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Related Experiment Videos

Transmucosal macromolecular drug delivery.

C Prego1, M García, D Torres

  • 1Department Pharmaceutical Technology, University of Santiago de Compostela (USC), Campus Sur, 15782 Santiago de Compostela, Spain.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|December 14, 2004
PubMed
Summary

Chitosan (CS)-coated nanostructures effectively deliver large drug molecules across mucosal barriers. These nanoparticles enhance peptide and protein absorption, showing promise for drug delivery systems.

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Area of Science:

  • Biomedical Engineering
  • Materials Science
  • Pharmaceutics

Background:

  • Mucosal drug delivery is ideal for peptides and proteins, but barriers limit absorption.
  • Nanoparticulate carriers offer a promising strategy to overcome these limitations.
  • Chitosan (CS) is a mucoadhesive polysaccharide explored for drug delivery.

Purpose of the Study:

  • To compare the characteristics and drug delivery potential of three chitosan-based nanostructures: CS nanoparticles, CS-coated oil nanodroplets (nanocapsules), and CS-coated lipid nanoparticles.
  • To investigate the interaction of these nanostructures with epithelial models and their in vivo efficacy.
  • To evaluate the influence of the nanostructure's core material on drug absorption.

Main Methods:

  • Synthesis and characterization of CS nanocapsules.

Related Experiment Videos

  • Comparison of CS nanoparticles, CS nanocapsules, and CS-coated lipid nanoparticles.
  • Assessment of peptide/protein association capacity.
  • Investigation of epithelial interaction using Caco-2 cell monolayers (transepithelial resistance, internalization).
  • In vivo evaluation of intestinal absorption enhancement in rats using salmon calcitonin.

    • Main Results:

    • All three CS-coated nanostructures exhibited nanoscale dimensions and positive surface charge due to CS.
    • They effectively associated with model peptides (insulin, salmon calcitonin) and proteins (tetanus toxoid).
    • CS-coated systems reduced transepithelial resistance and were internalized by Caco-2 cells in a concentration-dependent manner.
    • Uptake was influenced by the lipid core's nature but not significantly by the CS coating alone.
    • Both CS nanocapsules and CS-coated nanoparticles enhanced salmon calcitonin intestinal absorption in rats, indicated by prolonged hypocalcemia.

    Conclusions:

    • Chitosan-coated nanostructures are effective carriers for macromolecular drugs across mucosal barriers.
    • These systems demonstrate potential for enhancing peptide and protein absorption via mucosal routes.
    • The choice of lipid core influences cellular uptake, but CS coating is crucial for enhanced in vivo absorption.