Abstract

Ocular drug delivery is challenging due to the presence of anatomical and physiological barriers. These barriers can affect drug entry into the eye following multiple routes of administration (e.g., topical, systemic, and injectable). Topical administration in the form of eye drops is preferred for treating anterior segment diseases, as it is convenient and provides local delivery of drugs. Major concerns with topical delivery include poor drug absorption and low bioavailability. To improve the bioavailability of topically administered drugs, novel drug delivery systems are being investigated. Nanocarrier delivery systems demonstrate enhanced drug permeation and prolonged drug release. This review provides an overview of ocular barriers to anterior segment delivery, along with ways to overcome these barriers using nanocarrier systems. The disposition of nanocarriers following topical administration, their safety, toxicity and clinical trials involving nanocarrier systems are also discussed.

Highlights

  • The human eye is a complex organ with intricate anatomical and physiological barriers

  • Prominent diseases affecting the posterior segment of the eye include age-related macular degeneration (AMD), diabetic retinopathy macular edema (DME), proliferative vitreoretinopathy (PVR), posterior uveitis, and cytomegalovirus (CMV) [1]

  • The study reported that in human cornea efflux transporters including MRP1–4, MRP6 were localized in the basal layer of corneal epithelium, whereas MRP7 and MDR1 were expressed in the entire corneal epithelium

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Summary

Introduction

The human eye is a complex organ with intricate anatomical and physiological barriers. Drug delivery to the anterior segment of the eye via the topical route typically involves the conventional dosage forms, such as solutions (62.4%), suspensions (8.7%), and ointments (17.4%), which compose an estimated 90% of marketed ophthalmic formulations. Topical drug administration demonstrates poor ocular bioavailability (

Metabolism in Ocular Tissues
Tear Turnover
Nasolacrimal Drainage
Efflux Pumps
Nanocarriers for Anterior Segment Drug Delivery
Microemulsions
Nanosuspensions
Liposomes
Surfactant Nanomicelles
Polymeric Nanomicelles
Polyion Complex Nanomicelles
Nanoparticles
3.12. Nanowafers
Disposition of Nanocarriers Following Topical Application
Nanocarriers in Clinical Trials
Safety and Toxicity of Nanocarrier Systems
Findings
Conclusions
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