Nanotechnology-based penetration enhancers provide novel mechanisms to improve current drug delivery methodologies. New developments in this field have been shown to overcome previous difficulties of ocular therapeutics like anatomical barriers and filtration mechanisms. Furthermore, nanoparticles exhibit additional benefits as a drug carrier, such as protection of drugs against degradation, biocompatible carrier structures, or reduction of adverse or immunological effects. Penetration enhancers exhibit great promise in ophthalmology. While much of the current research in the field surrounds lipid-based nanotechnologies, other innovative works have expanded the spectrum of ocular drug delivery.