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Radiolabelled biodegradable microspheres for lung imaging.

A Delgado1, I Soriano, E Sánchez

  • 1Departamento de Ingeniería Química y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de La Laguna, La Laguna, Spain.

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V
|August 30, 2000
PubMed
Summary

Modifying poly(lactide-co-glycolide) (PLGA) microsphere surfaces with poloxamer 188 surfactant significantly enhanced lung accumulation. This improved imaging quality, though liver uptake later interfered.

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Area of Science:

  • Biomedical Engineering
  • Radiopharmacy
  • Materials Science

Background:

  • Poly(lactide-co-glycolide) (PLGA) and PEG-PLGA microspheres are utilized in drug delivery.
  • Lung accumulation of intravenously injected microspheres is crucial for certain imaging applications.

Purpose of the Study:

  • To evaluate the impact of different surfactants on the lung accumulation of (99m)Tc-labeled PLGA and PEG-PLGA microspheres.
  • To assess the potential of surfactant-modified microspheres for lung imaging.

Main Methods:

  • Preparation of (99m)Tc-labeled PLGA and PEG-PLGA microspheres using emulsion solvent evaporation with various surfactants (PVA, PEG, BSA, poloxamer 188).
  • Intravenous injection of microspheres into rats and assessment of lung accumulation via gamma camera imaging.
  • Comparison with commercial human albumin microspheres (HAM) as a reference.

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Main Results:

  • PLGA microspheres formulated with 8% poloxamer 188 achieved 67% lung accumulation, significantly higher than other surfactants.
  • PLGA microspheres with 1-4% poloxamer 188 showed >50% lung accumulation.
  • Microspheres with 8% poloxamer 188 provided initial good quality lung images, but liver uptake later obscured lung visualization.

Conclusions:

  • Surface modification of PLGA microspheres with poloxamer 188 is an effective strategy to enhance lung accumulation.
  • Optimized PLGA microspheres show promise for lung imaging applications, but further investigation is needed to address later liver interference.