Targeted Oral Fixed-Dose Combination of Amphotericin B-Miltefosine for Visceral Leishmaniasis.

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Tác giả: M Paloma Ballesteros, Francisco Bolás-Fernández, Jéssica A de Jesus, María Auxiliadora Dea-Ayuela, Raquel Fernández-García, Anne Marie Healy, Aikaterini Lalatsa, Marcia Dalastra Laurenti, Peter O'Connell, Luiz Felipe D Passero, Dolores R Serrano, David Walsh

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: United States : Molecular pharmaceutics , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 179513

 The incidence of visceral leishmaniasis (VL) remains a significant health threat in endemic countries. Fixed-dose combination (FDC) of amphotericin B (AmB) and miltefosine (MLT) is a promising strategy for treating VL, but the parenteral administration of AmB leads to severe side effects, limiting its use in clinical practice. Here, we developed novel FDC granules combining AmB in the core with a MLT coating using wet granulation followed by the fluidized bed technology. The granules maintained the crystalline structure of AmB throughout manufacturing, achieving an AmB loading of ∼20%. The MLT coating layer effectively sustained AmB release from 3 to 24 h following Korsmeyer-Peppas kinetics. The formulation demonstrated remarkable stability, maintaining >
 90% drug content for over a year at both 4 °C and room temperature under desiccated conditions. In vivo efficacy studies in
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