PLGA Nanoparticles Containing Natural Flavanones for Ocular Inflammation

Area of Science:

• Pharmacology
• Materials Science
• Ophthalmology

Background:

• Flavanones are natural compounds with known anti-inflammatory properties.
• Poly(lactic-co-glycolic) acid (PLGA) nanoparticles (NPs) offer a promising drug delivery system.
• Ocular inflammation requires effective and safe topical therapies.

Purpose of the Study:

• To prepare and characterize PLGA nanoparticles (NP I and NP II) containing natural flavanones.
• To evaluate the potential of these flavanone-loaded NPs for topical anti-inflammatory ocular therapy.
• To assess the in vitro anti-inflammatory efficacy and safety of the NPs.

Main Methods:

• In silico analysis using Molinspiration and PASS Online.
• In vitro release studies and ex vivo permeation through porcine cornea and sclera.
• HPLC method validation, histological studies, and in vitro cytotoxicity assays in HCE-2 cells.
• Evaluation of anti-inflammatory activity by measuring IL-8 production in LPS-treated HCE-2 cells.

Main Results:

• Flavanones I and II were successfully encapsulated in PLGA NPs.
• Hyperbolic release kinetics were observed for both flavanones.
• NPs did not permeate ocular tissues but were morphologically well-tolerated.
• NP I and NP II showed no cytotoxicity up to 25 µM.
• NP I exhibited significant reduction in IL-8 production, indicating superior anti-inflammatory activity.

Conclusions:

• PLGA nanoparticles loaded with flavanones I and II are safe for ocular tissues.
• NP I demonstrates significant potential as a topical anti-inflammatory agent for ocular conditions.
• Further development of NP I could lead to novel therapies for inhibiting ocular inflammation.