Cyclodextrin-based Pickering nanoemulsions containing amphotericin B: Part II. Formulation, antifungal activity, and chemical stability

Journal of Drug Delivery Science and Technology(2022)

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摘要
In this study, cyclodextrin (CD)-stabilized, amphotericin B (AmB)-loaded Pickering and non-Pickering nanoemulsions (NEs) were developed using a high-pressure homogenization technique. The physicochemical and chemical properties of the formulations, including pH, osmolality, viscosity, particle size, size distribution, zeta potential, drug content, and entrapment efficiency, were acceptable for eye drops. The developed formulations showed a lower degree of AmB aggregation and lower hemolytic activity than commercial Amphotericin-B®. Because of the high AmB entrapment in their inner core, Pickering NEs displayed sustained in vitro drug release. The antifungal activity of AmB-loaded NEs was superior to that of intact AmB, comparable to that of Amphotericin-B® against C. albicans, and poorer than that of Amphotericin-B® against filamentous fungi. Stability studies showed that CD-based Pickering NEs exhibited good physical and chemical stability compared with their respective non-Pickering NEs. Thus, αCD-based Pickering NEs are a promising platform for loading AmB and should undergo in vivo studies for the treatment of fungal keratitis.
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关键词
Cyclodextrins,Amphotericin B,Pickering nanoemulsions,Eye drops,Antifungal
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