri butter ( Platonia insignis Mart.) for the treatment of cutaneous leishmaniasis: characterization and in vitro assays

2018; Taylor & Francis; Volume: 44; Issue: 10 Linguagem: Inglês

10.1080/03639045.2018.1492610

1520-5762

Elvilene de Sousa Coêlho, Gláucia Laís Nunes Lopes, Iluska Martins Pinheiro, Josefa Natália Policarpo de Holanda, Michel Muálem de Moraes Alves, Naiane Carvalho Nogueira, Fernando Aécio de Amorim Carvalho, André Luís Menezes Carvalho,

Phytochemistry Medicinal Plant Applications

Objective: This work aimed to develop and characterize a topical emulgel of amphotericin B (AmB) with bacuri butter (Platonia insignis Mart.) and evaluate its antileishmanial activity using in vitro assays.Significance: Leishmaniasis is considered an infectious disease, with high incidence and capacity to produce deformities. The first-line treatment recommended by WHO, with pentavalent antimonials, is aggressive and very toxic. Therefore, the development of topical treatments can emerge as a promising and less offensive alternative.Methods: The developed formulations were evaluated for organoleptic characteristics, centrifugation resistance, globule size, pH, electrical conductivity, viscosity, spreadability, drug content, preliminary stability, in vitro release profile, evaluation of antileishmanial activity using promastigotes forms of Leishmania major as infecting agents, macrophage cytotoxicity and selectivity index (IS).Results: Formulated emulsions presented organoleptic characteristics compatible with its constituents; pH values were suitable for topical application, ranging from 4.73 to 5.02; introduced non-Newtonian shear thinning system; drug content was within the established standards, and the most suitable kinetic model of release was the first order. Regarding the in vitro assays, formulations containing both 1% and 3% of AmB presented similar outcomes, indicating a synergism between the bacuri butter and the drug, possibly showing a reduction on cytotoxicity to host cells.Conclusions: It was concluded that the formulations developed showed promising antileishmanial action and high potential for topical use.