Liposome Inner Membrane Functional Lipid Encapsulation

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Conventional liposome production methods do not effectively enhance the encapsulation ratio, dispersion stability, and controlled release of medicines, as they typically use the same constituting components for both the inner and outer membranes, lacking a method to differentiate the constituting components for improved performance.

Innovation Solution

A method is developed to produce liposomes with different constituting compositions for the inner and outer membranes, using a higher amount of functional lipids in the inner membrane, which chemically interact with the medicine, enhancing encapsulation efficiency, stability, and controlled release, by employing a two-step emulsion preparation process involving supercritical or semi-supercritical carbon dioxide.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If the same constituting components are used for both inner and outer membranes in conventional liposome production, then the manufacturing process is simple, but the encapsulation ratio and controlled release properties are insufficient

Engineering Contradiction:
Improvemanufacturing process simplicityVSAvoidencapsulation ratio
Core Design Contradiction:
Ease of manufactureVSManufacturing precision

Solution Approach 1:

The patent applies local quality by using different lipid compositions for the inner and outer membranes of the liposome. The inner membrane contains specific lipids that interact with the medicine to enhance encapsulation, while the outer membrane has different composition for controlled release, allowing each part to have optimized properties for its specific function.

Inventive Principle:
Principle #3Local quality

2Manufacturing precision

If functional lipids are increased in the inner membrane to improve medicine interaction, then encapsulation ratio improves, but manufacturing complexity increases

Engineering Contradiction:
Improveencapsulation ratioVSAvoidmanufacturing process complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent segments the liposome manufacturing process into distinct steps: first forming the inner membrane with functional lipids that interact with medicine, then forming the outer membrane with different composition. This segmentation allows independent optimization of each membrane's lipid composition while maintaining overall process feasibility.

Inventive Principle:
Principle #1Segmentation

3Reliability

If different constituting components are used for inner and outer membranes, then controlled release properties improve, but the production method becomes more complex

Engineering Contradiction:
Improvecontrolled release propertiesVSAvoidproduction method complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies preliminary action by first forming the inner membrane with lipids pre-selected for medicine interaction and encapsulation, then subsequently forming the outer membrane with lipids pre-selected for controlled release properties. This preliminary preparation of each membrane layer with its optimized composition enables the complex dual-functionality to be achieved through sequential, manageable steps.

Inventive Principle:
Principle #10Preliminary action

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 method results in liposomes with improved encapsulation ratios, dispersion stability, and controlled release properties, effectively addressing the limitations of conventional liposome production techniques.

Implementation Method 1

mixing: supercritical or semi-supercritical carbon dioxide or an organic solvent (O); a water-soluble solvent (W1); and a mixed lipid component (F1) which forms an inner membrane of the liposome so as to prepare a W1/CO2 emulsion or a W1/O emulsion

Methodology Applied
Scientific EffectSupercritical fluid: Supercritical Fluid

Data Source

PatentEP3494964B1Liposome and method for producing liposome
Publication Date: 2021.04.07 KONICA MINOLTA INC

AI summary

It is intended to provide a liposome preparation which is a liposome, has a lipid bilayer membrane composed of an inner membrane constituted by a lipid including one or more types of functional lipids (a lipid capable of chemically interacting with another compound such as a charged lipid, a polarizable lipid, a lipid-soluble lipid or a water-soluble lipid) and an outer membrane constituted by a lipid with or without including one or more types of functional lipids, and is characterized in that at least a condition that the amount of any one type of functional lipid contained in the inner membrane is larger than in the outer membrane is satisfied. The liposome preparation is suitable as a liposome for encapsulating a contrast agent (a neutral substance having a hydroxy group), siRNA (an anionic substance) having an anticancer activity or the like. Its encapsulation ratio of drug agents, dispersion stability, control release and the like have been improved.