Fernanda dos Santos Ocampo1; Leny Angélica Henrique do Nascimento1 ; Francisco Alexandrino Jr1 ; Michelle Alvares Sarcinelli1 ; Érika Christina Ashton Nunes Chrismann2 ; Kattya Gyselle de Holanda e Silva2 ; Helvécio Vinícius Antunes Rocha1 ; Beatriz Ferreira de Carvalho Patrício1,3

1 Farmanguinhos/ Fiocruz; 2 Federal University of Rio de Janeiro; 3 Federal University of the State of Rio de Janeiro

Amphotericin B (AmB) is one of the main drugs used in the of systemic fungal diseases and leishmaniasis. Due to its low aqueous solubility and oral absorption, there are only commercially available intravenous AmB formulations. However, these have adverse effects such as irreversible nephrotoxicity, in addition to the high cost. Therefore, the development of an oral formulation of AmB has the potential to remedy these obstacles. Between the lipid nanoparticles, it is possible to highlight the nanostructured lipid carriers (CLN), which are systems formed by surfactant, solid lipids (LS) and liquid lipids (LL), which must be miscible. Therefore, this work objective to develop a CLN containing AmB for oral use. For this, a D-optimal factorial design was used, in which 6 LS, 2 LL and 2 non-ionic surfactants were combined. 16 test formulations were prepared and, in response to the experimental design, particle size (TP), polydispersion index (PDI) and AmB concentration ([AmB]) were evaluated. The results demonstrate that the proportion Inwitor 900 (4%), Capmul MCM (1%), Tween 20 (5%) and water (90%) was the one that presented the best results ([AmB] of 2 mg / g, 119 nm and PDI of 0.3). So, it is concluded that the developed formulation has high [AmB] and biopharmaceutical parameters consistent with what is recommended in the literature for adequate oral absorption. However, additional tests must be performed in order to assess its performance in vivo.



Keyword: Amphotericin B; Oral use; Nanostructure lipid carriers.
Support: Fiocruz; CNPq; BNDES

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