Electrosprayed Therapeutic Particles for Low-Viscosity High Doses
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Solution Overview
Problem
Existing therapeutic and diagnostic formulations, particularly those containing monoclonal antibodies, face challenges in achieving high concentrations while maintaining stability and injectability, often leading to high fluid dynamic viscosity and rapid degradation.
Innovation Solution
The method involves electrospraying a stream of a therapeutic or diagnostic agent to form particles with concentrations ranging from 0.0001 to 1000 mg/mL, using encapsulants like poly(vinyl alcohol) and suspending these particles in a pharmaceutically acceptable medium, or formulating them as a dry powder, to create stable and injectable formulations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If high concentrations of therapeutic or diagnostic agents are formulated in aqueous solution, then the dose delivery efficiency is improved, but the fluid dynamic viscosity increases excessively
Solution Approach 1:
The patent changes the physical state parameter of the formulation from aqueous solution to non-aqueous suspension. This parameter change allows achieving high therapeutic agent concentrations (improving dose delivery efficiency) while the non-aqueous medium maintains lower viscosity compared to aqueous solutions at equivalent concentrations.
2Productivity
If high concentrations of therapeutic or diagnostic agents are formulated in aqueous solution, then the dose delivery efficiency is improved, but standard injection devices cannot be used
Solution Approach 1:
The formulation transitions from aqueous to non-aqueous medium, which fundamentally changes the rheological parameters. This enables high-concentration formulations to be administered through standard injection devices by reducing the viscosity to within acceptable injection ranges while maintaining high therapeutic payload.
3Productivity
If high concentrations of therapeutic or diagnostic agents are formulated in aqueous solution, then the dose delivery efficiency is improved, but degradation of the active ingredient accelerates
Solution Approach 1:
The patent changes the chemical environment from aqueous to non-aqueous medium. This parameter change alters the degradation pathways and kinetics of the therapeutic or diagnostic agents, reducing hydrolysis and other water-mediated degradation mechanisms, thereby improving stability while maintaining high concentration formulations.
4Quantity of substance
If high concentrations of therapeutic or diagnostic agents are formulated, then the administration volume is reduced, but the formulation becomes uninjectable
Solution Approach 1:
The patent introduces a non-aqueous medium as an intermediary carrier for the therapeutic or diagnostic agents. This intermediary medium enables the formulation to achieve high concentrations while maintaining physical properties (low viscosity) that allow injectability, effectively mediating between the conflicting requirements of high concentration and low viscosity.
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, stable formulations with improved injectability, reducing administration volume and frequency, and minimizing degradation.
Implementation Method 1
a method of forming particles by electrospraying, e.g., conventional electrospraying, a stream of a first liquid including a first therapeutic or diagnostic agent toward a collector
Implementation Method 2
an encapsulant is in the first liquid
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.