Liposome Preparation Without Organic Solvents

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Existing methods for preparing liposomes often rely on the use of organic solvents, proteins, and heat, which are undesirable due to toxicity, flammability, and environmental concerns, as well as increased production costs and safety risks, and result in unstable formulations.

Innovation Solution

A method for preparing liposomes without the use of heat, organic solvents, proteins, and inorganic salts, involving the combination of lipids in an aqueous medium at ambient temperature, dispersion of lipids, and addition of sugars to form liposomes, which can incorporate active agents such as pharmaceutical agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If organic solvents are used to prepare liposomes, then liposomes can be formed, but toxicity and flammability increase

Engineering Contradiction:
Improveliposome formationVSAvoidtoxicity and flammability
Core Design Contradiction:
Ease of manufactureVSObject-affected harmful factors

Solution Approach 1:

The patent removes organic solvents from the liposome preparation process entirely. Instead of using organic solvents to dissolve lipids before hydration, the method directly hydrates lipid films or powders with aqueous buffers, eliminating the harmful organic solvent step while maintaining liposome formation capability.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent introduces lipid films or lipid powders as intermediaries. Lipids are first converted to a dry film or powder state, which then serves as an intermediary form that can be directly hydrated with aqueous buffers to form liposomes, bypassing the need for organic solvents.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of manufacture

If heat is used to prepare liposomes, then liposome formation is facilitated, but production costs and safety risks increase

Engineering Contradiction:
Improveliposome formationVSAvoidproduction costs and safety risks
Core Design Contradiction:
Ease of manufactureVSObject-affected harmful factors

Solution Approach 1:

The patent replaces thermal energy input with mechanical energy input. Instead of using heat to facilitate lipid hydration and liposome formation, the method uses mechanical agitation, vortexing, or extrusion through membranes to achieve the same effect at ambient temperature.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The patent enables liposomes to form spontaneously through self-assembly of lipid molecules when hydrated with aqueous buffers at ambient temperature. The lipids naturally organize into bilayer structures without requiring external heat energy input.

Inventive Principle:
Principle #25Self-service

3Ease of manufacture

If conventional methods are used to prepare liposomes, then liposomes can be formed, but formulation stability decreases

Engineering Contradiction:
Improveliposome formationVSAvoidformulation stability
Core Design Contradiction:
Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent changes the preparation parameters by conducting the entire process at ambient temperature without organic solvents. This parameter change results in liposomes with improved stability characteristics, as they are formed without exposure to conditions that cause degradation or aggregation.

Inventive Principle:
Principle #35Parameter changes

4Quantity of substance

If organic solvents are used in injectable solutions, then drugs can be solubilized, but hemolysis and side effects occur

Engineering Contradiction:
Improvedrug solubilityVSAvoidhemolysis and side effects
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

The patent removes organic solvents from injectable formulations by incorporating drugs directly into liposomes formed without organic solvents. The liposomal structure provides an alternative mechanism for drug solubilization and delivery that eliminates the need for harmful organic co-solvents.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses liposomes as intermediary carriers for drug delivery. Instead of directly dissolving drugs in organic solvents for injection, the drugs are incorporated into liposomal structures that serve as safe intermediaries, enabling drug delivery without direct exposure to harmful solvents.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS9402812B2Methods for the preparation of liposomes
Publication Date: 2016.08.02 FORMATECH INC

AI summary

Provided herein are methods for preparing liposomes and uses thereof. In certain embodiments, liposomes are prepared without using heat, organic solvents, proteins, and/or inorganic salts in the process. In certain embodiments, the liposomal preparation contains one or more active agents. In certain embodiments, the liposomal preparations are used in the treatment of diseases or disorders.