Formulation And Evaluation Of Opthalmic Leciplex
DOI:
https://doi.org/10.64252/b9m88f40Keywords:
Brinzolamide, Leciplex, Timolol, Ocular drug delivery, Mucoadhesion, Box–Behnken Design, Controlled release, GlaucomaAbstract
Background: Brinzolamide is a carbonic anhydrase inhibitor used in the treatment of glaucoma, but its ocular bioavailability is limited due to rapid precorneal clearance. Enhancing its retention and controlled release in the ocular cavity may significantly improve therapeutic outcomes.
Objective: To develop and optimize a phospholipid-based cationic lecithin complex (leciplex) incorporating brinzolamide to improve ocular retention, bioavailability, and therapeutic efficacy.
Methods: Leciplex formulations were prepared via a simple one-step process using phospholipids and cationic surfactants to promote mucoadhesion through electrostatic interaction with mucin. FTIR spectroscopy confirmed drug–excipient compatibility, while DSC and XRD were used to evaluate drug encapsulation and physical state. A Box–Behnken Design (BBD) was applied for optimization using Derringer-Suich desirability function. The optimized batch (F2) was characterized for particle size, PDI, encapsulation efficiency (%EE), drug loading (%DL), and stability. In vitro drug release and stability studies under accelerated conditions were also conducted.
FTIR revealed no significant interactions between brinzolamide and excipients. DSC and XRD analyses indicated successful encapsulation and conversion of the drug to an amorphous form. The optimized batch (F2) achieved a desirability score of 0.998 and exhibited ideal particle size, narrow PDI, and high %EE and %DL. In vitro studies showed sustained release of 95.4% ± 1.1% over 8 hours, following first-order kinetics, compared to 93.8% ± 2.1% in 5 hours for the pure drug solution. The formulation remained stable with minimal variation in physicochemical properties under accelerated conditions.
Conclusion: The brinzolamide-loaded cationic lecithin complex developed in this study demonstrated enhanced mucoadhesion, controlled release, and physical stability, suggesting strong potential for improved ocular delivery in glaucoma treatment. Further in vivo and clinical studies are warranted to confirm its therapeutic benefits.
