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Related Concept Videos

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 Formulations: Types and Delivery01:27

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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.
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Insulin Secretory Vesicles01:05

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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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Glucagon-like Receptor Agonists01:24

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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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Insulin: Biosynthesis, Chemistry, and Preparation01:25

Insulin: Biosynthesis, Chemistry, and Preparation

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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.
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Glucose Homeostasis: Pancreatic Islets and Insulin Secretion01:27

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The pancreatic islets comprising only 1%-2% of the volume are highly vascularized and innervated mini-organs. They contain five endocrine cell types, including β cells that secrete insulin, which is synthesized as a single polypeptide chain, preproinsulin, processed to proinsulin, and finally to insulin and C-peptide. This process is complex and regulated, involving the Golgi complex, the endoplasmic reticulum, and the secretory granules of the β cell.
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Related Experiment Video

Updated: Aug 6, 2025

Injectable Supramolecular Polymer-Nanoparticle Hydrogels for Cell and Drug Delivery Applications
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Glucose-Responsive Charge-Switchable Lipid Nanoparticles for Insulin Delivery.

Yun Liu1,2, Yanfang Wang1,2, Yuejun Yao1,2

  • 1Key Laboratory of Advanced Drug Delivery Systems of Zhejiang Province, College of Pharmaceutical Sciences, Zhejiang University, 310058, Hangzhou, China.

Angewandte Chemie (International Ed. in English)
|March 16, 2023
PubMed
Summary

Researchers developed glucose-responsive lipid nanoparticles for insulin delivery. These nanoparticles offer prolonged blood glucose regulation and triggered insulin release in a type 1 diabetic mouse model.

Keywords:
DiabetesDrug DeliveryGlucose-ResponsiveInsulin DeliveryLipid Nanoparticles

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Pharmacology

Background:

  • Lipid nanoparticles (LNPs) are crucial for nucleic acid delivery in therapy and vaccination.
  • Current insulin delivery methods lack precise glucose-responsiveness.
  • Recombinant human insulin, like mRNA, is negatively charged and suitable for LNP encapsulation.

Purpose of the Study:

  • To design and develop novel glucose-responsive lipid nanoparticles for targeted insulin delivery.
  • To investigate the glucose-triggered release mechanism of encapsulated insulin.
  • To evaluate the efficacy of LNP-encapsulated insulin in a type 1 diabetic mouse model.

Main Methods:

  • Synthesized phenylboronic acid-based quaternary amine cationic lipids.
  • Self-assembled cationic lipids into spherical lipid nanoparticles in aqueous solution.
  • Formed insulin-LNP complexes via electrostatic attraction and tested glucose-responsive release in vitro and in vivo.

Main Results:

  • Designed cationic lipids self-assembled into stable, spherical lipid nanoparticles.
  • Formed heterostructured insulin-LNP complexes with immediate electrostatic attraction.
  • Demonstrated reduced nanoparticle charge and subsequent insulin release in hyperglycemia-relevant glucose solutions.
  • Observed prolonged blood glucose regulation and glucose-triggered insulin release in a type 1 diabetic mouse model.

Conclusions:

  • Phenylboronic acid-based cationic lipids enable the creation of glucose-responsive insulin-loaded lipid nanoparticles.
  • These novel nanoparticles provide a promising platform for advanced diabetes management.
  • The developed system offers improved blood glucose control through triggered insulin release.