Ocular bioerodible minitablets as strategy for the management of microbial keratitis.
OBJECTIVE
Evaluation in volunteers of ciprofloxacin-containing ocular gelling minitablets with prolonged release properties.


METHODS
The irritation potential of ciprofloxacin-containing bioadhesive powder mixtures, used to prepare ocular bioerodible minitablets, was evaluated with a slug mucosal-irritation test. The tear pharmacokinetic profiles of ciprofloxacin were determined in six healthy volunteers after topical administration of a minitablet and a single eye drop in the lower fornix. The drug concentrations in the tear samples collected were measured by using a validated HPLC METHOD: Each volunteer was asked to give an evaluation of the preparations applied by answering a standard questionnaire.


RESULTS
The results of the mucosal-irritation test demonstrated the nonirritating properties of the bioadhesive powder mixtures. The ocular minitablet, applied in the fornix was in general well tolerated by the healthy volunteers. The mean tear concentration of ciprofloxacin was 33.0, 135.2, and 33.7 microg/g at 30, 300, and 480 minutes after application of the minitablet. Mean tear levels of 84.7, 45.6, and 8.4 microg/g were obtained at 5, 30, and 60 minutes after application of an eye drop.


CONCLUSIONS
Due to their prolonged drug release properties, the ocular minitablets containing ciprofloxacin can be considered as a promising drug delivery system to be used in the treatment of ulcerative bacterial keratitis.
Weyenberg
Wim
W
Laboratory of Pharmaceutical Technology and Biopharmacy, University of Antwerp, Antwerp, Belgium.
Vermeire
An
A
Dhondt
Marijke M M
MM
Adriaens
Els
E
Kestelyn
Philippe
P
Remon
Jean Paul
JP
Ludwig
Annick
A
D020341:Absorbable Implants; D000287:Administration, Topical; D000328:Adult; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D002939:Ciprofloxacin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003228:Conjunctiva; D003320:Corneal Ulcer / Q000382:microbiology*; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D004343:Drug Implants; D005260:Female; D005782:Gels; D006801:Humans; D007239:Infections / Q000188:drug therapy*; D008297:Male; D009883:Ophthalmic Solutions; D009994:Osmolar Concentration; D013607:Tablets; D013666:Tears / Q000378:metabolism
D000890:Anti-Infective Agents; D003692:Delayed-Action Preparations; D004343:Drug Implants; D005782:Gels; D009883:Ophthalmic Solutions; D013607:Tablets; D002939:Ciprofloxacin