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Pharmaceutics
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Nanotechnology in Ocular Drug Delivery
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Nanotechnology in Ocular Drug Delivery

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (31 August 2022) | Viewed by 23123

Special Issue Editors

Dr. Priyanka Agarwal

E-Mail Website
Guest Editor
Buchanan Ocular Therapeutics Unit, Department of Ophthalmology, University of Auckland, Auckland 1142, New Zealand
Interests: ocular drug delivery; non-aqueous; eye drops; dry eye disease; topical
Prof. Dr. Thakur Raghu Raj Singh

E-Mail Website
Guest Editor
Chair in Pharmaceutics, McClay Research Centre, School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, UK
Interests: long-acting drug delivery systems; microneedles; ocular drug delivery; polymer/peptide synthesis; 3D printing

Special Issue Information

Dear Colleagues,

The eye, although seemingly easy to access, is a complex and dynamic organ that presents unique challenges for drug delivery. With formidable tissue barriers and a rich perfusion of blood vessels, the eye significantly restricts the entry of foreign substances; meanwhile, due to its vulnerable nature, the toxicity and irritation potential of conventionally used formulations and excipients are often heightened. As such, ocular drug delivery is essentially a compromise between safety and efficacy.  

In recent years, “nanomedicine” has been extensively investigated due to its proposed advantages of sustained and targeted drug delivery, reduced adverse effects, and enhanced bioavailability of hydrophobic and hydrophilic drugs, macromolecules, proteins, and peptides as well as biological vectors, including genes and antibodies. Thus, nanotechnology may facilitate the delivery of ocular therapeutics in clinically relevant concentrations to the anterior, and possibly even posterior, ocular tissues.  

This Special Issue highlights new and emerging research in nanomedicine for both the topical and intraocular administration of ocular therapeutics and its application in the treatment and management of ocular pathologies.

Dr. Priyanka Agarwal
Prof. Dr. Thakur Raghu Raj Singh
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • nanotechnology
  • ocular drug delivery
  • topical administration
  • nanoparticles
  • micelles
  • liposomes

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Published Papers (5 papers)

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Research

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18 pages, 3661 KiB  
Article
Fabrication and Characterisation of 3D-Printed Triamcinolone Acetonide-Loaded Polycaprolactone-Based Ocular Implants
by Febri Annuryanti, Juan Domínguez-Robles, Qonita Kurnia Anjani, Muhammad Faris Adrianto, Eneko Larrañeta and Raghu Raj Singh Thakur
Pharmaceutics 2023, 15(1), 243; https://doi.org/10.3390/pharmaceutics15010243 - 11 Jan 2023
Cited by 12 | Viewed by 3826
Abstract
Triamcinolone acetonide (TA) is a corticosteroid that has been used to treat posterior segment eye diseases. TA is injected intravitreally in the management of neovascular disorders; however, frequent intravitreal injections result in many potential side effects and poor patient compliance. In this work, [...] Read more.
Triamcinolone acetonide (TA) is a corticosteroid that has been used to treat posterior segment eye diseases. TA is injected intravitreally in the management of neovascular disorders; however, frequent intravitreal injections result in many potential side effects and poor patient compliance. In this work, a 3D bioprinter was used to prepare polycaprolactone (PCL) implants loaded with TA. Implants were manufactured with different shapes (filament-, rectangular-, and circle-shaped) and drug loadings (5, 10, and 20%). The characterisation results showed that TA was successfully mixed and incorporated within the PCL matrix without using solvents, and drug content reached almost 100% for all formulations. The drug release data demonstrate that the filament-shaped implants (SA/V ratio~7.3) showed the highest cumulative drug release amongst all implant shapes over 180 days, followed by rectangular- (SA/V ratio~3.7) and circle-shaped implants (SA/V ratio~2.80). Most implant drug release data best fit the Korsmeyer–Peppas model, indicating that diffusion was the prominent release mechanism. Additionally, a biocompatibility study was performed; the results showed >90% cell viability, thus proving that the TA-loaded PCL implants were safe for ocular application. Full article
(This article belongs to the Special Issue Nanotechnology in Ocular Drug Delivery)
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16 pages, 3682 KiB  
Article
Development of α-Tocopherol Succinate-Based Nanostructured Lipid Carriers for Delivery of Paclitaxel
by Sushrut Marathe, Gauri Shadambikar, Tabish Mehraj, Suresh P. Sulochana, Narendar Dudhipala and Soumyajit Majumdar
Pharmaceutics 2022, 14(5), 1034; https://doi.org/10.3390/pharmaceutics14051034 - 11 May 2022
Cited by 16 | Viewed by 4468
Abstract
The management of retinoblastoma (RB) involves the use of invasive treatment regimens. Paclitaxel (PTX), an effective antineoplastic compound used in the treatment of a wide range of malignant tumors, poses treatment challenges due to systemic toxicity, rapid elimination, and development of resistance. The [...] Read more.
The management of retinoblastoma (RB) involves the use of invasive treatment regimens. Paclitaxel (PTX), an effective antineoplastic compound used in the treatment of a wide range of malignant tumors, poses treatment challenges due to systemic toxicity, rapid elimination, and development of resistance. The goal of this work was to develop PTX-loaded, α-tocopherol succinate (αTS)-based, nanostructured lipid carrier (NLCs; αTS-PTX-NLC) and PEGylated αTS-PTX-NLC (αTS-PTX-PEG-NLC) to improve ocular bioavailability. The hot homogenization method was used to prepare the NLCs, and repeated measures ANOVA analysis was used for formulation optimization. αTS-PTX-NLC and αTS-PTX-PEG-NLC had a mean particle size, polydispersity index and zeta potential of 186.2 ± 3.9 nm, 0.17 ± 0.03, −33.2 ± 1.3 mV and 96.2 ± 3.9 nm, 0.27 ± 0.03, −39.15 ± 3.2 mV, respectively. The assay and entrapment efficiency of both formulations was >95.0%. The NLC exhibited a spherical shape, as seen from TEM images. Sterilized (autoclaved) formulations were stable for up to 60 days (last time point checked) under refrigerated conditions. PTX-NLC formulations exhibited an initial burst release and 40% drug release, overall, in 48 h. The formulations exhibited desirable physicochemical properties and could lead to an effective therapeutic option in the management of RB. Full article
(This article belongs to the Special Issue Nanotechnology in Ocular Drug Delivery)
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14 pages, 2595 KiB  
Article
Melatonin-Eluting Contact Lenses Effect on Tear Volume: In Vitro and In Vivo Experiments
by María Serramito, Ana F. Pereira-da-Mota, Carlos Carpena-Torres, Fernando Huete-Toral, Carmen Alvarez-Lorenzo and Gonzalo Carracedo
Pharmaceutics 2022, 14(5), 1019; https://doi.org/10.3390/pharmaceutics14051019 - 9 May 2022
Cited by 8 | Viewed by 2853
Abstract
(1) Background: The purpose of this study was to synthesize melatonin-eluting contact lenses (CLs) and evaluate both the ocular kinetics of the released melatonin and its effect on tear volume and intraocular pressure. (2) Methods: In vitro, melatonin-eluting CLs were synthesized by using [...] Read more.
(1) Background: The purpose of this study was to synthesize melatonin-eluting contact lenses (CLs) and evaluate both the ocular kinetics of the released melatonin and its effect on tear volume and intraocular pressure. (2) Methods: In vitro, melatonin-eluting CLs were synthesized by using non-functionalized (HEMA) and functionalized (HEMA/APMA) monomers. In vivo, a short-term prospective and randomized study was performed on 15 rabbits divided into two groups: 12 rabbits wearing functionalized CLs and 3 rabbits without CLs as a control. The melatonin levels in tears, aqueous humor, vitreous body and retina, tear volume, and intraocular pressure were measured for 8 h. (3) Results: In vitro, both monomers did not show differences in terms of melatonin loading and release (p ≥ 0.05). In vivo, the melatonin concentration was elevated in tears and aqueous humor after 2 and 4 h of wearing CLs, respectively (p < 0.05). Additionally, the CLs increased tear volume for 2 h (p < 0.05). (4) Conclusions: The melatonin-eluting CLs released their content over the ocular surface for at least 2 h, which was associated with a secretagogue effect on tear volume. However, the increased amount of melatonin found in the aqueous humor had no effect on intraocular pressure. Full article
(This article belongs to the Special Issue Nanotechnology in Ocular Drug Delivery)
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17 pages, 4341 KiB  
Article
Chitosan Nanoparticles for Meloxicam Ocular Delivery: Development, In Vitro Characterization, and In Vivo Evaluation in a Rabbit Eye Model
by Hebatallah B. Mohamed, Mohamed Ali Attia Shafie and Aml I. Mekkawy
Pharmaceutics 2022, 14(5), 893; https://doi.org/10.3390/pharmaceutics14050893 - 20 Apr 2022
Cited by 22 | Viewed by 5250
Abstract
Eye inflammation is considered one of the most common co-morbidities associated with ocular disorders and surgeries. Conventional management of this condition with non-steroidal anti-inflammatory drugs as eye drops is associated with low corneal bioavailability and ocular irritancy. In the current study, we first [...] Read more.
Eye inflammation is considered one of the most common co-morbidities associated with ocular disorders and surgeries. Conventional management of this condition with non-steroidal anti-inflammatory drugs as eye drops is associated with low corneal bioavailability and ocular irritancy. In the current study, we first investigated the capacity of different solvent systems to enhance the solubility of Meloxicam (MLX). Then, we prepared chitosan nanoparticles loaded with meloxicam (MLX-CS-NPs) through electrostatic interaction between the cationic chitosan and the anionic MLX using either 100% v/v polyethylene glycol 400 or 0.25% w/v tripolyphosphate solution as solvents based on the MLX solubility data. In further studies, MLX-CS-NPs were characterized in vitro and assessed for their ex vivo corneal and scleral permeability. The morphology, average particle size (195–597 nm), zeta potential (25–54 mV), and percent entrapment efficiencies (70–96%) of the prepared MLX-CS-NPs were evaluated. The in vitro release study of MLX from the selected MLX-CS-NPs showed a sustained drug release for 72 h with accepted flux and permeation through the cornea and sclera of rabbits. In the in vivo studies, MLX-CS-NPs eye drop dispersion showed enhanced anti-inflammatory activity and no ocular irritancy compared to MLX-eye drop solution. Our findings suggest the potential for using chitosan nanotechnology for ocular delivery of MLX with high contact time and activity. Full article
(This article belongs to the Special Issue Nanotechnology in Ocular Drug Delivery)
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Review

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32 pages, 2842 KiB  
Review
Metallic Engineered Nanomaterials and Ocular Toxicity: A Current Perspective
by Krista M. Cosert, Soohyun Kim, Iman Jalilian, Maggie Chang, Brooke L. Gates, Kent E. Pinkerton, Laura S. Van Winkle, Vijay Krishna Raghunathan, Brian C. Leonard and Sara M. Thomasy
Pharmaceutics 2022, 14(5), 981; https://doi.org/10.3390/pharmaceutics14050981 - 3 May 2022
Cited by 14 | Viewed by 5339
Abstract
The ocular surface, comprised of the transparent cornea, conjunctiva, and protective tear film, forms a protective barrier defending deeper structures of the eye from particulate matter and mechanical trauma. This barrier is routinely exposed to a multitude of naturally occurring and engineered nanomaterials [...] Read more.
The ocular surface, comprised of the transparent cornea, conjunctiva, and protective tear film, forms a protective barrier defending deeper structures of the eye from particulate matter and mechanical trauma. This barrier is routinely exposed to a multitude of naturally occurring and engineered nanomaterials (ENM). Metallic ENMs are particularly ubiquitous in commercial products with a high risk of ocular exposure, such as cosmetics and sunscreens. Additionally, there are several therapeutic uses for metallic ENMs owing to their attractive magnetic, antimicrobial, and functionalization properties. The increasing commercial and therapeutic applications of metallic ENMs come with a high risk of ocular exposure with poorly understood consequences to the health of the eye. While the toxicity of metallic ENMs exposure has been rigorously studied in other tissues and organs, further studies are necessary to understand the potential for adverse effects and inform product usage for individuals whose ocular health may be compromised by injury, disease, or surgical intervention. This review provides an update of current literature on the ocular toxicity of metallic ENMs in vitro and in vivo, as well as the risks and benefits of therapeutic applications of metallic ENMs in ophthalmology. Full article
(This article belongs to the Special Issue Nanotechnology in Ocular Drug Delivery)
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