Although the eye is an accessible organ for direct drug application, ocular drug delivery remains a major challenge due to multiple barriers within the eye. Key barriers include static barriers imposed by the cornea, conjunctiva, and retinal pigment epithelium and dynamic barriers including tear turnover and blood and lymphatic clearance mechanisms. Systemic administration by oral and parenteral routes is limited by static blood-tissue barriers that include epithelial and endothelial layers, in addition to rapid vascular clearance mechanisms. Together, the static and dynamic barriers limit the rate and extent of drug delivery to the eye. Thus, there is an ongoing need to identify novel delivery systems and approaches to enhance and sustain ocular drug delivery. This chapter summarizes current and recent experimental approaches for drug delivery to the anterior and posterior segments of the eye.