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Multifunctional polyelectrolyte microparticles for oral insulin delivery.

Nadezhda G Balabushevich1, Mikhail A Pechenkin, Elena D Shibanova

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New microparticles enhance oral insulin delivery. These novel drug delivery systems improve insulin bioavailability and show effectiveness in diabetic rats, offering a promising alternative to injections.

Keywords:
chitosaninsulinlayer-by-layermicroencapsulationoral drug delivery systemsprotease inhibitor

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Area of Science:

  • Biomaterials Science
  • Drug Delivery
  • Nanotechnology

Background:

  • Oral insulin delivery remains a significant challenge due to enzymatic degradation and poor absorption.
  • Developing effective insulin formulations requires overcoming barriers in the gastrointestinal tract.
  • Microparticle-based systems offer potential for protecting and delivering therapeutic proteins orally.

Purpose of the Study:

  • To develop and characterize multicomponent insulin-containing microparticles for improved oral bioavailability.
  • To investigate the influence of formulation components on insulin release kinetics and mucoadhesion.
  • To evaluate the efficacy of oral microencapsulated insulin in a diabetic rat model.

Main Methods:

  • Layer-by-layer assembly of dextran sulfate and chitosan on a protein-polyanion core.
  • Physico-chemical characterization including pH-dependent release, mucoadhesion, and Ca(2+) binding.
  • Inclusion of protease inhibitors to prevent insulin degradation.
  • Pharmacological evaluation in streptozotocin-induced diabetic rats.

Main Results:

  • Successfully prepared insulin-loaded microparticles with tunable pH-dependent release profiles.
  • Demonstrated enhanced mucoadhesive properties and Ca(2+) binding capabilities.
  • Protease inhibitors (2-3%) effectively prevented human insulin proteolysis.
  • Significant pharmacological effect observed in diabetic rats after oral administration of microencapsulated insulin.

Conclusions:

  • Multicomponent microparticles represent a viable strategy for enhancing oral insulin bioavailability.
  • The formulation design allows for controlled release and improved interaction with the gastrointestinal environment.
  • Oral administration of encapsulated insulin in this system shows therapeutic potential for managing diabetes.