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Establishing a Porcine Ex Vivo Cornea Model for Studying Drug Treatments against Bacterial Keratitis
Published on: May 12, 2020
Ocular bioerodible minitablets as strategy for the management of microbial keratitis
Wim Weyenberg1, An Vermeire, Marijke M M Dhondt
1Laboratory of Pharmaceutical Technology and Biopharmacy, University of Antwerp, Antwerp, Belgium.
Purpose:
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.
Insights
New ciprofloxacin ocular minitablets offer prolonged drug release for treating bacterial keratitis. These non-irritating drug delivery systems show promise for sustained therapeutic effects.
Area of Science:
- Ophthalmology
- Pharmaceutics
- Drug Delivery Systems
Background:
- Bacterial keratitis requires effective antimicrobial treatment.
- Current eye drop formulations may have limited ocular drug retention and efficacy.
- Novel drug delivery systems are needed to improve ocular drug bioavailability and therapeutic outcomes.
Purpose of the Study:
- To evaluate ciprofloxacin-containing ocular gelling minitablets for prolonged drug release.
- To assess the safety and tolerability of these novel ocular drug delivery systems in volunteers.
- To compare the tear pharmacokinetic profiles of minitablets with conventional eye drops.
Main Methods:
- The mucosal irritation potential of bioadhesive powder mixtures was assessed using a slug mucosal-irritation test.
- Tear pharmacokinetics of ciprofloxacin were determined in six healthy volunteers after topical administration of minitablets and eye drops.
- Drug concentrations in tear samples were quantified using a validated High-Performance Liquid Chromatography (HPLC) method.
Main Results:
- The bioadhesive powder mixtures exhibited non-irritating properties.
- Ocular minitablets were generally well tolerated by volunteers.
- Mean tear concentrations of ciprofloxacin were sustained for up to 480 minutes with minitablets, compared to rapid decline with eye drops.
Conclusions:
- Ciprofloxacin-containing ocular minitablets demonstrate prolonged drug release properties.
- These minitablets represent a promising drug delivery system for treating ulcerative bacterial keratitis.
- The developed system offers potential for improved therapeutic efficacy in ocular infections.
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