Mucoadhesive microparticles in a rapidly dissolving tablet for sustained drug delivery to the eye.
OBJECTIVE
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.
Department of Biomedical Engineering, College of Medicine and Institute of Medical and Biological Engineering, Medical Research Center, Seoul National University, Seoul, Republic of Korea.
Young Bin
YB
Choy
Samirkumar R
SR
Patel
Jung-Hwan
JH
Park
Bernard E
BE
McCarey
Henry F
HF
Edelhauser
Mark R
MR
Prausnitz
D000268:Adhesiveness; D000818:Animals; D001682:Biological Availability; D004337:Drug Carriers; D016503:Drug Delivery Systems / Q000295:instrumentation* / Q000379:methods; D005260:Female; D007498:Iris / Q000378:metabolism; D008863:Microspheres; D008916:Miotics / Q000008:administration & dosage* / Q000493:pharmacokinetics; D010862:Pilocarpine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011092:Polyethylene Glycols; D011098:Polyglactin 910; D011680:Pupil / Q000187:drug effects*; D011817:Rabbits; D013607:Tablets
D004337:Drug Carriers; D008916:Miotics; D013607:Tablets; C102418:poly(lactic-glycolic acid)-poly(ethyleneglycol) copolymer; D010862:Pilocarpine; D011098:Polyglactin 910; D011092:Polyethylene Glycols
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