Barrier Properties of the Human Eye and the Need for Novel Formulations, Drug Delivery Technologies and Medical Devices to Combat Age-Related Sight Loss

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmaceutical Technology, Manufacturing and Devices".

Deadline for manuscript submissions: closed (30 November 2023) | Viewed by 6157

Special Issue Editors


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1. Faculty of Science, Engineering and Computing, Kingston University London, Penrhyn Road, Kingston upon Thames, London KT1 2EE, UK
2. Faculty of Medical and Health Sciences, The University of Auckland, Auckland CBD, Auckland 1010, New Zealand
Interests: ophthalmic drugs and delivery systems; veterinary pharmaceuticals
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Guest Editor
UCL School of Pharmacy, 29-39 Brunswick Square, Bloomsbury, London WC1N 1AX, UK
Interests: formulation of proteins; ocular drug delivery; implantable devices; in vitro models

E-Mail Website
Guest Editor
Auckland University of Technology, 55 Wellesley Street East, Auckland CBD, Auckland 1010, New Zealand
Interests: implants; nano- and microcapsules; 3D printing for biomedical applications; veterinary medicines

Special Issue Information

Dear Colleagues,

The size of the global ophthalmic drugs market is expected to reach USD 43.1 billion by 2026. Finding efficient alternatives to conventional eye drops and intravitreal injections is desirable. The delivery of drugs and biologics to the ocular surface, anterior chamber, and posterior segment of the eye poses formidable challenges due the unique physiological and pharmacological constraints of the human eye. With the global rise of the elderly population, conditions such as cataract, presbyopia, glaucoma, dry eye, age-related macular degeneration, keratitis, and diabetic retinopathy are becoming ever more prevalent. Low ocular bioavailability along with poor patient adherence are characteristic of the topical ocular hypotensive eye drops that are routinely used in glaucoma management. Recurrent intravitreal injections of the costly anti-VEGF medications, regulatory and clinical challenges associated with the emergence of various biosimilars and the cost associated with developing sophisticated devices that can target and deliver their cargo to inaccessible locations such as the macula, choroid, retina, and optic disc are amongst the numerous challenges facing those working in the field. The emergence of new technologies of controlled and continuous drug release, 3D printing, polymeric scaffolds, contact lenses, punctal plugs, and ambitious devices that would allow simultaneous bidirectional delivery of drugs to the front and back of the eye is exciting and promising. Better understanding of the fundamentals, and the integration of basic formulation and drug delivery science with clinical knowledge could give rise to new modalities that improve patient outcomes. This Special Issue focuses on the barrier properties of the human eye and the need for novel formulations, drug delivery technologies, and medical devices to combat age-related sight loss.

Prof. Dr. Raid Alany
Prof. Dr. Steve Brocchini
Dr. Ali Seyfoddin
Guest Editors

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Keywords

  • ocular drug delivery
  • ophthalmic medication
  • corneal/scleral penetration
  • vitreous drug delivery
  • 3D printing
  • hydrogels
  • scaffolds
  • ocular implants
  • colloidal and nanoparticulate drug carriers
  • controlled drug release

Published Papers (2 papers)

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Research

15 pages, 3670 KiB  
Article
The Protective Effect of Topical Spermidine on Dry Eye Disease with Retinal Damage Induced by Diesel Particulate Matter2.5
by Hyesook Lee, Da Hye Kim, Hyun Hwangbo, So Young Kim, Seon Yeong Ji, Min Yeong Kim, Jung-Hyun Shim, Sun-Hee Leem, Jin Won Hyun, Gi-Young Kim and Yung Hyun Choi
Pharmaceutics 2021, 13(9), 1439; https://doi.org/10.3390/pharmaceutics13091439 - 10 Sep 2021
Cited by 7 | Viewed by 2459
Abstract
Air pollutants, especially ambient fine particulate matter2.5, may contribute to various ocular surface disorders, including dry eye disease, keratitis and conjunctivitis. A natural polyamine spermidine has a protective effect on the retina and optic nerve; however, no study has been conducted on the [...] Read more.
Air pollutants, especially ambient fine particulate matter2.5, may contribute to various ocular surface disorders, including dry eye disease, keratitis and conjunctivitis. A natural polyamine spermidine has a protective effect on the retina and optic nerve; however, no study has been conducted on the application of spermidine in particulate matter2.5-induced dry eye disease. In the present study, we investigated the effect of spermidine eye drops in topically exposed particulate matter2.5-induced dry eye models of Sprague-Dawley rats, by hematological, biochemical and histological evaluation. Spermidine eye drops attenuated the particulate matter2.5 exposure-induced reduction of tear secretion and corneal epithelial damage. Furthermore, spermidine protected against conjunctival goblet cell loss and retinal ganglion cell loss induced by particulate matter2.5. Additionally, spermidine markedly prevented particulate matter2.5-induced infiltration of cluster of differentiation3+ and cluster of differentiation4+ T lymphocytes and F4/80+ macrophages on lacrimal gland. Moreover, over expression of pro-inflammatory cytokines, including tumor necrosis factor-α, interleukin-6 and interleukin-17 in the lacrimal gland and cornea. Meanwhile, the levels of serum total cholesterol and low-density lipoprotein cholesterol were markedly increased by topical exposure to particulate matter2.5, but this change in the lipid profile was decreased by spermidine. Taken together, spermidine may have protective effects against particulate matter2.5-induced dry eye symptoms via stabilization of the tear film and suppression of inflammation and may in part contribute to improving retinal function and lipid metabolism disorder. Full article
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17 pages, 3664 KiB  
Article
Curcumin In Situ Gelling Polymeric Insert with Enhanced Ocular Performance
by Hamdy Abdelkader, David Wertheim, Barbara Pierscionek and Raid G. Alany
Pharmaceutics 2020, 12(12), 1158; https://doi.org/10.3390/pharmaceutics12121158 - 28 Nov 2020
Cited by 17 | Viewed by 2748
Abstract
The search for an ocular drug delivery system that could provide long-acting effects without a detriment to the anatomy and physiology of the eye remains a challenge. Polyphenolic compounds (curcumin in particular) have recently gained popularity due to their powerful antioxidant properties; yet [...] Read more.
The search for an ocular drug delivery system that could provide long-acting effects without a detriment to the anatomy and physiology of the eye remains a challenge. Polyphenolic compounds (curcumin in particular) have recently gained popularity due to their powerful antioxidant properties; yet curcumin suffers poor stability and water solubility. A conventional eye drop formulation of curcumin in the form of a suspension is likely to suffer a short duration of action requiring multiple instillations. On the other hand, polymeric in-situ gelling inserts offer the prospect of overcoming these limitations. The aim of this study was to prepare, characterize and evaluate in vivo, polymeric, in-situ gelling and mucoadhesive inserts for ocular surface delivery of curcumin. Different types and ratios of biocompatible polymers (HPMC, CMC, PL 127 and PVA) and three plasticizers along with the solvent casting method were adopted to prepare curcumin inserts. The inserts were investigated for their physicochemical characteristics, applicability, and suitability of use for potential placement on the ocular surface. The prepared inserts revealed that curcumin was mainly dispersed in the molecular form. Insert surfaces remained smooth and uniform without cracks appearing during preparation and thereafter. Improved mechanical and mucoadhesive properties, enhanced in vitro release (7.5- to 9-fold increases in RRT300 min) and transcorneal permeation (5.4- to 8.86-fold increases in Papp) of curcumin was achieved by selected in-situ gelling inserts compared to a control curcumin suspension. The developed inserts demonstrated acceptable ocular tolerability, enhanced corneal permeability, and sustained release of curcumin along with retention of insert formulation F7 on the ocular surface for at least two-hours. This insert provides a viable alternative to conventional eye drop formulations of curcumin. Full article
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