The aim of this project was to explore novel strategies to optimize the delivery of low and high-molecular-weight drugs in the anterior and posterior segments of the eye such as the use of nanoformulations, chemical modification of drug properties and physical enhancement strategies to improve the treatment of ocular diseases. Chapter I presents a literature review on the fascinating anatomy of the eye, the different routes of ocular administration of drugs and the challenges and strategies to reach the anterior and posterior segments are presented. Chapters II and III present different strategies to improve the treatment of fungal keratitis. Chapter II describes the formulation of triple antifungal nanosystems (micelles and liposomes) containing Natamycin (NAT), voriconazole (VOR) and caspofungin acetate (CAS) to assess their potential for simultaneous drug delivery into the cornea and anterior segment of the eye. In Chapter III a second approach to improve the treatment of fungal keratitis was explored with the use of iontophoresis to increase CAS delivery to the anterior and posterior portions of the eye. Chapter IV explores the use of the prodrug approach to obtain aciclovir derivatives with suitable characteristics (charge and high aqueous solubility) to be transported across ocular membranes by iontophoresis. Finally, the results obtained in Chapter V demonstrate that the use of iontophoresis is not limited to small molecules, as it was shown that the transscleral delivery of a small protein - Cyt c - can be modulated by modifying the iontophoretic conditions. The different strategies presented in this work are promising options to improve the treatment of ophthalmic diseases.