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mPEG-PCL modified Caffeic acid eye drops for endotoxin-induced uveitis treatment
Yiping Wu1, Lixu Wang2, Chengda Hu3
1Eye Hospital of Shandong First Medical University, Jinan, Shandong, China.
Scientific Reports
|March 16, 2025
Summary
New caffeic acid (CA) nanoparticles (NanoCA) offer improved solubility and efficacy for treating endotoxin-induced uveitis (EIU). This non-invasive eye drop formulation enhances anti-inflammatory effects while ensuring ocular safety and tolerance.
Area of Science:
- Ophthalmology
- Nanomedicine
- Pharmacology
Background:
- Uveitis management requires modulating inflammatory mediators, but current therapies have systemic side effects.
- Caffeic acid (CA), a natural anti-inflammatory polyphenol, shows promise but has poor solubility and causes ocular irritation.
- Developing novel drug delivery systems is crucial for effective and safe uveitis treatment.
Purpose of the Study:
- To develop mPEG-PCL-modified CA-loaded nanoparticles (NanoCA) for non-invasive eye drop delivery.
- To enhance CA's solubility, bioavailability, and therapeutic efficacy in endotoxin-induced uveitis (EIU).
- To evaluate the safety and ocular tolerance of the NanoCA formulation.
Main Methods:
- NanoCA synthesized via thin-film hydration and characterized for size, zeta potential, drug loading, and release kinetics.
- Cytotoxicity assessed in human corneal epithelial and RAW264.7 cells.
- In vivo efficacy evaluated in an EIU rat model using clinical scoring, histopathology, and immunofluorescence.
Main Results:
- NanoCA formed uniform nanospheres (42.40 nm) with high encapsulation efficiency (99.17%) and sustained release over 12 hours.
- NanoCA exhibited reduced cytotoxicity compared to free CA and demonstrated excellent ocular biocompatibility without corneal damage.
- In EIU rats, NanoCA significantly suppressed inflammation, downregulated CD68 expression, and preserved aqueous barrier integrity.
Conclusions:
- mPEG-PCL-modified CA nanoparticles (NanoCA) provide a safe and effective non-invasive eye drop formulation for EIU.
- NanoCA enhances anti-inflammatory efficacy and ocular tolerance, presenting a promising alternative to conventional CA delivery.
- This nanoformulation holds potential for improved uveitis management.
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