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 â¼1250-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.
Asunto(s)
Alquinos , Curcumina , Ciclopropanos , Humanos , Células CACO-2 , Disponibilidad Biológica , Benzoxazinas , Solubilidad , Micelas , Portadores de Fármacos , Administración Oral , Tamaño de la PartículaRESUMEN
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RESUMEN
Equisetum giganteum L. (Equisetaceae) is a species native to South America and Central America, which is used in traditional medicine as a diuretic and in treating of various diseases. The aim of this paper was to study the polyphenol profile and antioxidant activity of extracts obtained from lateral branches and main stem of the plants. Quali- and quantitative differences were detected with higher contents of phenols, tannins, condensed tannins, flavonoids and hydroxicinnamic acids in the lateral branches. The proanthocyanidins propelargonidin and procyanidin only were detected in lateral branches. These extracts showed the highest antioxidant activity. Due to their higher concentration and chemical composition, lateral branches could be considered as a sort of source of compounds that would act as antioxidant.
Equisetum giganteum L. (Equisetaceae) es una especie nativa de Sudamérica y América Central, que es empleada en la medicina tradicional como diurético y en el tratamiento de diversas patologías. El objetivo de este trabajo fue estudiar el perfil de polifenoles y la actividad antioxidante de extractos obtenidos de las ramas laterales (tallos finos), tallos entrenudos y tallos basales. Se detectaron diferencias cuali-cuantitativas, con mayor contenido de fenoles, taninos, taninos condensados, flavonoides y ácidos hidroxicinámicos en las ramas laterales. Las proantocianidinas propelargonidina y procianidina sólo se detectaron en las ramas laterales. En estos extractos se detectó la mayor actividad antioxidante. Debido a la alta concentración y composición química, los tallos laterales podrían ser empleados como fuente de compuestos con actividad antioxidante.