期刊
ADVANCED SCIENCE
卷 5, 期 1, 页码 -出版社
WILEY
DOI: 10.1002/advs.201700455
关键词
antiinflammation; flurbiprofen nanomicelles; functional peptide; ocular delivery system
资金
- National Key R&D Program of China [2016YFC1101201]
- Chinese National Natural Science Foundation [31600808]
- Beijing Natural Science Foundation [7164316]
- National Distinguished Young Scholars grant [31225009]
- Chinese Natural Science Foundation [31630027, 31430031]
- Chinese Academy of Sciences [XDA09030301]
- external cooperation program BIC of the Chinese Academy of Science [121D11KYSB20130006]
Ocular inflammations are common diseases that may lead to serious vision-threatening obstacles. Eye drops for antiinflammation therapy need to be administered multiple times daily at a high dosage due to the rapid precorneal removal and low bioavailability of drugs. To overcome these problems, a cRGD-functionalized DSPE-PEG(2000) nanomicelle (DSPE-PEG(2000)-cRGD) encapsulated with flurbiprofen is proposed. The tailored nanomicelles trigger specific binding to integrin receptors on the ocular surface, which leads to rapid and robust mucoadhesion, superior ocular surface retention, and transcorneal penetration behaviors of nanomicelles. Due to the enhanced drug delivery on ocular surface and in aqueous humor, the functionalized nanoformulation significantly improves ocular antiinflammation efficacy at a low dosage by blocking the synthesis of inflammatory mediators and cytokines. The present study demonstrates a promising strategy that uses a functional peptide combined with nanomicelles for targeted delivery to the eye in ophthalmologic applications.
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