4.7 Article

A dual-functional chitosan derivative platform for fungal keratitis

期刊

CARBOHYDRATE POLYMERS
卷 275, 期 -, 页码 -

出版社

ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2021.118762

关键词

Fungal keratitis; Topical administration; Ocular intrinsic barriers; Corneal penetration; Dosing concentration and frequency

资金

  1. National Natural Science Foundation of China [52173143, 81600775, 21504082]
  2. Zhongyuan Thousand Talents Plan Project
  3. Science and Technology Program of Henan Province, China [202102310072]
  4. Basic Science Key Project of Henan Eye Institute/Henan Eye Hospital [20JCZD002, 20JCQN001]

向作者/读者索取更多资源

A chitosan-based platform was developed for ocular topical delivery of econazole, which effectively enhanced drug penetration and therapeutic effects while improving patient compliance. Its high structural adaptability also suggests potential benefits for other ocular anterior segment-related diseases.
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.

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