Objective To construct ophthalmic nanomicelles based on α-tocopheryl polyethylene glycol succinate-polyoxyeth-ylene castor oil for loading the antibacterial drug voriconazole(TPGS-EL/VRC),and to investigate its ocular drug delivery per-formance and in vitro anti-Candida albican efficacy.Methods TPGS-EL/VRC mixed micelles were prepared by thin film hydra-tion method.The particle size distribution and Zeta potential of the micelles were measured by a particle size analyzer.The mor-phology of the micelles was investigated by transmission electron microscope.High performance liquid chromatography(HPLC)was used to determine the drug loading and encapsulation efficiency.The in vitro biocompatibility of TPGS-EL/VRC was evalua-ted by cytotoxicity assay and hen's egg test-chorioallantoic membrane(HET-CAM).The uptake capacity of corneal epithelial cells(HCE-T)to nanomicelles and its uptake pathway were studied by flow cytometry.The antibacterial activity of nanomicelles against Candida albicans was evaluated by in vitro antifungal activity assay and ring inhibition assay.Results TPGS-EL/VRC mixed micelles were spherical particles with a particle size of(109.63±0.25)nm and potential of(-29.3±0.20)mV,and showed good encapsulation efficiency for VRC.TPGS-EL/VRC had low cytotoxicity to HCE-T cells and were biocompatible.TPGS-EL nanomicelles effectively increased the uptake of drugs by HCE-T cells by 5.8 times that of the normal solution group,and showed better anti-candida albicans efficacy in both in vitro models.Conclusion TPGS-EL/VRC nanomicelles demonstrated excellent formulation properties,biocompatibility,and improved intracellular transport of VRC and in vitro anti-Candida albicans efficacy.As a result,it provides an innovative delivery vehicle for the efficient treatment of ocular fungal infections.
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