Abstract

Currently, ocular inserts and nanoparticles have received much attention due to the limited bioavailability of conventional eye preparations and the toxicity problems of systemic drug administration. The current systematic review aims to present recent studies on the use of electrospun nanofiber-based ocular inserts to improve the bioavailability of drugs used for different ophthalmic diseases. A systematic search was performed in PubMed, Ovid Medline, Web of Science, ScienceDirect, Scopus, Reaxys, Google Scholar, and Google Patents/Espacenet taking “drug-loaded”, “nanofibers”, and “ophthalmic inserts” and their equivalent terms as keywords. The search was limited to original and peer-reviewed studies published in 2011–2021 in English language. Only 13 out of 795 articles and 15 out of 197 patents were included. All results revealed the success of nanofiber-based ocular inserts in targeting and improved bioavailability. Ocular inserts based on nanofibers can be used as safe, efficient carriers for the treatment of anterior and posterior eye diseases.

Highlights

  • The unique anatomy and physiology of the eye, because of the physical and blood barriers, makes the targeting of ocular diseases a very difficult and challenging process [1,2].These barriers interfere with drug absorption and diminish the drug concentration in the eye due to dilution and early drainage through lacrimation and poor permeation due to the effect of blood-retinal and blood-aqueous barriers [3,4,5]

  • Zealand albino rabbits and some in vitro models are used to study eye toxicity, and the results revealed no or lower eye toxicity

  • The results showed the possibility of modulating the drug release from a few minutes up to a month based on the polymer base used and the properties of nanofibers, and the majority of studies showed controlled drug release

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Summary

Introduction

The unique anatomy and physiology of the eye, because of the physical and blood barriers, makes the targeting of ocular diseases a very difficult and challenging process [1,2] These barriers interfere with drug absorption and diminish the drug concentration in the eye due to dilution and early drainage through lacrimation and poor permeation due to the effect of blood-retinal and blood-aqueous barriers [3,4,5]. The most frequently used method is administration of drugs through the conventional topical route, which is characterized by being non-invasive, easy to self-administer, and more acceptable to patients It can only be used for the treatment of diseases affecting the surface and anterior segment of the eye, because it has poor bioavailability (less than about 5% of the drug is retained on the ocular surface). Direct administration of the drug to the site of action with lower bioavailability can be done invasively based on intraocular routes [6], with intravitreal injection being the most promising for targeting posterior diseases, but it can be accompanied by retinal detachment, increased intraocular pressure, intravitreal hemorrhage, cataract, or endophthalmitis, which results in poor patient adherence [2,12]

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