Core-shell composite for targeted drug delivery
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Solution Overview
Problem
Current delivery systems for compounds face challenges such as limited bioavailability due to poor solubility and instability in gastric fluid, leading to premature degradation before reaching the small intestine, and are not suitable for pH variations across individuals.
Innovation Solution
A core-shell composite material with a core containing an active ingredient, a shell structure of alternating protein and polyphenol layers resistant to gastric conditions but degradable by intestinal enzymes, ensuring targeted delivery to the small intestine.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If gelatin capsules are used for delayed release of food ingredients, then the capsules are safe, readily available and low cost, but the capsules are soluble in gastric fluid and cannot protect compounds for delivery to the small intestine
Solution Approach 1:
The patent uses a composite capsule shell made of gelatin and polyphenol layers. The gelatin provides ease of manufacture and biocompatibility, while the polyphenol layer provides resistance to gastric fluid degradation. This composite structure resolves the contradiction by combining materials with complementary properties.
Solution Approach 2:
The patent modifies the chemical composition parameters of the capsule shell by incorporating polyphenols that are resistant to gastric acid degradation. This parameter change allows the capsule to maintain structural integrity in gastric fluid while still being manufacturable using standard processes.
2Reliability
If multilayer capsules are used to prevent degradation in gastric fluid, then the compounds are protected from premature release, but the capsules require storage under acidic conditions which affects palatability and stability of other food components
Solution Approach 1:
The patent extracts the acidification requirement from the storage process by using a capsule shell that is inherently resistant to gastric acid. The polyphenol layer provides this resistance without requiring the food product itself to be acidified, thereby protecting the compound while avoiding negative impacts on palatability and other food components.
3Ease of operation
If pH-triggered release mechanisms are used, then controlled release of compounds is achieved, but the system must account for individual variations in gastrointestinal pH profile caused by diet, genetics and disorders
Solution Approach 1:
The patent changes the triggering mechanism from pH-dependent to enzyme-dependent release. The polyphenol layer is designed to be degraded by specific intestinal enzymes (such as polyphenol oxidase) rather than responding to pH changes. This parameter change in the release mechanism improves adaptability to individual variations in gastrointestinal pH while maintaining controlled release functionality.
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 composite material effectively protects the active ingredient from gastric degradation, allowing it to reach the small intestine intact and be released by intestinal enzymes, providing controlled and targeted delivery.
Implementation Method 1
the shell structure is selected to be resistant to degradation under gastric conditions but is degradable by one or more intestinal enzymes
Implementation Method 2
a polyelectrolyte layer interfacing said core and said shell structure, said polyelectrolyte layer being disposed adjacent to said protein layer or said polyphenol layer
Implementation Method 3
the shell structure is selected to be resistant to degradation under gastric conditions but is degradable by one or more intestinal enzymes
Data Source
AI summary
Disclosed herein is a core-shell composite material comprising: a core optionally comprising an active ingredient compound; a shell structure comprising at least two alternating layers; the alternating layers being a protein layer and a polyphenol layer; and optionally a polyelectrolyte layer interfacing said core and said shell structure, said polyelectrolyte layer being disposed adjacent to said protein layer or said polyphenol layer, wherein said shell structure is selected to be resistant to degradation under gastric conditions but is degradable by one or more intestinal enzymes. In a preferred embodiment the protein is bovine serum albumin (BSA) or pepsin, the polyphenol layer is tannin or tannic acid, and the shell structure is degradable by pepsin.