A dual-functional chitosan derivative platform for fungal keratitis

Fungal keratitis remains a serious infectious ocular disease, and the traditional administration of eye drops is limited by ocular intrinsic barriers and drug shortages. Herein, we fabricated a chitosan-based dual-functional platform for ocular topical delivery of econazole. The platform can prolong...

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Bibliographic Details
Published in:Carbohydrate polymers 2022-01, Vol.275, p.118762-118762, Article 118762
Main Authors: Shi, Liuqi, Li, Zhanrong, Liang, Zhen, Zhang, Junjie, Liu, Ruixing, Chu, Dandan, Han, Lei, Zhu, Lei, Shen, Jianliang, Li, Jingguo
Format: Article
Language:English
Subjects:
Administration, Ophthalmic
Animals
Antifungal Agents - administration & dosage
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
Biocompatible Materials - administration & dosage
Biocompatible Materials - chemistry
Biocompatible Materials - pharmacology
Carbohydrate Conformation
Chitosan - administration & dosage
Chitosan - chemistry
Chitosan - pharmacology
Corneal penetration
Dosing concentration and frequency
Drug Delivery Systems
Eye Infections, Fungal - drug therapy
Eye Infections, Fungal - microbiology
Female
Fungal keratitis
Fusarium - drug effects
Humans
Keratitis - drug therapy
Keratitis - microbiology
Mice
Mice, Inbred C57BL
Microbial Sensitivity Tests
Ocular intrinsic barriers
Ophthalmic Solutions - administration & dosage
Ophthalmic Solutions - chemistry
Ophthalmic Solutions - pharmacology
Topical administration
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Summary:Fungal keratitis remains a serious infectious ocular disease, and the traditional administration of eye drops is limited by ocular intrinsic barriers and drug shortages. Herein, we fabricated a chitosan-based dual-functional platform for ocular topical delivery of econazole. The platform can prolong the residence time on the ocular surface due to its strong interaction with the mucin layer by physical adhesion and covalent bonding, and also open corneal epithelial tight junctions for being positively charged, thereby enhancing corneal penetration of drug. Using these strategies, dosing concentration was reduced from 0.3 wt% to 0.1 wt%, dosing frequency was reduced from once-an-hour to twice-daily, in vitro and in vivo antifungal therapeutic effects were achieved and patient compliance could be improved. Given its high structural adaptability, many other ocular anterior segment-related diseases would benefit from this platform. A dual-functional bio-based eye drops is prepared for fungal keratitis. This eye drops significantly enhances corneal penetration of the drug and exhibits outstanding antifungal activity in vitro and in vivo. [Display omitted]
ISSN:0144-8617
1879-1344
DOI:10.1016/j.carbpol.2021.118762