Methods and compositions are provided for treating an ocular disease in a subject in need thereof by increasing the bioavailability of a drug in the subjects eye. By one approach, the ocular disease is endophthalmitis. The methods and compositions provided herein include an efflux transporter inhibitor and a drug effective for treating the ocular disease. The efflux transporter inhibitor is effective to reduce the efflux of the drug through at least one of Pglycoprotein (Pgp), breast cancer resistant protein (BCRP), and multidrug resistant associated protein 19 (MRP19). In one aspect, cyclosporine A is the efflux transporter inhibitor.
