Development of Sustained-Release Ophthalmic Formulation Based on Tranilast Solid Nanoparticles

Area of Science:

• Ophthalmology
• Materials Science
• Nanotechnology

Background:

• Traditional eye drops for allergic conjunctivitis have low bioavailability due to limited conjunctival sac volume and short ocular surface residence time.
• Tranilast (TL) is an anti-allergic agent used in ophthalmic formulations, but its effectiveness is limited by poor bioavailability.
• There is a need for improved drug delivery systems to enhance the efficacy and duration of ophthalmic drugs like TL.

Purpose of the Study:

• To design and evaluate a sustained-release drug delivery system (DDS) for Tranilast (TL) nanoparticles.
• To improve the solubility, stability, and ocular surface residence time of TL.
• To investigate the potential of TL nanoparticles in a gel formulation for enhanced ophthalmic drug delivery.

Main Methods:

• Tranilast (TL) nanoparticles were prepared using bead mill treatment.
• Gel formulations containing TL nanoparticles (TL-NPs-Gel) were created using carboxypolymethylene.
• Particle size, solubility, photo/thermal stability, and drug release profiles of TL-NPs-Gel were analyzed.
• In vitro release studies were conducted to determine the sustained release over time.

Main Results:

• TL nanoparticles (50-100 nm) were successfully prepared and formulated into a gel.
• TL solubility in nanoparticle gel formulations was 5.3-fold higher than in microparticle gel formulations.
• TL-NPs-Gel exhibited enhanced photo and thermal stability compared to dissolved TL.
• Sustained release of TL from TL-NPs-Gel was observed over 180 minutes.

Conclusions:

• The developed TL nanoparticle gel formulation represents a promising sustained-release DDS for ophthalmic applications.
• This DDS significantly improves TL solubility and stability, potentially leading to enhanced therapeutic outcomes for allergic conjunctivitis.
• The findings support the development of nanoparticle-based drug delivery systems for prolonged drug action on the ocular surface.