Amphotericin B nanohydrogel ocular formulation using alkyl glyceryl hyaluronic acid: Formulation, characterization, and in vitro evaluation

被引：11

作者：

Banshoya, Kengo ^{[1
]}

Fujita, Chiaki ^{[1
]}

Hokimoto, Yuka ^{[1
]}

Ohnishi, Masatoshi ^{[1
]}

Inoue, Atsuko ^{[1
]}

Tanaka, Tetsuro ^{[1
]}

Kaneo, Yoshiharu ^{[1
]}

机构：

[1] Fukuyama Univ, Fac Pharm & Pharmaceut Sci, Gakuen Cho 1, Fukuyama, Hiroshima 7290292, Japan

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2021年 / 610卷

关键词：

Amphotericin B; Hyaluronic acid; Hydrophobized polysaccharide; Nanohydrogel; Ocular formulation; Fungal keratitis; HEMOLYTIC-ACTIVITY; FUNGAL KERATITIS; DELIVERY-SYSTEMS; EYE DROPS; NANOPARTICLES; MICELLES; WATER; SOLUBILIZATION; CYTOTOXICITY; DRUGS;

D O I：

10.1016/j.ijpharm.2021.121061

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 (R), 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 selfaggregated 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.

引用

页数：9

共 57 条

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