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Insulin Formulations: Types and Delivery

Insulin Formulations: Types and Delivery

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 rapid-acting...

Insulin: Biosynthesis, Chemistry, and Preparation

Insulin: Biosynthesis, Chemistry, and Preparation

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 primarily uses...

Insulin: Dosing Regimen and Adverse Effects

Insulin: Dosing Regimen and Adverse Effects

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...

Glucagon-like Receptor Agonists

Glucagon-like Receptor Agonists

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 the...

Oral Hypoglycemic Agents: Glinides

Oral Hypoglycemic Agents: Glinides

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 manages...

Production of Pharmaceuticals

Production of Pharmaceuticals

Industrial insulin production uses genetically engineered E. coli expressing a proinsulin gene controlled by a tryptophan promoter and containing a methionine linker for later cleavage. The cells also carry ampicillin resistance for selective growth. Seed cultures are stored at −80 °C and production begins by thawing a small amount to inoculate starter cultures, which are progressively scaled to a 50,000-L bioreactor. In the bioreactor, E. coli grow in nutrient-rich media under sterile, tightly...

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Related Experiment Video

Updated: May 22, 2026

Homogeneous Time-resolved Förster Resonance Energy Transfer-based Assay for Detection of Insulin Secretion

Homogeneous Time-resolved Förster Resonance Energy Transfer-based Assay for Detection of Insulin Secretion

Published on: May 10, 2018

Insulins: past, present, and future.

Carla A Borgoño¹, Bernard Zinman

¹Division of General Internal Medicine, Department of Medicine, University of Toronto, 200 Elizabeth Street, Toronto, Ontario, Canada.

Endocrinology and Metabolism Clinics of North America

|May 12, 2012

Summary

Over 90 years, insulin therapy has evolved from animal extracts to advanced human analogues for diabetes. Ongoing research in injectable insulin formulations promises enhanced glucose control for type 1 and type 2 diabetes.

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Area of Science:

Endocrinology
Pharmacology
Diabetology

Background:

Insulin therapy is a cornerstone in managing diabetes mellitus.
Significant advancements have occurred in insulin production and delivery over the past 90 years.
Current insulin treatments aim to mimic physiological insulin secretion but face challenges.

Purpose of the Study:

To review key milestones in insulin discovery and development.
To highlight progress in insulin therapy for diabetes management.
To discuss the future of injectable insulin formulations.

Main Methods:

Historical review of insulin discovery and therapeutic evolution.
Analysis of advancements in insulin formulations and delivery systems.
Discussion of pharmacokinetic and pharmacodynamic improvements.

Main Results:

Insulin therapy has progressed from crude animal extracts to sophisticated human insulin analogues.
Despite challenges in complete physiological replacement, significant improvements in glucose control have been achieved.
Novel insulin formulations offer enhanced pharmacokinetics and pharmacodynamics.

Conclusions:

Continued development of injectable insulin formulations is crucial for improving diabetes care.
Advanced insulin therapies represent important clinical progress for type 1 and type 2 diabetes.
Future innovations will further enhance glucose management in diabetic patients.