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Enzyme structure and function protection from gastrointestinal degradation using enteric coatings.

Ruben Gracia1, Cristina Yus1, Olga Abian2

  • 1Department of Chemical Engineering, Aragon Institute of Nanoscience (INA), University of Zaragoza, Campus Río Ebro-Edificio I + D, C/ Poeta Mariano Esquillor S/N, 50018 Zaragoza, Spain; Networking Research Center on Bioengineering, Biomaterials and Nanomedicine, CIBER-BBN, 28029 Madrid, Spain.

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Summary

This study developed Eudragit RS100 microparticles for oral delivery of therapeutic proteins like Bovine Serum Albumin (BSA) and Horseradish Peroxidase (HRP). The microparticles demonstrated excellent encapsulation, stability, and gastroresistance, preserving protein function upon release.

Keywords:
Enteric microparticlesEudragitProtein encapsulationProtein stabilitySustained release

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Area of Science:

  • Biomaterials Science
  • Pharmaceutical Technology
  • Drug Delivery Systems

Background:

  • Oral delivery of therapeutic proteins faces challenges due to enzymatic degradation in the gastrointestinal tract.
  • Developing protective delivery systems is crucial for enhancing protein bioavailability and therapeutic efficacy.

Purpose of the Study:

  • To encapsulate Bovine Serum Albumin (BSA) and Horseradish Peroxidase (HRP) into Eudragit RS100 microparticles.
  • To evaluate the stability, gastroresistance, and functional integrity of encapsulated proteins.
  • To assess the potential of these microparticles as oral delivery vectors for therapeutic proteins.

Main Methods:

  • Water-in-oil-in-water double emulsion solvent evaporation technique for microparticle preparation.
  • Encapsulation efficiency determined using standard assays.
  • Protein stability assessed via circular dichroism and fluorescence spectroscopy.
  • Gastroresistance evaluated under simulated gastric conditions.
  • Enzymatic activity of released Horseradish Peroxidase (HRP) measured using a peroxidase substrate.

Main Results:

  • High encapsulation efficiencies achieved for BSA (88.4%) and HRP (95.8%).
  • Encapsulated proteins maintained structural integrity and stability.
  • Microparticles exhibited excellent gastroresistance, protecting proteins from simulated gastric conditions.
  • Released HRP retained 100% of its enzymatic activity.
  • High drug loadings and reduced cytotoxicity observed.

Conclusions:

  • Eudragit RS100 microparticles are effective carriers for oral protein delivery.
  • These carriers offer enhanced gastrointestinal protection and controlled release.
  • Potential for improved oral absorption and targeted intestinal delivery of therapeutic proteins.