Next Article in Journal
Nano- and Microcarriers as Drug Delivery Systems for Usnic Acid: Review of Literature
Previous Article in Journal
Transporter-Mediated Delivery of Small Molecule Drugs to the Brain: A Critical Mechanism That Can Advance Therapeutic Development for Ischemic Stroke
Previous Article in Special Issue
Retinal Cell Protection in Ocular Excitotoxicity Diseases. Possible Alternatives Offered by Microparticulate Drug Delivery Systems and Future Prospects
Open AccessArticle

Novel Sustained-Release Drug Delivery System for Dry Eye Therapy by Rebamipide Nanoparticles

Faculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashi-Osaka, Osaka 577-8502, Japan
Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo 105-8512, Japan
Okamoto Eye Clinic, 5-11-12-312 Izumicho, Suita, Osaka 564-0041, Japan
Department of Small Animal Internal Medicine, School of Veterinary Medicine, University of Kitasato, Towada, Aomori 034-8628, Japan
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(2), 155;
Received: 17 January 2020 / Revised: 7 February 2020 / Accepted: 13 February 2020 / Published: 14 February 2020
(This article belongs to the Special Issue Ophthalmic Drug Delivery)
The commercially available rebamipide ophthalmic suspension (CA-REB) was approved for clinical use in patients with dry eye; however, the residence time on the ocular surface for the traditional formulations is short, since the drug is removed from the ocular surface through the nasolacrimal duct. In this study, we designed a novel sustained-release drug delivery system (DDS) for dry eye therapy by rebamipide nanoparticles. The rebamipide solid nanoparticle-based ophthalmic formulation (REB-NPs) was prepared by a bead mill using additives (2-hydroxypropyl-β-cyclodextrin and methylcellulose) and a gel base (carbopol). The rebamipide particles formed are ellipsoid, with a particle size in the range of 40–200 nm. The rebamipide in the REB-NPs applied to eyelids was delivered into the lacrimal fluid through the meibomian glands, and sustained drug release was observed in comparison with CA-REB. Moreover, the REB-NPs increased the mucin levels in the lacrimal fluid and healed tear film breakup levels in an N-acetylcysteine-treated rabbit model. The information about this novel DDS route and creation of a nano-formulation can be used to design further studies aimed at therapy for dry eye.
Keywords: rebamipide; sustained delivery system; dry eye; eyelid; mucin rebamipide; sustained delivery system; dry eye; eyelid; mucin
Show Figures

Graphical abstract

MDPI and ACS Style

Nagai, N.; Ishii, M.; Seiriki, R.; Ogata, F.; Otake, H.; Nakazawa, Y.; Okamoto, N.; Kanai, K.; Kawasaki, N. Novel Sustained-Release Drug Delivery System for Dry Eye Therapy by Rebamipide Nanoparticles. Pharmaceutics 2020, 12, 155.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

Back to TopTop