Related Experiment Video
Updated: Jun 4, 2026
07:45
Retroductal Nanoparticle Injection to the Murine Submandibular Gland
Published on: May 3, 2018
Salivary Enzyme-Responsive Switching Nanoparticles Overcoming Diffusion and Absorption Barriers for Transmucosal
Se Kye Park1,2, Lam Tan Hao1, Hee Jung Park3
1Research Center for Bio-Based Chemistry, Korea Research Institute of Chemical Technology (KRICT), Ulsan 44429, Republic of Korea.
ACS Applied Materials & Interfaces
|June 3, 2026
Summary
Salivary enzyme-responsive nanoparticles (SEPAS NPs) overcome mucus barriers for buccal drug delivery. These nanoparticles switch from penetration to adhesion, enhancing drug retention and efficacy.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Drug Delivery Systems
Background:
- Transmucosal drug delivery offers a noninvasive route but faces challenges due to the mucus layer's penetration-adhesion trade-off.
- Efficient drug delivery requires overcoming mucus barriers while ensuring prolonged residence time at the target site.
Purpose of the Study:
- To develop enzyme-responsive nanoparticles (SEPAS NPs) that dynamically switch between mucus penetration and mucoadhesion for buccal drug delivery.
- To address the inherent limitations of transmucosal drug delivery systems by resolving the penetration-adhesion dilemma.
Main Methods:
- Design of SEPAS NPs with a dual-regime architecture: an inner N-guanidinium chitosan oligosaccharide (G-COS) layer for mucoadhesion and a degradable starch-based outer layer.
- Evaluation of NP-mucin interactions under mucus-mimicking conditions, assessing penetration and adhesion dynamics.
- In vitro assessment of drug release kinetics (dexamethasone), cytocompatibility, and anti-inflammatory activity.
Main Results:
- SEPAS NPs demonstrated transient shielding during penetration, followed by enzyme-mediated degradation of the outer layer, exposing the G-COS core.
- Enhanced retention at mucin-coated interfaces by approximately 6-fold due to the exposed mucoadhesive G-COS layer.
- Sustained, diffusion-dominated release of dexamethasone (DEX) without compromising therapeutic efficacy, alongside excellent cytocompatibility (>90% cell viability).
Conclusions:
- The developed enzyme-responsive nanoparticle strategy effectively resolves the penetration-adhesion trade-off in transmucosal drug delivery.
- SEPAS NPs offer a promising, broadly adaptable platform for enhanced buccal drug delivery, maintaining drug release kinetics and biocompatibility.
- This approach provides a novel solution for overcoming mucus barriers in various transmucosal environments.
Related Concept Videos
01:27Bioavailability Enhancement: Drug Permeability Enhancement
After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
01:16Bioavailability Enhancement: Drug Solubility Enhancement
Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
01:24Site-Targeted Drug Delivery Systems: Polymeric Carriers
Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
01:23Oral Drug Delivery Systems: Introduction
Oral drug delivery is the most common route of administration due to its convenience, cost-effectiveness, and high patient compliance. It enables precise formulation to ensure proper drug dosage and bioavailability. The development of oral dosage forms considers drug properties such as solubility, stability, and absorption to optimize therapeutic efficacy.Tablets, capsules, liquids, and chewable formulations enhance drug stability, mask undesirable tastes, and improve patient experience.
01:11Oral Drug Delivery Systems: Delayed-Release Systems
Delayed-release drug delivery systems are specialized pharmaceutical formulations designed to postpone the release of active compounds until the drug reaches a specific region of the gastrointestinal (GI) tract, typically the intestine. These systems are essential for drugs that may cause gastric irritation, are unstable in acidic environments, or need to exert therapeutic effects locally in the intestinal or colonic regions.The core feature of delayed-release systems is the use of enteric...
01:18Drug Delivery: Enteral Route
The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
Drugs in...
Drugs in...