Abstract
The objective of this study was to formulate sodium alginate based ophthalmic mucoadhesive system of gatifloxacin and its in vitro antibacterial potential on pathogenic microorganisms, Staphylococcus aureus and Escherichia coli. Sodium carboxymethylcellulose (NaCMC) was added to the formulations to enhance the gel bioadhesion properties. The prepared formulations were evaluated for their in vitro drug release, gelation behaviour, rheological behavior, and mucoadhesion force. All formulations in non-physiological and physiological condition showed pseudo plastic behavior. Increase in the concentration of sodium alginate and sodium CMC enhanced the mucoadhesive force significantly. In vitro release of gatifloxacin from the system in simulated tear fluid (STF, pH – 7.4), was influenced significantly by the properties and concentration of sodium alginate, NaCMC. Significant reduction in total bacterial count was observed between control and treatment groups with both the test organisms.
Highlights
The design of an ocular dosage form which prolongs the precorneal residence time of the drug and enhances the corneal permeation is an exciting challenge
The objective of the present work was to develop a mucoadhesive system of Gatifloxacin (GTN), a fluroquinolone derivative used in external infections of the eye using sodium alginate alone and in combination with sodium carboxymethyl cellulose, which would undergo gelation when instilled into the cul-de-sac of the eye and provide prolonged retention on the external ocular surface by a combination of gelation and mucoadhesivity of the formulation
The results clearly showed that the mucoadhesive system has the ability to retain gatifloxacin in its matrix network and that premature drug release will not occur
Summary
The design of an ocular dosage form which prolongs the precorneal residence time of the drug and enhances the corneal permeation is an exciting challenge. Incorporation of soluble polymers into an aqueous solution can be applied to extend the drug residence time, thereby prolonging drug absorption. When adding mucoadhesive polymers to the formulation to prolong the precorneal residence time of ocular dosage forms, some special features, which are characteristic for ocular drug delivery, have to be taken into consideration. In ocular drug delivery, less than 2 min are available for drug absorption after instillation of a drug solution into the eye, since it is removed rapidly by solution drainage; the ability to extend the contact time of a topically delivered drug would undoubtedly improve drug bioavailability
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