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Antimicrobial Agents and Chemotherapy, September 2004, p. 3396-3401, Vol. 48, No. 9
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.9.3396-3401.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

A Mucoadhesive Polymer Extracted from Tamarind Seed Improves the Intraocular Penetration and Efficacy of Rufloxacin in Topical Treatment of Experimental Bacterial Keratitis

Emilia Ghelardi,1* Arianna Tavanti,1 Paola Davini,1 Francesco Celandroni,1 Sara Salvetti,1 Eva Parisio,1 Enrico Boldrini,2 Sonia Senesi,1 and Mario Campa1

Dipartimento di Patologia Sperimentale, Biotecnologie Mediche, Infettivologia ed Epidemiologia, Università di Pisa,1 Farmigea S.p.A., Pisa, Italy2

Received 3 November 2003/ Returned for modification 5 February 2004/ Accepted 19 May 2004

Bacterial keratitis is a serious infectious ocular disease requiring prompt treatment to prevent frequent and severe visual disabilities. Standard treatment of bacterial keratitis includes topical administration of concentrated antibiotic solutions repeated at frequent intervals in order to reach sufficiently high drug levels in the corneal tissue to inhibit bacterial growth. However, this regimen has been associated with toxicity to the corneal epithelium and requires patient hospitalization. In the present study, a mucoadhesive polymer extracted from tamarind seeds was used for ocular delivery of 0.3% rufloxacin in the treatment of experimental Pseudomonas aeruginosa and Staphylococcus aureus keratitis in rabbits. The polysaccharide significantly increased the intra-aqueous penetration of rufloxacin in both infected and uninfected eyes. Rufloxacin delivered by the polysaccharide reduced P. aeruginosa and S. aureus in the cornea at a higher rate than that obtained by rufloxacin alone. In particular, use of the polysaccharide allowed a substantial reduction of S. aureus in the cornea to be achieved even when the time interval between drug administrations was extended. These results suggest that the tamarind seed polysaccharide prolongs the precorneal residence times of antibiotics and enhances drug accumulation in the cornea, probably by reducing the washout of topically administered drugs. The tamarind seed polysaccharide appears to be a promising candidate as a vehicle for the topical treatment of bacterial keratitis.

* Corresponding author. Mailing address: Dipartimento di Patologia Sperimentale, Biotecnologie Mediche, Infettivologia ed Epidemiologia, Università di Pisa, Via S. Zeno 37, 56127 Pisa, Italy. Phone: (39) 050 2213699. Fax: (39) 050 2213711. E-mail: ghelardi{at}biomed.unipi.it.

Antimicrobial Agents and Chemotherapy, September 2004, p. 3396-3401, Vol. 48, No. 9
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.9.3396-3401.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.





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