Abstract
Owing to biological barriers of eye, topically administered drugs through conventional eye drops have very low ocular bioavailability and especially water-soluble drugs possess even low. Henceforth, development of novel drug delivery systems such as nanoparticles becomes unmet need. The aim of current study is to formulate water-soluble drug (Moxifloxacin) loaded nanoparticles laden in situ gel demonstrating sustained drug release, possessing efficacy against bacterial keratitis and being tolerant to eye. Formulation was optimized by statistical design of experiments, 3-level 2-factor Factorial design. Temperature induced gelation of the formulation was confirmed by its rheological behaviour, Thixotropic at physiological conditions while Newtonian at ambient temperature. In vitro diffusion study exhibited sustained drug release following Korsmeyer–Peppas model. Ex vivo efficacy study in caprine keratitis model revealed significant reduction in bacterial load, 4-logs CFU/ml in infected corneas. Histopathology of corneas confirmed reduced bacterial load and showed recovery in corneal epithelium. HET-CAM demonstrated that developed formulation is non-irritant and safe at provided dosage to cornea. It can be concluded that optimized Moxifloxacin loaded nanoparticles laden in situ gel which is transformed from solution to viscous gel in the eye sustain the drug release, possess anti-bacterial efficacy, is ocular tolerant and would further enhance ocular bioavailability.
Published Version
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