Jelly Fig Pectin Hydrogel for Colon-Targeted Active Agent Release
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Solution Overview
Problem
Current oral dosage forms face challenges such as poor bioavailability due to incomplete absorption and hepatic first-pass effect, and there is a need for improved delivery systems for biologics and poorly soluble drugs, particularly for mRNA vaccines and CRISPR components, which are not efficiently delivered through non-invasive routes.
Innovation Solution
A colon-targeted active agent delivery carrier using low methoxyl pectin derived from Jelly fig, crosslinked with calcium ions to form a hydrogel matrix that protects the active agent from stomach and small intestine enzymes, allowing targeted release in the colon.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral dosage forms are used to deliver active agents, then non-invasive administration is achieved, but bioavailability is poor due to incomplete absorption and hepatic first-pass effect
Solution Approach 1:
The gastrointestinal tract is segmented into different regions with distinct functional characteristics. The delivery system is designed to withstand the acidic environment of the stomach and enzymatic conditions of the small intestine, then release the active agent specifically in the colon, utilizing the unique physiological conditions of each segment to achieve targeted delivery and improved bioavailability
Solution Approach 2:
A colon-targeting carrier system acts as an intermediary vehicle between the oral administration and the colon. This carrier protects the active agent from degradation in the stomach and small intestine, and facilitates its release in the colon, thereby improving bioavailability while maintaining non-invasive oral administration
2Ease of operation
If biologics and CRISPR components are delivered through non-invasive routes, then oral administration is achieved, but delivery efficiency is poor
Solution Approach 1:
The delivery system is designed with location-specific functionality, utilizing the unique physiological conditions of the colon (different pH, enzyme composition, and microbiota) to trigger release of the active agent. This local quality approach ensures that biologics and CRISPR components are protected during transit and efficiently delivered to the colon, improving delivery efficiency while maintaining oral administration
Solution Approach 2:
The delivery system exploits parameter changes in the gastrointestinal tract, particularly the transition from acidic to neutral pH and changes in enzymatic activity along the tract. The carrier is designed to respond to these parameter changes, remaining stable in the stomach and small intestine then releasing the active agent in the colon, thereby improving delivery efficiency for biologics and CRISPR components
3Reliability
If mRNA vaccines are administered by injection, then effective delivery is achieved, but logistical difficulties with cold chain storage and transportation occur
Solution Approach 1:
The injection-based delivery system is replaced with an oral delivery system that does not require cold chain storage and transportation. The mRNA vaccine is incorporated into a colon-targeting carrier that protects the mRNA from degradation and facilitates its delivery to the colon, eliminating the need for complex cold chain logistics while maintaining effective delivery
Solution Approach 2:
The delivery system utilizes parameter changes in the gastrointestinal tract to protect and deliver mRNA vaccines. The carrier is designed to remain stable under ambient conditions during storage and transportation, then triggers release in the colon through physiological parameter changes, eliminating the need for cold chain storage and transportation while maintaining effective delivery
4Stability of the object's composition
If active agents are protected from stomach and small intestine enzymes, then integrity is maintained, but release in the colon is delayed
Solution Approach 1:
The carrier system is designed with dynamic properties that allow it to adapt to changing physiological conditions along the gastrointestinal tract. It remains stable in the stomach and small intestine, then triggers release in the colon through responses to pH changes, enzymatic conditions, or other physiological parameters, thereby maintaining integrity while achieving timely release in the colon
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
Enhances bioavailability and safety of active agents by maintaining integrity through the digestive tract and releasing them selectively in the colon, improving efficacy for biologics and ensuring stable delivery of mRNA vaccines and CRISPR components.
Implementation Method 1
low methoxyl pectin derived from Jelly fig, crosslinked with calcium ions to form a hydrogel matrix
Implementation Method 2
crosslinked with calcium ions to form a hydrogel matrix that protects the active agent
Implementation Method 3
releasing them selectively in the colon
Data Source
AI summary
A colon-targeted active agent delivery carrier includes a low methoxyl pectin derived from Jelly fig (Jelly fig LM pectin) and a divalent cation, wherein the Jelly fig LM pectin crosslinks with the divalent cation in an egg-box conformation, wherein the colon-targeted composition is degraded by at least one enzyme in the colon of the subject to release the active agent.