Cold Process Liposome Preparation for Oral Delivery

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Solution Overview

Problem

Existing methods for preparing liposomes, particularly for nutraceutical applications, often use non-food grade ingredients and involve heating steps that can degrade sensitive agents, making them unsuitable for oral delivery and affecting the efficacy of the encapsulated compounds.

Innovation Solution

A cold process method for preparing liposomes at room temperature without a heating step, using vesicle-forming lipids and an aqueous solvent, such as alcohol, to form stable liposomes with entrapped agents like ascorbic acid, GSH, or ALA, which are suitable for oral administration and maintain the integrity of the active agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If heating steps are used to solubilize lipids, then lipid solubility is improved, but agent degradation increases

Engineering Contradiction:
Improvelipid solubilityVSAvoidagent degradation
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent changes the temperature parameter from elevated (conventional heating) to room temperature (20-25°C), eliminating thermal degradation of heat-sensitive agents while maintaining lipid solubility through alternative mechanisms. The lipid solution is prepared at room temperature by direct mixing of lipids with aqueous solvent containing the agent, avoiding thermal stress entirely.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent replaces the thermal mechanism (heating) with a mechanical/molecular mechanism (molecular-level mixing and solvation at room temperature). The lipids are solubilized through vigorous mixing and molecular interaction with the aqueous solvent at room temperature, eliminating the need for thermal energy input that causes agent degradation.

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

2Reliability

If conventional liposomal preparation methods are used, then liposome formation is achieved, but suitability for oral delivery decreases

Engineering Contradiction:
Improveliposome formationVSAvoidsuitability for oral delivery
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the temperature parameter from elevated (conventional methods) to room temperature, making the process suitable for nutraceutical and oral applications. This parameter change transforms the method from pharmaceutical-grade (heat-based) to nutraceutical-grade (cold process), enabling oral delivery while maintaining liposome formation reliability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs self-assembly of lipids into liposomes at room temperature without requiring external heating or complex equipment. The lipids spontaneously form liposomal structures when mixed with the aqueous solvent containing the agent, making the process inherently suitable for oral and nutraceutical applications.

Inventive Principle:
Principle #25Self-service

3Manufacturing precision

If heating is applied to prepare liposomes, then encapsulation efficiency is improved, but agent integrity deteriorates

Engineering Contradiction:
Improveencapsulation efficiencyVSAvoidagent integrity
Core Design Contradiction:
Manufacturing precisionVSStability of the object's composition

Solution Approach 1:

The patent performs preliminary solubilization of both lipids and the agent in the aqueous solvent at room temperature before liposome formation. This preliminary action ensures the agent is already dissolved and stable when liposomes form, preventing thermal degradation that would occur if heating were applied during or after encapsulation.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent replaces thermal energy (heating) with mechanical mixing energy to achieve encapsulation. Vigorous mixing at room temperature drives the lipid self-assembly and agent entrapment process, maintaining agent integrity while achieving high encapsulation efficiency through mechanical rather than thermal activation.

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

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 cold process method produces stable liposomes with minimal agent degradation, achieving high encapsulation efficiency and maintaining the stability of the active agents, even at elevated temperatures, making them suitable for various therapeutic applications.

Implementation Method 1

vesicle-forming lipids are solubilized in an aqueous solvent at or about room temperature to form a lipid solution

Methodology Applied
Scientific EffectSolubilization: Solvation

Implementation Method 2

The agent to be entrapped is separately solubilized in an aqueous solvent at or about room temperature to form an agent containing solution

Methodology Applied
Scientific EffectSolubilization: Solvation

Implementation Method 3

The aqueous solvent for solubilizing the lipids and the agent to be entrapped may be the same or different... the lipid solution and agent-containing solution are combined... a stream of the lipid solution is injected into the agent-containing solution with mixing

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 4

the resulting solution is allowed to hydrate for a suitable period of time... the solution is allowed to hydrate for at least one hour with frequent mixing

Methodology Applied
Scientific EffectHydration: Hydrates

Data Source

PatentUS10016389B2Method of making liposomes, liposome compositions made by the methods, and methods of using the same
Publication Date: 2018.07.10 LIVON LAB
  • US10016389B2 patent drawing
  • US10016389B2 patent drawing
  • US10016389B2 patent drawing

AI summary

A method of preparing liposomes, liposome compositions formed by the process, and methods of using the liposome composition are provided herein.