Strategies to prolong the residence time of drug delivery systems on ocular surface

Abstract

Ocular diseases may be treated via different routes of administration, such as topical, intracameral, intravitreal, oral and parenteral. Among them the topical route is most accepted by patients, although it provides in many cases the lowest bioavailability. Indeed, when a topical formulation reaches the precorneal area, i.e., the drug absorption and/or action site, it is rapidly eliminated due to eye protection mechanisms such as blinking, basal and reflex tearing, and naso-lacrimal draining. To avoid this and to reduce the frequency of dosing, various strategies have been developed to prolong drug residence time after topical administration. These strategies include the use of viscosity increasing and mucoadhesive excipients as well as combinations thereof. From the drug delivery system point of view, liquid and semisolid formulations are preferred over solid formulations such as ocular inserts and contact lenses. Furthermore, liquid and semisolid formulations can contain nano- and microcarrier systems that contribute to a prolonged residence time. Within this review an overview about the different types of excipients and formulations as well as their performance in valid animal models and clinical trials is provided.

Keywords: Contact lenses; Eye drops; In situ gelling polymers; Liposomes; Microcarriers; Mucoadhesive excipients; Nanocarriers; Nanostructured lipid carriers (NLC); Ocular inserts; Self-emulsifying drug delivery systems; Semisolid formulations; Solid lipid nanoparticles (SLN).