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Article Dans Une Revue Biochimie Année : 2014

Development of antileishmanial lipid nanocomplexes

Résumé

Visceral leishmaniasis is a life-threatening disease that affects nearly a million people every year. The emergence of Leishmania strains resistant to existing drugs complicates its treatment. The purpose of this study was to develop a new lipid formulation based on nanocochleates combining two active drugs: Amphotericin B (AmB) and Miltefosine (HePC). Nanocochleates composed of dioleoylphosphatidylserine (DOPS) and Cholesterol (Cho) and Ca2þ, in which HePC and AmB were incorporated, were prepared. Properties such as particle size, zeta potential, drug payload, in-vitro drug release and storage stability were investigated. Moreover, in-vitro stability in gastrointestinal fluid was performed in view of an oral administration. AmBeHePC-loaded nanocochleates with a mean particle size of 250 ± 2 nm were obtained. The particles displayed a narrow size distribution and a drug payload of 29.9 ± 0.5 mg/g for AmB, and 14.0 ± 0.9 mg/g for HePC. Drug release occurred preferentially in intestinal medium containing bile salts. Therefore, AmBeHePC-loaded nanocochleates could be a promising oral delivery system for the treatment of visceral leishmaniasis.
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Dates et versions

hal-04529815 , version 1 (02-04-2024)

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T.T.H. Pham, C. Gueutin, M. Cheron, S. Abreu, P. Chaminade, et al.. Development of antileishmanial lipid nanocomplexes. Biochimie, 2014, 107, pp.143-153. ⟨10.1016/j.biochi.2014.06.007⟩. ⟨hal-04529815⟩
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