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Related Concept Videos

Insulin Formulations: Types and Delivery01:27

Insulin Formulations: Types and Delivery

283
Insulin preparations are categorized by their duration of action into short-acting and long-acting types. Two strategies are used to modify insulin's absorption and pharmacokinetic profile: slowing the absorption post-subcutaneous injection, or altering human insulin's amino acid sequence or protein structure. These changes retain the insulin's ability to bind to the insulin receptor, but alter its behavior in solution or after injection.
Short-acting insulins are divided into...
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Oral Hypoglycemic Agents: Glinides01:06

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Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively...
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IgG functionalized polymeric nanoparticles for oral insulin administration.

J G B De Marchi1, R Cé2, G Onzi3

  • 1Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, RS 90610-000, Brazil; Universidade de Coimbra, Faculdade de Farmácia, Coimbra, Portugal.

International Journal of Pharmaceutics
|May 17, 2022
PubMed
Summary

Developing functionalized nanoparticles with immunoglobulin G enhances oral insulin delivery. This approach shows promise for improving the absorption of low-absorption peptide drugs through the intestinal epithelium.

Keywords:
FunctionalizationIntestinal permeationNanoparticleOral deliveryRelease profile

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Area of Science:

  • Biomaterials Science
  • Pharmaceutical Sciences
  • Drug Delivery Systems

Background:

  • Oral drug administration is ideal but challenging for peptide drugs like insulin, with low systemic bioavailability (<0.5%).
  • Nanoparticle-based oral delivery systems offer potential for enhanced peptide permeability and stability in the gastrointestinal tract.
  • Active targeting strategies are needed to further improve nanoparticle absorption across the intestinal epithelium.

Purpose of the Study:

  • To develop and characterize an improved nanoparticle formulation for oral insulin delivery.
  • To enhance intestinal epithelial absorption by functionalizing nanoparticle surfaces with immunoglobulin G (IgG).
  • To evaluate the impact of IgG functionalization on nanoparticle characteristics and insulin release profiles.

Main Methods:

  • Nanoparticle formulation and characterization (size, entrapment efficiency).
  • Surface functionalization of nanoparticles with immunoglobulin G.
  • Assessment of insulin release kinetics from functionalized nanoparticles.
  • Physicochemical analysis using differential scanning calorimetry, infrared spectroscopy, and paper chromatography to confirm component interactions.

Main Results:

  • Formulations exhibited adequate nanoparticle size and high entrapment efficiency.
  • IgG functionalization slightly increased nanoparticle size without aggregation.
  • Functionalized nanoparticles demonstrated an extended insulin release time.
  • Physicochemical analyses confirmed interactions between nanoparticle components and IgG.

Conclusions:

  • The developed IgG-functionalized nanoparticles are suitable carriers for oral insulin delivery.
  • This formulation shows potential for increased internalization by intestinal epithelial cells.
  • It represents a promising alternative to current formulations for orally administered, poorly absorbed peptides.