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Related Concept Videos

Insulin Formulations: Types and Delivery01:27

Insulin Formulations: Types and Delivery

190
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...
190
Insulin: Biosynthesis, Chemistry, and Preparation01:25

Insulin: Biosynthesis, Chemistry, and Preparation

372
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...
372
Insulin: Dosing Regimen and Adverse Effects01:16

Insulin: Dosing Regimen and Adverse Effects

166
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...
166
Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

316
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...
316
Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

152
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...
152

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Author Spotlight: Innovative Microneedle-Based Strategies for Enhanced Exosome Delivery and Stability
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Converting Short-Acting Insulin into Thermo-Stable Longer-Acting Insulin Using Multi-Layer Detachable Microneedles.

Theerapat Phoka1, Nisha Wanichwecharungruang2, Narintorn Dueanphen1

  • 1Center of Excellence in Materials and Bio-Interfaces, Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok, Thailand.

Journal of Pharmaceutical Sciences
|June 10, 2024
PubMed
Summary

Detachable dissolving microneedles (DDMNs) improve insulin's storage stability and delivery. These microneedles offer enhanced thermal stability and efficient transdermal delivery for diabetes management.

Keywords:
InsulinIntradermalPeptide deliveryPharmacodynamicPharmacokineticsSkin

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Area of Science:

  • Biomaterials Science
  • Pharmaceutical Sciences
  • Endocrinology

Background:

  • Insulin therapy for diabetes requires efficient delivery and stable formulations.
  • Current insulin delivery methods face challenges with stability and patient compliance.
  • Microneedle technology offers a promising alternative for transdermal drug delivery.

Purpose of the Study:

  • To develop and characterize detachable dissolving microneedles (DDMNs) for improved insulin delivery.
  • To enhance the thermal stability and storage of insulin using a microneedle formulation.
  • To evaluate the in vitro and in vivo efficacy of insulin-loaded DDMNs.

Main Methods:

  • Fabrication of multi-layered insulin-loaded DDMNs incorporating hyaluronic acid and sorbitol.
  • Assessment of insulin's thermal stability within the DDMN matrix using differential scanning calorimetry.
  • Evaluation of ex vivo skin permeation and in vivo pharmacokinetic studies in diabetic rats.

Main Results:

  • Insulin-DDMNs demonstrated significantly enhanced thermal stability, with insulin denaturation temperature increased to 186 °C.
  • High in vitro delivery efficiency of 91±1.59% was achieved using ex vivo porcine skin.
  • In vivo studies in diabetic rats showed sustained insulin release, delayed hypoglycemic onset, and prolonged duration compared to subcutaneous injection.

Conclusions:

  • Insulin-DDMNs provide a stable and efficient platform for transdermal insulin delivery.
  • This microneedle system offers potential for improved diabetes management through enhanced insulin stability and controlled release.
  • DDMNs represent a promising advancement in needle-free insulin administration technologies.