Probiotic Coating for Intestinal Delivery
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Solution Overview
Problem
Probiotics face challenges in surviving the harsh gastric environment and achieving effective intestinal colonization due to low availability and short retention time after oral administration, limiting their therapeutic efficacy for GI tract-related diseases.
Innovation Solution
A double-layer coating strategy using tannic acid and a copolymer like EUDRAGIT L100, where tannic acid enhances mucoadhesion and the copolymer provides pH-responsive protection and delayed release in the intestine, ensuring prolonged retention and viability of probiotics.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If probiotics are administered orally to treat GI tract diseases, then therapeutic efficacy is improved, but survival through harsh gastric environment and intestinal colonization is reduced
Solution Approach 1:
The coating system is divided into two distinct layers: an inner layer providing mucoadhesion and an outer layer providing pH-responsive protection. This segmentation allows each layer to specialize in one function, optimizing both mucoadhesion strength and gastric resistance without compromise
Solution Approach 2:
The invention uses a composite coating structure combining tannic acid (natural polymer) and EUDRAGIT L100 (synthetic polymer). This composite approach leverages the mucoadhesive properties of tannic acid and the pH resistance of EUDRAGIT L100, creating a synergistic effect that addresses both adhesion and protection requirements
2Reliability
If probiotics are delivered to the intestine, then treatment of GI disorders is achieved, but retention time in the gastro-intestinal tract is insufficient
Solution Approach 1:
The mucoadhesive inner layer is applied in advance to the probiotic surface, creating a pre-formed adhesive interface that immediately engages with intestinal mucosa upon delivery. This preliminary preparation ensures rapid attachment and extended retention without requiring additional activation steps
Solution Approach 2:
The tannic acid layer acts as an intermediary between the probiotic and the intestinal mucosa, facilitating strong adhesion through interactions with mucin. This intermediary layer enables prolonged residence time by mediating the attachment process without directly involving the probiotic cells in adhesion
3Reliability
If probiotics are protected from gastric acid, then viability is improved, but selective delivery to the intestine is compromised
Solution Approach 1:
The outer coating layer's solubility parameter changes in response to pH variation. It remains insoluble in acidic gastric environment (pH 1-3) to protect probiotics, then dissolves in neutral intestinal environment (pH 6-7) to enable release. This parameter change provides both protection and selective delivery automatically
Solution Approach 2:
The invention exploits the harmful acidic environment as a protective mechanism - the low gastric pH triggers the pH-responsive outer layer to remain intact and protective, while the higher intestinal pH automatically triggers release. The harmful acid becomes a useful trigger for maintaining protection during the critical gastric transit period
4Duration of action of moving object
If tannic acid layer is used for mucoadhesion, then retention time is prolonged, but potential side effects from long-term adhesion increase
Solution Approach 1:
The outer EUDRAGIT L100 layer is designed to be temporarily retained during the adhesion period to protect and anchor the probiotic, then automatically discarded (dissolved) in the intestine to release the probiotic and eliminate the coating material. This temporary retention followed by dissolution minimizes long-term side effects
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
This approach significantly enhances the therapeutic efficacy of probiotics by protecting them from gastric stress and prolonging their retention in the intestine, leading to improved treatment outcomes for GI tract disorders like colitis.
Implementation Method 1
the pH-responsive degradation of the outer copolymer layer leads to the selective delivery of TA-EcN to the intestine
Implementation Method 2
the strong mucoadhesive capability of the TA layer prolongs the retention time of EcN
Data Source
AI summary
A method of encapsulating a probiotic including the steps of (a) coating a probiotic with a compound or composition of matter dimensioned and configured to increase adhesion of the probiotic to intestinal mucosa; and (b) coating the probiotic of step (a) with a polymer or copolymer that resists degradation in the stomach and at least partially degrades in the small intestine: the composition of matter resulting therefrom, methods of using the composition of matter to deliver probiotics to the small intestine by mouth, and methods of treating colitis and IBD by administering the compositions of matter by mouth to a subject.