Mucoadhesive, antioxidant, and lubricant catechol-functionalized poly(phosphobetaine) as biomaterial nanotherapeutics for treating ocular dryness

Hoang Linh Bui, Yun Han Su, Chia Jung Yang, Chun Jen Huang*, Jui Yang Lai*

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

2 Scopus citations

Abstract

Dry eye disease (DED) is associated with ocular hyperosmolarity and inflammation. The marketed topical eye drops for DED treatment often lack bioavailability and precorneal residence time. In this study, we investigated catechol-functionalized polyzwitterion p(MPC-co-DMA), composed of 2-methacryloyloxyethyl phosphorylcholine (MPC) and dopamine methacrylamide (DMA) monomers, as potential topical nanotherapeutics for DED. The copolymers were synthesized via random free-radical copolymerization, producing different proportions of catecholic functionalization. All as-prepared polymer compositions displayed good ocular biocompatibility. At a feeding ratio of 1:1, p(MPC1-co-DMA1) can facilitate a robust mucoadhesion via Michael addition and/or Schiff base reaction, thus prolonging ocular residence time after 4 days of topical instillation. The hydration lubrication of MPC and radical-scavenging DMA endow the nano-agent to ease tear-film hyperosmolarity and corneal inflammation. A single dose of p(MPC1-co-DMA1) (1 mg/mL) after 4 days post-instillation can protect the cornea against reactive oxygen species, inhibiting cell apoptosis and the over-expression of pro-inflammatory factors (IL-6 and TNF-α). In clinical assessment, DED-induced rabbit eyes receiving p(MPC1-co-DMA1) could increase lacrimal fluid secretion by 5-fold higher than cyclosporine A. The catechol-functionalized polyzwitterion with enhanced lubricity, mucoadhesion, and anti-oxidation/anti-inflammation properties has shown high promise as a bioactive eye drop formulation for treating DED.

Original languageEnglish
Article number160
Pages (from-to)160
JournalJournal of Nanobiotechnology
Volume22
Issue number1
DOIs
StatePublished - 08 04 2024

Bibliographical note

Publisher Copyright:
© The Author(s) 2024.

Keywords

  • Biomaterial nanotherapeutics
  • Catechol
  • Multifunctional polyzwitterion
  • Ocular dryness
  • Poly(phosphobetaine)
  • Rabbits
  • Antioxidants/pharmacology
  • Lubricants
  • Anti-Inflammatory Agents
  • Catechols
  • Inflammation
  • Animals
  • Ophthalmic Solutions
  • Biocompatible Materials

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