期刊
JOURNAL OF CONTROLLED RELEASE
卷 220, 期 -, 页码 180-188出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jconrel.2015.10.027
关键词
Drug delivery; Glaucoma; Microparticles; Mucosal adhesion; Nanostructured surface; Ophthalmology
资金
- BK21 Plus Program [22A20130011025]
- Basic Science Research Program through the National Research Foundation of Korea (NRF) - Ministry of Education [NRF-2013R1A1A2A10011055]
Topical drug administration to the eye is limited by low drug bioavailability due to its rapid clearance from the preocular surface. Thus, multiple daily administrations are often needed, but patient compliance is low, hence a high chance of unsatisfactory treatment of ocular diseases. To resolve this, we proposemucoadhesive microparticles with a nanostructured surface as potential carriers for delivery of brimonidine, an ocular drug for glaucoma treatment. For sustained drug delivery, the microparticles were composed mainly of a diffusion-wall material, poly(lactic-co-glycolic acid) and a mucoadhesive polymer, polyethylene glycol, was used as an additive. Due to their nanostructured surface, the microparticles with a mucoadhesive material exhibited a 13-fold increase in specific surface area and could thus adhere better to the mucous layer on the eye, as compared with the conventional spherical microparticles. When loaded with brimonidine, the mucoadhesive microparticles with a nanostructured surface increased both drug bioavailability and its activity period by a factor of more than 2 over Alphagan P, a marketed eye drop of brimonidine. (C) 2015 Elsevier B.V. All rights reserved.
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