Glucosinolate Topical Formulation with Myrosinase Segmentation

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Solution Overview

Problem

Exposure to UV and solar radiation causes significant skin ailments and skin cancer due to DNA damage, oxidative stress, and immunosuppression, with existing treatments not effectively addressing the rising incidence of nonmelanoma skin cancers.

Innovation Solution

Topical formulations comprising a phase II enzyme inducer precursor, such as glucosinolates, and an activating agent, like myrosinase, are provided, with minimal contact between the two to prevent premature activation, allowing for long-term storage and application to reduce skin damage and cancer risk.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If glucosinolates and myrosinase are kept in separated form to prevent premature hydrolysis, then stability during storage is improved, but activation and therapeutic effect require additional steps

Engineering Contradiction:
Improvestability during storageVSAvoidactivation process
Core Design Contradiction:
Stability of the object's compositionVSEase of operation

Solution Approach 1:

The formulation divides the system into two separate components: glucosinolates (precursor) and myrosinase (activating agent), which are stored separately to prevent premature reaction. This segmentation maintains stability during storage while allowing controlled activation when needed.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The glucosinolates are pre-loaded into the topical formulation during manufacturing, while the myrosinase is added separately at the time of use. This preliminary preparation ensures the precursor is ready for action, and the activating agent is introduced only when activation is desired, resolving the contradiction between stability and ease of operation.

Inventive Principle:
Principle #10Preliminary action

2Reliability

If glucosinolates are hydrolyzed to isothiocyanates to induce phase II enzymes, then cancer protection is improved, but premature activation during storage reduces potency

Engineering Contradiction:
Improvecancer protectionVSAvoidpotency loss
Core Design Contradiction:
ReliabilityVSLoss of substance

Solution Approach 1:

The myrosinase enzyme is extracted or added separately from the glucosinolate precursor in the topical formulation. This separation prevents the enzyme from being present during storage, thereby preventing premature hydrolysis and potency loss, while ensuring the precursor remains available for cancer protection when activated at the appropriate time.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent introduces a temporal intermediary approach where the activating agent (myrosinase) is introduced at a specific moment (time of use) rather than being present continuously. This intermediary timing mechanism ensures that hydrolysis to the protective isothiocyanate occurs only when needed, preventing potency loss during storage while maintaining reliability for cancer protection.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 formulations effectively induce phase II enzymes to protect skin cells from damage, providing therapeutic benefits and preventing skin ailments and cancers by maintaining potency over time and ensuring controlled activation upon application.

Implementation Method 1

Isothiocyanates are generally produced when their precursors, glucosinolates, (β-thioglucoside N-hydrosulfate), are hydrolyzed by the enzyme myrosinase (β-thioglucoside glucohydrolase)

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentUS8927007B2Formulations for treatment with glucosinolates
Publication Date: 2015.01.06 JOHNS HOPKINS UNIVERSITY

AI summary

The application relates to topical formulations comprising a phase II enzyme inducer precursor and an activating agent. Methods for producing and using the topical formulations are also provided.