Search

Various strategies for ocular drug delivery are considered; from basic formulation techniques for improving availability of drugs; viscosity enhancers and mucoadhesives aid drug retention and penetration enhancers promote drug transport into the eye. The use of drug-loaded contact lenses and ocular inserts allows drugs to be better placed where they are needed for more direct delivery. Developments in ocular implants gives a means to overcome the physical barriers that traditionally prevented effective treatment. Implant technologies are under development allowing long-term drug delivery from a single procedure, these devices allow posterior chamber diseases to be effectively treated. Future developments could bring artificial corneas to eliminate the need for donor tissue and one-off implantable drug depots lasting the patient's lifetime.

A novel nanoscale-dispersed eye ointment (NDEO) for the treatment of severe evaporative dry eye has been successfully developed. The excipients used as semisolid lipids were petrolatum and lanolin, as used in conventional eye ointment, which were coupled with medium-chain triglycerides (MCT) as a liquid lipid; both phases were then dispersed in polyvinyl pyrrolidone solution to form a nanodispersion. Single-factor experiments were conducted to optimize the formulations. A transmission electron micrograph showed that the ointment matrix was entrapped in the nanoemulsion of MCT, with a mean particle size of about 100 nm. The optimized formulation of NDEO was stable when stored for six months at 4 °C, and demonstrated no cytotoxicity to human corneal epithelial cells when compared with commercial polymer-based artificial tears (Tears Natural Forte). The therapeutic effects of NDEO were evaluated on a mouse model with 'dry eye'. Both the tear break-up time and fluorescein staining demonstrated therapeutic improvement, displaying a trend of positive correlation with higher concentrations of ointment matrix in the NDEO formulations compared to a marketed product. Histological evaluation demonstrated that the NDEO restored the normal corneal and conjunctival morphology and is safe for ophthalmic application.

There are following forms of the most frequently used ocular therapeutics: eye drops, ointments and inserts. In dependence on the physico-chemical properties of the therapeutical substance and the kind of disease one has to formulate the form of the drug in the manner to obtain its maximal bioavailability. By increasing their viscosity one can keep the watery solutions in the conjunctival sac for around 60 min. The time of the contact of the drug given in the form of suspension is limited mainly by the viscosity of the solution and the size of the molecules suspended in it. The ointments stay on the surface of the eye up to 2 hours. The ocular inserts secure a steady flow of the therapeutical substance up to 7 days. The compounds penetrate to the anterior chamber aqueous mainly through the cornea. Therefore the physiological factors of the lacrimal fluid, the properties of the cornea are influencing the penetration of the corneo-chamber barrier by the therapeutical substance.