Abstract
Purpose: The objective of this study was to design and develop nanoemulsion formulations of Itraconazole (ITZ), a water-insoluble, potent antifungal drug using the spontaneous emulsification method, to improve the ocular delivery and achieve a sustained release of the drug. Methods: The oil was selected on the basis of the ITZ solubility while the surfactant and co-surfactant were selected based on the thermodynamic stability and globule size. Following the selection of components, a pseudo-ternary phase diagram was constructed for the most promising formulation (F11) using benzyl benzoate (BB) as the oil, Eumulgin CO40 as the surfactant, and propylene glycol as the co-surfactant, by the design of experiments (DoE). Results: F7 and F11 formulations were found to have an average globule size of 223.5 ± 10.7 nm and 157.5 ± 14.2 nm, besides thermodynamic stability and suitable physicochemical properties. F11 possessed an almost seven-fold higher cumulative percentage of in vitro released ITZ, in comparison to ITZ aqueous suspension after 24 hours. The release data suggested that the best fitted kinetical model for F11 and F7 was the Higuchi and Korsmeyer-Peppas model. Conclusion: The extended-release of the drug beside an acceptable amount of loaded ITZ suggested that nanoemulsion is suitable for the delivery of the ITZ.
Highlights
F7 and F11 formulations were found to have an average globule size of 223.5 ± 10.7 nm and 157.5 ± 14.2 nm, besides thermodynamic stability and suitable physicochemical p properties
Construction of Pseudo-ternary Phase Duiagram Following the selection of surfactant and co-surfactant, the design of experiments (DoE) was used to n construct a pseudo-ternary phase diagram for the nanoemulsion with best globule size, polydispersity index (PDI), and thermodynamic stability, consisting of benzyl benzoate (BB) as oil phase, Eumulgin CO40 and propylene glycol (PG) as surfactant mixture (Smix 1:1, 1:3, 3:1), and 1% w/v polyvinyl alcohol (PVA) solution as the aqueous phase
Nanoemulsions could be designed to overcome the problems associated with the poor bioavailability of the hydrophobic antifungal drug, itraconazole, in ocular delivery
Summary
F7 and F11 formulations were found to have an average globule size of 223.5 ± 10.7 nm and 157.5 ± 14.2 nm, besides thermodynamic stability and suitable physicochemical p properties. It was expected that formulating ITZ to nanoemulsion could enhance the intraocular bioavailability of this drug as a result p of improved solubility, prolonged residence time, and sustained release of the drug
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