Liposomes with Calcium Phosphate Precipitate for Bioactive Release

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Solution Overview

Problem

Current lipid-comprising delivery systems for bioactive compounds, such as polynucleotides and proteins, face challenges in efficiently releasing these compounds into cells and are often associated with toxic side effects due to inflammatory responses.

Innovation Solution

Development of biodegradable ionic precipitate-based delivery system complexes, where a bioactive compound is encapsulated within a liposome or surrounded by a lipid bilayer, allowing for targeted and efficient delivery to cells while minimizing immunogenic effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional lipid-comprising delivery systems are used to deliver bioactive compounds, then the delivery systems can be formulated to carry polynucleotides and proteins, but they are unable to efficiently release the incorporated bioactive compounds into the cytoplasm of cells

Engineering Contradiction:
Improverelease efficiencyVSAvoiddelivery effectiveness
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent combines lipids with calcium phosphate precipitate to create a composite delivery system. The calcium phosphate precipitate serves as a biodegradable core that releases bioactive compounds, while the lipid component provides membrane-like properties for cellular interaction. This composite structure enables efficient release of bioactive compounds into the cytoplasm while maintaining delivery effectiveness.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent modifies the physical and chemical parameters of the delivery system by incorporating calcium phosphate precipitate with specific properties (biodegradability, ionic character) into the lipid-based system. This parameter change enables the system to transition from merely carrying compounds to actively releasing them into the cytoplasm, improving both release efficiency and delivery effectiveness.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If conventional lipid-comprising delivery systems are used to deliver bioactive compounds, then the delivery systems can be formulated to carry polynucleotides and proteins, but they are associated with toxic side effects due to the stimulation of an inflammatory response when administered in vivo

Engineering Contradiction:
Improvedelivery capabilityVSAvoidtoxicity
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent employs calcium phosphate precipitate as a biodegradable, short-lived carrier that naturally breaks down into calcium and phosphate ions in the body. This disposable-like approach eliminates the need for persistent synthetic carriers, reducing long-term toxicity and inflammatory responses while maintaining effective delivery capability during the active phase.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent changes the material composition parameter by replacing conventional synthetic lipid carriers with a natural, biodegradable calcium phosphate-based system. This parameter change reduces immunogenicity and toxic side effects while preserving the ability to deliver bioactive compounds effectively, as the calcium phosphate precipitate is metabolically compatible with human tissues.

Inventive Principle:
Principle #35Parameter changes

3Productivity

If biodegradable ionic precipitate-based delivery systems are developed, then efficient release of bioactive compounds into cells is achieved, but the system complexity increases

Engineering Contradiction:
Improverelease efficiencyVSAvoidsystem complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent merges the calcium phosphate precipitate delivery mechanism with the lipid-based delivery platform into a unified system. By combining these two components, the system achieves efficient release of bioactive compounds while the integration itself manages the complexity through synergistic interaction, where the calcium phosphate provides the release mechanism and the lipid component provides the delivery vehicle, reducing overall system complexity compared to separate systems.

Inventive Principle:
Principle #5Merging (Combining)

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 delivery system complexes effectively release bioactive compounds into cells, enhancing therapeutic efficacy while reducing toxicity and immunogenic responses, making them suitable for treating various disorders, including cancers.

Implementation Method 1

a biodegradable ionic precipitate comprising a bioactive compound surrounded by a lipid bilayer, wherein the biodegradable ionic precipitate is ionically bound to the inner leaflet of the lipid bilayer

Methodology Applied
Scientific EffectIonic binding: Ion Repulsion/Attraction

Data Source

PatentUS10624852B2Liposomes comprising a calcium phosphate-containing precipitate
Publication Date: 2020.04.21 THE UNIV OF NORTH CAROLINA AT CHAPEL HILL
  • US10624852B2 patent drawing
  • US10624852B2 patent drawing
  • US10624852B2 patent drawing

AI summary

Provided herein are methods and compositions for the delivery of bioactive compounds to a cell, tissue, or physiological site. The compositions comprise delivery system complexes comprising liposomes encapsulating a biodegradable ionic precipitate having incorporated therein a bioactive compound and delivery system complexes comprising a biodegradable ionic precipitate ionically bound to a surrounding lipid bilayer, wherein the biodegradable ionic precipitate comprises a bioactive compound. Also provided herein are methods for the treatment of a disease or an unwanted condition in a subject, wherein the methods comprise administering the delivery system complexes comprising bioactive compounds that have therapeutic activity against the disease or unwanted condition to the subject.