Mucoadhesive micelles for the treatment of dry eye disease

Statement of Purpose: Despite topical drops being ubiquitously used for the treatment of ocular diseases, it is estimated that only ~5% of topically administered drug reaches the anterior structures of the eye. This requires frequent dosing, which can lead to patient issues including drop out and delayed clinical efficacy. This is particularly true in dry eye disease, where patients have limited treatment options that require multiple drops daily that can be painful to administer and can take months to show clinical efficacy. We previously proposed the use of mucoadhesive self-assembling micelles as a solution to these problems [1]. Phenylboronic acid (PBA) is a synthetic molecule with a strong affinity for mucin due to its ability to complex with 1,2-cis-diols and has been used previously in biomedical applications. Thus, a series of block copolymer micelles incorporating mucoadhesive PBA into their outer shells was developed capable of targeted drug delivery to ocular tissues. Here we demonstrate the efficacy of these micelles in a diseased animal model.