Related Experiment Video
Updated: Jun 22, 2025
09:24
Mucin Agarose Gel Electrophoresis: Western Blotting for High-molecular-weight Glycoproteins
Published on: June 14, 2016
25.5K
Assessment of polymeric mucin-drug interactions
Hisanao Kishimoto1,2, Caroline Ridley2, Katsuhisa Inoue1
1Department of Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, Hachioji, Tokyo, Japan.
Plos One
|June 27, 2024
Summary
This study reveals that drugs like paclitaxel can interact with and aggregate polymeric mucins (MUC2, MUC5B), impacting drug absorption. Understanding these mucin-drug interactions is crucial for mucosal drug delivery.
Area of Science:
- Biochemistry
- Pharmacology
- Biomaterials science
Background:
- Mucosal drug delivery requires traversing the mucus layer.
- Polymeric mucins are key mucus components and potential regulators of drug absorption.
- Systematic evaluation of mucin-drug interactions is lacking.
Purpose of the Study:
- To assess interactions between human polymeric mucins (MUC2, MUC5B, MUC5AC) and various drugs.
- To investigate how mucin-drug interactions affect drug absorption and cellular effects.
Main Methods:
- Simple centrifugal method
- Fluorescence analysis
- Cellular assays using A549 cells with mucin deletion
Main Results:
- Paclitaxel, rifampicin, and theophylline induced aggregation of MUC5B and/or MUC2.
- Drug binding affinity varied significantly between drugs and mucin subtypes.
- Deletion of MUC5AC and MUC5B in A549 cells enhanced the cytotoxicity of cyclosporin A and paclitaxel, suggesting a role for mucin-drug interaction.
Conclusions:
- Drug binding to mucins is a critical factor influencing mucosal drug absorption.
- The impact of drugs on mucin network properties needs to be determined.
- This research highlights the importance of considering mucin-drug interactions in the development of mucosal drug delivery systems.
Related Concept Videos
01:24Drugs for Peptic Ulcer Disease: Sucralfate as Mucosal Protective Agents
439
In the intricate landscape of the gastric lumen, excessive acid secretion disrupts the natural defense mechanisms, weakening the mucus-bicarbonate barrier. This vulnerability allows pepsin to infiltrate epithelial cells, digesting mucosal proteins and triggering erosion, leading to ulcer formation.
In this scenario, mucosal protective agents like sucralfate play an essential role. Sucralfate, a complex of sulfated sucrose and aluminum hydroxide, demonstrates its usefulness in acidic conditions,...
In this scenario, mucosal protective agents like sucralfate play an essential role. Sucralfate, a complex of sulfated sucrose and aluminum hydroxide, demonstrates its usefulness in acidic conditions,...
439
01:23Factors Affecting Protein-Drug Binding: Drug Interactions
130
Drug interactions are a critical aspect of pharmacology and can occur when two or more drugs compete for the same binding site. This competition can result in one drug displacing another, altering the effect of the displaced drug. Drug interactions are complex processes that rely heavily on how much of the displacer drug is present and how strongly it can bind to the same sites as the displaced drug.
Displacement interactions can have varying outcomes, ranging from toxicity to virtually...
Displacement interactions can have varying outcomes, ranging from toxicity to virtually...
130
01:20Drugs for Peptic Ulcer Disease: Prostaglandin Analogs as Mucosal Protective Agents
399
The gastric mucosa produces prostaglandins E2 (PGE2) and prostacyclin (PGI2), crucial in maintaining gastric health. They exert cytoprotective effects, including increasing bicarbonate secretion, releasing protective mucin, reducing gastric acid output, and preventing harmful vasoconstriction. These effects are mediated through various receptors, such as EP1, EP2, EP3, and EP4.
Non-steroidal anti-inflammatory drugs (NSAIDs) can induce peptic ulcers by inhibiting cyclooxygenase, decreasing...
Non-steroidal anti-inflammatory drugs (NSAIDs) can induce peptic ulcers by inhibiting cyclooxygenase, decreasing...
399
01:24Cholinergic Antagonists: Pharmacokinetics
429
Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations, while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and...
429
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
196
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
196
01:27Combined Effects of Drugs: Synergism
3.8K
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
3.8K