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Related Experiment Videos

Nanosphere based oral insulin delivery.

G P Carino1, J S Jacob, E Mathiowitz

  • 1Department of Molecular Pharmacology, Physiology and Biotechnology, Brown University, Providence, RI 02912, USA.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|March 4, 2000
PubMed
Summary

Researchers developed oral zinc insulin nanoparticles using Phase Inversion Nanoencapsulation (PIN). The novel poly(lactide-co-glycolide) (PLGA) formulation demonstrates significant oral efficacy for diabetes management.

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Area of Science:

  • Biomaterials Science
  • Drug Delivery
  • Nanotechnology

Background:

  • Oral delivery of protein-based therapeutics like insulin is challenging due to enzymatic degradation and poor absorption in the gastrointestinal tract.
  • Nanoparticle formulations offer a promising strategy to protect insulin and enhance its oral bioavailability.
  • Polyester and polyanhydride nanospheres are being explored for encapsulating sensitive biomolecules.

Purpose of the Study:

  • To develop and evaluate novel nanosphere formulations for oral delivery of zinc insulin.
  • To assess the biological activity, release kinetics, and oral efficacy of encapsulated zinc insulin.
  • To identify key formulation properties contributing to successful oral delivery.

Main Methods:

  • Zinc insulin was encapsulated into various polyester and polyanhydride nanospheres using Phase Inversion Nanoencapsulation (PIN).

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  • A specific formulation comprising zinc insulin in poly(lactide-co-glycolide) (PLGA) with fumaric anhydride oligomer and iron oxide additives was selected for further study.
  • In vitro release kinetics and in vivo oral efficacy, including plasma glucose control during a glucose challenge, were evaluated.

    • Main Results:

    • Encapsulated zinc insulin maintained biological activity and exhibited a release profile of approximately 6 hours.
    • The specific PLGA-based formulation demonstrated oral activity, achieving 11.4% of the efficacy of intraperitoneally delivered zinc insulin.
    • This formulation effectively controlled plasma glucose levels in response to an oral glucose challenge.

    Conclusions:

    • Phase Inversion Nanoencapsulation (PIN) is a viable method for creating orally active zinc insulin nanospheres.
    • The PLGA-based formulation shows potential for oral insulin therapy, with properties like size, release, and gastrointestinal traversal contributing to its efficacy.
    • Further research into nanocarrier properties can optimize oral delivery of protein therapeutics.