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Advanced Nanosystems for Ophthalmic Administration

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A special issue of Nanomaterials (ISSN 2079-4991).

Deadline for manuscript submissions: closed (30 September 2019) | Viewed by 13395

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Special Issue Editor

Dr. Simona Sapino

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Guest Editor

Department of Drug Science and Technology, University of Torino, 10125 Turin, Italy
Interests: lipid nanoparticles; microemulsions; ophthalmic therapeutics; anticancer therapy; retinal diseases; combinational therapies; in vitro preclinical models; veterinary medicine
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Special Issue Information

Dear Colleagues,

Ophthalmic therapies have recently been improved by the introduction of novel drug delivery approaches using implants or devices, advanced biomaterials, nanomedicines, stimuli-responsive systems, cell therapy, etc. These technologies are applied for the treatment of several anterior/posterior-segment diseases such as dry eye, allergy, inflammations, infections, glaucoma, cataract and retinal disorders (age-related macular degeneration, diabetic retinopathy, and others). Most of the inserts/implants are invasively applied and require surgical procedures, and advanced drug delivery systems (DDSs) based on nanotechnologies appear to provide more effective non-invasive therapies even though they require increasing efforts to obtain high clinical impacts. The employment of in vitro models to estimate the ocular drug release residence time and clearance plays an important role in this research progress. This Special Issue of Nanomaterials will survey the challenges and the current state-of-the-art in the use of nanomaterials to create advanced DDSs for the treatment of ocular diseases.

Dr. Simona Sapino
Guest Editor

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Keywords

Ocular diseases
Nanotechnologies
Intraocular drug delivery
Ocular barriers
Ophthalmic implants
Biomaterials
Stimuli-responsive systems
In vitro ocular models
Cell cultures

Published Papers (3 papers)

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Research

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26 pages, 4121 KiB

Open AccessArticle

Thermosensitive Nanocomposite Hydrogels for Intravitreal Delivery of Cefuroxime

by Simona Sapino, Elena Peira, Daniela Chirio, Giulia Chindamo, Stefano Guglielmo, Simonetta Oliaro-Bosso, Raffaella Barbero, Cristina Vercelli, Giovanni Re, Valentina Brunella, Chiara Riedo, Antonio Maria Fea and Marina Gallarate

Nanomaterials 2019, 9(10), 1461; https://doi.org/10.3390/nano9101461 - 15 Oct 2019

Cited by 21 | Viewed by 3492

Abstract

Endophthalmitis is a rare, but serious, intravitreal inflammatory disorder that can arise after cataract surgery. The intracameral injection of 1 mg cefuroxime (CEF) followed by three-times daily antibiotic topical administration for a week is generally recognized as the routine method of prophylaxis after cataract surgery. This procedure is controversial because of both the low efficacy and the low adherence to therapy by elderly patients. A unique slow release antibiotic intravitreal injection could solve these problems. The objective of the present study was to design ophthalmic nanocomposite delivery systems based on in situ gelling formulations that undergo sol-to-gel transition upon change in temperature to prolong the effect of CEF. Oil in water (O/W) microemulsion (µE) and solid lipid nanoparticles (SLN), obtained with an innovative formulation technology called cold microemulsion dilution, were evaluated as ocular drug delivery systems for CEF. Drug entrapment efficiency up to 80% was possible by esterifying CEF with 1-dodecanol to obtain dodecyl-CEF (dCEF). Both dCEF-loaded SLN and µE were then added with Pluronic®F127 (20% w/v) to obtain a nanocomposite hydrogel-based long acting system. The prepared thermosensitive formulations were evaluated for their physical appearance, drug content, gelation temperature, injectability and rheological properties, in vitro release studies and stability studies. Moreover, cell proliferation assays on human retinal pigment epithelial ARPE-19 cells were performed to evaluate the influence of this innovative system on the cellular viability. In addition, minimal inhibitory concentration (MIC) was assessed for both CEF and dCEF, revealing the need of dCEF hydrolysis for the antimicrobial activity. Although further experimental investigations are required, the physico-chemical characterization of the nanocomposite hydrogels and the preliminary in vitro release studies highlighted the potential of these systems for the sustained release of CEF. Full article

(This article belongs to the Special Issue Advanced Nanosystems for Ophthalmic Administration)

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12 pages, 2937 KiB

Open AccessArticle

Therapeutic Potential of a Combination of Magnesium Hydroxide Nanoparticles and Sericin for Epithelial Corneal Wound Healing

by Noriaki Nagai, Yoshie Iwai, Saori Deguchi, Hiroko Otake, Kazutaka Kanai, Norio Okamoto and Yoshikazu Shimomura

Nanomaterials 2019, 9(5), 768; https://doi.org/10.3390/nano9050768 - 19 May 2019

Cited by 13 | Viewed by 3557

Abstract

We previously found the instillation of sericin to be useful as therapy for keratopathy with or without diabetes mellitus. In this study, we investigated whether a combination of solid magnesium hydroxide nanoparticles (MHN) enhances epithelial corneal wound healing by sericin using rabbits, normal rats and type 2 diabetes mellitus rats with debrided corneal epithelium (ex vivo and in vivo studies). Ophthalmic formulations containing sericin and MHN (N-Ser) were prepared using a bead mill method. The mean particle size of the N-Ser was 110.3 nm at the time of preparation, and 148.1 nm one month later. The instillation of N-Ser had no effect on the amount of lacrimal fluid in normal rabbits (in vivo), but the MHN in N-Ser was found to expand the intercellular space in ex vivo rat corneas. In addition, the instillation of N-Ser increased the phosphorylation of Extracellular Signal-regulated Kinase (ERK)1/2, a factor involved in cell adhesion and cell proliferation in the corneal epithelium, in comparison with the instillation of sericin alone. The combination with MHN enhanced epithelial corneal wound healing by sericin in rat debrided corneal epithelium (in vivo). This study provides significant information to prepare potent drugs to cure severe keratopathy, such as diabetic keratopathy. Full article

(This article belongs to the Special Issue Advanced Nanosystems for Ophthalmic Administration)

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Review

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19 pages, 774 KiB

Open AccessFeature PaperReview

Ocular Drug Delivery: A Special Focus on the Thermosensitive Approach

by Simona Sapino, Daniela Chirio, Elena Peira, Elena Abellán Rubio, Valentina Brunella, Sushilkumar A. Jadhav, Giulia Chindamo and Marina Gallarate

Nanomaterials 2019, 9(6), 884; https://doi.org/10.3390/nano9060884 - 14 Jun 2019

Cited by 40 | Viewed by 5892

Abstract

The bioavailability of ophthalmic therapeutics is reduced because of the presence of physiological barriers whose primary function is to hinder the entry of exogenous agents, therefore also decreasing the bioavailability of locally administered drugs. Consequently, repeated ocular administrations are required. Hence, the development of drug delivery systems that ensure suitable drug concentration for prolonged times in different ocular tissues is certainly of great importance. This objective can be partially achieved using thermosensitive drug delivery systems that, owing to their ability of changing their state in response to temperature variations, from room to body temperature, may increase drug bioavailability. In the case of topical instillation, in situ forming gels increase pre-corneal drug residence time as a consequence of their enhanced adhesion to the corneal surface. Otherwise, in the case of intraocular and periocular, i.e., subconjunctival, retrobulbar, peribulbar administration, among others, they have the undoubted advantage of being easily injectable and, owing to their sudden thickening at body temperature, have the ability to form an in situ drug reservoir. As a result, the frequency of administration can be reduced, also favoring the patient’s adhesion to therapy. In the main section of this review, we discuss some of the most common treatment options for ocular diseases, with a special focus on posterior segment treatments, and summarize the most recent improvement deriving from thermosensitive drug delivery strategies. Aside from this, an additional section describes the most widespread in vitro models employed to evaluate the functionality of novel ophthalmic drug delivery systems. Full article

(This article belongs to the Special Issue Advanced Nanosystems for Ophthalmic Administration)

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