Abstract

DEVELOPMENT AND CHARACTERIZATION OF CYCLOSPORINE LOADED BIOADHESIVE NANOPARTICLES FOR THE TREATMENT OF DRY EYE

Seraj Alam Siddique*, Mohd Kalim and Ankur Yadav

ABSTRACT

Dry eye is a common disease of the tear film caused by decreased tear production or increased evaporation. Dry eye is characterized by chronic dryness of the cornea and conjunctiva which is caused by unstable tear film associated with abnormality of the lipid, protein, and mucin profiles. Changes in tear composition resulting from lacrimal dysfunction, increased evaporation, and poor clearance have pro inflammatory effects on the ocular surface. According to the Dry Eye Workshop (DEWS, 2007) report, prevalence of dry eye ranges from 5–30% in people aged 50 years and older. Prevalence of DES is estimated that about 3.2 million women and 1.7 million men, for a total of 4.9 million patients 50 years and older, have dry eye. Topical cyclosporine is currently the only and safe pharmacologic treatment of dry eye. The objective of this study was to evaluate the potential effectiveness of cyclosporine nanoparticles (NPs) for the treatment of dry eye. Cyclosporine belongs to BCS (Biopharmaceutical Classification System) Class II and a group of immunosuppressive compounds having an anti-inflammatory activity. Arginine is having positive charge and a potent vasodilator. Hyaluronic acid is having a negative charge and act as a natural lubricating agent. Therefore, when these are mixed with cyclosporine by ionic-gelation method, it leads to formation of nanoparticles, consequently improve retention time and provide controlled release. So, it will retard the evaporation of water and also improve water holding capacity of eyes. The aim of the proposed study was to develop a controlled release formulation of cyclosporine using natural bioadhesive carriers for the management of dry eye treatment. So, objectives of the proposed study was to formulate cyclosporine bioadhesive nanoparticles for dry eye treatment to achieve control release of cyclosporine from the formulation at the target site and to improve therapeutic outcome.

Keywords: Dry Eye, Chronic Dryness, Mucin Profile, Lacrimal Dysfunction, Pro Inflammatory Effects, Prevalence, Immunosuppressive Compound, Cyclosporine, Arginine, Potent Vasodilator, Hyaluronic Acid.