Stratified Cyclodextrin Inclusion Vehicles with Enzyme-Activated Release

Solution Overview

Problem

Existing cyclodextrin-based delivery systems face challenges due to variability in amylase activity among patients, particularly those with pancreatic insufficiency or reduced gastric acid production, leading to unpredictable drug release and potential pharmacokinetic perturbations.

Innovation Solution

Cyclodextrin inclusion complexes are designed with a co-formulated or co-packaged enzyme, such as amylase, that activates upon delivery to the target, ensuring predictable release of guest molecules from the cyclodextrin cavity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If cyclodextrin inclusion complexes are used for drug delivery, then drug solubility and stability are improved, but unpredictable drug release occurs due to variability in amylase activity among patients

Engineering Contradiction:

Improvepredictability of drug releaseVSAvoidvariability in amylase activity among patients

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The cyclodextrin inclusion complex is designed to release the drug through its own inherent structure without relying on external enzymes. The complex naturally dissociates or releases the guest molecule through physical-chemical mechanisms such as changes in solubility, pH, or concentration gradients, eliminating dependence on variable amylase activity in different patients.

Inventive Principle:

Principle #25Self-service

Solution Approach 2:

The patent extracts the drug release mechanism from dependence on biological enzymes (amylase) and replaces it with a controlled physical-chemical release mechanism inherent to the cyclodextrin structure. This separation allows predictable release kinetics independent of patient-specific enzymatic variability.

Inventive Principle:

Principle #2Taking out (Extraction)

2Productivity

If cyclodextrin inclusion complexes are used without enzyme co-formulation, then formulation complexity is reduced, but drug release becomes unpredictable and therapeutic efficacy decreases

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidformulation complexity

Core Design Contradiction:

ProductivityVSDevice complexity

Solution Approach 1:

The cyclodextrin inclusion complex is designed to release the drug through its own inherent structure without relying on external enzymes. The complex naturally dissociates or releases the guest molecule through physical-chemical mechanisms such as changes in solubility, pH, or concentration gradients, eliminating dependence on variable amylase activity in different patients.

Inventive Principle:

Principle #25Self-service

Solution Approach 2:

The patent extracts the drug release mechanism from dependence on biological enzymes (amylase) and replaces it with a controlled physical-chemical release mechanism inherent to the cyclodextrin structure. This separation allows predictable release kinetics independent of patient-specific enzymatic variability.

Inventive Principle:

Principle #2Taking out (Extraction)

3Stability of the object's composition

If cyclodextrins are resistant to digestion, then inclusion complex stability is improved, but pharmacokinetic properties of coadministered drugs are perturbed

Engineering Contradiction:

Improveinclusion complex stabilityVSAvoidpharmacokinetic perturbations

Core Design Contradiction:

Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The patent extracts the drug release mechanism from dependence on biological enzymes (amylase) and replaces it with a controlled physical-chemical release mechanism inherent to the cyclodextrin structure. This separation allows predictable release kinetics independent of patient-specific enzymatic variability.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent modifies parameters of the cyclodextrin system (such as type of cyclodextrin, inclusion ratio, guest molecule selection) to optimize both stability and compatibility with coadministered drugs, minimizing pharmacokinetic perturbations while maintaining inclusion complex integrity.

Inventive Principle:

Principle #35Parameter changes

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

Enzyme-activated release mechanisms provide controlled and consistent delivery of biologically active molecules, addressing variability in amylase activity and enhancing therapeutic efficacy.

Implementation Method 1

an enzyme having a cyclodextrin-degrading activity capable of digesting the cyclodextrin

Methodology Applied

Scientific EffectEnzymatic hydrolysis: Hydrolysis

Implementation Method 2

the guest molecule is stably retained by the cyclodextrin within the biologically acceptable carrier

Methodology Applied

Scientific EffectMolecular inclusion: Absorption (physical)

Data Source

PatentUS20250255920A1Controlled-Release and Stratified Cyclodextrin Inclusion Complex Vehicles

Publication Date: 2025.08.14 CZAP RESEACH & DEV LLC

AI summary

The invention provides cyclodextrin inclusion complex delivery vehicles, in which the cyclodextrin inclusion complex is provided together with enzyme having a cyclodextrin-degrading activity capable of digesting the cyclodextrin, so that upon delivery of the vehicle to a target the enzyme is activated and releases the guest molecule from the cyclodextrin cavity. In alternative aspects, these cyclodextrin inclusion complex delivery vehicles are for example provided in the form of medicaments, food ingredients, medical food ingredients, nutritional supplement ingredients, dietary supplement ingredients, herbicides, insecticides, fungicides, animal repellents, pheromones, plant growth regulators, fragrances, fabrics or packaging materials.