Progress in drug formulation design and delivery of medicinal substances used in ophthalmology

Due to the very low bioavailability of drugs administered to the surface of the eyeball, issues related to the formulation of an ophthalmic drug pose a technological challenge. The essence of an ophthalmic drug is the selection of an appropriate active substance (API), but also auxiliary substances that determine the desired drug quality and API availability. The ophthalmic drug is not only classic eye drops. Therefore, on the basis of the literature data, the properties and application of auxiliary substances increasing the pharmaceutical availability of API, improving the penetration of API into the eye structures and modifying the viscosity of eye drops were characterized. The possibility of chemical modification of API and the use of prodrugs in ophthalmic drug forms was also noted. Taking into account the progress in the field of ophthalmic drug formulation, the use of multicompartment systems (lipid particles, nanoparticles, microparticles, liposomes, niosomes, dendrimers) and modern ophthalmic drug delivery systems (inserts, implants, microneedles, contact lenses, ionophoretic systems) have been indicated. Examples of solutions already used by manufacturers, as well as those in the phase of laboratory or clinical trials, were indicated.

Automated summary

Formulating ophthalmic drugs presents a technological challenge due to the low bioavailability of drugs on the surface of the eye. The selection of appropriate active substances and auxiliary substances is crucial for desired drug quality and API availability. Literature data suggests that auxiliary substances can increase pharmaceutical availability of API, enhance penetration into eye structures, and modify eye drop viscosity.