The present study focused on the development of an amphotericin B (AmB) nanoformulation for ophthalmic applications. Accordingly, AmB nanohydrogels (AHA/AmB) using alkyl glyceryl hyaluronic acid (Hyalorepair®, AHA), a hydrophobized hyaluronic acid, were prepared by employing the dialysis method, followed by assessments of physical properties, drug efficacy, and toxicity. In the AHA/AmB formulation, AmB existed in a self-aggregated and amorphous state in the hydrophobic environment of the AHA moiety. AHA/AmB was shown in vitro to interact with mucin, which is known to be expressed in the corneal epithelium and was expected to improve its corneal retention. Compared with the conventional AmB formulation, amphotericin B sodium deoxycholate, AHA/AmB had the same in vitro antifungal activity but significantly lower in vitro toxicity. These findings indicate that nanohydrogels prepared with AHA possess high fungal selectivity and serve as a promising system for ophthalmic AmB delivery.

本研究的重点是开发用于眼科应用的两性霉素 B (AmB) 纳米制剂。因此，使用烷基甘油透明质酸 (Hyalorepair®, AHA)（一种疏水化透明质酸）的 AmB 纳米水凝胶（AHA/AmB）通过透析方法制备，然后评估物理性质、药物功效和毒性。在 AHA/AmB 配方中，AmB 在 AHA 部分的疏水环境中以自聚集和无定形状态存在。AHA/AmB体外显示与粘蛋白相互作用，粘蛋白已知在角膜上皮中表达并有望改善其角膜保留。与常规AmB制剂相比，两性霉素B脱氧胆酸钠、AHA/AmB在体外具有相同抗真菌活性，但体外毒性显着降低。这些发现表明，用 AHA 制备的纳米水凝胶具有高真菌选择性，可作为眼科 AmB 递送的有前途的系统。