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Protein delivery using nanoparticles based on microemulsions with different structure-types.

Anja Graf1, Kevin S Jack, Andrew K Whittaker

  • 1School of Pharmacy, University of Otago, P.O. Box 913, Dunedin, New Zealand. anja.graf@stonebow.otago.ac.nz

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
|March 11, 2008
PubMed
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Researchers developed poly(alkylcyanoacrylate) nanoparticles using microemulsions for oral insulin delivery. These biocompatible nanoparticles showed effective insulin encapsulation and controlled release, offering a promising platform for protein drug delivery.

Area of Science:

  • Polymer Science and Nanotechnology
  • Pharmaceutical Sciences
  • Colloid and Surface Chemistry

Background:

  • Developing effective oral delivery systems for proteins like insulin remains a significant challenge due to enzymatic degradation and poor absorption.
  • Microemulsions offer a versatile platform for encapsulating sensitive biomolecules due to their unique structural properties and ability to stabilize interfaces.

Purpose of the Study:

  • To prepare and characterize poly(alkylcyanoacrylate) nanoparticles using various microemulsion structures for insulin encapsulation.
  • To investigate the influence of microemulsion type on nanoparticle formation, insulin entrapment, and release kinetics.
  • To evaluate the potential of these nanoparticles for oral insulin delivery.

Main Methods:

  • Construction of a phase diagram for a pseudoternary system to identify microemulsion regions (water-in-oil, bicontinuous, oil-in-water).

Related Experiment Videos

  • Characterization of microemulsions using viscosity, conductivity, differential scanning calorimetry, and self-diffusion NMR.
  • Preparation of poly(alkylcyanoacrylate) nanoparticles via interfacial polymerization using ethyl and butyl cyanoacrylate.
  • Analysis of nanoparticle size distribution, insulin entrapment efficiency, and in vitro release profiles over 6 hours.

    • Main Results:

    • Microemulsions with different structures (w/o, bicontinuous, o/w) were successfully prepared and characterized.
    • Nanoparticle size ranged from 160 to 400 nm, dependent on microemulsion template and monomer used.
    • Insulin entrapment efficiency was between 11.5% and 20.9%.
    • A near zero-order release of insulin was observed after an initial burst release, with loaded nanoparticles measuring 320-350 nm.
    • Microemulsion structure was maintained during polymerization, confirmed by NMR.

    Conclusions:

    • Microemulsions provide a flexible and adaptable platform for designing nanoparticle encapsulation processes for peptides and proteins.
    • Poly(alkylcyanoacrylate) nanoparticles derived from these microemulsions demonstrate potential for the oral delivery of insulin.
    • The microstructure of the microemulsion plays a crucial role in the characteristics of the resulting nanoparticles and their drug delivery capabilities.