Core-Shell Nanoparticle Encapsulation for Controlled Biologic Release
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Solution Overview
Problem
Existing methods for delivering protein and peptide therapeutics face challenges such as rapid clearance from the bloodstream, enzymatic degradation, and difficulty in formulating and delivering them effectively, particularly through the gastrointestinal tract, necessitating improved encapsulation and controlled release strategies.
Innovation Solution
A method of encapsulating water-soluble molecules into nanoparticles using rapid controlled precipitation, where a copolymer stabilizing agent forms a hydrophilic core and a less polar shell, allowing for the formation of nanoparticles that are protected and coated with an amphiphilic polymer, enabling controlled release and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If proteins and peptides are administered as therapeutics, then treatment specificity is improved, but clearance from bloodstream occurs rapidly due to renal clearance or enzymatic degradation
Solution Approach 1:
The patent encapsulates water-soluble biologics (proteins, peptides, antibodies) inside nanoparticle carriers with a core-shell structure. The biologic is nested within the core region while the shell provides protective stabilization, preventing direct contact with degrading enzymes and renal filtration mechanisms, thereby extending circulation time while maintaining therapeutic specificity
Solution Approach 2:
The patent introduces nanoparticle carriers as intermediary vehicles between the biologic therapeutic and the bloodstream. These carriers act as mediators that protect the biologic from rapid clearance while delivering it to target tissues, effectively extending the duration of action without compromising the specific therapeutic effect
2Duration of action of moving object
If nanocarriers are used to encapsulate biologics, then extended release and reduced clearance are achieved, but formulation complexity increases
Solution Approach 1:
The patent employs rapid controlled precipitation with controlled solvent removal to form nanoparticle carriers. By controlling parameters such as solvent type, precipitation rate, and core-shell structure formation, the method achieves extended release of biologics while maintaining a relatively simple formulation process that can be scaled for manufacturing
Solution Approach 2:
The patent creates composite nanoparticle carriers combining water-soluble biologic materials with stabilizing copolymer shells. This composite structure provides both the extended release function and the necessary stability for formulation, achieving prolonged duration of action through a unified material system rather than complex multi-component formulations
3Reliability
If copolymer stabilizing agents are used to form nanoparticle shells, then encapsulation efficiency is improved, but manufacturing precision requirements increase
Solution Approach 1:
The patent uses copolymer stabilizing agents that self-assemble into nanoparticle shells during the precipitation process. The copolymer automatically organizes itself around the forming core, providing stable encapsulation without requiring external stabilization mechanisms. This self-assembly process improves encapsulation efficiency while reducing the need for precise manual control of nanoparticle formation parameters
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 enables high encapsulation efficiency and controlled release of biologics, reducing clearance times and frequency of administration, while maintaining stability and targeting specific tissues, suitable for both parenteral and oral delivery.
Implementation Method 1
A method of encapsulating water soluble molecules using rapid, controlled precipitation is presented. Water soluble molecules—including peptides, proteins, DNA, RNA, non-biologic therapeutics, polysaccharide-based therapeutics (e.g., tobramycin) and imaging agents—precipitate into nanoparticles that are protected by a copolymer stabilizing agent.
Implementation Method 2
The particles may be coated with an amphiphilic polymer, or processed into microparticles or larger monoliths.
Data Source
AI summary
An “inverse” precipitation route to precipitate aqueous soluble species with copolymers as nanoparticles having a hydrophilic, polar core and a less polar shell is described.