Related Experiment Video

Updated: Sep 19, 2025

Sustained Administration of β-cell Mitogens to Intact Mouse Islets Ex Vivo Using Biodegradable Poly(lactic-co-glycolic acid) Microspheres
09:31

Sustained Administration of β-cell Mitogens to Intact Mouse Islets Ex Vivo Using Biodegradable Poly(lactic-co-glycolic acid) Microspheres

Published on: November 5, 2016

7.3K

FcRn-targeted Pluronic F127-Poly (L-lactic Acid) polymersomes for oral insulin delivery

Pin Pin Ma1, Zi Ling Li1, Hong Xia Gao1

  • 1School of Life Science, Jiangxi Science and Technology Normal University, Jiangxi Key Laboratory of Natural Microbial Medicine Research, Key Laboratory of Microbial Resources and Metabolism of Nanchang City, Nanchang 330013, China.

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V
|June 6, 2025
PubMed

Insights

Researchers developed Fc-binding peptide (FcBP)-modified polymersomes for oral insulin delivery. These targeted carriers significantly enhanced insulin transport across the intestinal barrier and improved bioavailability in vivo, showing promise for oral insulin therapy.

Area of Science:

  • Biomaterials Science
  • Drug Delivery Systems
  • Nanotechnology

Background:

  • The intestinal epithelium poses a significant barrier to oral drug delivery, particularly for large molecules like insulin.
  • The Neonatal Fc receptor (FcRn) in the intestinal epithelium can enhance transcytosis of molecules bound to its ligand.
  • Fc-binding peptides (FcBP) can leverage FcRn for improved drug transport.

Purpose of the Study:

  • To develop FcRn-targeted polymersomes for enhanced oral insulin delivery.
  • To investigate the effect of FcBP modification on the transepithelial transport of polymersomes.
  • To evaluate the in vivo efficacy and bioavailability of insulin loaded into FcBP-modified polymersomes.

Main Methods:

  • FcBP ligand was conjugated to Pluronic F127-polylactic acid (F127-PLA) polymersomes using biotin-avidin bridging.
  • Insulin loading efficiency was determined.
  • Transepithelial transport of Coumarin-6 loaded polymersomes was assessed using Caco-2 cell monolayers.
  • In vivo hypoglycemic effects and bioavailability of oral insulin were evaluated in animal models.

Main Results:

  • FcBP-F127-PLA polymersomes successfully encapsulated insulin with a loading efficiency of 12.01%.
  • FcBP-modified polymersomes showed a 1.7-fold increase in cumulative permeability and a 1.8-fold increase in apparent permeability coefficient (Papp) compared to unmodified polymersomes.
  • Optimal FcBP ligand density was identified, with 10% FcBP molar content yielding the best transport.
  • In vivo studies demonstrated a 1.27-fold increase in relative pharmacological bioavailability (PaR%) for oral insulin delivered via 10%FcBP-F127-PLA polymersomes, reaching 43.6%.

Conclusions:

  • FcBP-F127-PLA polymersomes represent a viable strategy for overcoming the intestinal barrier in oral insulin delivery.
  • FcRn-mediated transcytosis significantly enhances the transport of FcBP-modified nanocarriers.
  • These targeted polymersomes hold potential as an effective oral delivery system for insulin, improving therapeutic outcomes.

Keywords:
FcBPFcRn-targetedOral insulin deliveryPolymersomes

More Related Videos

Rapid, Scalable Assembly and Loading of Bioactive Proteins and Immunostimulants into Diverse Synthetic Nanocarriers Via Flash Nanoprecipitation06:57

Rapid, Scalable Assembly and Loading of Bioactive Proteins and Immunostimulants into Diverse Synthetic Nanocarriers Via Flash Nanoprecipitation

Published on: August 11, 2018

8.0K
Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells09:34

Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells

Published on: February 9, 2019

9.1K

Related Concept Videos

Insulin Formulations: Types and Delivery01:27

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...
278
Insulin Secretory Vesicles01:05

Insulin Secretory Vesicles

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...
5.4K