Crystalline Matrix for Oral Protein Delivery Stability
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Solution Overview
Problem
Current drug delivery systems face challenges in stabilizing bioactive agents, particularly proteins, for oral administration, as they are prone to degradation in the harsh gastrointestinal environment, and lack selectivity in targeting specific tissue systems.
Innovation Solution
The development of compositions featuring a crystalline matrix that embeds bioactive agents, providing enhanced stability and allowing them to pass through the stomach without degradation, with preferential absorption by the Peyer's patches and mesenteric lymph nodes, enabling both local and systemic delivery depending on polymer presence.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If proteins are administered orally, then they can be delivered to the gastrointestinal tract, but they undergo degradation by peptidase enzymes and low pH in the stomach
Solution Approach 1:
The patent uses an amorphous polymer matrix as an intermediary carrier to protect proteins from degradation. The matrix embeds the protein within its structure, shielding it from peptidase enzymes and low pH conditions in the stomach, thereby enabling oral administration while maintaining protein stability and bioactivity.
Solution Approach 2:
The patent employs amorphous solid dispersions where the physical state of the polymer matrix is changed from crystalline to amorphous. This parameter change in molecular arrangement provides enhanced protection to embedded proteins, allowing them to survive the harsh gastrointestinal environment while maintaining their therapeutic efficacy.
2Reliability
If conventional polymeric systems are used to protect bioactive agents, then they can shield agents from external solvents and degradants, but they lack selectivity in targeting specific tissue systems
Solution Approach 1:
The patent applies local quality by creating particles with specific surface properties that differ from their internal structure. The amorphous polymer matrix is formulated to interact specifically with Peyer's patches and mesenteric lymph nodes, enabling preferential uptake at these target sites while maintaining general protection throughout the gastrointestinal tract.
Solution Approach 2:
The patent utilizes the porous or network structure of the amorphous polymer matrix to enable selective interaction with target tissues. The matrix structure allows for specific molecular recognition and uptake by Peyer's patches and mesenteric lymph nodes, providing tissue-targeting selectivity while the embedded protein remains protected within the matrix.
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 crystalline matrix effectively stabilizes bioactive agents, allowing them to maintain bioactivity and be delivered selectively to the gastrointestinal tract or systemically, improving the stability and delivery efficacy of proteins and other drugs.
Implementation Method 1
The bioactive agents are embedded in the matrix, effectively shielding them from environments that promote degradation
Implementation Method 2
the matrix is able to pass through the stomach after oral administration without substantial degradation
Implementation Method 3
following oral administration, the matrix is preferentially absorbed by the Peyer's patches and mesenteric lymph nodes found in the small intestine
Data Source
AI summary
Compositions for stabilizing and delivering proteins and/or other bioactive agents are disclosed. The bioactive agents are embedded or encapsulated in a crystalline matrix. Typically the bioactive agents are in the form of micro- or nanoparticles. The crystalline matrix confers enhanced stability to the agents embedded therein relative to other microparticulate or nanoparticulate bioactive agents. The carriers are especially useful for stabilizing bioactive macromolecules, such as proteins.