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AAPS PharmSciTech ; 21(7): 272, 2020 Oct 06.
Artículo en Inglés | MEDLINE | ID: mdl-33025308

RESUMEN

The aim the study was to design, formulate, and evaluate self-nanoemulsifying drug delivery systems (SNEDDS) of itraconazole for improving the topical antifungal properties of the drug by adopting the nanoemulsion intermediate gel of the optimized system. Solubility study was conducted to select the most appropriate oils and surfactants for formulation. Different possible systems were created. Ternary phase diagrams were constructed to select the most promising system for further study. The nanoemulsion intermediate gel of the selected system was evaluated for stability, dilution effect, viscosity, pH, antifungal activity, droplet size, PDI, and zeta potential. In vitro release of the drug from the selected intermediate gel was investigated, and the kinetic model of drug release was determined. Ex vivo permeation of itraconazole was studied, and the amount of drug accumulated in the skin was calculated. Solubility and phase diagrams revealed that the system consisting of 60% cotton seed oil and 40% span 80 provided the nanoemulsion intermediate gel with the highest drug concentration. The selected system had a droplet size of about 236 nm and zeta potential of - 59.8. The viscosity of the corresponding intermediate gel was 1583.47 cp. The system exhibited high stability at 4°C and 25°C for 12 months and improved antifungal activity. In vitro release study showed complete release of itraconazole within 4 h, while the ex vivo permeation study revealed accumulation of the majority of the drug within the skin layers (72.5%).


Asunto(s)
Antifúngicos/administración & dosificación , Sistemas de Liberación de Medicamentos , Emulsiones/química , Geles/química , Itraconazol/administración & dosificación , Nanopartículas/química , Animales , Antifúngicos/química , Liberación de Fármacos , Itraconazol/química , Tamaño de la Partícula , Piel/efectos de los fármacos , Solubilidad , Tensoactivos/química , Viscosidad
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