Development of topical chitosan/ β-glycerophosphate-based hydrogel loaded with levofloxacin in the treatment of keratitis: An ex-vivo study

Abstract

Staphylococcus species are responsible for most cases of post-operative endophthalmitis. Topical ocular drug was applied for post-operative infection prevention, but the way of delivery encounters many challenges in terms of patient's compliance, drug efficacy, and drug penetration. We used the levofloxacin-loaded chitosan/gelatin/ β-glycerophosphate hydrogel sustained releasing system with good in vitro anti-bacterial efficacy and biocompatibility, which we had previously designed, for ex vivo keratitis model to test the preclinical drug efficacy and to determine drug level in the anterior chamber of the eye. The result showed that the ex-vivo corneal keratitis model with S. aureus infection revealed mild opacity over the central cornea with stromal infiltrate, but without obvious stromal infiltration post levofloxacin-loaded hydrogel treatment after 24 h of infection. Quantification of viable bacteria showed a significant anti-bacterial activity. The histological evidence also showed no visible S. aureus after levofloxacin-loaded hydrogel treatment, with a significant anti-inflammatory effect. We also examined the drug concentration in the aqueous humor 24 h after instilling one drop of the levofloxacin-loaded hydrogel. The concentration achieved to a desired drug level. These results suggested that by the ex-vivo model, levofloxacinloaded hydrogel can be applied for treatment in post-operative endophthalmitis or keratitis after the ophthalmic surgery.

Antimicrobial Natural Hydrogels in Biomedicine: Properties, Applications, and Challenges—A Concise Review

“…It was demonstrated that the obtained hydrogel significantly inhibited bacterial growth indeed, with no histological evidence of the bacteria in the studied ex vivo rabbit model of keratitis. Moreover, the hydrogel exhibited remarkable anti-inflammatory effects and sustained release of levofloxacin [112]. In another study, the delivery of levofloxacin from hyaluronic acid nanohydrogels for the treatment of bacterial intracellular infections studied by Montanari et al The minimal inhibitory concentration values for Staphylococcus aureus and Pseudomonas aeruginosa were compared with pure and hydrogel-loaded levofloxacin-loaded nanohydrogels indicating the increase in antibacterial efficacy of the latter.…”

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