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Paper Information

Journal:   DARU JOURNAL OF PHARMACEUTICAL SCIENCE   FALL 2010 , Volume 18 , Number 4; Page(s) 237 To 246.
 
Paper: 

PREPARATION AND IN VITRO ANTIBACTERIAL EVALUATION OF GATIFLOXACIN MUCOADHESIVE GELLAN SYSTEM

 
 
Author(s):  KESAVAN K.*, NATH G., PANDIT JK.
 
* DEPARTMENT OF PHARMACEUTICS, INSTITUTE OF TECHNOLOGY
 
Abstract: 
Background and the purpose of the study: The poor bioavailability and therapeutic response exhibited by the conventional ophthalmic solutions due to precorneal elimination of the drug may be overcome by the use of mucoadhesive in situ gel forming systems that are instilled as drops into the eye and undergo a sol-gel transition in the cul-de-sac and have good mucoadhesion with ocular mucus layers. The objective of this study was to formulate ophthalmic mucoadhesive system of gatifloxacin (GTN) and to evaluate its in vitro antibacterial potential against, Staphylococcus aureus and Escherichia coli.
Methods: Mucoadhesive systems were prepared using gellan combined with sodium carboxymethylcellulose (NaCMC) or sodium alginate to enhance the gel bioadhesion properties. The prepared formulations were evaluated for their gelation, and rheological behaviors, mucoadhesion force, in vitro drug release, and antibacterial activity.
Results: All formulations in non-physiological or physiological conditions showed pseudoplastic behaviors. Increase in the concentration of mucoadhesive agent enhanced the mucoadhesive force significantly. In vitro release of gatifloxacin from the mucoadhesive system in simulated tear fluid (STF, pH of 7.4) was influenced significantly by the properties and concentration of gellan, sodium carboxymethyl cellulose and sodium alginate. Significant reduction in the total bacterial count was observed between drug solution (control) and mucoadhesive batches against both tested organisms. Major conclusion: The developed mucoadhesive system is a viable alternative to conventional eye drops of GTN due to its ability to enhance bioavailability through its longer precorneal residence time and ability to sustain the release of the drug.
 
Keyword(s): MUCOADHESIVE, MUCIN, RHEOLOGICAL, GELLAN GUM, SODIUM CARBOXYMETHYL CELLULOSE, SODIUM ALGINATE
 
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