Nanomicelle-Assisted Targeted Ocular Delivery with Enhanced Antiinflammatory Efficacy In Vivo

Yu Hua Weng, Xiao Wei Ma, Jing Che, Chan Li, Juan Liu, Shi Zhu Chen, Yu Qin Wang, Ya Ling Gan, Hao Chen, Zhong Bo Hu*, Kai Hui Nan, Xing Jie Liang

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

66 Citations (Scopus)

Abstract

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-PEG2000 nanomicelle (DSPE-PEG2000-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.

Original languageEnglish
Article number1700455
JournalAdvanced Science
Volume5
Issue number1
DOIs
Publication statusPublished - Jan 2018
Externally publishedYes

Keywords

  • antiinflammation
  • flurbiprofen nanomicelles
  • functional peptide
  • ocular delivery system

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Weng, Y. H., Ma, X. W., Che, J., Li, C., Liu, J., Chen, S. Z., Wang, Y. Q., Gan, Y. L., Chen, H., Hu, Z. B., Nan, K. H., & Liang, X. J. (2018). Nanomicelle-Assisted Targeted Ocular Delivery with Enhanced Antiinflammatory Efficacy In Vivo. Advanced Science, 5(1), Article 1700455. https://doi.org/10.1002/advs.201700455