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Combinatorial Synthesis of and High-throughput Protein Release from Polymer Film and Nanoparticle Libraries
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Published on: September 6, 2012

Novel composite microparticles for protein stabilization and delivery.

Aurélie Schoubben1, Paolo Blasi, Stefano Giovagnoli

  • 1Department of Chemistry and Technology of Drugs, School of Pharmacy, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy.

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
|October 28, 2008
PubMed
Summary

This study developed novel alginate/poly(lactic-co-glycolic) acid microparticles for enhanced protein delivery. These composite systems improved insulin stability and enabled sustained release for up to four months.

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Area of Science:

  • Biomaterials Science
  • Drug Delivery Systems
  • Protein Stabilization

Background:

  • Protein-based therapeutics, like insulin, require effective stabilization and controlled delivery systems to maintain efficacy.
  • Conventional microparticle formulations often face challenges with protein degradation and premature release.
  • Developing novel composite materials can overcome these limitations for improved therapeutic outcomes.

Purpose of the Study:

  • To engineer a novel composite alginate/poly(lactic-co-glycolic) acid (PLGA) microparticulate system.
  • To evaluate this system for the stabilization and controlled delivery of bovine insulin.
  • To compare the performance of composite microparticles against conventional ones.

Main Methods:

  • Alginate particles were prepared via ionic gelation and embedded into PLGA microparticles using solvent diffusion-evaporation.
  • Insulin loading was quantified using micro-BCA assay and reversed-phase high-performance liquid chromatography (RP-HPLC).
  • In vitro release studies and protein adsorption were assessed under specific buffer conditions (10 mM glycine, pH 2.8, 37°C).

Main Results:

  • Composite microparticles demonstrated reproducible encapsulation efficiency and higher soluble insulin content compared to conventional microparticles.
  • Bovine insulin alone showed instability in the buffer, with 55% loss after 7 days.
  • The composite microparticles exhibited sustained insulin release for up to 4 months with minimal burst effect and no significant peptide adsorption on PLGA, but showed strong interaction with alginate.

Conclusions:

  • The developed alginate/PLGA composite microparticles offer a promising platform for stabilizing and delivering proteins like insulin.
  • The system effectively protects insulin from degradation and provides sustained release, overcoming limitations of conventional methods.
  • The observed interaction between alginate and insulin suggests a role in the enhanced stability and controlled release profile.