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Pharmaceutics
Special Issues
Advanced Formulations for Non-invasive and Minimally Invasive Ocular Drug Delivery
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Advanced Formulations for Non-invasive and Minimally Invasive Ocular Drug Delivery

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (28 February 2023) | Viewed by 11081

Special Issue Editors

Prof. Dr. Sara Nicoli

E-Mail Website
Guest Editor
Department of Food and Drug, University of Parma, 43124 Parma, Italy
Interests: ocular drug delivery; dermal and transdermal drug delivery; innovative drug delivery systems for topical application; enhancement of drug absorption across biological tissues
Special Issues, Collections and Topics in MDPI journals
Dr. Silvia Pescina

E-Mail Website
Guest Editor
Department of Food and Drug, University of Parma, 43124 Parma, Italy
Interests: ocular drug delivery; ex vivo ocular models; permeation enhancers; ophthalmic formulations

Special Issue Information

Dear Colleagues,

In the last few years, we have witnessed extraordinary research efforts in the field of ocular drug delivery. The development and optimization of new drug delivery platforms and, concurrently, the improvement of in vitro and ex vivo models for their evaluation, have made it possible to address old and new unmet needs. Many aspects remain to be investigated, particularly the fulfilment of non-invasive or, at least, minimally invasive approaches for the treatment of both anterior and posterior segment diseases.

Therefore, the aim of this Special Issue is to collect original research papers and review articles that address the use of innovative formulations such as nano- and micro-carriers, hydrogels, stimuli-responsive systems and physical and chemical enhancers for more effective and better accepted ophthalmic delivery.

Prof. Dr. Sara Nicoli
Dr. Silvia Pescina
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

  • ophthalmic formulations
  • ocular delivery
  • nanoparticles
  • microparticles
  • enhancers
  • ex vivo models
  • permeation
  • non-invasive delivery
  • biopharmaceutics
  • ocular devices

Published Papers (4 papers)

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Research

19 pages, 2873 KiB  
Article
Formulation and Characterization of Epalrestat-Loaded Polysorbate 60 Cationic Niosomes for Ocular Delivery
by Axel Kattar, Ana Quelle-Regaldie, Laura Sánchez, Angel Concheiro and Carmen Alvarez-Lorenzo
Pharmaceutics 2023, 15(4), 1247; https://doi.org/10.3390/pharmaceutics15041247 - 14 Apr 2023
Cited by 5 | Viewed by 2293
Abstract
The aim of this work was to develop niosomes for the ocular delivery of epalrestat, a drug that inhibits the polyol pathway and protects diabetic eyes from damage linked to sorbitol production and accumulation. Cationic niosomes were made using polysorbate 60, cholesterol, and [...] Read more.
The aim of this work was to develop niosomes for the ocular delivery of epalrestat, a drug that inhibits the polyol pathway and protects diabetic eyes from damage linked to sorbitol production and accumulation. Cationic niosomes were made using polysorbate 60, cholesterol, and 1,2-di-O-octadecenyl-3-trimethylammonium propane. The niosomes were characterized using dynamic light scattering, zeta-potential, and transmission electron microscopy to determine their size (80 nm; polydispersity index 0.3 to 0.5), charge (−23 to +40 mV), and shape (spherical). The encapsulation efficiency (99.76%) and the release (75% drug release over 20 days) were measured with dialysis. The ocular irritability potential (non-irritating) was measured using the Hen’s Egg Test on the Chorioallantoic Membrane model, and the blood glucose levels (on par with positive control) were measured using the gluc-HET model. The toxicity of the niosomes (non-toxic) was monitored using a zebrafish embryo model. Finally, corneal and scleral permeation was assessed with the help of Franz diffusion cells and confirmed with Raman spectroscopy. Niosomal permeation was higher than an unencapsulated drug in the sclera, and accumulation in tissues was confirmed with Raman. The prepared niosomes show promise to encapsulate and carry epalrestat through the eye to meet the need for controlled drug systems to treat the diabetic eye. Full article
(This article belongs to the Special Issue Advanced Formulations for Non-invasive and Minimally Invasive Ocular Drug Delivery)
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20 pages, 3510 KiB  
Article
Nanostructured Lipid Carriers for Enhanced Transscleral Delivery of Dexamethasone Acetate: Development, Ex Vivo Characterization and Multiphoton Microscopy Studies
by Felipe M. González-Fernández, Andrea Delledonne, Sara Nicoli, Paolo Gasco, Cristina Padula, Patrizia Santi, Cristina Sissa and Silvia Pescina
Pharmaceutics 2023, 15(2), 407; https://doi.org/10.3390/pharmaceutics15020407 - 25 Jan 2023
Cited by 6 | Viewed by 2286
Abstract
Corticosteroids, although highly effective for the treatment of both anterior and posterior ocular segment inflammation, still nowadays struggle for effective drug delivery due to their poor solubilization capabilities in water. This research work aims to develop nanostructured lipid carriers (NLC) intended for periocular [...] Read more.
Corticosteroids, although highly effective for the treatment of both anterior and posterior ocular segment inflammation, still nowadays struggle for effective drug delivery due to their poor solubilization capabilities in water. This research work aims to develop nanostructured lipid carriers (NLC) intended for periocular administration of dexamethasone acetate to the posterior segment of the eye. Pre-formulation studies were initially performed to find solid and liquid lipid mixtures for dexamethasone acetate solubilization. Pseudoternary diagrams at 65 °C were constructed to select the best surfactant based on the macroscopic transparency and microscopic isotropy of the systems. The resulting NLC, obtained following an organic solvent-free methodology, was composed of triacetin, Imwitor® 491 (glycerol monostearate >90%) and tyloxapol with Z-average = 106.9 ± 1.2 nm, PDI = 0.104 ± 0.019 and zeta potential = −6.51 ± 0.575 mV. Ex vivo porcine sclera and choroid permeation studies revealed a considerable metabolism in the sclera of dexamethasone acetate into free dexamethasone, which demonstrated higher permeation capabilities across both tissues. In addition, the NLC behavior once applied onto the sclera was further studied by means of multiphoton microscopy by loading the NLC with the fluorescent probe Nile red. Full article
(This article belongs to the Special Issue Advanced Formulations for Non-invasive and Minimally Invasive Ocular Drug Delivery)
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13 pages, 3593 KiB  
Article
Combination of Lanosterol and Nilvadipine Nanosuspensions Rescues Lens Opacification in Selenite-Induced Cataractic Rats
by Saori Deguchi, Reita Kadowaki, Hiroko Otake, Atsushi Taga, Yosuke Nakazawa, Manju Misra, Naoki Yamamoto, Hiroshi Sasaki and Noriaki Nagai
Pharmaceutics 2022, 14(7), 1520; https://doi.org/10.3390/pharmaceutics14071520 - 21 Jul 2022
Cited by 1 | Viewed by 1609
Abstract
It has recently been reported that lanosterol (LAN) plays a preventive role against lens opacification through the reversal of crystalline aggregation. However, the effect of LAN is not sufficient to restore lens transparency. In this study, we designed ophthalmic nanosuspensions (LAN-ONSs and NIL-ONSs) [...] Read more.
It has recently been reported that lanosterol (LAN) plays a preventive role against lens opacification through the reversal of crystalline aggregation. However, the effect of LAN is not sufficient to restore lens transparency. In this study, we designed ophthalmic nanosuspensions (LAN-ONSs and NIL-ONSs) based on LAN and nilvadipine (NIL), which can counteract cataract-related factors (e.g., enhanced Ca2+ and calpain levels), and investigated whether the combination of LAN-ONSs and NIL-ONSs can restore the nuclear lens opacity in sodium-selenite-induced cataractic rats (cataractic rats). The mean particle sizes of the LAN-ONSs and NIL-ONSs were 108.8 nm and 89.0 nm, respectively. The instillation of the LAN-ONSs or NIL-ONSs successfully delivered the drugs (LAN or NIL) into the lenses of the rats, although the instillation of LAN-ONSs or NIL-ONSs alone did not increase lens transparency in the cataractic rats. On the other hand, the cataract-related factors (enhanced Ca2+ and calpain levels) were significantly alleviated by the combination of LAN-ONSs and NIL-ONSs; furthermore, the perinuclear refractile ring in the lens nucleus and enhanced number of swollen fibers were attenuated by the LAN-ONS and NIL-ONS combination. Moreover, the opacity levels in the cataractic rats were reduced after treatment with the combination of LAN-ONSs and NIL-ONSs. It is possible that the combination of LAN and NIL will be useful for the treatment of lens opacification in the future. Full article
(This article belongs to the Special Issue Advanced Formulations for Non-invasive and Minimally Invasive Ocular Drug Delivery)
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17 pages, 2581 KiB  
Article
New Preservative-Free Formulation for the Enhanced Ocular Bioavailability of Prostaglandin Analogues in Glaucoma
by Gabriel Alviset, Yohann Corvis, Karim Hammad, Josiane Lemut, Marc Maury, Nathalie Mignet and Vincent Boudy
Pharmaceutics 2022, 14(2), 453; https://doi.org/10.3390/pharmaceutics14020453 - 20 Feb 2022
Cited by 6 | Viewed by 3664
Abstract
Glaucoma is a wide-spread eye disease caused by elevated intraocular pressure. Uncontrolled, this pressure may lead to damages to the optic nerve. Prostaglandin analogues, such as latanoprost and travoprost (which are water-insoluble active substances), are the most used class of active pharmaceutical ingredient. [...] Read more.
Glaucoma is a wide-spread eye disease caused by elevated intraocular pressure. Uncontrolled, this pressure may lead to damages to the optic nerve. Prostaglandin analogues, such as latanoprost and travoprost (which are water-insoluble active substances), are the most used class of active pharmaceutical ingredient. To administer them as eye drops, preservatives, such as benzalkonium chloride, are used as solubilizers. The latter is known to cause a local inflammation when used chronically and is not recommended for patients with ocular surface disorders. In this work, we sought to use polysorbate 80 (PS80) as a solubilizing agent simultaneously with sodium hyaluronate (NaHA) as a thickener and cytoprotective agent for the corneal surface. The first part of this study assessed the compatibility of the excipients with the active substance, using physicochemical methods such as spectra fluorescence and differential scanning calorimetry (DSC), as well as the solubilization mechanism of PS80 regarding prostaglandin analogues using nuclear magnetic resonance (NMR). The second part evaluated the stability of a formula candidate, its viscosity upon instillation, and its pharmacokinetic profile in rabbits as compared to the commercially approved medicine Travatan®. The results show that sodium hyaluronate is inert with respect to travoprost, while PS80 successfully solubilizes it, meaning that benzalkonium chloride is no longer required. Moreover, the pharmacokinetic profiles of the rabbits showed that the original formula described in the present study enhanced the ocular bioavailability of the drug, making it a promising product to control intraocular pressure with a potential reduced dosage of travoprost, therefore minimizing its related side effects. Full article
(This article belongs to the Special Issue Advanced Formulations for Non-invasive and Minimally Invasive Ocular Drug Delivery)
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