Abstract
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of a gel system. The present work describes the formulation and evaluation of an ophthalmic delivery system containing an antibacterial agent, enoxacin, based on the concept of ophthalmic sustained gel, in which 2-hydroxypropyl-beta-cyclo-dextrin (HP-beta-CD) was used as a penetration enhancer in combination with hydroxypropylmethylcellulose (Methocel F4M) which acted as a vehicle. The developed formulation was therapeutically efficacious, nonirritant, and provided sustained release of the drug over 8 h period in vitro and 7 h period in vivo. The developed system is a viable alternative to conventional eye drops.
MeSH terms
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2-Hydroxypropyl-beta-cyclodextrin
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Algorithms
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Animals
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Anti-Infective Agents / administration & dosage*
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Anti-Infective Agents / pharmacokinetics
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Anti-Infective Agents / toxicity
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Aqueous Humor
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Area Under Curve
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Chemistry, Pharmaceutical
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Cornea / chemistry
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Cornea / metabolism
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Delayed-Action Preparations
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Drug Compounding
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Enoxacin / administration & dosage*
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Enoxacin / pharmacokinetics
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Enoxacin / toxicity
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Excipients
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Eye / metabolism
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Hypromellose Derivatives
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In Vitro Techniques
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Irritants
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Linear Models
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Methylcellulose / analogs & derivatives
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Methylcellulose / chemistry
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Microdialysis
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Pharmaceutical Vehicles
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Rabbits
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beta-Cyclodextrins / chemistry
Substances
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Anti-Infective Agents
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Delayed-Action Preparations
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Excipients
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Irritants
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Pharmaceutical Vehicles
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beta-Cyclodextrins
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2-Hydroxypropyl-beta-cyclodextrin
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Enoxacin
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Hypromellose Derivatives
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Methylcellulose