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Related Concept Videos

Insulin Formulations: Types and Delivery01:27

Insulin Formulations: Types and Delivery

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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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Insulin: Biosynthesis, Chemistry, and Preparation01:25

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The endoplasmic reticulum (ER) of pancreatic β-cells synthesizes preproinsulin, which consists of a signal peptide, A and B chains, and a C-peptide. Preproinsulin is then cleaved and folded into proinsulin, which translocates to the Golgi apparatus for sorting and packaging into secretory granules. In these granules, enzymatic clipping generates insulin and C-peptide.
Damage or functional impairment of β-cells inhibits insulin production, leading to diabetes. Diabetes treatment...
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Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

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Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
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Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

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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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Insulin: Dosing Regimen and Adverse Effects01:16

Insulin: Dosing Regimen and Adverse Effects

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Insulin-replacement therapy usually includes both long-acting insulin (basal) and short-acting insulin (to cater to postprandial needs). In a diverse group of type 1 diabetes patients, the average daily insulin dose is typically 0.5-0.7 units/kg body weight. However, obese patients and pubertal adolescents may need more due to insulin resistance.
The basal dose constitutes about 40%-50% of the total daily dose, with the rest as premeal insulin. The mealtime insulin dose should mirror...
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Insulin Secretory Vesicles01:05

Insulin Secretory Vesicles

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Insulin secretory vesicles release insulin to stimulate blood glucose uptake and regulate carbohydrate metabolism. When the blood glucose levels increase, glucose enters the pancreatic β-islet cells through glucose transporters. Once inside, glucose is metabolized through glycolysis, the citric acid cycle, and the electron transport chain, producing ATP. This increase in ATP concentration closes ATP-sensitive potassium channels, leading to depolarization of the membrane and the opening of...
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Sustained Administration of β-cell Mitogens to Intact Mouse Islets Ex Vivo Using Biodegradable Poly(lactic-co-glycolic acid) Microspheres
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Small Intestine-Targeted Long-Acting Oral Insulin Formulation Based on Engineered Milk Protein Nanoparticles.

Anbu Mozhi Thamizhchelvan1, Yuancheng Li1,2, Jonathan Padelford2

  • 1Department of Radiology and Imaging Sciences, Emory University School of Medicine, Atlanta, Georgia 30322, United States.

ACS Applied Bio Materials
|December 24, 2025
PubMed
Summary

This study developed an oral insulin formulation using casein nanocarriers with sodium caprate. The new oral insulin effectively lowers blood sugar and improves bioavailability, offering a promising alternative to injections for diabetes management.

Keywords:
diabetesinsulinlong actingmilk proteinnanoparticleoral delivery

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Area of Science:

  • Biomaterials Science
  • Drug Delivery Systems
  • Endocrinology

Background:

  • Subcutaneous insulin injections are standard for diabetes, but face challenges like poor compliance and hypoglycemia.
  • Oral insulin formulations aim to improve adherence and mimic natural insulin release, yet face bioavailability issues.

Purpose of the Study:

  • To develop and evaluate a novel oral insulin formulation using casein nanocarriers coencapsulating insulin and sodium caprate.
  • To assess the stability, release kinetics, bioavailability, and glycemic control efficacy of the oral insulin formulation.

Main Methods:

  • Insulin and sodium caprate (C10) were coencapsulated into casein-based nanocarriers (casNP).
  • Formulation stability was tested in simulated gastric and jejunal fluids.
  • Ex vivo gut sac studies optimized C10 concentration.
  • Oral administration in mice assessed pharmacokinetic and pharmacodynamic parameters.

Main Results:

  • casNP/insulin/C10 showed stability in simulated gastric fluid and release in jejunal fluid.
  • Oral delivery in mice achieved 10.8% small intestine delivery and 18.1% bioavailability.
  • Oral casNP/insulin/C10 demonstrated comparable glycemic control to subcutaneous insulin Aspart, with a longer duration of action and no hypoglycemia.

Conclusions:

  • Casein nanocarriers effectively deliver insulin orally, enhancing bioavailability and efficacy.
  • This oral insulin formulation shows significant potential for improved diabetes management and patient compliance.
  • Further clinical studies are warranted to validate this promising oral insulin delivery system.