Hormone Liposome Emulsification for Stable Extended Release

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Existing liposomal preparations with encapsulated drugs experience fluctuating serum levels in the blood, requiring frequent administration, which leads to poor patient compliance and increased costs.

Innovation Solution

A method using a rotor-stator emulsifier with specific stator perforations and rotational speed to produce liposomes with encapsulated hormones, enabling a prolonged release of at least 8 to 32 hours, allowing for fewer applications.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional liposomal preparations are used, then drugs can be delivered through skin layers, but serum levels of the drug do not remain constant and frequent re-administration is required

Engineering Contradiction:

Improvestability of serum drug levelsVSAvoidduration of drug release

Core Design Contradiction:

ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent modifies the physical and chemical parameters of the liposomal preparation, specifically the phase transition temperature of the lipid bilayer and the size distribution of liposomes, to achieve controlled and prolonged drug release. By adjusting these parameters, the preparation maintains stable serum drug levels over extended periods without requiring frequent re-administration

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a dynamic release system where the liposomal preparation adapts its drug release rate based on physiological conditions. The preparation transitions between different release phases (initial burst release followed by sustained release) to maintain therapeutic drug levels dynamically over time

Inventive Principle:

Principle #15Dynamics

2Reliability

If liposomal preparations require frequent administration to maintain therapeutic levels, then drug efficacy can be maintained, but patient compliance deteriorates

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidpatient compliance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent formulates the liposomal preparation with pre-optimized characteristics (lipid composition, particle size, drug loading) that enable prolonged drug release from the outset. This preliminary design ensures that a single application can maintain therapeutic levels for extended periods, eliminating the need for frequent dosing and improving patient compliance

Inventive Principle:

Principle #10Preliminary action

3Ease of manufacture

If conventional emulsification methods are used to prepare liposomes, then production can be achieved, but the release profile does not provide prolonged sustained release

Engineering Contradiction:

Improvemanufacturability of liposomal preparationVSAvoidduration of hormone release

Core Design Contradiction:

Ease of manufactureVSDuration of action of moving object

Solution Approach 1:

The patent replaces conventional mechanical emulsification methods with an ultrasonic emulsification system. This substitution enables precise control over liposome formation and drug encapsulation, creating a preparation that achieves both ease of manufacture and prolonged sustained release through controlled ultrasonic energy input

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 method achieves stable serum hormone levels for extended periods, reducing the frequency of applications and enhancing patient compliance and cost-effectiveness.

Implementation Method 1

The invention relates to a method for producing a liposomal preparation by emulsification... use of a rotor-stator emulsifier provided with a stator with perforations

Methodology Applied

Scientific EffectUltrasonic vibration: Ultrasonic Vibration

Implementation Method 2

method for producing a liposomal preparation by emulsification

Methodology Applied

Scientific EffectEmulsification: Emulsion

Implementation Method 3

provides a stable, slow and prolonged release of the encapsulated hormone

Methodology Applied

Scientific EffectDiffusion: Diffusion

Implementation Method 4

The liposomal preparation... releases the encapsulated hormones or esters thereof particularly efficiently

Methodology Applied

Scientific EffectLipid bilayer erosion:

Data Source

PatentUS20260014080A1Liposomal preparation with encapsulated hormones, method of production and use thereof

Publication Date: 2026.01.15 PURNA PHARMA NV

AI summary

The present invention relates to a method for producing a liposomal preparation by emulsification, the preparation containing liposomes with encapsulated hormones, comprising: a first emulsification step of emulsifying a first composition, the first composition comprising water, propylene glycol, an emulsifier and a hormone to be encapsulated; characterized in that for the emulsification of the first emulsification step, a rotor-stator emulsifier is used, which is provided with a stator with perforations with a diameter between 0.8 and 5 mm, and wherein the rotational speed is at least 6000 rpm. The invention also relates to a liposomal preparation comprising liposomes with encapsulated hormones or esters thereof, and a liposomal preparation for use in hormone therapy or for use in the treatment of hypogonadism and/or adrenal insufficiency.