Crystalline Drug Particles in Biocompatible Polymers

Solution Overview

Problem

Current drug-eluting polymeric compositions face challenges with the stability of therapeutic agents, particularly amorphous agents which degrade easily and become plasticized during sterilization, leading to variable drug release kinetics.

Innovation Solution

The development of polymeric compositions with a significant portion of therapeutic agents in a crystalline phase, achieved by forming crystalline particles of therapeutic agents and encapsulating them in biocompatible polymers, ensuring stability and controlled release.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If therapeutic agents are used in amorphous phase to enhance solubility and dissolution rate, then drug release speed is improved, but drug stability deteriorates leading to degradation and variable release kinetics

Engineering Contradiction:

Improvedrug release speedVSAvoiddrug stability

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

The patent changes the physical state parameter of the therapeutic agent from amorphous to crystalline phase. This parameter change resolves the contradiction by providing both improved stability (crystalline phase resists degradation) and controlled release (through surface area control and encapsulation geometry) without the plasticization issues of amorphous phases during sterilization.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent utilizes phase transition from amorphous to crystalline state of the therapeutic agent. By forming crystalline particles within the polymer matrix, the drug maintains structural order and stability while controlling release through the crystalline lattice structure and particle surface area, eliminating the harmful effects of amorphous phase plasticization.

Inventive Principle:

Principle #36Phase transitions

2Reliability

If amorphous therapeutic agents are encapsulated in biocompatible polymers to achieve controlled release, then drug delivery control is improved, but drug stability deteriorates during sterilization due to plasticization

Engineering Contradiction:

Improvedrug release controlVSAvoiddrug stability during sterilization

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent changes the physical state parameter of the therapeutic agent from amorphous to crystalline phase. This parameter change resolves the contradiction by providing both improved stability (crystalline phase resists degradation) and controlled release (through surface area control and encapsulation geometry) without the plasticization issues of amorphous phases during sterilization.

Inventive Principle:

Principle #35Parameter changes

3Speed

If therapeutic agents are highly dispersed in polymer matrix to increase surface area for release, then drug release rate is improved, but drug stability deteriorates due to increased exposure and degradation

Engineering Contradiction:

Improvedrug release rateVSAvoiddrug stability against degradation

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

The patent changes the physical state parameter of the therapeutic agent from amorphous to crystalline phase. This parameter change resolves the contradiction by providing both improved stability (crystalline phase resists degradation) and controlled release (through surface area control and encapsulation geometry) without the plasticization issues of amorphous phases during sterilization.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent embeds crystalline drug particles within the polymer matrix structure, creating a nested configuration where the crystalline particles are contained within the polymer network. This nesting provides protection to the drug particles while maintaining controlled release through the polymer matrix, resolving the contradiction between release rate and stability.

Inventive Principle:

Principle #7Nested doll (Nesting)

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 crystalline phase enhances the stability and prolonged release of therapeutic agents, reducing degradation and maintaining effectiveness over time, thereby improving drug release kinetics and bioavailability.

Implementation Method 1

at least a portion of the therapeutic agent in such a polymeric composition is crystalline

Methodology Applied

Scientific EffectCrystallization: Crystallisation

Data Source

PatentUS7842312B2Polymeric compositions comprising therapeutic agents in crystalline phases, and methods of forming the same

Publication Date: 2010.11.30 CORDIS US CORP

AI summary

The present invention relates to a drug-containing polymeric composition comprising at least one therapeutic agent encapsulated in at least one biocompatible polymer, wherein at least a portion of the therapeutic agent in this polymeric composition is crystalline. The at least one biocompatible polymer may form a substantially continuous polymeric matrix with the at least one therapeutic agent encapsulated therein. Alternatively, the at least one biocompatible polymer may form polymeric particles with the at least one therapeutic agent encapsulated therein.