Related Experiment Video
Updated: Nov 18, 2025
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
7.5K
pH-Responsive Cellulose-Based Microspheres Designed as an Effective Oral Delivery System for Insulin
Yaqi Gong1, Shabbir Mohd1, Simei Wu1
1School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, LiuFang Campus, No.206, Guanggu 1st road, Donghu New & High Technology Development Zone, Wuhan, 430205 Hubei Province, P.R. China.
ACS Omega
|February 8, 2021
Summary
Researchers developed pH-responsive carboxylated cellulose microspheres (CCMs) for enhanced oral insulin delivery. These biocompatible microspheres show controlled insulin release in the intestine, offering a promising carrier for oral insulin therapy.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Nanotechnology
Background:
- Cellulose microspheres (CMs) show potential for various applications, including drug delivery.
- Oral insulin delivery faces challenges due to insulin's instability and low bioavailability.
- Developing effective oral carriers is crucial for improving diabetes management.
Purpose of the Study:
- To design pH-responsive carboxylated cellulose microspheres (CCMs) for enhanced oral insulin bioavailability.
- To investigate the controlled release of insulin from CCMs in simulated gastrointestinal environments.
- To evaluate the biocompatibility and potential of CCMs as oral insulin carriers.
Main Methods:
- Carboxylated cellulose microspheres (CCMs) were synthesized using a green citric/hydrochloric acid hydrolysis method.
- Microsphere characterization involved field emission scanning electron microscopy (FE-SEM), Fourier transform infrared spectroscopy (FT-IR), and X-ray photoelectron spectroscopy (XPS).
- Insulin loading and release studies were conducted in artificial gastric fluid (AGF) and artificial intestinal fluid (AIF), with release kinetics analyzed using the Korsmeyer-Peppas model.
Main Results:
- FE-SEM and FT-IR confirmed the spherical porous structure and carboxylation of the prepared cellulose microspheres.
- Insulin loading was achieved via electrostatic interactions, with controlled release dependent on carboxyl group ionization and proton balance.
- In vitro studies showed suppressed insulin release in AGF and significant release in AIF, following Fickian diffusion kinetics.
Conclusions:
- The developed CCMs demonstrate pH-responsive behavior, effectively controlling insulin release in simulated intestinal conditions.
- The excellent biocompatibility and lack of cytotoxicity indicate CCMs are a promising candidate for oral insulin delivery.
- This green synthesis route offers a viable strategy for creating advanced drug delivery systems based on modified cellulose.
Related Concept Videos
01:27Insulin Formulations: Types and Delivery
398
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...
Short-acting insulins are divided into...
398
01:25Insulin: Biosynthesis, Chemistry, and Preparation
834
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...
Damage or functional impairment of β-cells inhibits insulin production, leading to diabetes. Diabetes treatment...
834
01:05Insulin Secretory Vesicles
6.1K
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...
6.1K
01:06Oral Hypoglycemic Agents: Glinides
403
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...
403
01:17Oral Hypoglycemic Agents: Sulfonylureas
517
Sulfonylureas are oral hypoglycemic agents utilized in treating type 2 diabetes. They are characterized by their unique sulfonylurea chemical structure. The family of sulfonylureas is divided into generations. First-generation sulfonylureas, including tolbutamide (Orinase), chlorpropamide (Diabinese), and tolazamide (Tolinase), trigger insulin release from pancreatic β cells and enhance peripheral tissues' insulin sensitivity. The second-generation members, such as glipizide...
517
01:19Oral Hypoglycemic Agents: α-Glucosidase Inhibitors
391
α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
Acarbose and miglitol are...
391