Amphotericin B loaded ethyl cellulose nanoparticles with magnified oral bioavailability for safe and effective treatment of fungal infection - 18/06/20
páginas | 10 |
Iconografías | 10 |
Vídeos | 0 |
Otros | 0 |
Graphical abstract |
AmB-EC-NPs were synthesized using a high-pressure emulsification solvent evaporation and evaluated for in vitro and in vivo studies. This method yields small, monodisperse AmB-EC-NPs along with smooth surface morphology and improved encapsulation efficiency. AmB-EC-NPs could be effective, viable and a better alternative to currently existing iv formulations, for magnified oral delivery of AmB in the treatment of fungal infection without associated adverse effects.
Highlights |
• | Ethyl cellulose nanoparticles (EC-NPs) are used as a nanocarrier for magnified oral delivery of Amphotericin B (AmB). |
• | High pressure emulsification solvent evaporation (HPESE) method is used for the encapsulation of amphiphilic drugs. |
• | AmB loaded EC-NPs (AmB-EC-NPs) exhibited gastric and storage stability. |
• | AmB is present in monomeric form inside the biocompatible EC matrix, in contrast to aggregated form of AmB in Fungizone®. |
• | Antifungal activity is performed against C. albicans. |
• | The developed formulation shows reduced hemolytic toxicity, nephrotoxicity. |
Abstract |
Amphotericin B is a gold standard drug used in various fungal and parasitic infection treatment. Most of the marketed formulations are administered intravenously, but show dose-dependent adverse effects i.e., nephrotoxicity and hemolysis. Oral route eliminates the toxic concern but exhibits poor bioavailability. Therefore, ethylcellulose nanoparticles (EC-NPs) have been used for magnified oral delivery of AmB, where EC provides gastrointestinal stability. These nanoparticles were synthesized by high-pressure emulsification solvent evaporation (HPESE) method and evaluated for in vitro and in vivo studies. This method yields small, monodisperse AmB-EC-NPs along with smooth surface morphology and improved encapsulation efficiency. The developed formulation showed a sustained release pattern following Higuchi diffusion kinetics along with gastric and storage stability. Aggregation study revealed that AmB was present in its monomeric form inside the biocompatible EC matrix. The antifungal result demonstrated that the MIC of AmB-EC-NPs was reduced ∼1/3rd than AmB and Fungizone® at 24 h whereas it was observed ∼1/8th at 48 h. in vivo pharmacokinetic analysis demonstrated 1.3-fold higher AUC than Fungizone® even at a 4.5-time lesser dose via the oral route and a ∼15-fold rise in the bioavailability in contrast to the native AmB. The hemolytic study revealed that the developed formulation exhibited 8-fold lesser hemolysis than Fungizone®. Furthermore, the biosafety profile of AmB-EC-NPs was ensured by the significantly lesser level of blood urea nitrogen and plasma creatinine along with the normal pattern of renal tubules in comparison to AmB and Fungizone®. In conclusion, the results stipulated that the AmB-EC-NPs could be effective, viable and a better alternative to currently existing iv formulations, for magnified oral delivery of AmB in the treatment of fungal infection without associated adverse effects.
El texto completo de este artículo está disponible en PDF.Keywords : Amphotericin B, Magnified oral delivery, Ethylcellulose, Antifungal activity, Pharmacokinetic, Nephrotoxicity, Hemolysis
Esquema
Vol 128
Artículo 110297- août 2020 Regresar al númeroBienvenido a EM-consulte, la referencia de los profesionales de la salud.
El acceso al texto completo de este artículo requiere una suscripción.
Bienvenido a EM-consulte, la referencia de los profesionales de la salud.
La compra de artículos no está disponible en este momento.
¿Ya suscrito a @@106933@@ revista ?