Taxane Coating Solid Form Conditioning for Controlled Release

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Solution Overview

Problem

There is a need for medical device coatings that can control the release rate of taxane therapeutic agents like paclitaxel without compromising durability, as existing coatings either release the agent too quickly or are not durable enough, and current packaging systems do not adequately protect these coatings from environmental factors.

Innovation Solution

A method of conditioning medical device coatings to alter the solid form of taxane therapeutic agents from amorphous to dihydrate forms, which slows down the release rate while maintaining durability, involves maintaining the coating at elevated humidity and temperature levels before implantation, allowing for a controlled release of the taxane therapeutic agent.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a medical device coating is made with high durability to withstand handling and implantation, then the coating durability is improved, but the release rate of the therapeutic agent becomes too slow

Engineering Contradiction:
Improvecoating durabilityVSAvoidtherapeutic agent release rate
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent applies parameter changes by controlling the relative humidity and temperature during packaging to transform the taxane solid form from amorphous to dihydrate, thereby adjusting the release rate parameter while preserving coating durability

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent implements preliminary action by performing the solid form transformation during the packaging process before implantation, so that the coating is pre-conditioned with the desired release characteristics before being deployed in the patient

Inventive Principle:
Principle #10Preliminary action

2Reliability

If the taxane therapeutic agent is stored in amorphous form for durability, then the coating durability is improved, but the agent releases too quickly after implantation

Engineering Contradiction:
Improvecoating durabilityVSAvoidpremature release duration
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent changes the physical state parameter of the taxane from amorphous to dihydrate crystalline form through controlled humidity exposure during packaging, which fundamentally alters the release kinetics while preserving the durable coating structure

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses the packaging environment as a temporary, disposable medium to induce the solid form transformation, after which the packaging is discarded and the device proceeds to implantation with the modified release characteristics

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Productivity

If the coating is conditioned at elevated humidity to slow release rate, then the release control is improved, but the coating may lose durability

Engineering Contradiction:
Improverelease rate controlVSAvoidcoating durability
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent performs the humidity conditioning action during the packaging phase before implantation, so that the release rate is controlled without requiring prolonged high-humidity exposure that would compromise coating durability during device handling and storage

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

This approach allows for a controlled and sustained release of taxane therapeutic agents, reducing premature release and maintaining coating durability, thereby enhancing the therapeutic efficacy and longevity of the medical device.

Implementation Method 1

A taxane therapeutic agent can be formed in an amorphous form, or in at least two different crystalline polymorphs... This phenomenon is known as polymorphism, and the distinct species are known as polymorphs.

Methodology Applied
Scientific EffectPolymorphism: Phase Change

Implementation Method 2

Taxane therapeutic agent molecules can exist in solvated or non-solvated solid forms... The dihydrate taxane solid form typically has an opaque white color, while the amorphous dihydrate taxane solid form typically has a clear transparent appearance.

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentEP2380606B1Methods of manufacturing and modifying taxane coatings for implantable medical devices
Publication Date: 2018.03.21 COOK MEDICAL TECHNOLOGIES LLC
  • EP2380606B1 patent drawingFigure 1A
  • EP2380606B1 patent drawingFigure 1B
  • EP2380606B1 patent drawingFigure 2A

AI summary

This disclosure relates to endolumenal medical devices coated with a taxane therapeutic agent in one or more solid form(s) having varying dissolution rates. Particularly preferred coatings comprise amorphous paclitaxel, dihydrate paclitaxel, or combinations thereof that provide durable coatings that release paclitaxel over a desired period of time, which can be on the order of hours, days or weeks. Preferred embodiments relate to medical device coatings of paclitaxel, or paclitaxel analogs or derivatives, having one or more polymorph solid forms that provide a prolonged release of paclitaxel within a body vessel without requiring a polymer carrier or barrier layer to achieve the desired rate of paclitaxel elution.