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Related Concept Videos

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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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 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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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.
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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 action is mediated through a receptor tyrosine kinase, akin to the IGF-1 receptor. The number of receptors per cell varies significantly, from 40 on erythrocytes to 300,000 on adipocytes and hepatocytes. The insulin receptor consists of linked α/β subunit dimers, forming a heterotetramer glycoprotein with two extracellular α subunits and two β subunits spanning the membrane. The α subunits inhibit the inherent tyrosine kinase activity of the β subunits, but...
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Updated: Aug 22, 2025

Injectable Supramolecular Polymer-Nanoparticle Hydrogels for Cell and Drug Delivery Applications
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Glucose-responsive nanoparticles designed via a molecular-docking-driven method for insulin delivery.

Di Shen1, Haojie Yu1, Li Wang1

  • 1State Key Laboratory of Chemical Engineering, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310027, PR China.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|November 7, 2022
PubMed
Summary

Researchers developed smart, glucose-responsive insulin nanoparticles for better diabetic treatment. The novel formulation effectively controlled nocturnal blood glucose in rats, reducing hypoglycemia risk compared to traditional methods.

Keywords:
Anti-hypoglycemia propertiesDiabetesGlucose-responsive nanoparticlesInsulin deliveryMolecular docking

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Area of Science:

  • Biomaterials Science
  • Polymer Chemistry
  • Nanotechnology
  • Diabetic Treatment

Background:

  • Nocturnal blood glucose regulation presents a significant challenge in diabetes management.
  • Current smart insulin delivery systems often rely on extensive empirical testing and researcher experience.
  • Developing glucose-responsive systems with mild and effective performance is crucial for improved patient outcomes.

Purpose of the Study:

  • To design and synthesize bioinspired, fatty-acid-modified, glucose-responsive polymeric nanoparticles for insulin delivery.
  • To utilize molecular docking for efficient screening of functional groups in polymer design.
  • To evaluate the efficacy and safety of the optimized nanoparticles in a preclinical model.

Main Methods:

  • Design of fatty-acid-modified glucose-responsive polymeric nanoparticles.
  • Application of molecular docking to screen functional groups for polymer modification.
  • In vivo evaluation of insulin-loaded nanoparticles (C10MS) in diabetic rats for nocturnal glycemic control.
  • Assessment of biocompatibility and pharmacokinetic profiles.

Main Results:

  • The optimized formulation (C10MS) demonstrated successful nocturnal glycemic control in diabetic rats.
  • The C10MS formulation exhibited a lower incidence of hypoglycemia compared to conventional insulin injections.
  • The nanoparticles showed good biocompatibility and moderate in vivo elimination kinetics, suitable for daily treatment.

Conclusions:

  • This study presents an efficient, experience-guided approach for designing functional polymeric materials for smart drug delivery.
  • Bioinspired fatty-acid-modified nanoparticles offer a promising strategy for improved diabetes management, particularly for nocturnal glucose regulation.
  • The developed system simplifies the optimization process for glucose-responsive insulin delivery systems.