Liposome-Based Permeable Eyedrops for Effective Posterior Segment Drug Delivery

Abstract

Topical eyedrop administration is identified as an ideal non-invasive strategy for ocular drug delivery. However, multiple complex ocular barriers greatly restrict their effectiveness in the treatment of posterior ocular disease. Herein, a liposome-based permeable eyedrops (pDrops) capable of overcoming multiple ocular barriers and achieving efficient posterior drug delivery is presented. pDrops have a core-shell structure in which drugs are encapsulated inside the liposome core with a chitosan shell. This chitosan coating significantly enhances the pDrops’ binding to mucin in tears and facilitates the temporary opening of tight junctions in cornea/conjunctive epithelial cells, thereby achieving prolonged preocular retention and enhanced posterior segment drug delivery. In this study, hydrophilic ganciclovir (GCV) and hydrophobic curcumin (CUR) are employed as model drugs. Upon topical instillation, pDrops effectively overcome ocular barriers and delivered GCV to the posterior segment in both rat and rabbit eyes. Notably, CUR delivery by pDrops demonstrates significantly enhanced therapeutic efficacy in light-damaged retina of mice. Considering that pDrops can deliver both hydrophobic and hydrophilic drugs to the posterior segment of the eye, it can potentially become a feasible platform for the non-invasive delivery of various drug molecules and improve the treatment efficiency of posterior ocular diseases.