Retinal Cyclodextrin Acetals for Skin Clarification

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Solution Overview

Problem

Current skin clarification products are limited in addressing a wide range of dermatological disorders, including those caused by cancer, diabetes, radiation treatments, and aging, as they often fail to effectively treat challenged skin, age spots, and skin changes associated with mitochondrial dysfunction, collagen loss, and UV damage.

Innovation Solution

The development of polyene cyclodextrin hemiacetals and acetals, specifically retinal and carotenoid derivatives, which form covalent bonds with cyclodextrins, providing a comprehensive treatment for various skin issues through their ability to deacetalize on the skin's acidic pH, releasing active compounds to address multiple skin concerns.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If conventional skin clarification products are used, then basic skin smoothing and brightening can be achieved, but they fail to effectively treat challenged skin and multiple dermatological disorders simultaneously

Engineering Contradiction:

Improvetreatment coverage for multiple skin disordersVSAvoideffectiveness on challenged skin

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The composition combines multiple active ingredients (retinoid, carotenoid, and polyene cyclodextrin hemiacetal or acetal) in a single formulation that addresses multiple skin disorders simultaneously, including challenged skin, age spots, acne, wrinkles, and UV damage, making one product serve multiple therapeutic functions

Inventive Principle:

Principle #6Universality (Multi-functionality)

Solution Approach 2:

The invention uses a composite formulation integrating retinoid derivatives, carotenoid derivatives, and polyene cyclodextrin hemiacetals or acetals with specific molecular structures (formula I and II), creating a synergistic mixture that enhances overall effectiveness for treating diverse skin conditions

Inventive Principle:

Principle #40Composite materials

2Stability of the object's composition

If stable compound formulations are used, then product shelf life is improved, but bioavailability and skin penetration may be reduced

Engineering Contradiction:

Improvecompound stabilityVSAvoidbioavailability

Core Design Contradiction:

Stability of the object's compositionVSReliability

Solution Approach 1:

The polyene cyclodextrin hemiacetal or acetal undergoes deacetalization in response to skin's acidic pH environment, transforming from a stable prodrug form into active compounds that can effectively treat skin disorders, thus adapting stability to functional requirements

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The polyene cyclodextrin hemiacetal or acetal acts as an intermediary prodrug that remains stable during storage but activates upon contact with skin's acidic pH, mediating between storage stability requirements and bioavailability needs

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

These compounds effectively treat challenged skin, age spots, and skin changes associated with aging, offering improved skin clarity and health by addressing collagen loss, UV damage, and other dermatological issues, while maintaining stability and bioavailability.

Implementation Method 1

providing a comprehensive treatment for various skin issues through their ability to deacetalize on the skin's acidic pH, releasing active compounds

Methodology Applied

Scientific EffectDeacetalization: Hydrolysis

Implementation Method 2

specifically retinal and carotenoid derivatives, which form covalent bonds with cyclodextrins, providing a comprehensive treatment

Methodology Applied

Scientific EffectCovalent bonding: Chemical Bonding

Data Source

PatentUS8871748B2Retinal cyclodextrin acetals and hemiacetals for treating skin complexion disorder

Publication Date: 2014.10.28 ISLAND KINETICS

AI summary

The present invention discloses certain polyene cyclodextrin acetals and hemiacetals that are effective in providing skin clarification, which is useful for the treatment of acne, and skin disfigurements and skin darkening resulting from acne; skin darkening from cancer, diabetes, radiation treatments, chemotherapy, and sun-burn; mitochondrial and DNA dysfunction; age spots; loss of cellular antioxidants; skin changes associated with aging including collagen loss, loss of skin pliability, loss of skin suppleness, skin wrinkles and fine lines, oxidation, damage from radiation, damage from free radicals, and damage from UV; dry skin; xerosis; ichthyosis; dandruff; brownish spots; keratoses; melasma; lentigines; liver spots; skin pigmentation including pigmented spots, dark circles under the eyes, darkened skin, and blemishes; oily skin; warts; eczema; pruritic skin; psoriasis; inflammatory dermatoses; topical inflammation; disturbed keratinization; scalp dryness, and combinations thereof.