Ocular Self-Microemulsifying Drug Delivery System of Prednisolone Improves Therapeutic Effectiveness in the Treatment of Experimental Uveitis.

Abstract

PURPOSE: The purpose of this study was to investigate the self-microemulsifying drug delivery systems (SMEDDS) for ophthalmic delivery of Prednisolone (PDN) to treat uveitis. MATERIALS AND METHODS: The pseudo-ternary phase diagrams were developed, and various SMEDDS were prepared using Linoleic acid as oil, Cremophore RH 40 as a surfactant, and propylene glycol as a co-surfactant. Physicochemical parameters (globule size, zeta potential, viscosity, and pH) and in vitro release of SMEDDS were studied. The in vivo efficacy of prepared formulations and the marketed drug solution was studied by administering them topically to an endotoxin-induced uveitis rabbit model. RESULTS: All formulations displayed an average globule size less than 100 nm. The developed SMEDDS exhibited acceptable physicochemical behavior and displayed sustained drug release. In vivo studies in a rabbit eye showed a marked improvement in the anti-inflammatory activity of developed formulation compared with a marketed formulation in a uveitis-induced rabbit eye model. CONCLUSIONS: The developed SMEDDS are a feasible option to conventional eye drops for its capability to improve bioavailability via its longer precorneal residence time and its capacity to sustain the release of the drug.