Coated Particles for Mucosal Drug Delivery
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Solution Overview
Problem
Current oral and mucosal drug delivery systems face challenges due to stomach acidity, enzymatic activity, and low penetration through GI tissue, leading to reduced efficiency as most polymeric particles are entrapped and eliminated by the GI mucosal lining.
Innovation Solution
Development of coated particles with a core (polymeric or hydrophobic drug) and a coating containing glycoproteins or a combination of sugars, oligosaccharides, and proteins with an amino acid backbone rich in serine and threonine, which enhances diffusion and reduces particle aggregation in mucus.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If polymeric particles are used for oral delivery, then drug administration is achieved, but particles are entrapped and eliminated by GI mucosal lining reducing efficiency
Solution Approach 1:
The patent modifies the surface properties of polymeric particles by changing their charge characteristics. Specifically, the particles are designed with negative zeta potentials (typically -10 mV to -50 mV) to enhance interaction with the positively charged mucus layer, thereby improving mucoadhesion and preventing premature elimination while maintaining penetration capability
Solution Approach 2:
The patent creates composite particle systems combining polymeric cores with specific surface coatings. The particles consist of a polymeric core (providing structural integrity and drug loading) combined with surface-modified regions that have enhanced mucoadhesive properties, creating a composite structure that simultaneously achieves retention and penetration
2Reliability
If particles are made bioadhesive to increase mucosal uptake, then absorption is improved, but particles aggregate in GI mucosa reducing delivery efficiency
Solution Approach 1:
The patent precisely controls the zeta potential parameter of the particles, maintaining it within a specific negative range (-10 mV to -50 mV). This parameter optimization ensures sufficient mucoadhesion for absorption while preventing excessive aggregation. The negative charge density is carefully regulated to balance adhesion strength with particle dispersion in the mucus layer
Solution Approach 2:
The patent applies different properties to different regions of the particle system. The core region maintains polymeric structure for integrity, while the surface region has modified charge characteristics for mucoadhesion. This local differentiation allows the particle to exhibit both strong adhesion for absorption and controlled dispersion to avoid aggregation
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The coated particles demonstrate improved diffusion coefficients and reduced aggregation in mucus, leading to increased systemic and local uptake of active agents following oral and mucosal administration compared to uncoated control particles.
Implementation Method 1
The coated particles demonstrate improved diffusion coefficients and reduced aggregation in mucus
Data Source
AI summary
Described are coated particles containing a core and a coating, and pharmaceutical formulations containing these coated particles. The core contains a polymer or a hydrophobic drug. The coating contains a glycoprotein or a combination of a sugar and a protein. The coating surrounds the core. The coated particles are effectively absorbed by mucosa such as intestinal mucosa, GI tissue, and/or vaginal mucosa, and show increased systemic uptake following oral or mucosal administration. Optionally, the coated particles contain one or more active agents encapsulated in the core and/or embedded in the coating of the particles, for systemic or local delivery.