The eye provides an interesting study in contrasts: it is a delicate structure with a transparent anterior wall as thin as 0.5mm; yet this structure in combination with the ocular adnexa provides a resilient physicochemical barrier. The lids, tears and lacrimal apparatus work in concert to continuously protect the cornea and conjunctiva with a stable tear film, which also serves as the primary refracting surface. This elaborate defence system simultaneously prevents ready intraocular access of pharmaceutical agents. Additionally, the trilaminate structure of the cornea has variable permeability to chemical agents, thereby further limiting the passage of highly hydrophobic and hydrophilic moieties. Presenting topical pharmaceutical agents to the eye via different delivery systems allows clinicians to directly affect the profile of drug bioavailability and, ultimately, bioactivity. While achieving optimum bioavailability is therapeutically important, one must simultaneously limit the occurrence of drug-induced adverse effects, both systemic and local. Utilising the different pharmacokinetic properties of drug delivery systems permits clinicians to maximise their therapeutic plans for addressing specific clinical situations while minimising the potential for adverse drug effects.