Artículo
Dual strategy to improve the oral bioavailability of efavirenz employing nanomicelles and curcumin as a bio-enhancer
Fuentes, Pedro; Bernabeu, Ezequiel Adrian
; Bertera, Facundo Martin; Garces, Mariana Soledad
; Oppezzo, Javier; Zubillaga, Marcela Beatriz
; Evelson, Pablo Andrés
; Salgueiro, María Jimena; Moretton, Marcela Analía
; Höcht, Christian; Chiappetta, Diego Andrés
Fecha de publicación:
02/2024
Editorial:
Elsevier Science
Revista:
International Journal Of Pharmaceutics
ISSN:
0378-5173
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
The present investigation was focused on the development of Soluplus®-based nanomicelles (NMs) (10 % w/v) loaded with Efavirenz (EFV) (5 mg/mL) and Curcumin (natural bio-enhancer) (CUR) (5, 10 and 15 mg/mL) to improve the oral bioavalability of EFV. Micellar formulations were obtained employing an acetone-diffusion technique. Apparent aqueous solubility was increased up to ∼1250-fold and 25,000-fold for EFV and CUR, respectively. Drug-loaded nanoformulations showed an excellent colloidal stability with unimodal size distribution and PDI values < 0.30. In vitro drug release was 41.5 % (EFV) and 2.6 % (CUR) from EFV-CUR-NMs over 6 h in simulated gastrointestinal fluids. EFV-CUR-loaded NMs resulted as safe nanoformulations according to the in vitro cytocompatibility assays in Caco-2 cells. Furthermore, CUR bio-enhancer activity was demonstrated for those nanoformulations. A CUR concentration of 15 mg/mL produced a significant (p < 0.05) increment (2.64-fold) of relative EFV oral bioavailability. Finally, the active role of the lymphatic system in the absorption process of EFV, after its oral administration was assessed in a comparative pharmacokinetic study in presence and absence of cycloheximide, a lymphatic transport inhibitor. Overall our EFV-CUR-NMs denoted their potential as a novel nanotechnological platform, representing a step towards an optimized “nano-sized” therapy for AIDS patients.
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Articulos(IBIMOL)
Articulos de INSTITUTO DE BIOQUIMICA Y MEDICINA MOLECULAR
Articulos de INSTITUTO DE BIOQUIMICA Y MEDICINA MOLECULAR
Articulos(OCA HOUSSAY)
Articulos de OFICINA DE COORDINACION ADMINISTRATIVA HOUSSAY
Articulos de OFICINA DE COORDINACION ADMINISTRATIVA HOUSSAY
Citación
Fuentes, Pedro; Bernabeu, Ezequiel Adrian; Bertera, Facundo Martin; Garces, Mariana Soledad; Oppezzo, Javier; et al.; Dual strategy to improve the oral bioavailability of efavirenz employing nanomicelles and curcumin as a bio-enhancer; Elsevier Science; International Journal Of Pharmaceutics; 651; 2-2024; 123734-123748
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