Electrosprayed Particles for High-Concentration Injection
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Solution Overview
Problem
Existing therapeutic and diagnostic formulations, particularly those containing monoclonal antibodies, face challenges with high fluid dynamic viscosity and rapid degradation, making standard injection devices impractical and frequent administration necessary.
Innovation Solution
The method involves electrospraying a stream of therapeutic or diagnostic agents with concentrations ranging from 0.0001 to 1000 mg/mL and viscosities from 0.1 to 5000 cP, forming particles with minimal aggregation, fragmentation, and charge variation, which are then suspended in a pharmaceutically acceptable medium or formulated as a dry powder.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If high concentration of therapeutic or diagnostic agents is formulated in aqueous solution, then the dose delivery efficiency is improved, but the fluid dynamic viscosity increases making standard injection devices impractical
Solution Approach 1:
The patent changes the physical state of the formulation from aqueous solution to non-aqueous suspension, and transforms the therapeutic agent from dissolved state to particle form. This parameter change enables high concentration formulations (10-1000 mg/mL) with low viscosity that can be administered via standard injection devices while maintaining high dose delivery efficiency
Solution Approach 2:
The patent introduces particles as an intermediary form of the therapeutic agent. These particles suspend in non-aqueous media and serve as a bridge between high concentration requirements and low viscosity requirements, enabling both high productivity and ease of operation
2Volume of moving object
If high concentration of therapeutic or diagnostic agents is formulated in aqueous solution, then the volume of formulation is reduced, but degradation of the active ingredient accelerates
Solution Approach 1:
Particles serve as a protective intermediary for the therapeutic agent. The particle matrix isolates the active ingredient from degradation pathways while maintaining high concentration, thereby improving stability without increasing formulation volume
Solution Approach 2:
The patent changes the solvent system from aqueous to non-aqueous, which fundamentally alters the degradation pathways and kinetics. This parameter change preserves therapeutic agent stability at high concentrations while minimizing formulation volume
3Reliability
If frequent administration is required to maintain therapeutic effect, then the therapeutic efficacy is maintained, but patient discomfort and treatment burden increase
Solution Approach 1:
The patent changes the formulation from aqueous solution to non-aqueous particle suspension, enabling high concentration formulations that reduce administration frequency. This maintains therapeutic efficacy while significantly improving patient comfort by requiring fewer injections
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 allows for high-concentration formulations with reduced aggregation, fragmentation, and charge variation, enabling minimal volume administration with maintained activity, thus reducing patient discomfort and frequency of administration.
Implementation Method 1
forming particles by electrospraying, e.g., conventional electrospraying, a stream of a first liquid including a first therapeutic or diagnostic agent
Implementation Method 2
electrospraying a first liquid including a first therapeutic or diagnostic agent to form droplets and removing (e.g., evaporating) the first liquid to produce particles from the droplets
Data Source
AI summary
The invention provides particles, compositions including the particles, and methods of making the particles using electrospray. In certain embodiments, the particles allow for high concentrations of a therapeutic or diagnostic agent to be delivered at low viscosity. Particles may also exhibit beneficial properties with respect to stability.