Abstract
Article history: Recently, in situ gel formation has been extensively studied to enhance ocular bioavailability and the duration of drug activity. Poor ocular bioavailability of drugs (<1%) from conventional eye drops is mainly due to the precorneal loss factors that include rapid tear turnover, nonproductive absorption, transient residence time in the cul-de-sac, and the relative impermeability of the drugs to corneal epithelial membrane. These problems may overcome by the use of in situ gel-forming systems that are instilled as drops into the eye and undergoes sol-gel transition in the cul-de-sac. In this study, in situ gelling system of Gatifloxacin were prepared using polymers carbopol 940 (0.1% to 0.5% w/v) and HPMC E4M (0.2% to 0.6% w/v). The developed formulation was characterized for various in vitro parameters such as clarity, temperature, pH, tonicity, sterility, rheological behavior, drug release profile, transcorneal permeation profile, and ocular irritation. Developed formulation was clear isotonic solution, converted into gel at temperatures above 35 °C and pH 6.9-7.0. The results demonstrated that the carbopol/ HPMC mixture can be used as an in situ gelling vehicle to enhance the ocular bioavailability of Gatifloxacin. The developed system is a viable alternative to conventional eye drops for the treatment of Bacterial conjunctivitis and various other ocular infections.
Highlights
Most commonly available ophthalmic preparation is eye drops and ointments
In situ gelling system of Gatifloxacin were prepared using polymers carbopol 940 (0.1% to 0.5% w/v) and HPMC E4M (0.2% to 0.6% w/v)
The results demonstrated that the carbopol/ HPMC mixture can be used as an in situ gelling vehicle to enhance the ocular bioavailability of Gatifloxacin
Summary
Most commonly available ophthalmic preparation is eye drops and ointments. But the preparations when instilled into the cul-de sac are rapidly drained away from the ocular cavity due to tear flow and lachrymal nasal drainage. Several new preparations have been developed for ophthalmic use, prolong the contact time of the vehicle at ocular surface, and to slow down the elimination of the drugs. This problem can be overcome by using In-situ gel forming ophthalmic drug delivery systems, prepared from polymers that exhibit reversible phase transition and pseudo-plastic behavior to minimize interference with blinking. Treatment of bacterial conjunctivitis requires frequent administration of antibiotics as eye drops This associated with transient peaks of high drug concentration in the eye, which in turn results in undesirable side effects. Malik and Satyananda / Journal of Applied Pharmaceutical Science 4 (01); 2014: 101-104
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