Development and optimization of controlled release bioerodable anti infective ophthalmic insert

Area of Science:

• Ophthalmology
• Pharmaceutics
• Drug Delivery

Background:

• Ophthalmic infections require sustained drug delivery for improved efficacy.
• Traditional eye drops offer short drug residence times, leading to frequent administration.
• Bioerodable inserts present a promising approach for prolonged ocular drug release.

Purpose of the Study:

• To formulate and optimize a bioerodable Azithromycin insert.
• To enhance ocular availability and prolong the release of Azithromycin.
• To evaluate the physicochemical, in-vitro release, and stability characteristics of the optimized insert.

Main Methods:

• A modified solvent casting method was employed using Hydroxyl Propyl Methyl Cellulose (HPMC) and Eudragit RL100.
• Formulations were evaluated for physical properties, drug content, and in-vitro drug release.
• Kinetic studies (zero order, first order, Higuchi, Korsmeyer-Peppas) and stability assessments were conducted.

Main Results:

• Optimized formulation H8 (1.5% HPMC, 3% Eudragit RL100) showed excellent uniformity, acceptable surface pH, and high folding endurance.
• In-vitro release studies demonstrated sustained drug release over 12 hours, achieving 99% drug release.
• The optimized insert exhibited a long shelf life (622 days) and superior ocular tolerability compared to the pure drug.

Conclusions:

• The optimized bioerodable Azithromycin insert provides sustained and controlled drug release for ophthalmic applications.
• The non-Fickian diffusion mechanism ensures prolonged therapeutic effect, reducing administration frequency.
• This novel formulation holds significant potential for effectively treating a broad spectrum of ocular infections.