Formulation and Evaluation of Nanoparticulate for Safe and Effective Treatment of Dry Eye Syndrome

Abstract

Dry eye disease (DED) is a highly common ocular surface condition affecting a significant newlinenumber of individuals globally. It is characterized by the elevated osmolarity of the tear newlinefilm and inflammation of the ocular surface. Existing treatment approaches for dry eye newlinedisorder, such as lubricating eye drops and anti-inflammatory drugs, may offer temporary newlinerelief by moisturizing the eyes and reducing inflammation. Although, they may not newlineeffectively address the root causes of dry eye syndrome. Rebamipide ophthalmic newlinesuspension addresses the root cause of the dry eye condition by promoting the production newlineof mucins in the tear film. However, its short ocular residence time necessitates frequent newlineadministration to achieve the desired therapeutic effect. The present study aims to newlineinvestigate the preparation and evaluation of rebamipide nanosuspension (REB-NS), which newlinecan offer enhanced ophthalmic bioavailability and prolonged drug release for dry eye newlineconditions. Rebamipide nanosuspension was formulated by solvent diffusion and probe newlinesonication method using chitosan and hydroxypropyl methylcellulose as the mucoadhesive newlinecomponents, and poloxamer 188 was incorporated into the formulation to enhance newlinestability. Box Behnken Designs (BBD) methodology was employed to optimize newlinerebamipide nanosuspension. The optimized formulation underwent characterization to newlineassess its particle size, charge, entrapment effectiveness, TEM analysis, permeability newlinestudies, and drug release profile. The optimized formulation showed a particle size of 196 newlinenm, a polydispersity index of 0.188, and the entrapment efficiency was found to be 87%. newlineIn-vitro release studies on REB-NS demonstrated a sustained drug release profile that newlineextended for 24 hours. The results showed that the cumulative drug release reached newline84.67% over the entire testing period and the Peppas Korsmeyer model provided the best newlinefit for the observed release profile. The ex-vivo permeation studies demonstrated that drug permeation through the cornea reached 86.7% over 8 hours.