Prodrugs and nanomicelles to overcome ocular barriers for drug penetration.

INTRODUCTION: Ocular barriers hinder drug delivery and reduce drug bioavailability. This article focuses on enhancing drug absorption across the corneal and conjunctival epithelium. Both, transporter targeted prodrug formulations and nanomicellar strategy is proven to enhance the drug permeation of therapeutic agents across various ocular barriers. These strategies can increase aqueous drug solubility and stability of many hydrophobic drugs for topical ophthalmic formulations. AREAS COVERED: The article discusses various ocular barriers, ocular influx, and efflux transporters. It elaborates various prodrug strategies used for enhancing drug absorption. Along with this, the article also describes nanomicellar formulation, its characteristic and advantages, and applications in for anterior and posterior segment drug delivery. EXPERT OPINION: Prodrugs and nanomicellar formulations provide an effective strategy for improving drug absorption and drug bioavailability across various ocular barriers. It will be exciting to see the efficacy of nanomicelles for treating back of the eye disorders after their topical application. This is considered as a holy grail of ocular drug delivery due to the dynamic and static ocular barriers, restricting posterior entry of topically applied drug formulations.