pH-induced in situ gelling system of an anti-infective drug for sustained ocular delivery.
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Date
2014-01
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Abstract
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.
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Keywords
pH induced in situ gel, Gatifloxacin, Carbopol 940, HPMC E50LV, HPMC E4M
Citation
Malik P H Abdul, Satyananda S. pH-induced in situ gelling system of an anti-infective drug for sustained ocular delivery. Journal of Applied Pharmaceutical Science. 2014 Jan; 4(1): 101-104.