Sustained ophthalmic delivery of Ciprofloxacin Hydrochloride from an ion-activated in situ gelling system

[摘要] Most eye diseases are treated with topical application of eye drops. The poor bioavailability and therapeutic response exhibited by these conventional eye drops due to rapid precorneal elimination of the drug may be overcome by the use of in situ gelling systems that are instilled as drops into the eye and undergo a sol-to-gel transition in the cul-de-sac. Hence, the purpose of the present work was to formulate and evaluate an ophthalmic delivery system for the ciprofloxacin hydrochloride, based on the concept of ionic interaction approach for in situ gelation. Sodium alginate was used as the gelling agent in combination with Hydroxy Propyl Methyl Cellulose (HPMC K4M) which acted as a viscosity enhancing agent. The prepared formulations were characterized for clarity, pH, drug content, viscosity, gelling capacity, in vitro drug release, antimicrobial efficacy, ocular irritation and stability. The clarity, pH viscosity and drug content of the developed formulation were found to be satisfactory. The developed formulation was therapeutically efficacious, stable, non-irritant, and provided sustained drug release over an 8-h period. The developed formulation is a viable alternative to conventional eye drops by virtue of its ability to enhance bioavailability through its longer precorneal residence time and ability to produce sustained drug release. Also important factor is the ease of instillation and the reduced frequency of instillation resulting in better patient acceptance.

[学科分类] 药理学