Degradable Compounds for Targeted Drug Delivery

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Solution Overview

Problem

Current drug delivery methods lack the ability to provide targeted, controlled release of pharmaceuticals at the sub-cellular level, particularly for gene therapy and other biologically active compounds, as they cannot effectively deliver specific materials to individual cells, and existing techniques often require high drug concentrations and lack specificity.

Innovation Solution

Development of degradable compounds with labile —Si-A-C— groups that are stable under defined conditions but degrade under physiological temperature or acidic conditions, which can be incorporated into a polymeric matrix to form discrete particles for targeted delivery and release of therapeutic agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If conventional drug delivery techniques are used, then drugs can be administered through various routes, but they cannot provide controlled release at sub-cellular dimensions or target specific cells effectively

Engineering Contradiction:
Improvedelivery precisionVSAvoiddelivery system complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent divides the drug delivery system into discrete micro- and nanoparticles with controlled sizes (1-1000 micrometers), enabling precise targeting of individual cells while maintaining manageable complexity through standardized particle formulations

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent utilizes pH-sensitive compounds that change their properties in response to pH variations, allowing controlled release at specific physiological locations without requiring complex active targeting mechanisms

Inventive Principle:
Principle #35Parameter changes

2Reliability

If high drug concentrations are used to ensure effectiveness, then therapeutic effect is improved, but toxicity and harmful effects increase

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoiddrug toxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent creates localized high drug concentrations at the target site through controlled release from particles, while maintaining low overall systemic drug concentrations, thereby achieving effective therapy with reduced toxicity

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent employs pH-sensitive compounds that remain stable during circulation and only degrade/release drug when encountering acidic conditions at the target site, ensuring drug effectiveness is activated only where needed

Inventive Principle:
Principle #10Preliminary action

3Adaptability or versatility

If degradable compounds with pH-sensitive bonds are used, then controlled release at specific conditions is achieved, but compound stability under defined conditions becomes challenging

Engineering Contradiction:
Improveconditional degradation capabilityVSAvoidcompound stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent employs compounds with bonds that are stable at one pH range but degrade at another pH range, allowing the same compound to exhibit both stability during circulation and controlled degradation at the target site through pH parameter changes

Inventive Principle:
Principle #35Parameter changes

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 degradable compounds enable targeted and controlled release of therapeutic agents at the cellular level, enhancing drug activity while reducing overall drug concentration, and can be tailored for specific delivery conditions, such as pH levels, to effectively treat various diseases.

Implementation Method 1

The compounds are stable under defined conditions but are degradable under specified conditions, such as, for example, physiological temperature (e.g., about 37° C.) or acidic conditions

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentUS8945527B2Degradable compounds and methods of use thereof, particularly with particle replication in non-wetting templates
Publication Date: 2015.02.03 LIQUIDIA TECHNOLOGIES INC
  • US8945527B2 patent drawing
  • US8945527B2 patent drawing
  • US8945527B2 patent drawing

AI summary

The present invention provides compounds that will degrade under specified conditions, methods of using such compounds, and compositions comprising such compounds. The degradable compounds of the invention may be characterized by the labile —Si-A-C— groups present in the compounds (A representing an atom, such as O, N, or S, or a group, such as C═O). The compounds may be incorporated into a composition that further may include a polymeric matrix and/or a cargo component. A wide variety of cargo components may also be used in the present invention. In particular embodiments, the cargo component comprises a drug or other therapeutic agent. Accordingly, the invention particularly provides pharmaceutical formulations and methods of delivering a drug or other therapeutic material.