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

Young Bin Choy1, Samirkumar R Patel, Jung-Hwan Park

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

Investigative Ophthalmology & Visual Science
|January 20, 2011
PubMed
Abstract

Insights

Mucoadhesive microparticles in a rapidly dissolving tablet offer sustained ocular drug delivery. This novel dosage form significantly prolongs drug presence in the eye, improving therapeutic outcomes.

Area of Science:

  • Ophthalmology
  • Pharmaceutics
  • Biomaterials Science

Background:

  • Ocular drug delivery faces challenges due to rapid clearance from the eye.
  • Sustained drug release is crucial for effective treatment of various ocular conditions.
  • Conventional eye drops often result in suboptimal drug concentrations and frequent administration.

Purpose of the Study:

  • To evaluate mucoadhesive microparticles within a rapidly dissolving tablet for sustained ocular drug delivery.
  • To test the hypothesis that this formulation enhances drug retention and therapeutic effect in the eye.
  • To assess the in vitro and in vivo performance of this novel drug delivery system.

Main Methods:

  • Fabrication of mucoadhesive microparticles (<5 μm) using poly(lactic-co-glycolic acid) and poly(ethylene glycol), encapsulating pilocarpine.
  • Embedding microparticles in a poly(vinyl alcohol) matrix to create a rapidly dissolving dry tablet.
  • In vitro drug release studies and in vivo mucoadhesion tests on rabbit eyes.

Main Results:

  • In vitro studies showed rapid initial release (90% in 10 min) followed by slow release for 3 hours.
  • In vivo tests demonstrated significantly better mucoadhesion of microparticles to the rabbit ocular surface compared to controls.
  • Pharmacodynamic assessment revealed prolonged pilocarpine-induced pupil constriction (up to 330 min) with the mucoadhesive microparticle tablet.

Conclusions:

  • Mucoadhesive microparticles integrated into a dry, rapidly dissolving tablet represent a promising approach for sustained ocular drug delivery.
  • This formulation enhances ocular drug retention and prolongs therapeutic effects.
  • The system offers a potential improvement over conventional ocular drug delivery methods.

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