Mucoadhesive microparticles with a nanostructured surface for enhanced bioavailability of glaucoma drug

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 th...

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Bibliographic Details
Published in:Journal of controlled release 2015-12, Vol.220 (Pt A), p.180-188
Main Authors: Park, Chun Gwon, Kim, Young Kook, Kim, Mi Jeung, Park, Min, Kim, Myung Hun, Lee, Seung Ho, Choi, Sung Yoon, Lee, Won Seok, Chung, You Jung, Jung, Young Eun, Park, Ki Ho, Choy, Young Bin
Format: Article
Language:English
Subjects:
Adhesiveness
Administration, Ophthalmic
Adrenergic alpha-2 Receptor Agonists - administration & dosage
Adrenergic alpha-2 Receptor Agonists - chemistry
Adrenergic alpha-2 Receptor Agonists - pharmacokinetics
Animals
Aqueous Humor - metabolism
Biological Availability
Brimonidine Tartrate - administration & dosage
Brimonidine Tartrate - chemistry
Brimonidine Tartrate - pharmacokinetics
Drug Carriers
Drug Compounding
Drug delivery
Glaucoma
Glaucoma - drug therapy
Male
Microparticles
Mucosal adhesion
Mucus - metabolism
Nanoparticles
Nanostructured surface
Nanotechnology
Ophthalmic Solutions
Ophthalmology
Polyethylene Glycols - chemistry
Polyethylene Glycols - metabolism
Polyethylene Glycols - toxicity
Polyglactin 910 - chemistry
Polyglactin 910 - metabolism
Polyglactin 910 - toxicity
Rabbits
Solubility
Technology, Pharmaceutical - methods
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Summary: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 propose mucoadhesive 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. [Display omitted]
ISSN:0168-3659
1873-4995
DOI:10.1016/j.jconrel.2015.10.027