Dexamethasone (Dex) is one of the most commonly used anti-vascular endothelial growth factor (anti-VEGF) drugs being used in ocular diseases whether it is associated with anterior segment or posterior segment. For diseases of posterior segment of eye, Dex is delivered as intravitreal implant but the route used for the same is very invasive and poses several hazards on long term use. Thus, topical formulation with ability to outreach retina from ocular surface was intended. Thus, polyethylene glycolylated (PEGylated) microemulsion (ME) was attempted as it can cross the membranous barrier of eye (cornea, conjunctiva, and sclera) and remain afloat in fluidic barrier (aqueous humor, choroid, etc.) as well. Present investigation involved development of Dex-loaded PEGylated ME which was stable, non-toxic to ocular surface, capable to cross cornea and enhanced residence as well as availability of loaded drug in retina. The developed PEGylated ME had physicochemical properties like size (15.98 ± 3.05 nm), polydispersity index (0.25 ± 0.04), zeta potential (-0.04 ± 0.47 mV), percentage transmittance (99.84 ± 1.17%), and drug content (99.32 ± 3.21%). It showed sustained Dex release in in vitro conditions. It also displayed efficiency in enhancing retention of drugs in retina in in vivo pharmacokinetic study on Sprague-Dawley rats. PEGylated ME can retain the drug in retina of rats longer than simple eye drop solution via topical ocular route.
Keywords: DSPE-PEG 2000; Microemulsion; dexamethasone; posterior segment of eye; topical ocular.