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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.
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Related Experiment Video

Updated: May 17, 2026

Intranasal Administration of CNS Therapeutics to Awake Mice

Intranasal Administration of CNS Therapeutics to Awake Mice

Published on: April 8, 2013

[Basic studies on the nasal delivery of insulin].

Toshinobu Seki¹

¹Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan. sekt1042@josai.ac.jp

Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan

|November 6, 2012

Summary

Nasal insulin delivery systems were explored to enhance absorption. Cationic polymers aided permeation, but PEGylation and cyclodextrin complexes show promise for improved insulin delivery, especially to the brain.

Area of Science:

Pharmacology
Biomaterials Science
Drug Delivery Systems

Background:

Insulin's molecular form (dimer, hexamer) impacts its nasal absorption.
Developing effective nasal insulin delivery systems is crucial for systemic or central nervous system targeting.
Understanding membrane transport mechanisms is key to optimizing drug permeation.

Purpose of the Study:

To investigate nasal absorption of insulin for targeted delivery.
To evaluate the role of penetration enhancers and insulin modification on nasal permeation.
To explore advanced formulations for enhanced insulin delivery.

Main Methods:

Utilized the Renkin function to analyze insulin penetration pathways through nasal mucosal membranes.
Assessed the impact of cationic polymers as penetration enhancers on pathway formation.

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Investigated PEGylation and modified cyclodextrin complexation for insulin formulation.

Main Results:

Cationic polymers increased hydrophilic compound pathways but excessive interaction hindered insulin permeation.
Insulin degradation during permeation necessitates protective strategies.
PEGylated insulin and cyclodextrin complexes demonstrated potential for modifying insulin's pharmacokinetic and pharmacodynamic profiles.

Conclusions:

Optimizing nasal insulin delivery requires careful selection of enhancers and protective strategies.
PEGylation and cyclodextrin complexation offer promising avenues for advanced insulin nasal delivery systems.
Well-designed complex systems may enable specific insulin delivery to the central nervous system.