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Related Experiment Videos

A new delivery system for antisense therapy: PLGA microspheres encapsulating oligonucleotide/polyethyleneimine solid

Giuseppe De Rosa1, Amélie Bochot, Fabiana Quaglia

  • 1Faculté de Pharmacie, Université Paris-Sud UMR CNRS 8612, Group of Drug targeting and delivery of poorly stable compounds, 5, rue Jean-Baptiste Clément, 92296 Châtenay-Malabry, France.

International Journal of Pharmaceutics
|March 5, 2003
PubMed
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Researchers developed microspheres for controlled release of antisense oligonucleotide targeting Transforming growth factor beta(1). These microspheres effectively encapsulate and slowly release oligonucleotide/polyethylenimine complexes for cellular uptake.

Area of Science:

  • Biomaterials Science
  • Drug Delivery
  • Molecular Biology

Background:

  • Transforming growth factor beta(1) is implicated in various diseases.
  • Antisense oligonucleotides offer targeted gene silencing strategies.
  • Controlled release systems are crucial for effective oligonucleotide delivery.

Purpose of the Study:

  • To design and characterize poly(lactide-co-glycolide) (PLGA) microspheres for the controlled release of an antisense oligonucleotide.
  • To investigate the impact of polyethylenimine (PEI) complexation and N/P ratios on microsphere properties.
  • To evaluate the in vitro release profile and potential for cellular internalization.

Main Methods:

  • Preparation of PLGA microspheres using the multiple emulsion-solvent evaporation technique.

Related Experiment Videos

  • Encapsulation of free antisense oligonucleotide or its solid complexes with PEI at varying N/P ratios.
  • Characterization of microspheres for loading efficiency, morphology, internal distribution, and in vitro release kinetics.

    • Main Results:

    • Microsphere characteristics, including loading, morphology, and oligonucleotide distribution, were influenced by the form of encapsulation (free vs. PEI complex), N/P ratio, and PLGA type.
    • The designed microspheres demonstrated successful encapsulation of oligonucleotide/PEI solid complexes.
    • A slow and controlled in vitro release of the encapsulated oligonucleotide/PEI complexes was observed.

    Conclusions:

    • PLGA microspheres effectively encapsulate antisense oligonucleotide/PEI complexes.
    • The formulation parameters (complexation, N/P ratio, PLGA type) significantly influence microsphere performance.
    • The developed microspheres facilitate the slow release of complexes, promoting potential cellular internalization for therapeutic applications.