FORMULATION AND EVALUATION OF SUSTAINED RELEASE IN-SITU GEL OF AMIKACIN BY USING 32 FULL FACTORIAL DESIGN

Objectives: This work aimed to formulate and evaluate amikacin, fourth-generation fluoroquinolone antibiotic agent containing an in-situ gelling system based on sol-to-gel transition for ophthalmic delivery to overcome the problems of poor bioavailability and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Methods: In the present work, poloxamer 407 as a temperature-activated gelling agent and gelrite as an ion activated gelling agent were used in combination to prepared ion-sensitive and temperature-sensitive ophthalmic in-situ gel. The prepared formulations were evaluated for the parameters like pH, appearance, drug content, in-vitro gelation study, viscosity, in-vitro release study, sterility test, and stability studies. Results: In this study, the release profile depends on the concentration of gelrite and poloxamer 407. The selected formulation showed sustained release for a period of 10 h. Thus it showed increased residence and contact time with the eye. The draize test was performed with an optimized formulation for eye irritation test. It was found to be non-irritant to the rabbit eye. The in-situ gelling system showed favorable results in all studies. Conclusion: The results indicate that the formulation can be considered as a better option than conventional ophthalmic drops.