Open AccessNanomicelle‐Assisted Targeted Ocular Delivery with Enhanced Antiinflammatory Efficacy In Vivo
Author(s) -
Weng YuHua,
Ma XiaoWei,
Che Jing,
Li Chan,
Liu Juan,
Chen ShiZhu,
Wang YuQin,
Gan YaLing,
Chen Hao,
Hu ZhongBo,
Nan KaiHui,
Liang XingJie
Publication year - 2018
Publication title -
advanced science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.388
H-Index - 100
ISSN - 2198-3844
DOI - 10.1002/advs.201700455
Subject(s) - mucoadhesion , flurbiprofen , drug delivery , bioavailability , in vivo , aqueous humor , pharmacology , medicine , drug , nasal administration , drug carrier , nanotechnology , ophthalmology , materials science , microbiology and biotechnology , biology
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.