Duodenum-Targeted Enteric Coating With Lipase-Triggered Release
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Solution Overview
Problem
Existing medicament delivery systems struggle to accurately and precisely target the duodenum of the gastrointestinal tract, often resulting in premature dissolution before reaching the desired site due to gastric conditions, which can affect therapeutic efficacy and increase side effects.
Innovation Solution
A system comprising a mucoadhesive layer and an enteric coating that degrades in response to duodenal pH and lipase, allowing precise delivery of medicaments to the duodenum, optionally using a needle delivery system for active administration, and incorporating a super absorbent expanding element for mechanical actuation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a conventional enteric coating is used to protect medicament from gastric dissolution, then the medicament can reach the intestine, but the dissolution occurs in a gradient process before the targeted region is reached, reducing delivery precision
Solution Approach 1:
The enteric coating is divided into multiple functional layers: an outer gradient layer providing gradual dissolution protection through the stomach, and an inner burst-release layer containing lipase-sensitive materials that trigger rapid dissolution at the duodenum. This segmentation allows the coating to perform different functions at different GI tract locations, achieving both protection and precision.
Solution Approach 2:
Different regions of the coating have different dissolution properties tailored to specific locations. The outer layer has pH-dependent dissolution characteristics suited for gastric conditions, while the inner layer has lipase-dependent dissolution characteristics activated specifically in the duodenum. This local differentiation enables precise targeting while maintaining reliable protection.
2Productivity
If the enteric coating is designed to dissolve rapidly at the target site, then therapeutic effect is achieved, but premature dissolution may occur due to gradient process before reaching the targeted region
Solution Approach 1:
Lipase acts as an intermediary trigger mechanism. The outer pH-resistant layer protects the inner lipase-sensitive layer during gastric transit, preventing premature activation. When the coated medicament reaches the duodenum, lipase from intestinal fluids penetrates the outer layer and triggers rapid dissolution of the inner layer, ensuring controlled rapid release only at the target site.
Solution Approach 2:
The coating structure is pre-configured with the outer protective layer already in place before administration. This preliminary protective action ensures that the inner burst-release layer remains intact during gastric transit, preventing premature dissolution. The system is prepared in advance to deliver rapid release only when the correct conditions (lipase presence in duodenum) are met.
3Quantity of substance
If high doses of medicament are used to achieve therapeutic effect, then the desired effect is achieved, but negative side effects increase due to premature dissolution
Solution Approach 1:
The patent converts the potentially harmful gradient dissolution process into a beneficial multi-stage release mechanism. The outer layer's gradual dissolution characteristics are repurposed to provide sustained protection through the stomach, while the inner layer's rapid dissolution capability is timed to activate only at the duodenum. This transforms what could be a source of premature release into a controlled delivery sequence that maximizes therapeutic effect while minimizing 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
Enables targeted and controlled release of medicaments in the duodenum, reducing systemic side effects and ensuring effective therapeutic delivery without the need for invasive injections.
Implementation Method 1
the enteric coating comprises at least a material degradable by a pH of the duodenum
Implementation Method 2
at least a material digestible by a lipase
Implementation Method 3
incorporating a super absorbent expanding element for mechanical actuation
Data Source
AI summary
A system for targeted delivery of a medicament to the gastrointestinal tract (e.g., selectively to the duodenum) of a subject. The system includes a medicament, a mucoadhesive layer at least partially surrounding the medicament, and an enteric coating encasing the medicament and mucoadhesive layer. The enteric coating comprises a material degradable by a pH of the GI tract and a material digestible by a lipase. Also provided are method of making and using the system for targeted delivery of a medicament to the gastrointestinal tract. Also provided are a system for deploying a medicament-containing needle system using an expanding element. The system includes a medicament-containing needle system and an expanding element within a capsule. The capsule is initially coated with an enteric coating. As the enteric coating degrades the expanding element absorbs fluid that enters the capsule and expands to deploy the medicament-containing needle system from the capsule.