In vitro pharmaceutical characterization and statistical optimization of a novel topically applied instantly-soluble...

Area of Science:

• Ophthalmology
• Pharmaceutics
• Materials Science

Background:

• Ocular diseases are increasing, necessitating advanced drug delivery systems.
• Topical ophthalmic drug delivery often faces challenges with conventional liquid eye drops.
• Novel formulations are required to enhance drug efficacy and patient compliance.

Purpose of the Study:

• To design and evaluate an instantly-soluble solid eye drop (ISED) for topical ophthalmic drug delivery.
• To utilize timolol maleate as a model drug for evaluating the ISED system.
• To optimize ISED properties for rapid dissolution and improved drug permeation.

Main Methods:

• Lyophilization technique was employed using hydroxypropylcellulose and pluronic® F68 as matrix-forming polymers.
• Polyacrylic acid sodium, di-glycine, and maltodextrin were incorporated to enhance solubility, prevent collapse, and improve matrix resilience.
• Statistical design was utilized to optimize texture, disintegration time, and mean dissolution time (MDT50%).

Main Results:

• A robust, rapidly disintegrating ISED was successfully produced with disintegration times as low as 0.20 seconds.
• Drug release ranged from 79% to 96%, indicating efficient drug availability.
• Enhanced corneal drug permeation was observed compared to a pure timolol dispersion.
• Maltodextrin concentration significantly impacted matrix resilience (p=0.007), while pluronic F68 strongly influenced disintegration time (p=0.000) and MDT (p=0.000).

Conclusions:

• The instantly-soluble solid eye drop (ISED) formulation demonstrates rapid dissolution and enhanced drug permeation.
• The ISED system offers a promising alternative to conventional liquid eye drops for ophthalmic drug delivery.
• This novel formulation has the potential to improve treatment outcomes for ocular diseases.