Vesicular Formulation for Transdermal Joint Lubrication

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Solution Overview

Problem

Current treatments for joint pain and reduced mobility due to loss of lubrication and structural integrity, such as osteoarthritis, are inadequate as they often require invasive procedures and provide only temporary relief, and existing vesicular formulations require intra-articular injection, which is inconvenient and painful.

Innovation Solution

A vesicular formulation comprising phospholipids and non-ionic surfactants, optionally with additional ingredients like co-solvents and antioxidants, is topically applied to provide lubrication and structural support to collagen structures, allowing for transdermal delivery and penetration into joints to restore lubrication and integrity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If hyaluronic acid is injected into the synovial capsule to provide enhanced temporary lubrication, then joint lubrication is improved, but the procedure becomes painful and requires repeated monthly injections by a medical professional

Engineering Contradiction:
Improvejoint lubricationVSAvoidtreatment convenience
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent uses phospholipid vesicles as an intermediary substance that can be topically applied to deliver lubricating agents to the joint. These vesicles penetrate through the skin and synovial capsule to replenish phospholipids in the cartilage and synovial fluid, providing lubrication without requiring direct injection into the joint space. This mediator approach transforms the treatment from an invasive intra-articular injection to a non-invasive topical application.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the mechanical injection procedure (using large bore needles directly into the joint) with a topical application system. The vesicular formulation penetrates through biological barriers (skin, synovial capsule) to deliver the lubricating phospholipids, substituting the mechanical invasion with a biochemical penetration mechanism that is less painful and more convenient for patients.

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

2Reliability

If phospholipids are replenished in the synovial fluid to restore cartilage protection, then joint structural integrity is improved, but existing methods require invasive intra-articular injection procedures

Engineering Contradiction:
Improvecartilage protectionVSAvoidadministration method
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent employs phospholipid-containing vesicles as a mediator that can be topically applied to deliver phospholipids to the joint. These vesicles serve as a vehicle that penetrates through the skin and synovial capsule barriers, releasing phospholipids into the synovial fluid and cartilage matrix. This intermediary system enables phospholipid replenishment without requiring direct injection into the joint space.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the delivery parameter from intra-articular injection to topical application. By formulating phospholipids in vesicular structures with specific penetration properties, the patent enables transdermal and trans-synovial delivery, fundamentally changing how phospholipids are administered to joints. This parameter change makes the treatment less invasive while maintaining therapeutic effectiveness.

Inventive Principle:
Principle #35Parameter changes

3Ease of operation

If lubricin is replenished to restore joint mobility, then joint movement is improved, but current treatments provide only temporary relief and require repeated procedures

Engineering Contradiction:
Improvejoint mobilityVSAvoidduration of relief
Core Design Contradiction:
Ease of operationVSDuration of action of moving object

Solution Approach 1:

The patent enables continuous replenishment of lubricating phospholipids through topical application. The vesicular formulation is designed to penetrate and release phospholipids over time, and can be reapplied regularly to maintain therapeutic levels. This creates a continuous action that prevents the temporary relief problem associated with single-dose intra-articular injections, allowing patients to maintain joint lubrication and mobility over the long term.

Inventive Principle:
Principle #20Continuity of useful action

Solution Approach 2:

The patent enables patients to self-administer the treatment through simple topical application. The vesicular formulation is designed for easy application to the skin over the joint, eliminating the need for medical professionals to perform repeated injections. This self-service capability improves patient compliance and allows for more frequent, consistent application, thereby extending the duration of therapeutic effect.

Inventive Principle:
Principle #25Self-service

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 formulation effectively reduces pain and improves mobility by replenishing phospholipids and proteoglycans, providing long-term relief without invasive procedures and minimizing systemic absorption, thus addressing the limitations of existing treatments.

Implementation Method 1

allowing for transdermal delivery and penetration into joints to restore lubrication and integrity

Methodology Applied
Scientific EffectTransdermal delivery: Permeation

Implementation Method 2

The surface of the cartilage layer found on the end of each bone is coated with a layer of phospholipids which are anchored within the cartilage structure. The hydrophilic head of each molecule is orientated into the synovial space and each is highly hydrated, which allows free movement of the joint without pain or discomfort.

Methodology Applied
Scientific EffectLubrication: Lubrication

Data Source

PatentEP2836203B1Vesicular formulations for use in the treatment of pain or reduced mobility of a joint
Publication Date: 2022.03.09 SEQUESSOME TECH HLDG
  • EP2836203B1 patent drawingFigure 1A~1D
  • EP2836203B1 patent drawingFigure 2
  • EP2836203B1 patent drawingFigure 3

AI summary

The present invention relates to vesicular formulations for use in the treatment of pain and/or reduced mobility associated with a loss of lubrication and/or structural integrity and/or swelling of a collagen structure. It also relates to a method of treating pain such as joint pain or tendonitis comprising topically administering a vesicular formulation according to the invention.