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Invest Ophthalmol Vis Sci. 2011 Apr 22;52(5):2627-33. doi: 10.1167/iovs.10-6465. Print 2011 Apr.

Mucoadhesive microparticles in a rapidly dissolving tablet for sustained drug delivery to the eye.

Author information

1
Department of Biomedical Engineering, College of Medicine and Institute of Medical and Biological Engineering, Medical Research Center, Seoul National University, Seoul, Republic of Korea.

Abstract

PURPOSE:

To test the hypothesis that mucoadhesive microparticles formulated in a rapidly dissolving tablet can achieve sustained drug delivery to the eye.

METHODS:

Mucoadhesive microparticles, smaller than 5 μm were fabricated with poly(lactic-co-glycolic acid) and poly(ethylene glycol) as a core material and mucoadhesion promoter, respectively, and encapsulated pilocarpine as a model drug. These microparticles were embedded in a poly(vinyl alcohol) matrix to form a dry tablet designed to reduce rapid clearance of the microparticles on initial application to the eye.

RESULTS:

This in vitro drug release study exhibited that for all formulations, approximately 90% of pilocarpine was released during the first 10 minutes, and the remaining 10% was released slowly for 3 hours. In vivo mucoadhesion test on the rabbit eye indicated that mucoadhesive microparticles adhered significantly better to the preocular surface than other formulations. To assess the pharmacodynamics, the most prolonged pilocarpine-induced pupil constriction was observed in rabbit eyes in vivo using a tablet with mucoadhesive microparticles; it lasted up to 330 minutes.

CONCLUSIONS:

The authors conclude that mucoadhesive microparticles formulated into a dry dosage form is a promising system for sustained drug delivery to the eye.

PMID:
21245405
PMCID:
PMC3088554
DOI:
10.1167/iovs.10-6465
[Indexed for MEDLINE]
Free PMC Article

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