Abstract

Objective: The purpose of the study was to formulate and evaluate thiolated chitosan based nanoparticulate mucoadhesive ophthalmic in situ gelling system of prulifloxacin for bacterial keratoconjunctivitis.

Method: Low molecular weight chitosan was modified to thiolated chitosan in the laboratory and confirmed with FTIR and DSC studies. Thiolated chitosan nanoparticles were prepared and incorporated in a polymeric sol-gel system containing prulifloxacin for the ophthalmic drug delivery. The prepared formulation was characterized for the various physicochemical properties i.e., particle size, zeta potential, gelation time, mucoadhesion strength study and the optimized formulation was characterized for in vitro drug release study, ocular irritation study, antimicrobial efficacy study and stability study etc.

Results: Gelation pH was found to be 7.2±0.2. The acquired SEM images of the optimized NPs showed good mean particle size below 16 nm. Drug entrapment efficiency was found to be more than 80%. PFL-TCS loaded NPs sol-gel system showed sustain release for a period of 12 hours. It was also confirmed that the formulation was non-irritant to the eye.

Conclusion: The developed formulation was found to be a better alternative to the conventional ophthalmic formulations.

Keywords: Thiolated chitosan, in situ gel, nanoparticles, ophthalmic, mucoadhesive, prulifloxacin.

Graphical Abstract