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Use of Rabbit Eyes in Pharmacokinetic Studies of Intraocular Drugs
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Pullulan Based Bioconjugates for Ocular Dexamethasone Delivery.

Eva Kicková1, Stefano Salmaso1, Francesca Mastrotto1

  • 1Department of Pharmaceutical and Pharmacological Sciences, University of Padova, via F. Marzolo 5, 35131 Padova, Italy.

Pharmaceutics
|June 2, 2021
PubMed
Summary
This summary is machine-generated.

New pullulan-dexamethasone conjugates offer sustained drug release for posterior eye diseases, reducing the need for frequent intravitreal injections. These nanoparticles show promise for improved ocular drug delivery.

Keywords:
controlled releasedexamethasonehydrazoneocular drug deliverypullulan

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Area of Science:

  • Ophthalmology
  • Biomaterials Science
  • Drug Delivery Systems

Background:

  • Posterior segment eye diseases often require invasive intravitreal injections for pharmacological treatment.
  • Frequent intravitreal administrations necessitate the development of advanced drug delivery systems for sustained release.

Purpose of the Study:

  • To develop and characterize pullulan-dexamethasone conjugates for prolonged intravitreal drug delivery.
  • To evaluate the stability, drug release kinetics, and in vitro toxicity of these novel conjugates.

Main Methods:

  • Dexamethasone was conjugated to pullulan via a hydrazone bond, forming nanoparticles characterized by dynamic light scattering and transmission electron microscopy.
  • Drug release profiles were assessed in physiological buffer and homogenized vitreous at various temperatures.
  • In vitro toxicity and cellular uptake studies were performed using the ARPE-19 cell line.

Main Results:

  • Pullulan-dexamethasone nanoparticles (400-460 nm) demonstrated good stability in physiological conditions for over 6 weeks.
  • Slow drug release was observed in vitreous (50% in ~2 weeks), with rapid release at acidic pH (50% in 2 days).
  • The conjugates exhibited no toxicity to ARPE-19 cells and showed cellular association with intracellular localization.

Conclusions:

  • Pullulan-dexamethasone conjugates are a promising platform for sustained intravitreal drug delivery.
  • These nanoparticles may reduce the frequency of injections for treating posterior eye diseases.
  • Further investigation into their therapeutic potential in ocular conditions is warranted.