Unveiling New Insights and Treatment Options for Ocular Surface Diseases

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

Deadline for manuscript submissions: 31 July 2024 | Viewed by 3278

Special Issue Editors


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Guest Editor
Institute of Biochemistry & Cell Biology (IBBC), National Research Council (CNR), Unit of Translational & Biomolecular Medicine “Rita Levi-Montalcini”, Viale dell’Università 33, 00185 Rome, Italy
Interests: drug delivery systems; neuroscience; neurotrophins
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Institute of Biochemistry & Cell Biology (IBBC), National Research Council (CNR), Unit of Translational & Biomolecular Medicine “Rita Levi-Montalcini”, Viale dell’Università 33, 00185 Rome, Italy
Interests: neuroscience; neuroinflammation; neurodegeneration
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Sense Organs, Sapienza University of Rome, Rome, Italy
Interests: ocular surface diseases; cornea; confocal imaging; anterior segment-OCT (AS-OCT); inflammation; immunology; neuropathic corneal pain; dry eye; neurotrophic keratitis; cornea surgery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Ocular surface diseases comprise a spectrum of disorders that affect the surface of the eyes, including dry eye disease (DED), neurotrophic keratitis (NK), and neuropathic corneal pain (NCP). These diseases can have significant impacts on visual acuity, comfort, and quality of life for affected individuals. Ocular surface diseases share a common feature of inflammation and immune responses driving their pathogenesis and progression. Inflammatory processes lead to the release of neuromediators and growth factors, contributing to the development and symptoms of ocular surface diseases. Insights into the underlying mechanisms of ocular surface diseases hold great promise for the identification of novel biomarkers and the development of targeted treatments that specifically address the molecular pathways involved in these diseases. This personalized approach is expected to enhance treatment efficacy and improve patient outcomes.

We are pleased to invite colleagues working in any field related to ocular surface diseases, from drug design and formulation to drug delivery and treatment, to submit their work for publication in this Special Issue. We are confident that, through the publication of innovative research, insightful reviews, and cutting-edge studies, this Special Issue in Pharmaceutics will help foster interdisciplinary collaboration and stimulate the further exploration of novel approaches and therapeutic strategies for ocular surface diseases. We encourage researchers and experts to contribute their valuable work to this issue, as together, we can advance our understanding and improve the management of these challenging conditions.

This Special Issue aims to provide a platform for scientists to publish their experimental results, novel findings, innovative methodologies, and theoretical assumptions in the field of ocular surface diseases. By providing an avenue for researchers to share their findings and insights, we aim to promote further exploration and advancements in this area of research. In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following: pharmaceutical sciences, ophthalmology, immunology, and bioengineering.

We look forward to receiving your contributions.

Dr. Paola Tirassa
Dr. Pamela Rosso
Dr. Fabiana Mallone
Guest Editors

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Keywords

  • ocular surface diseases
  • dry eye
  • neurotrophic keratitis
  • neuropathic corneal pain
  • inflammation
  • immune cells, dendritic cells
  • neuromediators and growth factors
  • biomarkers
  • drug delivery systems
  • advanced therapy
  • tissue engineering

Published Papers (3 papers)

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Research

10 pages, 679 KiB  
Article
Safety and Tolerability of KIO-101 Eye Drops in Healthy Volunteers and Patients with Ocular Surface Disease—A Phase I Study
by Doreen Schmidl, Nikolaus Hommer, Martin Kallab, Andreas Schlatter, Clemens Nadvornik, Franz Obermayr, Stefan Sperl, Eric J. Daniels and Gerhard Garhöfer
Pharmaceutics 2024, 16(3), 367; https://doi.org/10.3390/pharmaceutics16030367 - 05 Mar 2024
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Abstract
Purpose: Inhibitors of dihydroorotate dehydrogenase (DHODH) have been found to be potent anti-inflammatory agents. Recently, a topical formulation (KIO-101 eye drops) of a DHODH inhibitor has been developed. The aim of the present study was to evaluate the safety and tolerability of KIO-101 [...] Read more.
Purpose: Inhibitors of dihydroorotate dehydrogenase (DHODH) have been found to be potent anti-inflammatory agents. Recently, a topical formulation (KIO-101 eye drops) of a DHODH inhibitor has been developed. The aim of the present study was to evaluate the safety and tolerability of KIO-101 eye drops in Healthy Volunteers (HVs) and patients with conjunctival hyperemia. Methods: The study was carried out in a double-masked, placebo-controlled, randomized, parallel-group design with two parts. In part I, HVs received single and multiple instillations (four times daily for 12 consecutive days) of KIO-101 eye drops in ascending doses of 0.05%, 0.15%, and 0.30%, respectively. Part II was conducted in patients with conjunctival hyperemia who received 0.15% KIO-101 eye drops twice daily for 12 consecutive days. Ophthalmic and systemic safety examinations were performed on all participants. In part II, ocular hyperemia grading and an ocular surface disease index (OSDI) questionnaire were performed. Results: 24 HVs participated in part I and 21 patients in part II. KIO-101 eye drops were well tolerated in all subjects. No serious adverse events (SAEs) occurred, and all AEs that were reported were transient and considered mild to moderate. In the highest dose cohort (0.30%), epistaxis occurred in two subjects after multiple instillations. In part II, after 12 days treatment with 0.15% KIO-101, conjunctival hyperemia decreased by −1.1 ± 0.27 points in the treatment and −0.6 ± 0.79 points in the placebo group (p = 0.0385). OSDI decreased from 47.9 ± 18.7 to 27.6 ± 19.13 points in the treatment group, while in the placebo group, a change from 41.3 ± 12.08 to 27.3 ± 18.63 points occurred. Conclusions: A 12-day treatment regimen with topical KIO-101 eye drops at low and mid doses was safe and well tolerated in both HVs and patients with conjunctival hyperemia. The obtained results point towards an early sign of reduction in conjunctival hyperemia. Full article
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13 pages, 4792 KiB  
Article
Ectoine, from a Natural Bacteria Protectant to a New Treatment of Dry Eye Disease
by Xin Chen, Na Lin, Jin-Miao Li, Haixia Liu, Anmar Abu-Romman, Ebru Yaman, Fang Bian, Cintia S. de Paiva, Stephen C. Pflugfelder and De-Quan Li
Pharmaceutics 2024, 16(2), 236; https://doi.org/10.3390/pharmaceutics16020236 - 05 Feb 2024
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Abstract
Ectoine, a novel natural osmoprotectant, protects bacteria living in extreme environments. This study aimed to explore the therapeutic effect of ectoine for dry eye disease. An experimental dry eye model was created in C57BL/6 mice exposed to desiccating stress (DS) with untreated mice [...] Read more.
Ectoine, a novel natural osmoprotectant, protects bacteria living in extreme environments. This study aimed to explore the therapeutic effect of ectoine for dry eye disease. An experimental dry eye model was created in C57BL/6 mice exposed to desiccating stress (DS) with untreated mice as controls (UT). DS mice were dosed topically with 0.5–2.0% of ectoine or a vehicle control. Corneal epithelial defects were detected via corneal smoothness and Oregon Green dextran (OGD) fluorescent staining. Pro-inflammatory cytokines and chemokines were evaluated using RT-qPCR and immunofluorescent staining. Compared with UT mice, corneal epithelial defects were observed as corneal smoothness irregularities and strong punctate OGD fluorescent staining in DS mice with vehicle. Ectoine treatment protected DS mice from corneal damage in a concentration-dependent manner, and ectoine at 1.0 and 2.0% significantly restored the corneal smoothness and reduced OGD staining to near normal levels. Expression of pro-inflammatory cytokines (TNF-α, IL-1β, and IL-6) and chemokines CCL3 and CXCL11 was significantly elevated in the corneas and conjunctivas of DS mice, whereas 1.0 and 2.0% ectoine suppressed these inflammatory mediators to near normal levels. Our findings demonstrate that ectoine can significantly reduce the hallmark pathologies associated with dry eye and may be a promising candidate for treating human disease. Full article
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12 pages, 3542 KiB  
Article
The Effect of Systemic Parameters and Baseline Characteristics in Short-Term Response Analysis with Intravitreal Ranibizumab in Treatment-Naive Patients with Neovascular Age-Related Macular Degeneration
by Laura García-Quintanilla, Pablo Almuiña-Varela, María José Rodríguez-Cid, María Gil-Martínez, Maximino J. Abraldes, Francisco Gómez-Ulla, Miguel González-Barcia, Cristina Mondelo-García, Ana Estany-Gestal, Francisco J. Otero-Espinar, Maribel Fernández-Rodríguez and Anxo Fernández-Ferreiro
Pharmaceutics 2024, 16(1), 105; https://doi.org/10.3390/pharmaceutics16010105 - 13 Jan 2024
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Abstract
Anti-vascular endothelial growth factor drugs keep being the main therapy for neovascular age-related macular degeneration (AMD). Possible predictive parameters (demographic, biochemical and/or inflammatory) could anticipate short-term treatment response with ranibizumab. 46 treatment-naive patients were included in a prospective observational study. They underwent three [...] Read more.
Anti-vascular endothelial growth factor drugs keep being the main therapy for neovascular age-related macular degeneration (AMD). Possible predictive parameters (demographic, biochemical and/or inflammatory) could anticipate short-term treatment response with ranibizumab. 46 treatment-naive patients were included in a prospective observational study. They underwent three monthly injections of intravitreal ranibizumab for neovascular AMD and the clinical examination was made at baseline and one month after the third injection. Demographic characteristics, co-morbidities and concomitant treatments were recorded at the baseline visit. Biochemical parameters, complete blood count and inflammation biomarkers were also measured at these times. Uric Acid was found to be statistically significant with a one-point difference between good and poor responders in both basal and treated patients, but only in basal parameters was statistical significance reached (p = 0.007 vs. p = 0.071 in treated patients). Cholesterol and inflammatory parameters such as white blood cell count and neutrophils were significantly reduced over time when treated with intravitreal ranibizumab. On the other hand, women seemed to have a worse prognosis for short-term response to intravitreal ranibizumab treatment. Uric acid may help identify possible non-responders before initial treatment with ranibizumab, and cholesterol and white blood cells could be good candidates to monitor short-term response to ranibizumab treatment. Full article
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